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Sample records for release ibuprofen microspheres

  1. Microspheres prepared with biodegradable PHBV and PLA polymers as prolonged-release system for ibuprofen: in vitro drug release and in vivo evaluation

    Directory of Open Access Journals (Sweden)

    Giovana Carolina Bazzo

    2012-12-01

    Full Text Available In this study, poly(hydroxybutyrate-co-hydroxyvalerate (PHBV and poly(l-lactide (PLA microspheres containing ibuprofen were prepared with the aim of prolonging the drug release. The oil-in-water (O/W emulsion solvent evaporation technique was used, varying the polymer ratio. All formulations provided spherical particles with drug crystals on the surface and a porous and rough polymeric matrix when PHBV was used and smooth external surface when prepared with PLA. The in vitro dissolution profiles show that the formulation containing PHBV/PLA at the proportion of 30/70 presented the best results in terms of prolonging the ibuprofen release. The analysis of the concentration of ibuprofen in the blood of rats showed that maximum levels were achieved at between one and two hours after administration of the immediate-release form (pure drug, while the prolonged microspheres led to a small amount of the drug being released within the first two hours and reached the maximum level after six hours of administration. It was concluded that it is possible to prolong the release of ibuprofen through its incorporation into PHBV/PLA microspheres.No presente estudo foram preparadas microesferas de poli(hidroxibutirato-co-hidroxivalerato (PHBV e poli(ácido láctico (PLA com o objetivo de prolongar a liberação do ibuprofeno, utilizado como fármaco modelo. Empregou-se o método de emulsificação e evaporação do solvente óleo em água (O/A, variando-se a proporção entre os polímeros. Todas as formulações originaram partículas esféricas com cristais de fármaco aderidos à superfície externa. As microesferas apresentaram superfície rugosa e porosa, quando o PHBV foi utilizado, e superfície externa lisa, quando preparadas com o PLA. Os perfis de dissolução in vitro evidenciaram que a formulação que continha PHBV/PLA na proporção de 30/70 apresentou melhores resultados para prolongar a liberação do ibuprofeno. Através da análise da concentra

  2. Ibuprofen-loaded microspheres based on a co-polymer of Eudragit ...

    African Journals Online (AJOL)

    The objective of this study was to encapsulate ibuprofen in microspheres based on a co-polymer of Eudragit® RS100 and RL100 with a view to achieving a controlled release of the incorporated drug. The microparticles were prepared by an o/o emulsion-solvent evaporation method using varying polymer ratios and ...

  3. Preparation and characterization of ibuprofen-loaded microspheres consisting of poly(3-hydroxybutyrate) and methoxy poly (ethylene glycol)-b-poly (D,L-lactide) blends or poly(3-hydroxybutyrate) and gelatin composites for controlled drug release

    Energy Technology Data Exchange (ETDEWEB)

    Bidone, Juliana; Melo, Ana Paula P. [Laboratorio de Farmacotecnica, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis (Brazil); Bazzo, Giovana C. [Grupo de Estudos em Materiais Polimericos (POLIMAT), Departamento de Quimica, Universidade Federal de Santa Catarina, Florianopolis (Brazil); Carmignan, Francoise [Laboratorio de Farmacotecnica, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis (Brazil); Soldi, Marli S.; Pires, Alfredo T.N. [Grupo de Estudos em Materiais Polimericos (POLIMAT), Departamento de Quimica, Universidade Federal de Santa Catarina, Florianopolis (Brazil); Lemos-Senna, Elenara [Laboratorio de Farmacotecnica, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, Florianopolis (Brazil)], E-mail: lemos@ccs.ufsc.br

    2009-03-01

    Poly-(3-hydroxybutyrate) (P(3HB)) is a biodegradable and biocompatible polymer that has been used to obtain polymer-based drug carriers. However, due to the high crystallinity degree of this polymer, drug release from P(3HB) microspheres frequently occurs at excessive rates. In this study, two strategies for prolonging ibuprofen release from P(3HB)-based microspheres were tested: blending with poly(D,L-lactide)-b-polyethylene glycol (mPEG-PLA); and obtaining composite particles with gelatin (GEL). SEM micrographs showed particles that were spherical and had a rough surface. A slight decrease of the crystallinity degree of P(3HB) was observed only in the DSC thermogram obtained from unloaded-microspheres prepared from 1:1 P(3HB):mPEG-PLA blend. For IBF-loaded microspheres, a reduction of around 10 deg. C in the melting temperature of P(3HB) was observed, indicating that the crystalline structure of the polymer was affected in the presence of the drug. DSC studies also yielded evidence of the presence of a molecular dispersion coexisting with a crystalline dispersion in the drug in the matrix. Similar results were obtained from X-ray diffractograms. In spite of 1:1 mPEG-PLA:P(3HB) blends having contributed to the reduction of the burst effect, a more controlled drug release was provided by the use of the 3:1 P(3HB):mPEGPLA blend. This result indicated that particle hydration played an important role in the drug release. On the other hand, the preparation of P(3HB):GEL composite microspheres did not allow control of the IBF release.

  4. Preparation and characterization of ibuprofen-loaded microspheres consisting of poly(3-hydroxybutyrate) and methoxy poly (ethylene glycol)-b-poly (D,L-lactide) blends or poly(3-hydroxybutyrate) and gelatin composites for controlled drug release

    International Nuclear Information System (INIS)

    Bidone, Juliana; Melo, Ana Paula P.; Bazzo, Giovana C.; Carmignan, Francoise; Soldi, Marli S.; Pires, Alfredo T.N.; Lemos-Senna, Elenara

    2009-01-01

    Poly-(3-hydroxybutyrate) (P(3HB)) is a biodegradable and biocompatible polymer that has been used to obtain polymer-based drug carriers. However, due to the high crystallinity degree of this polymer, drug release from P(3HB) microspheres frequently occurs at excessive rates. In this study, two strategies for prolonging ibuprofen release from P(3HB)-based microspheres were tested: blending with poly(D,L-lactide)-b-polyethylene glycol (mPEG-PLA); and obtaining composite particles with gelatin (GEL). SEM micrographs showed particles that were spherical and had a rough surface. A slight decrease of the crystallinity degree of P(3HB) was observed only in the DSC thermogram obtained from unloaded-microspheres prepared from 1:1 P(3HB):mPEG-PLA blend. For IBF-loaded microspheres, a reduction of around 10 deg. C in the melting temperature of P(3HB) was observed, indicating that the crystalline structure of the polymer was affected in the presence of the drug. DSC studies also yielded evidence of the presence of a molecular dispersion coexisting with a crystalline dispersion in the drug in the matrix. Similar results were obtained from X-ray diffractograms. In spite of 1:1 mPEG-PLA:P(3HB) blends having contributed to the reduction of the burst effect, a more controlled drug release was provided by the use of the 3:1 P(3HB):mPEGPLA blend. This result indicated that particle hydration played an important role in the drug release. On the other hand, the preparation of P(3HB):GEL composite microspheres did not allow control of the IBF release

  5. Controlled release of ibuprofen using Mg Al LDH nano carrier

    Science.gov (United States)

    Dasgupta, Sudip

    2017-08-01

    In the present study, NSAID (non-steroidal anti-inflammatory drugs) such as ibuprofen in anionic form has been intercalated in-situ into the interlayer space of Mg Al LDH nanoparticle during co-precipitation of hydroxides. LDH nanohybrids are characterized by XRD, FTIR and UV spectroscopy. Mg1-xAlx(NO3)x(OH)2.nH2O nanoparticles were synthesized using co-precipitation method from an aqueous solution of Mg(NO3)2.6H2O and Al(NO3)3.9H2O. Ibuprofen was intercalated in inter layer space of Mg-Al LDH during coprecipitation of drug LDH conjugate in nitrogen atmosphere. The nanopowders synthesised were in the size range between 25 to 90 nm with an average particle size of 55 nm. XRD analysis proved that there is an increase in d003 spacing from 7.89 Å for pristine LDH to 14.71 Å for ibuprofen intercalated LDH due to the intercalation of bigger ibuprofen molecule in the interlayer space of LDH. FTIR analysis showed hydroxyl and carbonyl stretching of ibuprofen in LDH-IBU sample confirming the intercalation of ibuprofen in the interlayer structure of LDH. The drug release study in phosphate buffer solution at pH 7.4 using UV-Vis spectroscopy demonstrated that 50 % drug molecules were released in 15 hours and more than 85 % release was achieved after 36 hours.

  6. Controlled release of ibuprofen by meso–macroporous silica

    Energy Technology Data Exchange (ETDEWEB)

    Santamaría, E., E-mail: esthersantamaria@ub.edu; Maestro, A.; Porras, M.; Gutiérrez, J.M.; González, C.

    2014-02-15

    Structured meso–macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)–poly(propylene oxide)–poly(ethylene oxide) (EO{sub 19}PO{sub 39}EO{sub 19}) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption–desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso–macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system. - Graphical abstract: Ibuprofen release profiles for the materials obtained from samples P84{sub m}eso (black diamonds), P84{sub 2}0% (white squares), P84{sub 5

  7. Controlled release of ibuprofen by meso–macroporous silica

    International Nuclear Information System (INIS)

    Santamaría, E.; Maestro, A.; Porras, M.; Gutiérrez, J.M.; González, C.

    2014-01-01

    Structured meso–macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)–poly(propylene oxide)–poly(ethylene oxide) (EO 19 PO 39 EO 19 ) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption–desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso–macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system. - Graphical abstract: Ibuprofen release profiles for the materials obtained from samples P84 m eso (black diamonds), P84 2 0% (white squares), P84 5 0% (black triangles), P84 7

  8. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Numpilai, Thanapha [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Muenmee, Suthaporn [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Center for Advanced Studies in Nanotechnology and Its Applications in Chemical Food and Agricultural Industries, Kasetsart University, Bangkok 10900 (Thailand); Witoon, Thongthai, E-mail: fengttwi@ku.ac.th [Department of Chemical Engineering, Faculty of Engineering, Kasetsart University, Bangkok 10900 (Thailand); Center for Advanced Studies in Nanotechnology and Its Applications in Chemical Food and Agricultural Industries, Kasetsart University, Bangkok 10900 (Thailand); NANOTEC-KU-Center of Excellence on Nanoscale Materials Design for Green Nanotechnology, Kasetsart University, Bangkok 10900 (Thailand)

    2016-02-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N{sub 2}-sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5 nm to 10 nm increased the ibuprofen loading from 0.74 to 0.85 mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8–20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92 wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. - Highlights: • Impacts of pore characteristics of supports on adsorption and release of ibuprofen • Increasing mesopore size increased the ibuprofen loading and dissolution rate. • Macropores reduced the diffusion pathway of ibuprofen and dissolution medium.

  9. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen

    International Nuclear Information System (INIS)

    Numpilai, Thanapha; Muenmee, Suthaporn; Witoon, Thongthai

    2016-01-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N 2 -sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5 nm to 10 nm increased the ibuprofen loading from 0.74 to 0.85 mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8–20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92 wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. - Highlights: • Impacts of pore characteristics of supports on adsorption and release of ibuprofen • Increasing mesopore size increased the ibuprofen loading and dissolution rate. • Macropores reduced the diffusion pathway of ibuprofen and dissolution medium.

  10. Controlled release of ibuprofen by meso-macroporous silica

    Science.gov (United States)

    Santamaría, E.; Maestro, A.; Porras, M.; Gutiérrez, J. M.; González, C.

    2014-02-01

    Structured meso-macroporous silica was successfully synthesized from an O/W emulsion using decane as a dispersed phase. Sodium silicate solution, which acts as a silica source and a poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) (EO19PO39EO19) denoted as P84 was used in order to stabilize the emulsion and as a mesopore template. The materials obtained were characterized through transmission electron microscopy (TEM), scanning electron microscopy (SEM), small-angle X-ray diffraction scattering (SAXS) and nitrogen adsorption-desorption isotherms. Ibuprofen (IBU) was selected as the model drug and loaded into ordered meso-macroporous materials. The effect of the materials’ properties on IBU drug loading and release was studied. The results showed that the loading of IBU increases as the macropore presence in the material is increased. The IBU adsorption process followed the Langmuir adsorption isotherm. A two-step release process, consisting of an initial fast release and then a slower release was observed. Macropores enhanced the adsorption capacity of the material; this was probably due to the fact that they allowed the drug to access internal pores. When only mesopores were present, ibuprofen was probably adsorbed on the mesopores close to the surface. Moreover, the more macropore present in the material, the slower the release behaviour observed, as the ibuprofen adsorbed in the internal pores had to diffuse along the macropore channels up to the surface of the material. The material obtained from a highly concentrated emulsion was functionalized with amino groups using two methods, the post-grafting mechanism and the co-condensation mechanism. Both routes improve IBU adsorption in the material and show good behaviour as a controlled drug delivery system.

  11. Cubic phase nanoparticles for sustained release of ibuprofen: formulation, characterization, and enhanced bioavailability study

    Science.gov (United States)

    Dian, Linghui; Yang, Zhiwen; Li, Feng; Wang, Zhouhua; Pan, Xin; Peng, Xinsheng; Huang, Xintian; Guo, Zhefei; Quan, Guilan; Shi, Xuan; Chen, Bao; Li, Ge; Wu, Chuanbin

    2013-01-01

    In order to improve the oral bioavailability of ibuprofen, ibuprofen-loaded cubic nanoparticles were prepared as a delivery system for aqueous formulations. The cubic inner structure was verified by cryogenic transmission electron microscopy. With an encapsulation efficiency greater than 85%, the ibuprofen-loaded cubic nanoparticles had a narrow size distribution around a mean size of 238 nm. Differential scanning calorimetry and X-ray diffraction determined that ibuprofen was in an amorphous and molecular form within the lipid matrix. The in vitro release of ibuprofen from cubic nanoparticles was greater than 80% at 24 hours, showing sustained characteristics. The pharmacokinetic study in beagle dogs showed improved absorption of ibuprofen from cubic nanoparticles compared to that of pure ibuprofen, with evidence of a longer half-life and a relative oral bioavailability of 222% (P ibuprofen-loaded cubic nanoparticles provide a promising carrier candidate with an efficient drug delivery for therapeutic treatment. PMID:23468008

  12. Impact of pore characteristics of silica materials on loading capacity and release behavior of ibuprofen.

    Science.gov (United States)

    Numpilai, Thanapha; Muenmee, Suthaporn; Witoon, Thongthai

    2016-02-01

    Impact of pore characteristics of porous silica supports on loading capacity and release behavior of ibuprofen was investigated. The porous silica materials and ibuprofen-loaded porous silica materials were thoroughly characterized by N2-sorption, thermal gravimetric and derivative weight analyses (TG-DTW), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), transmission electron microscope (TEM) to determine the physical properties of materials, amount of ibuprofen adsorbed and position of ibuprofen. The detailed characterization reveals that the ibuprofen molecules adsorbed inside the mesopores. Increasing the mesopore size from 5nm to 10nm increased the ibuprofen loading from 0.74 to 0.85mmol/g, respectively. Incorporation of macropore into the structure of porous silica materials enhanced the ibuprofen loading capacity of 11.8-20.3%. The ibuprofen-loaded bimodal meso-macroporous silica materials exhibited the highest dissolution of 92wt.% within an hour. The ibuprofen particles deposited on the external surface of the porous silica materials showed a lower dissolution rate than the ibuprofen adsorbed inside the mesopores due to the formation of ibuprofen crystalline. Copyright © 2015 Elsevier B.V. All rights reserved.

  13. Optimization of sustained release aceclofenac microspheres using response surface methodology

    Energy Technology Data Exchange (ETDEWEB)

    Deshmukh, Rameshwar K.; Naik, Jitendra B., E-mail: jitunaik@gmail.com

    2015-03-01

    Polymeric microspheres containing aceclofenac were prepared by single emulsion (oil-in-water) solvent evaporation method using response surface methodology (RSM). Microspheres were prepared by changing formulation variables such as the amount of Eudragit® RS100 and the amount of polyvinyl alcohol (PVA) by statistical experimental design in order to enhance the encapsulation efficiency (E.E.) of the microspheres. The resultant microspheres were evaluated for their size, morphology, E.E., and in vitro drug release. The amount of Eudragit® RS100 and the amount of PVA were found to be significant factors respectively for determining the E.E. of the microspheres. A linear mathematical model equation fitted to the data was used to predict the E.E. in the optimal region. Optimized formulation of microspheres was prepared using optimal process variables setting in order to evaluate the optimization capability of the models generated according to IV-optimal design. The microspheres showed high E.E. (74.14 ± 0.015% to 85.34 ± 0.011%) and suitably sustained drug release (minimum; 40% to 60%; maximum) over a period of 12 h. The optimized microspheres formulation showed E.E. of 84.87 ± 0.005 with small error value (1.39). The low magnitudes of error and the significant value of R{sup 2} in the present investigation prove the high prognostic ability of the design. The absence of interactions between drug and polymers was confirmed by Fourier transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRPD) revealed the dispersion of drug within microspheres formulation. The microspheres were found to be discrete, spherical with smooth surface. The results demonstrate that these microspheres could be promising delivery system to sustain the drug release and improve the E.E. thus prolong drug action and achieve the highest healing effect with minimal gastrointestinal side effects. - Highlights: • Aceclofenac microspheres

  14. Ibuprofen Release from Poly(ethyl cyanoacrylate Nanoparticles Prepared by Semicontinuous Heterophase Polymerization

    Directory of Open Access Journals (Sweden)

    J. A. Balleño

    2018-01-01

    Full Text Available Ibuprofen-loaded poly(ethyl cyanoacrylate nanoparticles were prepared by semicontinuous heterophase polymerization of ethyl cyanoacrylate in the presence of ibuprofen; different surfactant concentration, pH, and temperature were used. Particle size was measured by quasi-light scattering and transmission electron microscopy, while the amount of drug released was determined by UV spectroscopy. Nanoparticles with diameters between 10 and 58 nm, loaded with ibuprofen, were obtained. The smallest particles and the higher drug loading were obtained at the highest pH tested. The analysis of the release data showed that the drug release profiles correspond to the Weibull model. Moreover, it was found that most of the ibuprofen is released within the first 80–120 min; initially the release rate is slow, but then it increases to finally decrease. This behavior contrasts with the reported burst of drug concentration in the plasma after oral administration of IB.

  15. Oxaliplatin loaded PLAGA microspheres: design of specific release profiles.

    Science.gov (United States)

    Lagarce, F; Cruaud, O; Deuschel, C; Bayssas, M; Griffon-Etienne, G; Benoit, J

    2002-08-21

    Oxaliplatin loaded PLAGA microspheres have been prepared by solvent extraction process. Parameters affecting the release kinetics in vitro have been studied in order to design specific release profiles suitable for direct intra-tumoral injection. By varying the nature and the relative proportions of different polymers we managed to prepare microspheres with good encapsulation efficiency (75-90%) and four different release profiles: zero order kinetics (type II) and the classical sigmoïd release profile with three different sizes of plateau and burst. These results, if correlated with in vivo activity, are promising to enhance effectiveness of local tumor treatment.

  16. Evaluation of Controlled Release Theophylline Microspheres ...

    African Journals Online (AJOL)

    Erah

    High drug/polymer ratio, low processing temperature and low HLB value of ... Keywords: Microsphere, Emulsion solvent evaporation, Theophylline, Temperature, ... evaporation, stirring rate, viscosity of ... organic solvent is removed from the.

  17. Ibuprofen-loaded poly(lactic-co-glycolic acid films for controlled drug release

    Directory of Open Access Journals (Sweden)

    Pang JM

    2011-04-01

    Full Text Available Jianmei Pang1, Yuxia Luan1, Feifei Li1, Xiaoqing Cai1, Jimin Du2, Zhonghao Li31School of Pharmaceutical Science, Shandong University, Jinan, Shandong Province, PR China; 2School of Chemistry and Chemical Engineering, Anyang Normal University, Henan Province, PR China; 3School of Materials Science and Engineering, Shandong University, Jinan, Shandong Province, PR ChinaAbstract: Ibuprofen- (IBU loaded biocompatible poly(lactic-co-glycolic acid (PLGA films were prepared by spreading polymer/ibuprofen solution on the nonsolvent surface. By controlling the weight ratio of drug and polymer, different drug loading polymer films can be obtained. The synthesized ibuprofen-loaded PLGA films were characterized with scanning electron microscopy, powder X-ray diffraction, and differential scanning calorimetry. The drug release behavior of the as-prepared IBU-loaded PLGA films was studied to reveal their potential application in drug delivery systems. The results show the feasibility of the as-obtained films for controlling drug release. Furthermore, the drug release rate of the film could be controlled by the drug loading content and the release medium. The development of a biodegradable ibuprofen system, based on films, should be of great interest in drug delivery systems.Keywords: ibuprofen, controlled release, poly(lactic-co-glycolic acid, films

  18. Synthesis and characterization of thermosensitive hydrogels and the investigation of modified release of ibuprofen

    Directory of Open Access Journals (Sweden)

    Ilić-Stojanović Snežana S.

    2013-01-01

    Full Text Available The method of the synthesis of poly(N-isopropylacrylamide-co-2-hydroxypropyl methacrylate hydrogels obtained by radical polymerization is described. Their characterization was carried out by the determination of the quantity of residual monomers and by investigating their structure using the FTIR. Three glass transitions were detected by DSC method. The porous surfaces of hydrogels with incorporated ibuprofen were shown in SEM micrographs. The swelling ratio of hydrogels decreased with the temperature increase and the swelling transport mechanism was changed from non-Fickian to Fickian. Ibuprofen was incorporated in hydrogel as a drug carrier and released quantity was monitored by HPLC method depending on the temperature. Hydrogel with the lower cross-linker content had the highest swelling degree (α = 34.72 at 10°C and released the largest amount of ibuprofen (64.21 mg/gxerogel at 40°C. [Projekat Ministarstva nauke Republike Srbije, br. TR-34012

  19. Combined use of an ibuprofen-releasing foam dressing and silver dressing on infected leg ulcers

    DEFF Research Database (Denmark)

    Jorgensen, B.; Gottrup, F.; Karlsmark, T.

    2008-01-01

    OBJECTIVE: To investigate the effect and safety of an ibuprofen-releasing foam (Biatain-Ibu, Coloplast A/S) combined with an ionised silver-releasing wound contact layer (Physiotulle Ag, Coloplast A/S) on painful, infected venous leg ulcers. METHOD: This open non-comparative study involved 24...... patients with painful, exuding, locally infected, and stalled venous leg ulcers. Persistent pain and pain at dressing change were monitored using a 11-point numerical box scale (NBS). The composition of the wound bed, the dressing combination's ability to absorb exudate and minimise leakage, ibuprofen...... dressing application, the mean concentration of ibuprofen in the wound exudate reached a constant level of 35 +/- 21 microg/ml.After 31 days, the relative wound area had reduced by 42%, with an associated decrease in fibrin and an increase in granulation tissue.The number of patients with wound malodour...

  20. Diclofenac salts, part 6: release from lipid microspheres.

    Science.gov (United States)

    Fini, Adamo; Cavallari, Cristina; Rabasco Alvarez, Antonio M; Rodriguez, Marisa Gonzalez

    2011-08-01

    The release of diclofenac (20%, w/w) was studied from lipidic solid dispersions using three different chemical forms (acid, sodium salt, and pyrrolidine ethanol salt) and two different lipid carriers (Compritol 888 ATO or Carnauba wax) either free or together with varying amounts (10%-30%, w/w) of stearic acid. Microspheres were prepared by ultrasound-assisted atomization of the molten dispersions and analyzed by scanning electron microscopy, differential scanning calorimetry, and hot stage microscopy. The effects of different formulations on the resulting drug release profiles as a function of pH were studied and the results were discussed. The formulation of the 18 systems and the chemical form of the drug were found to strongly affect the mode of the drug release. The solubility of the chemical forms in the lipid mixture is in the following order: pyrrolidine ethanol salt ≫ acid > sodium salt (according to the solubility parameters), and the nature of the systems thus obtained ranges from a matrix, for mutually soluble drug/carrier pairs, to a microcapsule, for pairs wherein mutual solubility is poor. Drug release from microspheres prepared by pure lipids was primarily controlled by diffusion, whereas the release from microspheres containing stearic acid was diffusion/erosion controlled at pH 7.4. Copyright © 2011 Wiley-Liss, Inc.

  1. INVESTIGATION OF DRUG RELEASE FROM BIODEGRADABLE PLG MICROSPHERES: EXPERIMENT AND THEORY

    Energy Technology Data Exchange (ETDEWEB)

    ANDREWS, MALCOLM J. [Los Alamos National Laboratory; BERCHANE, NADER S. [Los Alamos National Laboratory; CARSON, KENNETH H. [Los Alamos National Laboratory; RICE-FICHT, ALLISON C. [Los Alamos National Laboratory

    2007-01-30

    Piroxicam containing PLG microspheres having different size distributions were fabricated, and in vitro release kinetics were determined for each preparation. Based on the experimental results, a suitable mathematical theory has been developed that incorporates the effect of microsphere size distribution and polymer degradation on drug release. We show from in vitro release experiments that microsphere size has a significant effect on drug release rate. The initial release rate decreased with an increase in microsphere size. In addition, the release profile changed from first order to concave-upward (sigmoidal) as the system size was increased. The mathematical model gave a good fit to the experimental release data.

  2. A reproducible accelerated in vitro release testing method for PLGA microspheres.

    Science.gov (United States)

    Shen, Jie; Lee, Kyulim; Choi, Stephanie; Qu, Wen; Wang, Yan; Burgess, Diane J

    2016-02-10

    The objective of the present study was to develop a discriminatory and reproducible accelerated in vitro release method for long-acting PLGA microspheres with inner structure/porosity differences. Risperidone was chosen as a model drug. Qualitatively and quantitatively equivalent PLGA microspheres with different inner structure/porosity were obtained using different manufacturing processes. Physicochemical properties as well as degradation profiles of the prepared microspheres were investigated. Furthermore, in vitro release testing of the prepared risperidone microspheres was performed using the most common in vitro release methods (i.e., sample-and-separate and flow through) for this type of product. The obtained compositionally equivalent risperidone microspheres had similar drug loading but different inner structure/porosity. When microsphere particle size appeared similar, porous risperidone microspheres showed faster microsphere degradation and drug release compared with less porous microspheres. Both in vitro release methods investigated were able to differentiate risperidone microsphere formulations with differences in porosity under real-time (37 °C) and accelerated (45 °C) testing conditions. Notably, only the accelerated USP apparatus 4 method showed good reproducibility for highly porous risperidone microspheres. These results indicated that the accelerated USP apparatus 4 method is an appropriate fast quality control tool for long-acting PLGA microspheres (even with porous structures). Copyright © 2015 Elsevier B.V. All rights reserved.

  3. Characterization of unsaturated fatty acid sustained-release microspheres for long-term algal inhibition.

    Science.gov (United States)

    Ni, Lixiao; Jie, Xiaoting; Wang, Peifang; Li, Shiyin; Hu, Shuzhen; Li, Yiping; Li, Yong; Acharya, Kumud

    2015-02-01

    The unsaturated fatty acid (linoleic acid) sustained-release microspheres were prepared with linoleic acid (LA) using alginate-chitosan microcapsule technology. These LA sustained-release microspheres had a high encapsulation efficiency (up to 62%) tested by high performance liquid chromatography with a photo diode array. The dry microspheres were characterized by a scanning electron microscope, X-ray diffraction measurement, dynamic thermogravimetric analysis and Fourier transform infrared spectral analysis. The results of characterization showed that the microspheres had good thermal stability (decomposition temperature of 236°C), stable and temperature independent release properties (release time of more than 40 d). Compared to direct dosing of LA, LA sustained-released microspheres could inhibit Microcystis aeruginosa growth to the non-growth state. The results of this study suggested that the LA sustained-release microspheres may be a potential candidate for algal inhibition. Copyright © 2014 Elsevier Ltd. All rights reserved.

  4. An ibuprofen-antagonized plasmin inhibitor released by human endothelial cells.

    Science.gov (United States)

    Rockwell, W B; Ehrlich, H P

    1991-02-01

    Serum-free culture medium harvested from endothelial cell monolayer cultures derived from human scars and dermis was examined for inhibition of fibrinolysis using a fibrin plate assay. Human cultured fibroblasts and smooth muscle cells did not produce any detectable inhibitory activity. The inhibitor is spontaneously released from the cultured endothelial cells over time. In the fibrin plate assay of plasmin-induced fibrinolysis, one nonsteroidal antiinflammatory (NSAI) drug, ibuprofen, was demonstrated to antagonize the inhibition of fibrinolysis. The antagonistic activity of ibuprofen appears unrelated to its NSAI drug activity because other NSAI drugs such as indomethacin and tolmetin have minimal antagonistic activity. Heating the cultured endothelial cells to 42 degrees C stimulates greater release of the inhibitor in a shorter period of time. This plasmin inhibitor, which is produced by endothelial cells, may contribute to postburn vascular occlusion, leading to secondary progressive necrosis in burn-traumatized patients.

  5. Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

    Directory of Open Access Journals (Sweden)

    Hugo Almeida

    2012-09-01

    Full Text Available Ibuprofen is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory diseases. In its pure state, ibuprofen presents poor physical and mechanical characteristics and its use in solid dosage forms needs the addition of excipients that improve these properties. The selection of the best excipients and the most suitable pharmaceutical dosage form to carry ibuprofen is very important for the industrial success of this drug. Given these factors, lipid microparticles and solid dispersions of ibuprofen with cetyl alcohol, stearic acid, and hydrogenated castor oil were prepared. These formulations were intended to improve the physical and mechanical characteristics and to sustain the release of this drug. Physical mixtures were also prepared with the same ingredients in similar proportions. The solid dispersions of ibuprofen/stearic acid and ibuprofen/hydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Further, gelatin capsules filled with lipid microparticles and solid dispersions were submitted to dissolution tests in order to study the influence of the prepared systems in the release profiles of ibuprofen. Prolonged release of ibuprofen was achieved with the lipid microparticles and solid dispersions prepared with the different types of excipients.O ibuprofeno é um dos antiinflamatórios não esteróides mais utilizados no tratamento de patologias associadas a processos inflamatórios. Este fármaco, quando no seu estado puro, apresenta características físicas e mecânicas pouco satisfatórias e a sua utilização em formas sólidas só é possível se forem adicionados excipientes que permitam melhorar estas propriedades. A seleção dos excipientes ideais e da forma farmacêutica mais adequada para veicular o ibuprofeno é fundamental para o sucesso industrial deste fármaco. Tendo em conta estes fatores, prepararam-se micropartículas lipídicas e dispersões s

  6. Polymer based microspheres of aceclofenac as sustained release parenterals for prolonged anti-inflammatory effect

    Energy Technology Data Exchange (ETDEWEB)

    Kaur, Manpreet; Sharma, Sumit; Sinha, VR, E-mail: sinha_vr@rediffmail.com

    2017-03-01

    Poly(lactic-co-glycolic acid) (PLGA) (75:25) and polycaprolactone (PCL) microspheres were fabricated for prolonged release of aceclofenac by parenteral administration. Microspheres encapsulating aceclofenac were designed to release the drug at controlled rate for around one month. Biodegradable microspheres were prepared by solvent emulsification evaporation method in different polymer:drug ratios (1:1, 2:1 and 3:1). After drug loading, PLGA and PCL microspheres showed a controlled size distribution with an average size of 11.75 μm and 3.81 μm respectively and entrapment efficiency in the range of 90 ± 0.72% to 91.06 ± 4.01% with PLGA and 83.01 ± 2.13% to 90.4 ± 2.11% with PCL. Scanning electron microscopy has confirmed good spherical structures of microspheres. The percent yield of biodegradable polymeric microspheres ranged between 30.95 ± 10.14% to 92.84 ± 3.15% and 47.33 ± 4.72% to 80 ± 3.60% for PLGA and PCL microspheres respectively. PLGA microspheres followed Higuchi release pattern while Korsmeyer-Peppas explained the release pattern of PCL microspheres. Stability studies of microspheres were also carried out by storing the preparations at 2-8 °C for 30, 60 and 90 days and evaluating them for entrapment efficiency, residual drug content and polymer drug compatability. In-vivo studies showed significant anti-inflammatory activity of microspheres upto 48 hours using the carrageenan induced rat paw oedema model. - Highlights: • PLGA and PCL polymeric microspheres for parenteral prolonged drug delivery system were formulated. • Polymeric microspheres were characterized physically and drug excipient incompatability. • Three months accelerated stability studies were carried for drug loaded polymeric microspheres. • Pharmacodynamic studies prove the rationality of sustained therapeutic effect of designed drug delivery system.

  7. Comparative assessment of in vitro release kinetics of calcitonin polypeptide from biodegradable microspheres.

    Science.gov (United States)

    Prabhu, Sunil; Sullivan, Jennifer L; Betageri, Guru V

    2002-01-01

    The objective of our study was to compare the in vitro release kinetics of a sustained-release injectable microsphere formulation of the polypeptide drug, calcitonin (CT), to optimize the characteristics of drug release from poly-(lactide-co-glycolide) (PLGA) copolymer biodegradable microspheres. A modified solvent evaporation and double emulsion technique was used to prepare the microspheres. Release kinetic studies were carried out in silanized tubes and dialysis bags, whereby microspheres were suspended and incubated in phosphate buffered saline, sampled at fixed intervals, and analyzed for drug content using a modified Lowry protein assay procedure. An initial burst was observed whereby about 50% of the total dose of the drug was released from the microspheres within 24 hr and 75% within 3 days. This was followed by a period of slow release over a period of 3 weeks in which another 10-15% of drug was released. Drug release from the dialysis bags was more gradual, and 50% CT was released only after 4 days and 75% after 12 days of release. Scanning electron micrographs revealed spherical particles with channel-like structures and a porous surface after being suspended in an aqueous solution for 5 days. Differential scanning calorimetric studies revealed that CT was present as a mix of amorphous and crystalline forms within the microspheres. Overall, these studies demonstrated that sustained release of CT from PLGA microspheres over a 3-week period is feasible and that release of drug from dialysis bags was more predictable than from tubes.

  8. Full factorial design optimization of anti-inflammatory drug release by PCL–PEG–PCL microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Azouz, L' Hachemi, E-mail: azouz.chimie@gmail.com [Laboratoire des Matériaux Organiques (LMO), Faculté des Sciences Exactes, Département de Chimie, Université de Bejaia, 06000 Bejaia Algérie (Algeria); Dahmoune, Farid, E-mail: farid.dahmoune@yahoo.fr [Laboratoire de Biomathématiques, Biophysique, Biochimie et Scientométrie (L3BS-Bejaia), Faculté des Sciences de la Nature et de la Vie et des Sciences de la Terre, Université de Bouira 10000 Bouira (Algeria); Rezgui, Farouk, E-mail: rezgui-farouk@netcourrier.com [Laboratoire des Matériaux Organiques (LMO), Faculté de Technologie, Département de Génie des Procédés, Université de Bejaia, 06000 Bejaia (Algeria); G' Sell, Christian, E-mail: gsell.christian@univ-lorraine.fr [Université de Lorraine, Pôle scientifique M4, Institut Jean Lamour - UMR CNRS-UL 7198, Département SI2M, 54000 Nancy (France)

    2016-01-01

    A biodegradable triblock poly(ε-caprolactone)–poly(ethylene glycol)–poly(ε-caprolactone) copolymer was successfully synthesized by ring-opening polymerization of ε-caprolactone, and was characterized by intrinsic viscosimetry, {sup 1}H nuclear magnetic resonance, infrared spectroscopy and X-ray diffraction. Copolymer microparticles loaded with ibuprofen were prepared by an oil-in-water (o/w) emulsion solvent evaporation process. They were carefully weighted and characterized through their zeta potential. In this work, 4 selected process parameters (shaking speed X{sub 1}, time of contact X{sub 2}, poly(vinyl alcohol) concentration X{sub 3}, and ibuprofen concentration X{sub 4}) were adjusted at 2 different values. For each of the 16 experimental conditions, repeated twice, the drug encapsulation efficiency of the microspheres was determined, according to the following definition: EE (X{sub 1}, X{sub 2}, X{sub 3}, X{sub 4}) = mass of encapsulated ibuprofen / total weight of ibuprofen. A “full factorial design method” was applied to analyze the results statistically according to a polynomial fit and to determine the optimal conditions for the microencapsulation of the ibuprofen through an accurate statistical protocol. The microparticles obtained exhibit a spherical shape as shown by electron microscopy. - Highlights: • PCEC copolymer was synthesized by ring-opening polymerization of ε-caprolactone. • 2{sup 4} experimental design was used to optimize the IBF encapsulation efficiency (EE). • 88.86% of ibuprofen (IBF) was encapsulated in PCEC microspheres. • EE significantly decreases with increasing shaking speed (antagonist effect). • EE significantly increases with increasing IBF concentration (synergetic effect).

  9. Full factorial design optimization of anti-inflammatory drug release by PCL–PEG–PCL microspheres

    International Nuclear Information System (INIS)

    Azouz, L'Hachemi; Dahmoune, Farid; Rezgui, Farouk; G'Sell, Christian

    2016-01-01

    A biodegradable triblock poly(ε-caprolactone)–poly(ethylene glycol)–poly(ε-caprolactone) copolymer was successfully synthesized by ring-opening polymerization of ε-caprolactone, and was characterized by intrinsic viscosimetry, 1 H nuclear magnetic resonance, infrared spectroscopy and X-ray diffraction. Copolymer microparticles loaded with ibuprofen were prepared by an oil-in-water (o/w) emulsion solvent evaporation process. They were carefully weighted and characterized through their zeta potential. In this work, 4 selected process parameters (shaking speed X 1 , time of contact X 2 , poly(vinyl alcohol) concentration X 3 , and ibuprofen concentration X 4 ) were adjusted at 2 different values. For each of the 16 experimental conditions, repeated twice, the drug encapsulation efficiency of the microspheres was determined, according to the following definition: EE (X 1 , X 2 , X 3 , X 4 ) = mass of encapsulated ibuprofen / total weight of ibuprofen. A “full factorial design method” was applied to analyze the results statistically according to a polynomial fit and to determine the optimal conditions for the microencapsulation of the ibuprofen through an accurate statistical protocol. The microparticles obtained exhibit a spherical shape as shown by electron microscopy. - Highlights: • PCEC copolymer was synthesized by ring-opening polymerization of ε-caprolactone. • 2 4 experimental design was used to optimize the IBF encapsulation efficiency (EE). • 88.86% of ibuprofen (IBF) was encapsulated in PCEC microspheres. • EE significantly decreases with increasing shaking speed (antagonist effect). • EE significantly increases with increasing IBF concentration (synergetic effect).

  10. Kinetics of piroxicam release from low-methylated pectin/zein hydrogel microspheres

    Science.gov (United States)

    The kinetics of a model drug (piroxicam) release from pectin/zein hydrogel microspheres was studied under conditions simulating the gastrointestinal tract. It is established that the rate-limiting step in the release mechanism is drug diffusion out of the microspheres rather than its dissolution. ...

  11. Analgesic Efficacy of a New Immediate-Release/Extended-Release Formulation of Ibuprofen: Results From Single- and Multiple-Dose Postsurgical Dental Pain Studies.

    Science.gov (United States)

    Christensen, Steven; Paluch, Ed; Jayawardena, Shyamalie; Daniels, Stephen; Meeves, Suzanne

    2017-05-01

    Analgesic effects of ibuprofen immediate-release/extended-release (IR/ER) 600-mg tablets were evaluated in 2 randomized, double-blind, placebo-controlled dental pain studies. Patients 16-40 years old with moderate-severe pain following third-molar extraction received single-dose ibuprofen 600 mg IR/ER (formulation A or B), naproxen sodium 220 mg, or placebo (2:2:2:1; study 1) or 4 doses of ibuprofen 600 mg IR/ER (formulation A) or placebo (1:1; study 2). In study 1 (n = 196), mean (standard deviation [SD]) time-weighted sum of pain intensity difference scores for placebo, ibuprofen IR/ER A, ibuprofen IR/ER B, and naproxen, respectively, were 0.05 (9.2), 16.87 (9.4), 17.34 (10.5), and 12.66 (10.0) over 0-12 hours and -0.03 (4.1), 6.57 (4.4), 7.14 (5.2), and 5.14 (5.0) over 8-12 hours (all P ibuprofen IR/ER, respectively (P ibuprofen. Gastrointestinal adverse events predominated with placebo both after study medication administration and after rescue medication use, if applicable. Ibuprofen 600 mg IR/ER provided safe and effective analgesia after single and multiple doses. © 2016, The American College of Clinical Pharmacology.

  12. A controlled release of ibuprofen by systematically tailoring the morphology of mesoporous silica materials

    International Nuclear Information System (INIS)

    Qu Fengyu; Zhu Guangshan; Lin Huiming; Zhang Weiwei; Sun Jinyu; Li Shougui; Qiu Shilun

    2006-01-01

    A series of mesoporous silica materials with similar pore sizes, different morphologies and variable pore geometries were prepared systematically. In order to control drug release, ibuprofen was employed as a model drug and the influence of morphology and pore geometry of mesoporous silica on drug release profiles was extensively studied. The mesoporous silica and drug-loaded samples were characterized by X-ray diffraction, Fourier transform IR spectroscopy, N 2 adsorption and desorption, scanning electron microscopy, and transmission electron microscopy. It was found that the drug-loading amount was directly correlated to the Brunauer-Emmett-Teller surface area, pore geometry, and pore volume; while the drug release profiles could be controlled by tailoring the morphologies of mesoporous silica carriers. - Graphical abstract: The release of ibuprofen is controlled by tailoring the morphologies of mesoporous silica. The mesoporous silica and drug-loaded samples are characterized by powder X-ray diffraction, Fourier transform IR spectroscopy, N 2 adsorption and desorption, scanning electron microscopy, and transmission electron microscopy. The drug-loading amount is directly correlated to the Brunauer-Emmett-Teller surface area, pore geometry, and pore volume; while the drug release profiles can be controlled by tailoring the morphologies of mesoporous silica carriers

  13. The physical and chemical stability of suspensions of sustained-release diclofenac microspheres.

    Science.gov (United States)

    Lewis, L; Boni, R L; Adeyeye, C M

    1998-01-01

    The major challenge in liquid sustained-release oral suspensions is to minimize drug diffusion into the suspending medium and to retain the original properties of the microparticles during storage. Diclofenac wax microspheres prepared by the hydrophobic congealable disperse phase method were formulated as a sustained release suspension and stored at three different temperatures (25, 37 and 45 degrees C) for 3 months, to evaluate the physical and chemical stability of the suspended microspheres. Suspensions of microspheres stored at ambient temperatures were both physically and chemically stable, but at higher temperatures, up to 45 degrees C, there was a decrease in drug release due to scaling and melting on the microsphere surface as observed by scanning electron microscopy. However, on prolonged storage, up to 90 days, especially at 45 degrees C, temperature became a dominant factor causing an increase in drug release. The suspension of diclofenac microspheres was chemically stable for 3 months, while the plain drug suspension exhibited slight degradation.

  14. Preparation of magnetic polylactic acid microspheres and investigation of its releasing property for loading curcumin

    Energy Technology Data Exchange (ETDEWEB)

    Li Fengxia [Heilongjiang Key Laboratory of Molecular Design and Preparation of Flame Retarded Materials, College of Science, Northeast Forestry University, Harbin 150040 (China); Li Xiaoli, E-mail: lixiaoli0903@163.com [Heilongjiang Key Laboratory of Molecular Design and Preparation of Flame Retarded Materials, College of Science, Northeast Forestry University, Harbin 150040 (China); Li Bin, E-mail: libinzh62@163.com [Heilongjiang Key Laboratory of Molecular Design and Preparation of Flame Retarded Materials, College of Science, Northeast Forestry University, Harbin 150040 (China)

    2011-11-15

    In order to obtain a targeting drug carrier system, magnetic polylactic acid (PLA) microspheres loading curcumin were synthesized by the classical oil-in-water emulsion solvent-evaporation method. In the Fourier transform infrared spectra of microspheres, the present functional groups of PLA were all kept invariably. The morphology and size distribution of magnetic microspheres were observed with scanning electron microscopy and dynamic light scattering, respectively. The results showed that the microspheres were regularly spherical and the surface was smooth with a diameter of 0.55-0.75 {mu}m. Magnetic Fe{sub 3}O{sub 4} was loaded in PLA microspheres and the content of magnetic particles was 12 wt% through thermogravimetric analysis. The magnetic property of prepared microspheres was measured by vibrating sample magnetometer. The results showed that the magnetic microspheres exhibited typical superparamagnetic behavior and the saturated magnetization was 14.38 emu/g. Through analysis of differential scanning calorimetry, the curcumin was in an amorphous state in the magnetic microspheres. The drug loading, encapsulation efficiency and releasing properties of curcumin in vitro were also investigated by ultraviolet-visible spectrum analysis. The results showed that the drug loading and encapsulation efficiency were 8.0% and 24.2%, respectively. And curcumin was obviously slowly released because the cumulative release percentage of magnetic microspheres in the phosphate buffer (pH=7.4) solution was only 49.01% in 72 h, and the basic release of curcumin finished in 120 h. - Highlights: > We prepare magnetic polylactic acid microspheres loading curcumin. > The classical oil-in-water emulsion solvent-evaporation method is used. > The magnetic microspheres are regularly spherical with a diameter of 0.55-0.75 {mu}m. > They show a certain sustained release effect on in vitro drug releasing.

  15. Preparation of magnetic polylactic acid microspheres and investigation of its releasing property for loading curcumin

    International Nuclear Information System (INIS)

    Li Fengxia; Li Xiaoli; Li Bin

    2011-01-01

    In order to obtain a targeting drug carrier system, magnetic polylactic acid (PLA) microspheres loading curcumin were synthesized by the classical oil-in-water emulsion solvent-evaporation method. In the Fourier transform infrared spectra of microspheres, the present functional groups of PLA were all kept invariably. The morphology and size distribution of magnetic microspheres were observed with scanning electron microscopy and dynamic light scattering, respectively. The results showed that the microspheres were regularly spherical and the surface was smooth with a diameter of 0.55-0.75 μm. Magnetic Fe 3 O 4 was loaded in PLA microspheres and the content of magnetic particles was 12 wt% through thermogravimetric analysis. The magnetic property of prepared microspheres was measured by vibrating sample magnetometer. The results showed that the magnetic microspheres exhibited typical superparamagnetic behavior and the saturated magnetization was 14.38 emu/g. Through analysis of differential scanning calorimetry, the curcumin was in an amorphous state in the magnetic microspheres. The drug loading, encapsulation efficiency and releasing properties of curcumin in vitro were also investigated by ultraviolet-visible spectrum analysis. The results showed that the drug loading and encapsulation efficiency were 8.0% and 24.2%, respectively. And curcumin was obviously slowly released because the cumulative release percentage of magnetic microspheres in the phosphate buffer (pH=7.4) solution was only 49.01% in 72 h, and the basic release of curcumin finished in 120 h. - Highlights: → We prepare magnetic polylactic acid microspheres loading curcumin. → The classical oil-in-water emulsion solvent-evaporation method is used. → The magnetic microspheres are regularly spherical with a diameter of 0.55-0.75 μm. → They show a certain sustained release effect on in vitro drug releasing.

  16. Folic acid-functionalized magnetic ZnFe2O4 hollow microsphere core/mesoporous silica shell composite particles: synthesis and application in drug release.

    Science.gov (United States)

    Yang, Dandan; Wei, Kaiwei; Liu, Qi; Yang, Yong; Guo, Xue; Rong, Hongren; Cheng, Mei-Ling; Wang, Guoxiu

    2013-07-01

    A drug delivery system was designed by deliberately combining the useful functions into one entity, which was composed of magnetic ZnFe2O4 hollow microsphere as the core, and mesoporous silica with folic acid molecules as the outer shell. Amine groups coated magnetic ZnFe2O4 hollow microsphere core/mesoporous silica shell (MZHM-MSS-NH2) composite particles were first synthesized by a one-pot direct co-condensation method. Subsequently a novel kind of folic acid-functionalized magnetic ZnFe2O4 hollow microsphere core/mesoporous silica shell (MZHM-MSS-NHFA) composite particles were synthesized by conjugating folic acid as targeted molecule to MZHM-MSS-NH2. Ibuprofen, a well-known antiphlogistic drug, was used as a model drug to assess the loading and releasing behavior of the composite microspheres. The results show that the MZHM-MSS-NHFA system has the higher capacity of drug storage and good sustained drug-release property. Copyright © 2013 Elsevier B.V. All rights reserved.

  17. Preparation and drug controlled release of porous octyl-dextran microspheres.

    Science.gov (United States)

    Hou, Xin; Liu, Yanfei

    2015-01-01

    In this work, porous octyl-dextran microspheres with excellent properties were prepared by two steps. Firstly, dextran microspheres were synthesized by reversed-phase suspension polymerization. Secondly, octyl-dextran microspheres were prepared by the reaction between dextran microspheres and ethylhexyl glycidyl ether and freezing-drying method. Porous structure of microspheres was formed through the interaction between octyl groups and organic solvents. The structure, morphology, dry density, porosity and equilibrium water content of porous octyl-dextran microspheres were systematically investigated. The octyl content affected the properties of microspheres. The results showed that the dry density of microspheres decreased from 2.35 to 1.21 g/ml, porosity increased from 80.68 to 95.05% with the octyl content increasing from 0.49 to 2.28 mmol/g. Meanwhile, the equilibrium water content presented a peak value (90.18%) when the octyl content was 2.25 mmol/g. Octyl-dextran microspheres showed high capacity. Naturally drug carriers play an important role in drug-delivery systems for their biodegradability, wide raw materials sources and nontoxicity. Doxorubicin (DOX) was used as a drug model to examine the drug-loading capacity of porous octyl-dextran microspheres. The drug-loading efficiency increased with the increase in microspheres/drug ratio, while the encapsulation efficiency decreased. When microspheres/drug mass ratio was 4/1, the drug-loading efficiency and encapsulation efficiency were 10.20 and 51.00%, respectively. The release rate of DOX increased as drug content and porosity increased. In conclusion, porous octyl-dextran microspheres were synthesized successfully and have the potential to serve as an effective delivery system in drug controlled release.

  18. Controlled Release of Lysozyme from Double-Walled Poly(Lactide-Co-Glycolide (PLGA Microspheres

    Directory of Open Access Journals (Sweden)

    Rezaul H. Ansary

    2017-10-01

    Full Text Available Double-walled microspheres based on poly(lactide-co-glycolide (PLGA are potential delivery systems for reducing a very high initial burst release of encapsulated protein and peptide drugs. In this study, double-walled microspheres made of glucose core, hydroxyl-terminated poly(lactide-co-glycolide (Glu-PLGA, and carboxyl-terminated PLGA were fabricated using a modified water-in-oil-in-oil-in-water (w1/o/o/w2 emulsion solvent evaporation technique for the controlled release of a model protein, lysozyme. Microspheres size, morphology, encapsulation efficiency, lysozyme in vitro release profiles, bioactivity, and structural integrity, were evaluated. Scanning electron microscopy (SEM images revealed that double-walled microspheres comprising of Glu-PLGA and PLGA with a mass ratio of 1:1 have a spherical shape and smooth surfaces. A statistically significant increase in the encapsulation efficiency (82.52% ± 3.28% was achieved when 1% (w/v polyvinyl alcohol (PVA and 2.5% (w/v trehalose were incorporated in the internal and external aqueous phase, respectively, during emulsification. Double-walled microspheres prepared together with excipients (PVA and trehalose showed a better control release of lysozyme. The released lysozyme was fully bioactive, and its structural integrity was slightly affected during microspheres fabrication and in vitro release studies. Therefore, double-walled microspheres made of Glu-PLGA and PLGA together with excipients (PVA and trehalose provide a controlled and sustained release for lysozyme.

  19. Release of proteins via ion exchange from albumin-heparin microspheres

    NARCIS (Netherlands)

    Kwon, Glen S.; Bae, You Han; Cremers, H.F.M.; Cremers, Harry; Feijen, Jan; Kim, Sung Wan

    1992-01-01

    Albumin-heparin and albumin microspheres were prepared as ion exchange gels for the controlled release of positively charged polypeptides and proteins. The adsorption isotherms of chicken egg and human lysozyme, as model proteins, on microspheres were obtained. An adsorption isotherm of chicken egg

  20. Comparison of the effect of ibuprofen and slow-released Diclofenac Sodium in controlling post endodontic pain

    Directory of Open Access Journals (Sweden)

    Saatchi M

    2010-01-01

    Full Text Available "nBackground and Aims: Despite the significant improvement in dentistry, pain after endodontic therapy is still of concern for patients. Non-steroidal anti-inflammatory drugs are the most commonly prescribed oral analgesics used for dental pain relief after root canal treatment. The purpose of this study was to compare the effectiveness of Ibuprofen versus slow-released Diclofenac Sodium in controlling pain following root canal treatment. "nMaterials and Methods: In this randomized clinical trial, mandibular molars with irreversible pulpitis in 90 patients were selected. The patients were divided into three groups (Ibuprofen, slow-released Diclofenac Sodium and placebo. After examination patients filled in the consent form. Then they received one of the mentioned drugs. After inferior alveolar nerve block, access cavity was prepared and the root canals were prepared using passive step back method. The canals were dried and temporary filling material was placed. Then the pain evaluation form (visual analog scale was explained and delivered to the patients. Data were analyzed using Repeated Measurement ANOVA, Kruskal-wallis and Man-Whitney U tests. "nResults: The mean pain intensity in slow-released Diclofenac Sodium group was 0.87 0.95, 1.17 1.10 for Ibuprofen group, and 2.14  1.70 for placebo group. The differences between groups were statistically significant (P<0.001. The effect of Ibuprofen in controlling post endodontic pain in the first 2 hours was more than slow-released Diclofenac Sodium (P=0.01, but in 10, 18, and 36 hours after treatment, slow-released Diclofenac Sodium was more effective than Ibuprofen (P<0.001. "nConclusion: Premedication with single dose of slow-released Diclofenac Sodium can control post endodontic pain for a longer period of time compared with Ibuprofen. "n.

  1. Preparation of berbamine loaded chitosan-agarose microspheres and in vitro release study

    Directory of Open Access Journals (Sweden)

    Zhang Hu

    2012-01-01

    Full Text Available Berbamine loaded chitosan-agarose microspheres were prepared using a water-in-oil emulsion technique. Optimum preparing parameters were determined by orthogonal experiments as follows: ratio of berbamine to chitosan (w/w is 1:10; percentage of emulsifier (span 80, v/v is 6%; volume of glutaraldehyde is 2 mL; and reaction temperature is 70 ºC. Under these optimal conditions, the encapsulation efficiency and loading capacity of microspheres are 84.57% and 8.44%, respectively. The swelling tests showed that the microspheres possessed higher swelling ratio at pH 7.4 than at pH 1.2. FTIR indicated that berbamine had been successfully loaded in the chitosan-agarose microspheres by physical entrapment. In vitro release studies showed that berbamine was released from microspheres in a significantly sustained fashion.

  2. SOL-Gel microspheres and nanospheres for controlled release applications

    International Nuclear Information System (INIS)

    Barbe, C.; Beyer, R.; Kong, L.; Blackford, M.; Trautman, R.; Bartlett, J.

    2002-01-01

    We present a novel approach to the synthesis of inorganic sol-gel microspheres for encapsulating organic and bioactive molecules, and controlling their subsequent release kinetics. The bioactive species are incorporated, at ambient temperature, into the inorganic particles using an emulsion gelation process. Independent control of the release rate (by adapting the nanostructure of the internal pore network to the physico-chemical properties of the bioactive molecules) and particle size (by tailoring the emulsion chemistry) is demonstrated. Sol-gel chemistry has been shown to be a flexible technique for producing inorganic silica matrices with tailored microstructures, which can be used for the encapsulation and controlled release of organic and bioactive molecules. The present paper extends this concept by combining sol-gel chemistry with an emulsion approach for producing inorganic particles with controlled dimensions, and demonstrates how the particle size and microstructure can be independently controlled. Sol-Gel Chemistry and Encapsulation of Model Compounds. A stock solution of 4-(2-hydroxy-l-naphthylazo) benzene sulfonic acid (Orange II) was produced by dissolving Orange II in water (0.1 wt%), and adjusting the pH to the required value. Sol-gel solutions were subsequently prepared by mixing the aqueous solution with tetramethylorthosilicate (TMOS) and methanol (MeOH), to achieve H 2 O:TMOS (W] and MeOH:TMOS mole ratios (D) of four. The resulting solution was stirred and left to age at ambient temperature for one day. A transparent emulsion was prepared by mixing selected surfactants and organic solvents. The surfactants used included sorbitan monooleate, sorbitan monolaurate and bis-2-ethylhexylsulfo-succinate (AOT), while the organic phase was typically chosen from the group consisting of kerosene, hexane, heptane, octane, decane, dodecane and cyclohexane. The sol-gel solution was added to the emulsion, and the resulting mixture was stirred at 500 rpm for

  3. Sustained-release microsphere formulation containing an agrochemical by polyurethane polymerization during an agitation granulation process.

    Science.gov (United States)

    Terada, Takatoshi; Tagami, Manabu; Ohtsubo, Toshiro; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2016-07-25

    In this report, a new solventless microencapsulation method by synthesizing polyurethane (PU) from polyol and isocyanate during an agglomeration process in a high-speed mixing apparatus was developed. Clothianidin (CTD), which is a neonicotinoid insecticide and highly effective against a wide variety of insect pests, was used as the model compound. The microencapsulated samples covered with PU (CTD microspheres) had a median diameter of <75μm and sustained-release properties. The CTD microspheres were analyzed by synchrotron X-ray computed tomography measurements. Multiple cores of CTD and other solid excipient were dispersed in PU. Although voids appeared in the CTD microspheres after CTD release, the spherical shape of the microspheres remained stable and no change in its framework was observed. The experimental release data were highly consistent with the Baker-Lonsdale model derived from drug release of spherical monolithic dispersions and consistent with the computed tomography measurements. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

    Directory of Open Access Journals (Sweden)

    Vanessa L. Gonçalves

    2005-03-01

    Full Text Available In this work chitosan microspheres were prepared by the simple coacervation method and crosslinked using epichlorhydrin or glutaraldehyde for the controlled release of diclofenac sodium. The effects of the crosslinking agents on chitosan microspheres over a 12-hour period were assessed with regard to swelling, hydrolysis, porosity, crosslinking, impregnation of diclofenac sodium (DS, and consequently to the release of DS in buffer solutions, simulating the gastrointestinal tract. The degree of swelling varied with the pH for glutaraldehyde chitosan microspheres (GCM and epichlorhydrin chitosan microspheres (ECM. Partial acid and basic hydrolysis affected the swelling behavior of the GCM matrix. Release kinetics of diclofenac sodium from these matrices were investigated at pH 1.2, 6.8 and 9.0, simulating the gastrointestinal tract conditions. The results indicated that the release mechanism deviated slightly from Fickian transport.

  5. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    DEFF Research Database (Denmark)

    Guo, Wenjia; Quan, Peng; Fang, Liang

    2015-01-01

    -solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared...... release mechanism. After single-dose administration of DP microspheres via subcutaneous injection in rats, the plasma concentration of DP reached peak concentration at 0.50 d, and then declined gradually, but was still detectable at 15 d. A good correlation between in vitro and in vivo data was obtained...

  6. Effect of crosslinking agents on chitosan microspheres in controlled release of diclofenac sodium

    OpenAIRE

    Gonçalves,Vanessa L.; Laranjeira,Mauro C. M.; Fávere,Valfredo T.; Pedrosa,Rozângela C.

    2005-01-01

    In this work chitosan microspheres were prepared by the simple coacervation method and crosslinked using epichlorhydrin or glutaraldehyde for the controlled release of diclofenac sodium. The effects of the crosslinking agents on chitosan microspheres over a 12-hour period were assessed with regard to swelling, hydrolysis, porosity, crosslinking, impregnation of diclofenac sodium (DS), and consequently to the release of DS in buffer solutions, simulating the gastrointestinal tract. The degree ...

  7. Release kinetics and cell viability of ibuprofen nanocrystals produced by melt-emulsification.

    Science.gov (United States)

    Fernandes, A R; Dias-Ferreira, J; Cabral, C; Garcia, M L; Souto, E B

    2018-06-01

    The clinical use of poorly water-soluble drugs has become a big challenge in pharmaceutical development due to the compromised bioavailability of the drugs in vivo. Nanocrystals have been proposed as a formulation strategy to improve the dissolution properties of these drugs. The benefits of using nanocrystals in drug delivery, when compared to other nanoparticles, are related to their production facilities, simple structure, and suitability for a variety of administration routes. High pressure homogenization (HPH) is the most promising production process, which can be employed at low or high temperatures. Ibuprofen nanocrystals with a mean size below 175 nm, and polydispersity below 0.18, have been produced by melt-emulsification, followed by HPH. Two nanocrystal formulations, differing on the surfactant composition, have been produced, their in vitro ibuprofen release tested in Franz diffusion cells and adjusted to several kinetic models (zero order, first order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas, Baker-Lonsdale and Weibull model). Cell viability was assessed at 3, 6 and 24 h of incubation on human epithelial colorectal cells (Caco-2) by AlamarBlue ® colorimetric assay. For both formulations, Caco-2 cells viability was dependent on the drug concentration and time of exposure. Copyright © 2018 Elsevier B.V. All rights reserved.

  8. Evaluation of the Thermosensitive Release Properties of Microspheres Containing an Agrochemical Compound.

    Science.gov (United States)

    Terada, Takatoshi; Ohtsubo, Toshiro; Iwao, Yasunori; Noguchi, Shuji; Itai, Shigeru

    2017-01-01

    The purpose of this study was to develop a deeper understanding of the key physicochemical parameters involved in the release profiles of microsphere-encapsulated agrochemicals at different temperatures. Microspheres consisting of different polyurethanes (PUs) were prepared using our previously reported solventless microencapsulation technique. Notably, these microspheres exhibited considerable differences in their thermodynamic characteristics, including their glass transition temperature (T g ), extrapolated onset temperature (T o ) and extrapolated end temperature (T e ). At test temperatures below the T o of the PU, only 5-10% of the agrochemical was rapidly released from the microspheres within 1 d, and none was released thereafter. However, at test temperatures above the T o of the PU, the rate of agrochemical release gradually increased with increasing temperatures, and the rate of release from the microspheres was dependent on the composition of the PU. Taken together, these results show that the release profiles of the microspheres were dependent on their thermodynamic characteristics and changes in their PU composition.

  9. Core/shell PLGA microspheres with controllable in vivo release profile via rational core phase design.

    Science.gov (United States)

    Yu, Meiling; Yao, Qing; Zhang, Yan; Chen, Huilin; He, Haibing; Zhang, Yu; Yin, Tian; Tang, Xing; Xu, Hui

    2018-02-27

    Highly soluble drugs tend to release from preparations at high speeds, which make them need to be taken at frequent intervals. Additionally, some drugs need to be controlled to release in vivo at certain periods, so as to achieve therapeutic effects. Thus, the objective of this study is to design injectable microparticulate systems with controllable in vivo release profile. Biodegradable PLGA was used as the matrix material to fabricate microspheres using the traditional double emulsification-solvent evaporation method as well as improved techniques, with gel (5% gelatine or 25% F127) or LP powders as the inner phases. Their physicochemical properties were systemically investigated. Microspheres prepared by modified methods had an increase in drug loading (15.50, 16.72, 15.66%, respectively) and encapsulation efficiencies (73.46, 79.42, 74.40%, respectively) when compared with traditional methods (12.01 and 57.06%). The morphology of the particles was characterized by optical microscope (OM) and scanning electron microscopy (SEM), and the amorphous nature of the encapsulated drug was confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. To evaluate their release behaviour, the in vitro degradation, in vitro release and in vivo pharmacodynamics were subsequently studied. Traditional microspheres prepared in this study with water as the inner phase had a relatively short release period within 16 d when compared with modified microspheres with 5% gelatine as the inner phase, which resulted in a smooth release profile and appropriate plasma LP concentrations over 21 d. Thus this type of modified microspheres can be better used in drugs requiring sustained release. The other two formulations containing 25% F127 and LP micropowders presented two-stage release profiles, resulting in fluctuant plasma LP concentrations which may be suitable for drugs requiring controlled release. All the results suggested that drug release rates from

  10. Use of ibuprofen sustained release for treating osteoarthritic pain: findings from 15 general medical practices in Egypt

    Directory of Open Access Journals (Sweden)

    Khalifa N

    2014-05-01

    Full Text Available Nabil Khalifa,1 Timour El-Husseini,1 Ahmed Morrah,2 Elshenawy Mostafa,3 Hesham Hamoud41Department of Orthopedic Surgery, Ain Shams University, Cairo, Egypt; 2Department of Orthopedic Surgery, Cairo University, Cairo, Egypt; 3Department of Orthopedic Surgery, Mansoura University, Mansoura, Egypt; 4Department of Rheumatology, Azhar University, Cairo, EgyptPurpose: Ibuprofen sustained release (SR has been shown to provide effective symptomatic pain relief in chronic arthritic conditions such as osteoarthritis in European and US patient populations. Few studies have been conducted in other patient populations. A 4-week prospective multicenter open-label observational study was designed to explore and describe the combined effect of ibuprofen SR and standard medical care in patients suffering from osteoarthritis in 15 general medical practices in Egypt.Patients and methods: In total, 519 patients were prescribed ibuprofen SR 2 ×800 mg once daily for 4 weeks.Results: Ibuprofen SR combined with standard medical care significantly improved day and night pain, with 99.4% of the patients reporting improvement. The treatment reduced the symptom severity of joint tenderness/stiffness and the duration of morning stiffness, and allowed more patients to carry out normal activities. Overall compliance with the prescribed ibuprofen SR regimen was 98.6%. Ibuprofen SR was generally well tolerated with no serious adverse events reported during the study. There was no increase in blood pressure or heart rate.Conclusion: The combined treatment provided effective relief of pain in patients with osteoarthritis in a large real-life general medical practice setting in Egypt. Owing to its convenient once-daily dosing regimen, ibuprofen SR may enhance patient compliance.Keywords: chronic arthritis, compliance, pain score, real-life

  11. Sustained release of simvastatin from hollow carbonated hydroxyapatite microspheres prepared by aspartic acid and sodium dodecyl sulfate.

    Science.gov (United States)

    Wang, Ke; Wang, Yinjing; Zhao, Xu; Li, Yi; Yang, Tao; Zhang, Xue; Wu, Xiaoguang

    2017-06-01

    Hollow carbonated hydroxyapatite (HCHAp) microspheres as simvastatin (SV) sustained-release vehicles were fabricated through a novel and simple one-step biomimetic strategy. Firstly, hollow CaCO 3 microspheres were precipitated through the reaction of CaCl 2 with Na 2 CO 3 in the presence of aspartic acid and sodium dodecyl sulfate. Then, the as-prepared hollow CaCO 3 microspheres were transformed into HCHAp microspheres with a controlled anion-exchange method. The HCHAp microspheres were 3-5μm with a shell thickness of 0.5-1μm and were constructed of short needle nanoparticles. The HCHAp microspheres were then loaded with SV, exhibiting excellent drug-loading capacity and sustained release properties. These results present a new material synthesis strategy for HCHAp microspheres and suggest that the as-prepared HCHAp microspheres are promising for applications in drug delivery. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. The effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy

    International Nuclear Information System (INIS)

    Borin, M.T.; Khare, S.; Beihn, R.M.; Jay, M.

    1990-01-01

    The GI transit of radiolabeled sustained-release ibuprofen 800-mg tablets in eight healthy, fed volunteers was monitored using external gamma scintigraphy. Ibuprofen serum concentrations were determined from blood samples drawn over 36 hr following dosing. Sustained-release ibuprofen tablets containing 0.18% of 170Er2O3 (greater than 96% 170Er) in the bulk formulation were manufactured under pilot-scale conditions and were radiolabeled utilizing a neutron activation procedure which converted stable 170Er to radioactive 171Er (t1/2 = 7.5 hr). At the time of dosing, each tablet contained 50 mu Ci of 171Er. Dosage form position were reported at various time intervals. In five subjects the sustained-release tablet remained in the stomach and eroded slowly over 7-12 hr, resulting in gradual increases in small bowel radioactivity. In the remaining three subjects, the intact tablet was ejected from the stomach and a gastric residence time of approximately 4 hr was measured. This is in marked contrast to a previous study conducted in fasted volunteers in which gastric retention time ranged from 10 to 60 min. Differences in GI transit between fed and fasted volunteers had little effect on ibuprofen bioavailability. AUC and Tmax were unaltered and Cmax was increased by 24%, which is in agreement with results from a previous, crossover-design food effect study

  13. Deposition of Ibuprofen Crystals on Hydroxypropyl Cellulose/Polyacrylamide Gel: Experimental and Mathematic Modeling Releasing

    Directory of Open Access Journals (Sweden)

    Claudia Alicia Castillo-Miranda

    2016-01-01

    Full Text Available The crystallization of nonsteroidal anti-inflammatory drug [2-(4-isobutyl-phenyl propionic acid] ibuprofen (IBP on a hydroxypropyl cellulose (HPC and polyacrylamide (PAAm gel was studied as well as the release kinetics of the drug. The IBP was crystallized on the gel surface of HPC/PAAm. It had a prismatic shape and the growth was made in an aqueous medium; the crystallinity grade of the gels HPC/PAAm and HPC/PAAm-IBU increased to 68% and to 58%, respectively. The release of IBP is performed by two means: by a non-Fickian diffusion process and by relaxation of the chains of the gel; without regard to temperature and the diffusion media, this correlates with the lower critical solution temperature (LCST of the proposed gel. This polymer matrix provides an option for releasing nonsteroidal anti-inflammatory drugs in a temperature range of 35–39°C. Korsmeyer and Peppas mathematical model was simulated for data releases, statistically significant at 95% confidence level.

  14. Design of sustained-release nitrendipine microspheres having solid dispersion structure by quasi-emulsion solvent diffusion method

    DEFF Research Database (Denmark)

    Cui, Fude; Yang, Mingshi; Jiang, Yanyan

    2003-01-01

    crystallization technique, i.e. quasi-emulsion solvent diffusion method. The factors of effect on micromeritic properties and release profiles of the resultant microspheres were investigated. And the bioavailability of nitrendipine microspheres was evaluated in six healthy dogs. The results showed...... that the particle size of microspheres was determined mainly by the agitation speed. The dissolution rate of nitrendipine from microspheres was enhanced significantly with increasing the amount of dispersing agents, and sustained by adding retarding agents. The release rate of microspheres could be controlled...

  15. Effect of WOW process parameters on morphology and burst release of FITC-dextran loaded PLGA microspheres.

    Science.gov (United States)

    Mao, Shirui; Xu, Jing; Cai, Cuifang; Germershaus, Oliver; Schaper, Andreas; Kissel, Thomas

    2007-04-04

    Using fluorescein isothiocyanate labeled dextran (FITC-dextran 40, FD40) as a hydrophilic model compound, microspheres were prepared by a WOW double emulsion technique. Influence of process parameters on microsphere morphology and burst release of FD40 from PLGA microspheres was studied. Internal morphology of microspheres was investigated by stereological method via cryo-cutting technique and scanning electron microscopy (SEM). Drug distribution in microspheres was observed with confocal laser scanning microscopy (CLSM). Polymer nature (RG503 and RG503H) had significant influence on the micro-morphology of microspheres. Increase in continuous water phase volume (W2) led to increased surface porosity but decreased internal porosity. By increasing PVA concentration in the continuous phase from 0.1 to 1%, particle size changed marginally but burst release decreased from 12.2 to 5.9%. Internal porosity of microspheres decreased considerably with increasing polymer concentration. Increase in homogenization speed during the primary emulsion preparation led to decreased internal porosity. Burst release decreased with increasing drug loading but increased with drug molecular weight. Drug distribution in microspheres depended on preparation method. The porosity of microspheres decreased with time in the diffusion stage, but internal morphology had no influence on the release behavior in the bioerosion stage. In summary, surface porosity and internal morphology play a significant role in the release of hydrophilic macromolecules from biodegradable microspheres in the initial release phase characterized by pore diffusion.

  16. Building a polysaccharide hydrogel capsule delivery system for control release of ibuprofen.

    Science.gov (United States)

    Chen, Zhi; Wang, Ting; Yan, Qing

    2018-02-01

    Development of a delivery system which can effectively carry hydrophobic drugs and have pH response is becoming necessary. Here we demonstrate that through preparation of β-cyclodextrin polymer (β-CDP), a hydrophobic drug molecule of ibuprofen (IBU) was incorporated into our prepared β-CDP inner cavities, aiming to improve the poor water solubility of IBU. A core-shell capsule structure has been designed for achieving the drug pH targeted and sustained release. This delivery system was built with polysaccharide polymer of Sodium alginate (SA), sodium carboxymethylcellulose (CMC) and hydroxyethyl cellulose (HEC) by physical cross-linking. The drug pH-response control release is this hydrogel system's chief merit, which has potential value for synthesizing enteric capsule. Besides, due to our simple preparing strategy, optimal conditions can be readily determined and the synthesis process can be accurately controlled, leading to consistent and reproducible hydrogel capsules. In addition, phase-solubility method was used to investigate the solubilization effect of IBU by β-CDP. SEM was used to prove the forming of core and shell structure. FT-IR and 1 H-NMR were also used to perform structural characteristics. By the technique of UV determination, the pH targeted and sustained release study were also performed. The results have proved that our prepared polysaccharide hydrogel capsule delivery system has potential applications as oral drugs delivery in the field of biomedical materials.

  17. Electrospray synthesis and properties of hierarchically structured PLGA TIPS microspheres for use as controlled release technologies.

    Science.gov (United States)

    Malik, Salman A; Ng, Wing H; Bowen, James; Tang, Justin; Gomez, Alessandro; Kenyon, Anthony J; Day, Richard M

    2016-04-01

    Microsphere-based controlled release technologies have been utilized for the long-term delivery of proteins, peptides and antibiotics, although their synthesis poses substantial challenges owing to formulation complexities, lack of scalability, and cost. To address these shortcomings, we used the electrospray process as a reproducible, synthesis technique to manufacture highly porous (>94%) microspheres while maintaining control over particle structure and size. Here we report a successful formulation recipe used to generate spherical poly(lactic-co-glycolic) acid (PLGA) microspheres using the electrospray (ES) coupled with a novel thermally induced phase separation (TIPS) process with a tailored Liquid Nitrogen (LN2) collection scheme. We show how size, shape and porosity of resulting microspheres can be controlled by judiciously varying electrospray processing parameters and we demonstrate examples in which the particle size (and porosity) affect release kinetics. The effect of electrospray treatment on the particles and their physicochemical properties are characterized by scanning electron microscopy, confocal Raman microscopy, thermogravimetric analysis and mercury intrusion porosimetry. The microspheres manufactured here have successfully demonstrated long-term delivery (i.e. 1week) of an active agent, enabling sustained release of a dye with minimal physical degradation and have verified the potential of scalable electrospray technologies for an innovative TIPS-based microsphere production protocol. Copyright © 2016 The Authors. Published by Elsevier Inc. All rights reserved.

  18. Accelerated in vitro release testing method for naltrexone loaded PLGA microspheres.

    Science.gov (United States)

    Andhariya, Janki V; Choi, Stephanie; Wang, Yan; Zou, Yuan; Burgess, Diane J; Shen, Jie

    2017-03-30

    The objective of the present study was to develop a discriminatory and reproducible accelerated release testing method for naltrexone loaded parenteral polymeric microspheres. The commercially available naltrexone microsphere product (Vivitrol ® ) was used as the testing formulation in the in vitro release method development, and both sample-and-separate and USP apparatus 4 methods were investigated. Following an in vitro drug stability study, frequent media replacement and addition of anti-oxidant in the release medium were used to prevent degradation of naltrexone during release testing at "real-time" (37°C) and "accelerated" (45°C), respectively. The USP apparatus 4 method was more reproducible than the sample-and-separate method. In addition, the accelerated release profile obtained using USP apparatus 4 had a shortened release duration (within seven days), and good correlation with the "real-time" release profile. Lastly, the discriminatory ability of the developed accelerated release method was assessed using compositionally equivalent naltrexone microspheres with different release characteristics. The developed accelerated USP apparatus 4 release method was able to detect differences in the release characteristics of the prepared naltrexone microspheres. Moreover, a linear correlation was observed between the "real-time" and accelerated release profiles of all the formulations investigated, suggesting that the release mechanism(s) may be similar under both conditions. These results indicate that the developed accelerated USP apparatus 4 method has the potential to be an appropriate fast quality control tool for long-acting naltrexone PLGA microspheres. Copyright © 2017 Elsevier B.V. All rights reserved.

  19. Preparation of microspheres for slow release drug by radiation-induced suspension polymerization and their properties

    International Nuclear Information System (INIS)

    Yoshida, Masaru; Asano, Masaharu; Kaetsu, Isao

    1982-01-01

    The polymer microspheres containing drugs as drug delivery system were made by means of suspension-polymerization by radiation at low temperature by using glass-forming monomers which have stable supercooling properties and large polymerizability at low temperature. The particle distribution depended on the kind of monomer. It was found that the entrapping yield of drug in polymer microspheres increased with increasing viscosity of monomer and that the maximum value on the particle size distribution curve was also shifted to large particle diameter side. In the case of trimethylolpropane trimethacrylate monomer (43 cps), TMPT, the entrapping yield of drug reached 74% and the maximum value in particle size distribution curve appeared in the neighborhood of 105 to 210 mu m ranges. On the other hand, those values in neopentyl glycol dimethacrylate monomer (4 cps) were 12% in former and 44 -- 105 mu m in the latter. The release phenomenon of drugs from polymer microspheres was investigated. for example, the cumulative amount of mitomycin C (water soluble drug) released from TMPT polymer microsphere was about 90% after 30-day dissolution, while in the case of water-insoluble drug such as testosterone the amount of release was about 49% after 40-day dissolution. In all cases, the release rate is constant during the experimental period. Therefore, it was concluded that the release of drugs from polymer microspheres obtained in this study is possible over the long periods. (author)

  20. Sustained release donepezil loaded PLGA microspheres for injection: Preparation, in vitro and in vivo study

    Directory of Open Access Journals (Sweden)

    Wenjia Guo

    2015-10-01

    Full Text Available The purpose of this study was to develop a PLGA microspheres-based donepezil (DP formulation which was expected to sustain release of DP for one week with high encapsulation efficiency (EE. DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method. The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size, morphology, drug loading and EE, physical state of DP in the matrix and in vitro and in vivo release behavior. DP microspheres were prepared successfully with average diameter of 30 µm, drug loading of 15.92 ± 0.31% and EE up to 78.79 ± 2.56%. Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface. Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres. The Tg of PLGA was increased with the addition of DP. The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model, which suggested the diffusion governing release mechanism. After single-dose administration of DP microspheres via subcutaneous injection in rats, the plasma concentration of DP reached peak concentration at 0.50 d, and then declined gradually, but was still detectable at 15 d. A good correlation between in vitro and in vivo data was obtained. The results suggest the potential use of DP microspheres for treatment of Alzheimer's disease over long periods.

  1. Biocompatible magnetic and molecular dual-targeting polyelectrolyte hybrid hollow microspheres for controlled drug release.

    Science.gov (United States)

    Du, Pengcheng; Zeng, Jin; Mu, Bin; Liu, Peng

    2013-05-06

    Well-defined biocompatible magnetic and molecular dual-targeting polyelectrolyte hybrid hollow microspheres have been accomplished via the layer-by-layer (LbL) self-assembly technique. The hybrid shell was fabricated by the electrostatic interaction between the polyelectrolyte cation, chitosan (CS), and the hybrid anion, citrate modified ferroferric oxide nanoparticles (Fe3O4-CA), onto the uniform polystyrene sulfonate microsphere templates. Then the magnetic hybrid core/shell composite particles were modified with a linear, functional poly(ethylene glycol) (PEG) monoterminated with a biotargeting molecule (folic acid (FA)). Afterward the dual targeting hybrid hollow microspheres were obtained after etching the templates by dialysis. The dual targeting hybrid hollow microspheres exhibit exciting pH response and stability in high salt-concentration media. Their pH-dependent controlled release of the drug molecule (anticancer drug, doxorubicin (DOX)) was also investigated in different human body fluids. As expected, the cell viability of the HepG2 cells which decreased more rapidly was treated by the FA modified hybrid hollow microspheres rather than the unmodified one in the in vitro study. The dual-targeting hybrid hollow microspheres demonstrate selective killing of the tumor cells. The precise magnetic and molecular targeting properties and pH-dependent controlled release offers promise for cancer treatment.

  2. Clinically relevant pain relief with an ibuprofen-releasing foam dressing

    DEFF Research Database (Denmark)

    Fogh, Karsten; Andersen, Maibritt B; Bischoff-Mikkelsen, Morten

    2012-01-01

    The objective of this 6-week, 120-patient, double-blind, randomized, controlled trial was to investigate if a foam dressing with ibuprofen provided clinically relevant pain relief (PAR) for exuding, painful venous leg ulcers in comparison with a similar foam dressing without ibuprofen. Primary......) and the corresponding number needed to treat (NNT). Wound-related parameters such as ulcer healing, ulcer area reduction, and peri-ulcer skin condition as well as adverse events were recorded during all 6 weeks of the investigation. PAR was significantly greater in the ibuprofen foam group than the comparator group (p...... = 0.0438). There were 34% responders in the ibuprofen foam group vs. 19% in the comparator group (NNT = 6.8). When evening data were analyzed separately to evaluate PAR over daytime, NNT was 5.3. Wound healing parameters and adverse events were comparable. In conclusion, in this study, the ibuprofen...

  3. Preparation of hydroxypropyl cyclosophoraose/dextran microspheres for the controlled release of ciprofloxacin

    International Nuclear Information System (INIS)

    Lee, Benel; Jeong, Da Ham; Joo, Sang Woo; Choi, Jae Min; Jung, Seung Ho; Cho, Eun Na; Lee, Jae Yung; Park, Se Yeon

    2016-01-01

    Hydroxypropyl cyclosophoraose/dextran (HPCys/dextran) microspheres were prepared using an emulsion polymerization method for use as drug carriers to achieve the controlled release of a poorly water-soluble antibacterial drug, ciprofloxacin (CFX). Cyclosophoraoses are cyclic (1 → 2)-β-d-glucans isolated from the Rhizobium species. Characteristics of HPCys/dextran microspheres were investigated using Fourier transform infrared analysis, solid-state 13C nuclear magnetic resonance spectroscopy, and field emission scanning electron microscopy. The amount of CFX released from these microspheres at pH 7.4 (intestinal phase pH) was about two times higher than that released at pH 1.2 (gastric phase pH). Furthermore, HPCys/dextran microspheres did not show any toxicity in human embryonic kidney cells. We propose that HPCys/dextran microspheres could be used as an effective pH-dependent release system for poorly water-soluble drugs such as CFX

  4. Preparation of hydroxypropyl cyclosophoraose/dextran microspheres for the controlled release of ciprofloxacin

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Benel; Jeong, Da Ham; Joo, Sang Woo; Choi, Jae Min; Jung, Seung Ho; Cho, Eun Na [Center for Biotechnology Research in UBITA (CBRU), Konkuk University, Seoul (Korea, Republic of); Lee, Jae Yung [Dept. Biological Science, Mokpo National University, Mokpo (Korea, Republic of); Park, Se Yeon [Dept. Applied Chemistry, Dongduk Women' s University, Seoul (Korea, Republic of)

    2016-12-15

    Hydroxypropyl cyclosophoraose/dextran (HPCys/dextran) microspheres were prepared using an emulsion polymerization method for use as drug carriers to achieve the controlled release of a poorly water-soluble antibacterial drug, ciprofloxacin (CFX). Cyclosophoraoses are cyclic (1 → 2)-β-d-glucans isolated from the Rhizobium species. Characteristics of HPCys/dextran microspheres were investigated using Fourier transform infrared analysis, solid-state 13C nuclear magnetic resonance spectroscopy, and field emission scanning electron microscopy. The amount of CFX released from these microspheres at pH 7.4 (intestinal phase pH) was about two times higher than that released at pH 1.2 (gastric phase pH). Furthermore, HPCys/dextran microspheres did not show any toxicity in human embryonic kidney cells. We propose that HPCys/dextran microspheres could be used as an effective pH-dependent release system for poorly water-soluble drugs such as CFX.

  5. Synthesis and characterization of emamectin-benzoate slow-release microspheres with different surfactants.

    Science.gov (United States)

    Wang, Yan; Wang, Anqi; Wang, Chunxin; Cui, Bo; Sun, Changjiao; Zhao, Xiang; Zeng, Zhanghua; Shen, Yue; Gao, Fei; Liu, Guoqiang; Cui, Haixin

    2017-10-06

    Pesticide slow-release formulations provide a way to increase the efficiency of active components by reducing the amount of pesticide that needs to be applied. Slow-release formulations also increase the stability and prolong the control effect of photosensitive pesticides. Surfactants are an indispensable part of pesticide formulations, and the choice of surfactant can strongly affect formulation performance. In this study, emamectin-benzoate (EMB) slow-release microspheres were prepared by the microemulsion polymerization method. We explored the effect of different surfactants on the particle size and dispersity of EMB in slow-release microspheres. The results indicated that the samples had uniform spherical shapes with an average diameter of 320.5 ±5.24 nm and good dispersity in the optimal formulation with the polymeric stabilizer polyvinyl alcohol (PVA) and composite non-ionic surfactant polyoxyethylene castor oil (EL-40). The optimal EMB pesticide slow-release microspheres had excellent anti-photolysis performance, stability, controlled release properties, and good leaf distribution. These results demonstrated that EMB slow-release microspheres are an attractive candidate for improving pesticide efficacy and prolonging the control effect of EMB in the environment.

  6. Alginate microspheres containing temperature sensitive liposomes (TSL) for MR-guided embolization and triggered release of doxorubicin

    NARCIS (Netherlands)

    van Elk, M.; Ozbakir, B.; Barten-Rijbroek, A.D.; Storm, Gerrit; Nijsen, F.; Hennink, W.E.; Vermonden, T.; Deckers, R.

    2015-01-01

    Objective The objective of this study was to develop and characterize alginate microspheres suitable for embolization with on-demand triggered doxorubicin (DOX) release and whereby the microspheres as well as the drug releasing process can be visualized in vivo using MRI. Methods and Findings For

  7. Alginate Microspheres Containing Temperature Sensitive Liposomes (TSL) for MR-Guided Embolization and Triggered Release of Doxorubicin

    NARCIS (Netherlands)

    van Elk, Merel; Ozbakir, Burcin; Barten-Rijbroek, Angelique D.; Storm, Gert; Nijsen, JFW; Hennink, Wim E.; Vermonden, Tina; Deckers, RHR

    2015-01-01

    Objective The objective of this study was to develop and characterize alginate microspheres suitable for embolization with on-demand triggered doxorubicin (DOX) release and whereby the microspheres as well as the drug releasing process can be visualized in vivo using MRI. Methods and Findings For

  8. Controlled release profiles of dipyridamole from biodegradable microspheres on the base of poly(3-hydroxybutyrate.

    Directory of Open Access Journals (Sweden)

    2007-12-01

    Full Text Available Novel biodegradable microspheres on the base of poly(3-hydroxybutyrate (PHB designed for controlled release of antithrombotic drug, namely dipyridamole (DPD, have been kinetically studied. The profiles of release from the microspheres with different diameters 4, 9, 63, and 92 µm present the progression of nonlinear and linear stages. Diffusionkinetic equation describing both linear (PHB hydrolysis and nonlinear (diffusion stages of the DPD release profiles from the spherical subjects has been written down as the sum of two terms: desorption from the homogeneous sphere in accordance with diffusion mechanism and the zero-order release. In contrast to the diffusivity dependence on microsphere size, the constant characteristics (k of linearity are scarcely affected by the diameter of PHB microparticles. The view of the kinetic profiles as well as the low rate of DPD release are in satisfactory agreement with kinetics of weight loss measured in vitro for the PHB films. Taking into account kinetic results, we suppose that the degradation of both films and PHB microspheres is responsible for the linear stage of DPD release profiles. In the nearest future, combination of biodegradable PHB and DPD as a representative of proliferation cell inhibitors will give possibility to elaborate the novel injectable therapeutic system for a local, long-term, antiproliferative action.

  9. Fabrication and evaluation of a sustained-release chitosan-based scaffold embedded with PLGA microspheres

    International Nuclear Information System (INIS)

    Song, Kedong; Liu, Yingchao; Macedo, Hugo M.; Jiang, Lili; Li, Chao; Mei, Guanyu; Liu, Tianqing

    2013-01-01

    Nutrient depletion within three-dimensional (3D) scaffolds is one of the major hurdles in the use of this technology to grow cells for applications in tissue engineering. In order to help in addressing it, we herein propose to use the controlled release of encapsulated nutrients within polymer microspheres into chitosan-based 3D scaffolds, wherein the microspheres are embedded. This method has allowed maintaining a stable concentration of nutrients within the scaffolds over the long term. The polymer microspheres were prepared using multiple emulsions (w/o/w), in which bovine serum albumin (BSA) and poly (lactic-co-glycolic) acid (PLGA) were regarded as the protein pattern and the exoperidium material, respectively. These were then mixed with a chitosan solution in order to form the scaffolds by cryo-desiccation. The release of BSA, entrapped within the embedded microspheres, was monitored with time using a BCA kit. The morphology and structure of the PLGA microspheres containing BSA before and after embedding within the scaffold were observed under a scanning electron microscope (SEM). These had a round shape with diameters in the range of 27–55 μm, whereas the chitosan-based scaffolds had a uniform porous structure with the microspheres uniformly dispersed within their 3D structure and without any morphological change. In addition, the porosity, water absorption and degradation rate at 37 °C in an aqueous environment of 1% chitosan-based scaffolds were (92.99 ± 2.51) %, (89.66 ± 0.66) % and (73.77 ± 3.21) %, respectively. The studies of BSA release from the embedded microspheres have shown a sustained and cumulative tendency with little initial burst, with (20.24 ± 0.83) % of the initial amount released after 168 h (an average rate of 0.12%/h). The protein concentration within the chitosan-based scaffolds after 168 h was found to be (11.44 ± 1.81) × 10 −2 mg/mL. This novel chitosan-based scaffold embedded with PLGA microspheres has proven to be a

  10. Fabrication and evaluation of a sustained-release chitosan-based scaffold embedded with PLGA microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Song, Kedong, E-mail: kedongsong@dlut.edu.cn [Dalian R and D Center for Stem Cell and Tissue Engineering, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024 (China); Liu, Yingchao [Dalian R and D Center for Stem Cell and Tissue Engineering, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024 (China); Macedo, Hugo M. [Biological Systems Engineering Laboratory, Department of Chemical Engineering, Department of Chemical Engineering, South Kensington Campus, London SW7 2AZ (United Kingdom); Jiang, Lili; Li, Chao; Mei, Guanyu [Dalian R and D Center for Stem Cell and Tissue Engineering, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024 (China); Liu, Tianqing, E-mail: liutq@dlut.edu.cn [Dalian R and D Center for Stem Cell and Tissue Engineering, State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116024 (China)

    2013-04-01

    Nutrient depletion within three-dimensional (3D) scaffolds is one of the major hurdles in the use of this technology to grow cells for applications in tissue engineering. In order to help in addressing it, we herein propose to use the controlled release of encapsulated nutrients within polymer microspheres into chitosan-based 3D scaffolds, wherein the microspheres are embedded. This method has allowed maintaining a stable concentration of nutrients within the scaffolds over the long term. The polymer microspheres were prepared using multiple emulsions (w/o/w), in which bovine serum albumin (BSA) and poly (lactic-co-glycolic) acid (PLGA) were regarded as the protein pattern and the exoperidium material, respectively. These were then mixed with a chitosan solution in order to form the scaffolds by cryo-desiccation. The release of BSA, entrapped within the embedded microspheres, was monitored with time using a BCA kit. The morphology and structure of the PLGA microspheres containing BSA before and after embedding within the scaffold were observed under a scanning electron microscope (SEM). These had a round shape with diameters in the range of 27–55 μm, whereas the chitosan-based scaffolds had a uniform porous structure with the microspheres uniformly dispersed within their 3D structure and without any morphological change. In addition, the porosity, water absorption and degradation rate at 37 °C in an aqueous environment of 1% chitosan-based scaffolds were (92.99 ± 2.51) %, (89.66 ± 0.66) % and (73.77 ± 3.21) %, respectively. The studies of BSA release from the embedded microspheres have shown a sustained and cumulative tendency with little initial burst, with (20.24 ± 0.83) % of the initial amount released after 168 h (an average rate of 0.12%/h). The protein concentration within the chitosan-based scaffolds after 168 h was found to be (11.44 ± 1.81) × 10{sup −2} mg/mL. This novel chitosan-based scaffold embedded with PLGA microspheres has proven to be a

  11. Effects of Polymeric Additives on the Crystallization and Release Behavior of Amorphous Ibuprofen

    Directory of Open Access Journals (Sweden)

    Su Yang Lee

    2013-01-01

    Full Text Available Some polymeric additives were studied to understand their effects on the amorphous phase of ibuprofen (IBU, used as a poorly water soluble pharmaceutical model compound. The amorphous IBU in bulk, as well as in nanopores (diameter ~24 nm of anodic aluminum oxide, was examined with the addition of poly(acrylic acid, poly(N-vinyl pyrrolidone, or poly(4-vinylphenol. Results of bulk crystallization showed that they were effective in limiting the crystal growth, while the nucleation of the crystalline phase in contact with water was nearly instantaneous in all cases. Poly(N-vinyl pyrrolidone, the most effective additive, was in specific interaction with IBU, as revealed by IR spectroscopy. The addition of the polymers was combined with the nanoscopic confinement to further stabilize the amorphous phase. Still, the IBU with addition of polymeric additives showed sustained release behavior. The current study suggested that the inhibition of the crystal nucleation was probably the most important factor to stabilize the amorphous phase and fully harness its high solubility.

  12. Accelerated dissolution testing for controlled release microspheres using the flow-through dissolution apparatus.

    Science.gov (United States)

    Collier, Jarrod W; Thakare, Mohan; Garner, Solomon T; Israel, Bridg'ette; Ahmed, Hisham; Granade, Saundra; Strong, Deborah L; Price, James C; Capomacchia, A C

    2009-01-01

    Theophylline controlled release capsules (THEO-24 CR) were used as a model system to evaluate accelerated dissolution tests for process and quality control and formulation development of controlled release formulations. Dissolution test acceleration was provided by increasing temperature, pH, flow rate, or adding surfactant. Electron microscope studies on the theophylline microspheres subsequent to each experiment showed that at pH values of 6.6 and 7.6 the microspheres remained intact, but at pH 8.6 they showed deterioration. As temperature was increased from 37-57 degrees C, no change in microsphere integrity was noted. Increased flow rate also showed no detrimental effect on integrity. The effect of increased temperature was determined to be the statistically significant variable.

  13. Preparation and characterization of genipin-cross-linked silk fibroin/chitosan sustained-release microspheres

    Directory of Open Access Journals (Sweden)

    Zeng SG

    2015-05-01

    Full Text Available Shuguang Zeng,1,* Manwen Ye,1,2,* Junqi Qiu,1 Wei Fang,1 Mingdeng Rong,1 Zehong Guo,1 Wenfen Gao11Department of Oral and Maxillofacial Surgery, Guangdong Provincial Stomatological Hospital, Southern Medical University, 2Department of Stomatology, Guangdong Women and Children Hospital, Guangzhou Medical University, Guangzhou, Guangdong, People’s Republic of China*These authors contributed equally to this workAbstract: We report the effects of distinct concentrations of genipin and silk fibroin (SF:chitosan (CS ratios on the formation of SF–CS composite microspheres. We selected microspheres featuring an SF:CS ratio of 1:1, encapsulated various concentrations of bovine serum albumin (BSA, and then compared their encapsulation efficiency and sustained-release rate with those of pure CS microspheres. We determined that the following five groups of microspheres were highly spherical and featured particle sizes ranging from 70 µm to 147 µm: mass ratio of CS:SF =1:0.5, 0.1 g or 0.5 g genipin; CS:SF =1:1, 0.05 g or 1 g genipin; and CS:SF =1:2, 0.5 g genipin. The microspheres prepared using 1:1 CS:SF ratio and 0.05 g genipin in the presence of 10 mg, 20 mg, and 50 mg of BSA exhibited encapsulation efficiencies of 50.16%±4.32%, 56.58%±3.58%, and 42.19%±7.47%, respectively. Fourier-transform infrared spectroscopy (FTIR results showed that SF and CS were cross-linked and that the α-helices and random coils of SF were converted into β-sheets. BSA did not chemically react with CS or SF. Moreover, thermal gravimetric analysis (TGA results showed that the melting point of BSA did not change, which confirmed the FTIR results, and X-ray diffraction results showed that BSA was entrapped in microspheres in a noncrystalline form, which further verified the TGA and FTIR data. The sustained-release microspheres prepared in the presence of 10 mg, 20 mg, and 50 mg of BSA burst release 30.79%±3.43%, 34.41%±4.46%, and 41.75%±0.96% of the

  14. Encapsulation of naproxen in lipid-based matrix microspheres: characterization and release kinetics.

    Science.gov (United States)

    Bhoyar, P K; Morani, D O; Biyani, D M; Umekar, M J; Mahure, J G; Amgaonkar, Y M

    2011-04-01

    The objective of this study was to microencapsulate the anti-inflammatory drug (naproxen) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. Naproxen was microencapsulated with lipid-like carnauba wax, hydrogenated castor oil using modified melt dispersion (modified congealable disperse phase encapsulation) technique. Effect of various formulation and process variables such as drug-lipid ratio, concentration of modifier, concentration of dispersant, stirring speed, stirring time, temperature of external phase, on evaluatory parameters such as size, entrapment efficiency, and in vitro release of naproxen were studied. The microspheres were characterized for particle size, scanning electron microscopy (SEM), FT-IR spectroscopy, drug entrapment efficiency, in vitro release studies, for in vitro release kinetics. The shape of microspheres was found to be spherical by SEM. The drug entrapment efficiency of various batches of microspheres was found to be ranging from 60 to 90 %w/w. In vitro drug release studies were carried out up to 24 h in pH 7.4 phosphate buffer showing 50-65% drug release. In vitro drug release from all the batches showed better fitting with the Korsmeyer-Peppas model, indicating the possible mechanism of drug release to be by diffusion and erosion of the lipid matrix.

  15. Controlled drug release from a novel injectable biodegradable microsphere/scaffold composite based on poly(propylene fumarate).

    Science.gov (United States)

    Kempen, Diederik H R; Lu, Lichun; Kim, Choll; Zhu, Xun; Dhert, Wouter J A; Currier, Bradford L; Yaszemski, Michael J

    2006-04-01

    The ideal biomaterial for the repair of bone defects is expected to have good mechanical properties, be fabricated easily into a desired shape, support cell attachment, allow controlled release of bioactive factors to induce bone formation, and biodegrade into nontoxic products to permit natural bone formation and remodeling. The synthetic polymer poly(propylene fumarate) (PPF) holds great promise as such a biomaterial. In previous work we developed poly(DL-lactic-co-glycolic acid) (PLGA) and PPF microspheres for the controlled delivery of bioactive molecules. This study presents an approach to incorporate these microspheres into an injectable, porous PPF scaffold. Model drug Texas red dextran (TRD) was encapsulated into biodegradable PLGA and PPF microspheres at 2 microg/mg microsphere. Five porous composite formulations were fabricated via a gas foaming technique by combining the injectable PPF paste with the PLGA or PPF microspheres at 100 or 250 mg microsphere per composite formulation, or a control aqueous TRD solution (200 microg per composite). All scaffolds had an interconnected pore network with an average porosity of 64.8 +/- 3.6%. The presence of microspheres in the composite scaffolds was confirmed by scanning electron microscopy and confocal microscopy. The composite scaffolds exhibited a sustained release of the model drug for at least 28 days and had minimal burst release during the initial phase of release, as compared to drug release from microspheres alone. The compressive moduli of the scaffolds were between 2.4 and 26.2 MPa after fabrication, and between 14.9 and 62.8 MPa after 28 days in PBS. The scaffolds containing PPF microspheres exhibited a significantly higher initial compressive modulus than those containing PLGA microspheres. Increasing the amount of microspheres in the composites was found to significantly decrease the initial compressive modulus. The novel injectable PPF-based microsphere/scaffold composites developed in this study

  16. Albumin/gentamicin microspheres produced by supercritical assisted atomization: optimization of size, drug loading and release.

    Science.gov (United States)

    Della Porta, G; Adami, R; Del Gaudio, P; Prota, L; Aquino, R; Reverchon, E

    2010-11-01

    In this work, the supercritical assisted atomization (SAA) is proposed, for the first time, not only as a micronization technology but also as a thermal coagulation process for the production of bovine serum albumin (BSA) microspheres charged with Gentamicin sulfate (GS). Particularly, different water solutions of BSA/GS were processed by SAA to produce protein microspheres with different size and antibiotic content. SAA precipitation temperature was selected in the range 100-130 °C to generate protein coagulation and to recover micronized BSA in form of hydrophobic aggregates; GS loading was varied between 10% and 50% (w/w) with an encapsulation efficiency which often reached 100%. In all cases, spherical and noncoalescing particles were successfully produced with a mean particle size of 2 µm and with a standard deviation of about ±1 µm. The microspheres also showed a good stability and constant water content after 60 days of storage. The release profiles of the entrapped drug were monitored using Franz cells to evaluate the possible application of the produced microspheres in wound dressing formulations. Particularly, the microspheres with a BSA/GS ratio of 4:1 after the first burst effect (of 40% of GS loaded) were able to release the GS continuously over 10 days. © 2010 Wiley-Liss, Inc. and the American Pharmacists Association

  17. Correlation of ibuprofen bioavailability with gastrointestinal transit by scintigraphic monitoring of 171Er-labeled sustained-release tablets

    International Nuclear Information System (INIS)

    Parr, A.F.; Beihn, R.M.; Franz, R.M.; Szpunar, G.J.; Jay, M.

    1987-01-01

    External gamma scintigraphy was used to monitor the gastrointestinal (GI) transit of radiolabeled sustained-release tablets containing 800 mg ibuprofen in eight fasted healthy volunteers. Ibuprofen serum concentrations were determined from blood samples drawn sequentially over a 24-hr period. Serum concentrations and related parameters were correlated to the position of the dosage form in the GI tract from the scintiphotos. The sustained-release tablets were radiolabeled intact utilizing a neutron activation procedure, by incorporating 0.18% of 170 Er2O3 (enriched to greater than 96% 170 Er) into the bulk formulation. After manufacture of the final dosage forms, the tablets were irradiated in a neutron flux (4.4 x 10(13) n/cm2.sec) for 2 min, converting the stable 170 Er to radioactive 171 Er (t1/2 = 7.5 hr). Each tablet contained 50 microCi of 171 Er at the time of administration. The scintigraphy studies suggested that the greatest proportion of ibuprofen was absorbed from this dosage form while the tablet was in the large bowel. The dosage forms eroded slowly in the small bowel and appeared to lose their integrity in the large bowel. In vitro studies showed only minimal effects of the neutron irradiation procedure on the dosage form performance

  18. Accelerated in vitro release testing of implantable PLGA microsphere/PVA hydrogel composite coatings.

    Science.gov (United States)

    Shen, Jie; Burgess, Diane J

    2012-01-17

    Dexamethasone loaded poly(lactic-co-glycolic acid) (PLGA) microsphere/PVA hydrogel composites have been investigated as an outer drug-eluting coating for implantable devices such as glucose sensors to counter negative tissue responses to implants. The objective of this study was to develop a discriminatory, accelerated in vitro release testing method for this drug-eluting coating using United States Pharmacopeia (USP) apparatus 4. Polymer degradation and drug release kinetics were investigated under "real-time" and accelerated conditions (i.e. extreme pH, hydro-alcoholic solutions and elevated temperatures). Compared to "real-time" conditions, the initial burst and lag phases were similar using hydro-alcoholic solutions and extreme pH conditions, while the secondary apparent zero-order release phase was slightly accelerated. Elevated temperatures resulted in a significant acceleration of dexamethasone release. The accelerated release data were able to predict "real-time" release when applying the Arrhenius equation. Microsphere batches with faster and slower release profiles were investigated under "real-time" and elevated temperature (60°C) conditions to determine the discriminatory ability of the method. The results demonstrated both the feasibility and the discriminatory ability of this USP apparatus 4 method for in vitro release testing of drug loaded PLGA microsphere/PVA hydrogel composites. This method may be appropriate for similar drug/device combination products and drug delivery systems. Copyright © 2011 Elsevier B.V. All rights reserved.

  19. Fabrication and evaluation of a sustained-release chitosan-based scaffold embedded with PLGA microspheres.

    Science.gov (United States)

    Song, Kedong; Liu, Yingchao; Macedo, Hugo M; Jiang, Lili; Li, Chao; Mei, Guanyu; Liu, Tianqing

    2013-04-01

    Nutrient depletion within three-dimensional (3D) scaffolds is one of the major hurdles in the use of this technology to grow cells for applications in tissue engineering. In order to help in addressing it, we herein propose to use the controlled release of encapsulated nutrients within polymer microspheres into chitosan-based 3D scaffolds, wherein the microspheres are embedded. This method has allowed maintaining a stable concentration of nutrients within the scaffolds over the long term. The polymer microspheres were prepared using multiple emulsions (w/o/w), in which bovine serum albumin (BSA) and poly (lactic-co-glycolic) acid (PLGA) were regarded as the protein pattern and the exoperidium material, respectively. These were then mixed with a chitosan solution in order to form the scaffolds by cryo-desiccation. The release of BSA, entrapped within the embedded microspheres, was monitored with time using a BCA kit. The morphology and structure of the PLGA microspheres containing BSA before and after embedding within the scaffold were observed under a scanning electron microscope (SEM). These had a round shape with diameters in the range of 27-55 μm, whereas the chitosan-based scaffolds had a uniform porous structure with the microspheres uniformly dispersed within their 3D structure and without any morphological change. In addition, the porosity, water absorption and degradation rate at 37 °C in an aqueous environment of 1% chitosan-based scaffolds were (92.99±2.51) %, (89.66±0.66) % and (73.77±3.21) %, respectively. The studies of BSA release from the embedded microspheres have shown a sustained and cumulative tendency with little initial burst, with (20.24±0.83) % of the initial amount released after 168 h (an average rate of 0.12%/h). The protein concentration within the chitosan-based scaffolds after 168 h was found to be (11.44±1.81)×10(-2) mg/mL. This novel chitosan-based scaffold embedded with PLGA microspheres has proven to be a promising technique

  20. Investigation of surfactant/cosurfactant synergism impact on ibuprofen solubilization capacity and drug release characteristics of nonionic microemulsions.

    Science.gov (United States)

    Djekic, Ljiljana; Primorac, Marija; Filipic, Slavica; Agbaba, Danica

    2012-08-20

    The current study investigates the performances of the multicomponent mixtures of nonionic surfactants regarding the microemulsion stabilisation, drug solubilization and in vitro drug release kinetic. The primary surfactant was PEG-8 caprylic/capric glycerides (Labrasol). The cosurfactants were commercially available mixtures of octoxynol-12 and polysorbate 20 without or with the addition of PEG-40 hydrogenated castor oil (Solubilisant gamma 2421 and Solubilisant gamma 2429, respectively). The oil phase of microemulsions was isopropyl myristate. Phase behaviour study of the pseudo-ternary systems Labrasol/cosurfactant/oil/water at surfactant-to-cosurfactant weight ratios (K(m)) 40:60, 50:50 and 60:40, revealed a strong synergism in the investigated tensides mixtures for stabilisation of microemulsions containing up to 80% (w/w) of water phase at surfactant +cosurfactant-to-oil weight ratio (SCoS/O) 90:10. Solubilization of a model drug ibuprofen in concentration common for topical application (5%, w/w) was achieved at the water contents below 50% (w/w). Drug free and ibuprofen-loaded microemulsions M1-M6, containing 45% (w/w) of water phase, were prepared and characterized by polarized light microscopy, conductivity, pH, rheological and droplet size measurements. In vitro ibuprofen release kinetics from the microemulsions was investigated using paddle-over-enhancer cell method and compared with the commercial 5% (w/w) ibuprofen hydrogel product (Deep Relief, Mentholatum Company Ltd., USA). The investigated microemulsions were isotropic, low viscous Bingham-type liquids with the pH value (4.70-6.61) suitable for topical application. The different efficiency of the tensides mixtures for microemulsion stabilisation was observed, depending on the cosurfactant type and K(m) value. Solubilisant gamma 2429 as well as higher K(m) (i.e., lower relative content of the cosurfactant) provided higher surfactant/cosurfactant synergism. The drug molecules were predominantly

  1. Ketoprofen-loaded Eudragit RSPO microspheres: an influence of sodium carbonate on in vitro drug release and surface topology.

    Science.gov (United States)

    Pandit, Sachin S; Hase, Dinesh P; Bankar, Manish M; Patil, Arun T; Gaikwad, Naresh J

    2009-05-01

    Eudragit RSPO microspheres containing ketoprofen as model drug, prepared by solvent evaporation technique using acetone-liquid paraffin (heavy) solvent system were examined. Depending upon polymer concentration in the internal phase, microspheres of particle mean diameter (122.8, 213.6 and 309.5 μm) were obtained. The influence of surface washing of microspheres with n-hexane, i.e. untreated microspheres (UM) on the drug content, drug release and surface topology of microspheres were compared to those of microspheres washed with sodium carbonate, i.e. treated microspheres (TM) in order to make the non-encapsulated surface drug soluble. The significant reduction in encapsulation efficiency (p < 0.001) and drug content (p < 0.001) after treatment, in combination with the small crystalline peaks observed during XRD testing and lack of melting endotherm observed in DSC testing, suggests that the washing process actually removes a significant amount of drug (p < 0.001) from the surface and encapsulated near to the surface of the microsphere polymer matrix. Scanning electron microscopy (SEM) examination revealed that the removal of surface drug did not affect the size of microspheres but the topology of treated smallest microspheres was modified. The ketoprofen release profiles were examined in phosphate buffer pH 7.4, using USPXXIII paddle type dissolution apparatus. In general both UM and TM result in biphasic release patterns, but the initial burst effect (first release phase) of TM was lower than that of UM. The second release phase did not change for the bigger size but increased for the smallest microspheres, probably owing to the modification of matrix porosity.

  2. Preparation and Characterization of Zein and Zein-Chitosan Microspheres with Great Prospective of Application in Controlled Drug Release

    Directory of Open Access Journals (Sweden)

    Vinícius Müller

    2011-01-01

    Full Text Available Biomaterials applied as carriers for controlled drug delivery offer many advantages over the conventional systems. Among them, the increase of treatment effectiveness and also a significant reduction of toxicity, due to their biodegradability property, are some special features. In this work, microspheres based on the protein Zein (ZN and ZN associated to the natural polymer Chitosan (CHI were prepared and characterized. The microspheres of ZN and ZN/CHI were characterized by FT-IR spectroscopy and thermal analysis, and the morphology was analyzed by SEM images. The results confirmed the incorporation of CHI within the ZN-based microspheres. The morphological analysis showed that the CHI added increased the microspheres porosity when compared to the ZN microspheres. The chemical and physical characterization and the morphological analysis allow inferring that ZN/CHI microspheres are good candidates to act as a carrier for controlled drug release.

  3. Investigation of the parameters affecting the release of flurbiprofen from chitosan microspheres

    Directory of Open Access Journals (Sweden)

    Müşerref Günseli Yüksel Tilkan

    2018-04-01

    Full Text Available ABSTRACT Flurbiprofen (FLB, a NSAID, widely used for preventing pain generally for arthritis or dental problems. In this study, FLB loaded chitosan microspheres were prepared by ionotropic gelation method. In this method, microspheres were formed by dropping chitosan solutions containing FLB into sodium alginate solutions including sodium tripolyphosphate (TPP. A variety of formulation parameters like drug:polymer ratio, drug concentration, polymer’s molecular weight, polymer concentration, pH and the concentration of TPP solutions, drying method and stirring time were analyzed. The dissolution studies were performed in a shaking water bath in pH 7.4 phosphate buffer saline (PBS at 37 °C. Laser diffractometer was used for particle size analysis, and scanning electron microscope (SEM was used for morphological properties. Drug loading and loading efficiency were calculated by using UV spectrophotometer. The particles obtained were spherical with 0.7-1.3 mm size range, and the loading efficiency was approximately 21-79%. The dissolution studies conducted revealed that drug:polimer ratio and the polymer type and concentration affected the drug release from microspheres. It was observed that increasing the polymer concentration, polymer’s molecular weight and TPP concentration decreased the FLB release from microspheres, which was according to Higuchi kinetics.

  4. Retention and subsequent release of radioactivity from the incineration of wastes containing microspheres

    International Nuclear Information System (INIS)

    Emery, R.J.; Watson, J.E. Jr.

    1990-01-01

    Incineration is the preferred method for disposing of animal carcasses containing radioactive microspheres at the authors University. Routine surveys of ash from successive nonradioactive burns revealed significant contamination from previously incinerated microspheres. Past studies on microsphere incineration quantified the amount of activity retained in ash, but did not address any subsequent releases. This topic was not considered in earlier studies because, in most cases, the carcasses were placed in some type of container to facilitate recovery of ash, preventing contamination of the incinerator refractory. In this study, five sets of controlled burns were performed to quantify the subsequent releases of the microsphere radioisotopes 141 Ce, 113 Sn, 102 Ru, 95 Nb, and 46 Sc. Each set consisted of three successive burns. The first burn of each set incinerated a non-radioactive carcass, the second burn, a radioactive carcass, and the third, a non-radioactive carcass. In all of the burns, the carcasses were placed directly on the incinerator refractory floor, which is the standard procedure during normal operations

  5. Inhibition by local bupivacaine-releasing microspheres of acute postoperative pain from hairy skin incision.

    Science.gov (United States)

    Ohri, Rachit; Wang, Jeffrey Chi-Fei; Blaskovich, Phillip D; Pham, Lan N; Costa, Daniel S; Nichols, Gary A; Hildebrand, William P; Scarborough, Nelson L; Herman, Clifford J; Strichartz, Gary R

    2013-09-01

    Acute postoperative pain causes physiological deficits and slows recovery. Reduction of such pain by local anesthetics that are delivered for several days postoperatively is a desirable clinical objective, which is approached by a new formulation and applied in animal studies reported here. We subcutaneously injected a new formulation of poly-lactic-co-glycolic acid polymer microspheres, which provides steady drug release for 96+ hours into rats at the dorsal region 2 hours before surgery. A single 1.2-cm-long skin incision was followed by blunt dissection of skin away from the underlying fascia, and closed by 2 sutures, followed by 14 days of testing. Microspheres containing 5, 10, 20, and 40 mg bupivacaine were injected locally 2 hours before surgery; bupivacaine-free microspheres were the vehicle control, and bupivacaine HCl solution (0.5%), the positive control. Mechanical sensitivity was determined by the frequency of local muscle contractions to repeated pokes with nylon monofilaments (von Frey hairs) exerting 4 and 15 g forces, testing, respectively, allodynia and hyperalgesia, and by pinprick. Injection of bupivacaine microspheres (40 mg drug) into intact skin reduced responses to 15 g von Frey hairs for 6 hours and to pinprick for 36 hours. Respective reductions from bupivacaine HCl lasted for 3 and 2 hours. Skin incision and dissection alone caused mechanical allodynia and hyperalgesia for 14 days. Microspheres containing 20 or 40 mg bupivacaine suppressed postoperative hypersensitivity for up to 3 days, reduced integrated allodynia (area under curve of response versus time) over postoperative days 1 to 5 by 51% ± 20% (mean ± SE) and 78% ± 12%, and reduced integrated hyperalgesia by 55% ± 13% and 64% ± 11%, for the respective doses. Five and ten milligrams bupivacaine in microspheres and the 0.5% bupivacaine solution were ineffective in reducing postoperative hypersensitivity, as were 40 mg bupivacaine microspheres injected contralateral to the

  6. Polymer blend microspheres for controlled drug release: the techniques for preparation and characterization: a review article.

    Science.gov (United States)

    Dasan, K Priya; Rekha, C

    2012-11-01

    The use of polymers and their microspheres in drug delivery is well known for they are being widely used in the field of drug delivery. The polymer entraps a drug which is to be released in a predesigned manner in the body through biodegradation. The blending of polymers is one way of modifying and enhancing the properties of polymer- based products which is also a cost effective procedure rather than developing a new product. The molecular weight of the polymer, the composition of the blend, the sphere porosity and size, and drug distribution are found to be controllable factors on which drug delivery depends. Polymer blends are obtained by allowing two polymers to combine as one material which has the advantage of two or more polymers. Polymer microspheres are small spherical particles with diameters in the micrometer range between 1μm to 1000μm which are manufactured from various natural and synthetic materials. Microspheres are used to administer medication in a rate- controlled manner and sometimes in a targeted manner. This review presents various polymer blend- combinations in different ratios, the different processing techniques adopted and the details of their characterization through examples found in a literature survey. The characterization of the different polymer blends or microspheres showed changes in structure, increase in drug loading, encapsulation efficiency, biocompatibility and low cytotoxicity.

  7. Effect of cross-linked biodegradable polymers on sustained release of sodium diclofenac-loaded microspheres

    Directory of Open Access Journals (Sweden)

    Avik Kumar Saha

    2013-12-01

    Full Text Available The objective of this study was to formulate an oral sustained release delivery system of sodium diclofenac(DS based on sodium alginate (SA as a hydrophilic carrier in combination with chitosan (CH and sodium carboxymethyl cellulose (SCMC as drug release modifiers to overcome the drug-related adverse effects and to improve bioavailability. Microspheres of DS were prepared using an easy method of ionotropic gelation. The prepared beads were evaluated for mean particle size, entrapment efficiency, swelling capacity, erosion and in-vitro drug release. They were also subjected to various studies such as Fourier Transform Infra-Red Spectroscopy (FTIR for drug polymer compatibility, Scanning Electron Microscopy for surface morphology, X-ray Powder Diffraction Analysis (XRD and Differential Scanning Calorimetric Analysis (DSC to determine the physical state of the drug in the beads. The addition of SCMC during the preparation of polymeric beads resulted in lower drug loading and prolonged release of the DS. The release profile of batches F5 and F6 showed a maximum drug release of 96.97 ± 0.356% after 8 h, in which drug polymer ratio was decreased. The microspheres of sodium diclofenac with the polymers were formulated successfully. Analysis of the release profiles showed that the data corresponds to the diffusion-controlled mechanism as suggested by Higuchi.

  8. Release of a wound-healing agent from PLGA microspheres in a thermosensitive gel.

    Science.gov (United States)

    Machado, H A; Abercrombie, J J; You, T; Deluca, P P; Leung, K P

    2013-01-01

    The purpose of this research was to develop a topical microsphere delivery system in a thermosensitive 20% poloxamer 407 gel (Pluronic F127) to control release of KSL-W, a cationic antimicrobial decapeptide, for a period of 4-7 days for potential application in combat related injuries. KSL-W loaded microsphere formulations were prepared by a solvent extraction-evaporation method (water-oil-water), with poly (D,L-lactic-co-glycolic acid) (PLGA) (50 : 50, low-weight, and hydrophilic end) as the polymeric system. After optimization of the process, three formulations (A, B, and C) were prepared with different organic to water ratio of the primary emulsion while maintaining other components and manufacturing parameters constant. Formulations were characterized for surface morphology, porous nature, drug loading, in vitro drug release, and antimicrobial activity. Microspheres containing 20% peptide with porous surfaces and internal structure were prepared in satisfactory yields and in sizes varying from 25 to 50 μm. Gels of 20% Pluronic F127, which were liquid at or below 24.6°C and formed transparent films at body temperature, were used as carriers for the microspheres. Rheological studies showed a gelation temperature of 24.6°C for the 20% Pluronic F127 gel alone. Gelation temperature and viscosity of formulations A, B, and C as a function of temperature were very close to those of the carrier. A Franz diffusion cell system was used to study the release of peptide from the microspheres suspended in both, phosphate-buffered saline (PBS) and a 20% Pluronic F127 gel. In vitro release of greater than 50% peptide was found in all formulations in both PBS and the gel, and in one formulation there was a release of 75% in both PBS and the gel. Fractions collected from the release process were also tested for bactericidal activity against Staphylococcus epidermidis using the broth microdilution method and found to provide effective antimicrobial activity to warrant

  9. Poly(lactide-co-glycolide) encapsulated hydroxyapatite microspheres for sustained release of doxycycline

    Energy Technology Data Exchange (ETDEWEB)

    Wang Xiaoyun [School of Pharmacy, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016 (China); Department of Pharmacy, Shandong Drug and Food Vocational College, Science and Technology Town, Hightech Industrial Development Zone, Weihai 264210 (China); Xu Hui; Zhao Yanqiu [School of Pharmacy, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016 (China); Wang Shaoning, E-mail: wsn-xh@126.com [School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016 (China); Abe, Hiroya; Naito, Makio [Joining and Welding Research Institute, Osaka University, 11-1, Mihogaoka, Ibaraki, Osaka 567-0047 (Japan); Liu Yanli [School of Pharmacy, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016 (China); Wang Guoqing [School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103, Wenhua Road, Shenyang 110016 (China)

    2012-03-15

    Highlights: Black-Right-Pointing-Pointer PLGA encapsulated HAP-MSs were used for the sustained delivery of Doxycycline (Doxy, a broad spectrum tetracycline antibiotic). Black-Right-Pointing-Pointer Sustained Doxy release without obvious burst was observed. Black-Right-Pointing-Pointer Mechanism of the sustained Doxy release was illustrated. Black-Right-Pointing-Pointer Sustained Doxy release character in vivo was also obtained, the plasma Doxy levels were relatively lower and steady compared to that of the un-encapsulated HAP-MSs. - Abstract: The purpose of this study was to prepare a poly(lactide-co-glycolide) (PLGA) encapsulated hydroxyapatite microspheres (HAP-MSs) as injectable depot for sustained delivery of Doxycycline (Doxy). Doxy loaded HAP-MSs (Doxy-HAP-MSs) were encapsulated with PLGA by solid-in-oil-in-water (S/O/W) emulsion-solvent evaporation technique, the effects of the PLGA used (various intrinsic viscosity and LA/GA ratio) and ratio of PLGA/HAP-MSs on the formation of Doxy-HAP-MSs and in vitro release of Doxy were studied. The results showed that sustained drug release without obvious burst was obtained by using PLGA encapsulated HAP-MSs as the carrier, also the drug release rate could be tailored by changing the ratio of PLGA/HAP-MSs, or PLGA of various intrinsic viscosities or LA/GA ratio. Lower ratio of PLGA/HAP-MSs corresponded faster Doxy release, e.g. for the microspheres of PLGA/HAP-MSs ratio of 8 and 0.25, the in vitro Doxy release percents at the end of 7days were about 23% and 76%, respectively. Higher hydrophilicity (higher ratio of GA to LA) and lower molecular weight of PLGA corresponded to higher Doxy release rates. For in vivo release study, PLGA encapsulated HAP-MSs were subcutaneously injected to the back of mice, and the results showed good correlation between the in vivo and in vitro drug release. Meanwhile, the plasma Doxy levels after subcutaneous administration of PLGA encapsulated Doxy-HAP-MSs were relatively lower and steady

  10. Poly(lactide-co-glycolide) encapsulated hydroxyapatite microspheres for sustained release of doxycycline

    International Nuclear Information System (INIS)

    Wang Xiaoyun; Xu Hui; Zhao Yanqiu; Wang Shaoning; Abe, Hiroya; Naito, Makio; Liu Yanli; Wang Guoqing

    2012-01-01

    Highlights: ► PLGA encapsulated HAP-MSs were used for the sustained delivery of Doxycycline (Doxy, a broad spectrum tetracycline antibiotic). ► Sustained Doxy release without obvious burst was observed. ► Mechanism of the sustained Doxy release was illustrated. ► Sustained Doxy release character in vivo was also obtained, the plasma Doxy levels were relatively lower and steady compared to that of the un-encapsulated HAP-MSs. - Abstract: The purpose of this study was to prepare a poly(lactide-co-glycolide) (PLGA) encapsulated hydroxyapatite microspheres (HAP-MSs) as injectable depot for sustained delivery of Doxycycline (Doxy). Doxy loaded HAP-MSs (Doxy-HAP-MSs) were encapsulated with PLGA by solid-in-oil-in-water (S/O/W) emulsion-solvent evaporation technique, the effects of the PLGA used (various intrinsic viscosity and LA/GA ratio) and ratio of PLGA/HAP-MSs on the formation of Doxy-HAP-MSs and in vitro release of Doxy were studied. The results showed that sustained drug release without obvious burst was obtained by using PLGA encapsulated HAP-MSs as the carrier, also the drug release rate could be tailored by changing the ratio of PLGA/HAP-MSs, or PLGA of various intrinsic viscosities or LA/GA ratio. Lower ratio of PLGA/HAP-MSs corresponded faster Doxy release, e.g. for the microspheres of PLGA/HAP-MSs ratio of 8 and 0.25, the in vitro Doxy release percents at the end of 7days were about 23% and 76%, respectively. Higher hydrophilicity (higher ratio of GA to LA) and lower molecular weight of PLGA corresponded to higher Doxy release rates. For in vivo release study, PLGA encapsulated HAP-MSs were subcutaneously injected to the back of mice, and the results showed good correlation between the in vivo and in vitro drug release. Meanwhile, the plasma Doxy levels after subcutaneous administration of PLGA encapsulated Doxy-HAP-MSs were relatively lower and steady compared to that of the un-encapsulated microspheres. In conclusion, PLGA encapsulated HAP-MSs may

  11. Influence of excipients on characteristics and release profiles of poly(ε-caprolactone) microspheres containing immunoglobulin G

    Energy Technology Data Exchange (ETDEWEB)

    Erdemli, Özge [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Keskin, Dilek [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara (Turkey); Tezcaner, Ayşen, E-mail: tezcaner@metu.edu.tr [Department of Engineering Sciences, Middle East Technical University, Ankara (Turkey); Biomaterials and Tissue Engineering Center of Excellence, Middle East Technical University, Ankara (Turkey)

    2015-03-01

    Protein instability during microencapsulation has been one of the major drawbacks of protein delivery systems. In this study, the effects of various excipients (poly vinyl alcohol, glucose, starch, heparin) on the stability of encapsulated human immunoglobulin G (IgG) in poly(ε-caprolactone) (PCL) microspheres and on microsphere characteristics were investigated before and after γ-sterilization. Microspheres formulated without any excipients and with glucose had a mean particle size around 3–4 μm whereas the mean particle sizes of other microspheres were around 5–6 μm. Use of PVA significantly increased the IgG-loading and encapsulation efficiency of microspheres. After γ-irradiation, IgG stability was mostly maintained in the microspheres with excipients compared to microspheres without any excipients. According to the μBCA results, microspheres without any excipient showed a high initial burst release as well as a fast release profile among all groups. Presence of PVA decreased the loss in the activity of IgG released before (completely retained after 6 h and 15.69% loss after 7 days) and after γ-irradiation (26.04% loss and 52.39% loss after 6 h and 7 days, respectively). The stabilization effect of PVA on the retention of the activity of released IgG was found more efficient compared to other groups formulated with carbohydrates. - Highlights: • Good excipient provides retention of protein stability during microencapsulation. • PVA was more effective on retention of the IgG stability compared to carbohydrates. • Starch was not an appropriate excipient for the retention of IgG stability.

  12. Ibuprofen overdose

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/article/002655.htm Ibuprofen overdose To use the sharing features on this page, please enable JavaScript. Ibuprofen is a type of nonsteroidal anti-inflammatory drug ( ...

  13. Development of Poly Lactic/Glycolic Acid (PLGA Microspheres for Controlled Release of Rho-Associated Kinase Inhibitor

    Directory of Open Access Journals (Sweden)

    Sho Koda

    2017-01-01

    Full Text Available Purpose. The purpose of this study was to investigate the feasibility of poly lactic/glycolic acid (PLGA as a drug delivery carrier of Rho kinase (ROCK inhibitor for the treatment of corneal endothelial disease. Method. ROCK inhibitor Y-27632 and PLGA were dissolved in water with or without gelatin (W1, and a double emulsion [(W1/O/W2] was formed with dichloromethane (O and polyvinyl alcohol (W2. Drug release curve was obtained by evaluating the released Y-27632 by using high performance liquid chromatography. PLGA was injected into the anterior chamber or subconjunctiva in rabbit eyes, and ocular complication was evaluated by slitlamp microscope and histological analysis. Results. Y-27632 incorporated PLGA microspheres with different molecular weights, and different composition ratios of lactic acid and glycolic acid were fabricated. A high molecular weight and low content of glycolic acid produced a slower and longer release. The Y-27632 released from PLGA microspheres significantly promoted the cell proliferation of cultured corneal endothelial cells. The injection of PLGA did not induce any evident eye complication. Conclusions. ROCK inhibitor-incorporated PLGA microspheres were fabricated, and the microspheres achieved the sustained release of ROCK inhibitor over 7–10 days in vitro. Our data should encourage researchers to use PLGA microspheres for treating corneal endothelial diseases.

  14. Alginate Microspheres Containing Temperature Sensitive Liposomes (TSL for MR-Guided Embolization and Triggered Release of Doxorubicin.

    Directory of Open Access Journals (Sweden)

    Merel van Elk

    Full Text Available The objective of this study was to develop and characterize alginate microspheres suitable for embolization with on-demand triggered doxorubicin (DOX release and whereby the microspheres as well as the drug releasing process can be visualized in vivo using MRI.For this purpose, barium crosslinked alginate microspheres were loaded with temperature sensitive liposomes (TSL/TSL-Ba-ms, which release their payload upon mild hyperthermia. These TSL contained DOX and [Gd(HPDO3A(H2O], a T1 MRI contrast agent, for real time visualization of the release. Empty alginate microspheres crosslinked with holmium ions (T2* MRI contrast agent, Ho-ms were mixed with TSL-Ba-ms to allow microsphere visualization. TSL-Ba-ms and Ho-ms were prepared with a homemade spray device and sized by sieving. Encapsulation of TSL in barium crosslinked microspheres changed the triggered release properties only slightly: 95% of the loaded DOX was released from free TSL vs. 86% release for TSL-Ba-ms within 30 seconds in 50% FBS at 42°C. TSL-Ba-ms (76 ± 41 μm and Ho-ms (64 ± 29 μm had a comparable size, which most likely will result in a similar in vivo tissue distribution after an i.v. co-injection and therefore Ho-ms can be used as tracer for the TSL-Ba-ms. MR imaging of a TSL-Ba-ms and Ho-ms mixture (ratio 95:5 before and after hyperthermia allowed in vitro and in vivo visualization of microsphere deposition (T2*-weighted images as well as temperature-triggered release (T1-weighted images. The [Gd(HPDO3A(H2O] release and clusters of microspheres containing holmium ions were visualized in a VX2 tumor model in a rabbit using MRI.In conclusion, these TSL-Ba-ms and Ho-ms are promising systems for real-time, MR-guided embolization and triggered release of drugs in vivo.

  15. An investigation into the mechanisms of drug release from taste-masking fatty acid microspheres.

    Science.gov (United States)

    Qi, Sheng; Deutsch, David; Craig, Duncan Q M

    2008-09-01

    Fatty acid microspheres based on stearic and palmitic acids are known to form effective taste masking systems, although the mechanisms by which the drug is preferentially released in the lower gastrointestinal tract are not known. The objective of the present study was to identify the mechanisms involved, with a particular view to clarify the role of acid soap formation in the dissolution process. Microspheres were prepared by a spray chilling process. Using benzoic acid as a model drug and an alkaline dissolution medium, a faster drug release was observed in the mixed fatty acid formulation (50:50 stearic:palmitic acid (w/w)) compared to the single fatty acid component systems. Thermal and powder X-ray diffraction studies indicated a greater degree of acid soap formation for the mixed formulation in alkaline media compared to the single fatty acid systems. Particle size and porosity studies indicated a modest reduction in size for the mixed systems and an increase in porosity on immersion in the dissolution medium. It is proposed that the mixed fatty acid system form a mixed crystal system which in turn facilitates interaction with the dissolution medium, thereby leading to a greater propensity for acid soap formation which in turn forms a permeable liquid crystalline phase through which the drug may diffuse. The role of dissolution of palmitic acid into the dissolution medium is also discussed as a secondary mechanism.

  16. Prolonged amelioration of experimental postoperative pain by bupivacaine released from microsphere-coated hernia mesh.

    Science.gov (United States)

    Ohri, Rachit; Wang, Jeffery Chi-Fei; Pham, Lan; Blaskovich, Phillip D; Costa, Daniel; Nichols, Gary; Hildebrand, William; Scarborough, Nelson; Herman, Clifford; Strichartz, Gary R

    2014-01-01

    Postoperative pain alters physiological functions and delays discharge. Perioperative local anesthetics are effective analgesics in the immediate 1- to 2-day postoperative period, but acute pain often lasts longer. The goal of this work was to develop a local anesthetic formulation adhering to an intraoperative implanted device that reduces pain for at least 3 days after surgery. Six groups, each with 8 rats, were studied. In a control group (group I), one 1.2-cm-long incision of the skin was followed by blunt dissection to separate the skin away from the underlying tissues and closing with 2 sutures. In 3 of the treatment groups, the same surgical procedure was used, with the subcutaneous space formed by the blunt dissection lined with a 1-cm square patch of hernia mesh coated with poly lactide co-glycolic acid microspheres containing approximately 17 mg of bupivacaine (group II), no drug (placebo; group III), or bupivacaine free-base powder (group IV). Uncoated mesh implants (group V) served as a secondary control. A standard bupivacaine solution (0.4 mL, 0.5%; 2-mg dose) was infiltrated subcutaneously 30 minutes before the surgery and served as a standard control (group VI). Mechanosensitivity of the skin was tested by the local subcutaneous muscle responses to cutaneous tactile stimulation by von Frey hairs with forces of 4 g (for allodynia) and 15 g (for hyperalgesia) preoperatively and for 7 postoperative days. Control rats (group I) showed mechanohypersensitivity, indicative of postoperative allodynia and hyperalgesia, for all 7 postoperative days. Mechanohyperalgesia in rats that received mesh coated with bupivacaine-releasing microspheres (group II) was reduced during this period to 13% of control postoperative values (P < 0.001); mesh coated with bupivacaine base (group IV) reduced it by 50% (P = 0.034). The placebo mesh (group III) and uncoated mesh (group V) caused no significant reduction of mechanohypersensitivity, and bupivacaine solution infiltrated

  17. Single- and multiple-dose pharmacokinetics of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (MNK-155 compared with immediate-release hydrocodone bitartrate/ibuprofen and immediate-release tramadol HCl/acetaminophen

    Directory of Open Access Journals (Sweden)

    Devarakonda K

    2015-09-01

    Full Text Available Krishna Devarakonda,1 Kenneth Kostenbader,2 Michael J Giuliani,3 Jim L Young41Department of Clinical Pharmacology, Mallinckrodt Pharmaceuticals, 2Mallinckrodt Pharmaceuticals, 3Research and Development, Mallinckrodt Pharmaceuticals, 4Department of Clinical Affairs and Program Management, Mallinckrodt Pharmaceuticals, Hazelwood, MO, USAObjective: To characterize the single-dose and steady-state pharmacokinetics (PK of biphasic immediate-release/extended-release hydrocodone bitartrate/acetaminophen (IR/ER HB/APAP, IR HB/ibuprofen, and IR tramadol HCl/APAP.Methods: In this single-center, open-label, randomized, four-period crossover study, healthy participants received four treatments under fasted conditions: 1 a single dose of two IR/ER HB/APAP 7.5/325 mg tablets (15/650 mg total dose on day 1, followed by two tablets every 12 hours (q12h beginning on day 3; 2 a single dose of IR HB/ibuprofen 15/400 mg (divided as one 7.5/200 mg tablet at hour 0 and 6, followed by one tablet every 6 hours (q6h beginning on day 3; 3 a single dose of IR tramadol HCl/APAP 75/650 mg (divided as one 37.5/325 mg tablet at hour 0 and 6, followed by one tablet q6h beginning on day 3; and 4 a single dose of three IR/ER HB/APAP 7.5/325 mg tablets (22.5/975 mg total dose on day 1, a three-tablet initial dose at 48 hours followed by two-tablet doses q12h beginning on day 3. Hydrocodone and APAP single-dose and steady-state PK were assessed. Adverse events were monitored.Results: The PK analysis was carried out on 29 of 48 enrolled participants who completed all treatment periods. Single-dose hydrocodone exposure was similar for IR/ER HB/APAP 22.5/975 mg and IR HB/ibuprofen 15/400 mg; time to maximum observed plasma concentration was shorter and half-life was longer for IR/ER HB/APAP (22.5/975 mg and 15/650 mg vs IR HB/ibuprofen. Single-dose APAP exposure was similar for IR/ER HB/APAP 15/650 mg and IR tramadol HCl/APAP 75/650 mg. Steady-state hydrocodone and APAP exposures

  18. Preparation and characterization of glycidyl methacrylate organo bridges grafted mesoporous silica SBA-15 as ibuprofen and mesalamine carrier for controlled release

    International Nuclear Information System (INIS)

    Rehman, Fozia; Rahim, Abdur; Airoldi, Claudio; Volpe, Pedro L.O.

    2016-01-01

    Mesoporous silica SBA-15 was synthesized and functionalized with bridged polysilsesquioxane monomers obtained by the reaction of 3-aminopropyltriethoxy silane with glycidyl methacrylate in 2:1 ratio. The synthesized mesoporous silica materials were characterized by elemental analysis, infrared spectroscopy, nuclear magnetic resonance spectroscopy, nitrogen adsorption, X-ray diffraction, thermogravimetry and scanning electron microscopy. The nuclear magnetic resonance in the solid state is in agreement with the sequence of carbon distributed in the attached organic chains, as expected for organically functionalized mesoporous silica. After functionalization with organic bridges the BET surface area was reduced from 1311.80 to 494.2 m 2 g −1 and pore volume was reduced from 1.98 to 0.89 cm 3 g −1 , when compared to original precursor silica. Modification of the silica surface with organic bridges resulted in high loading capacity and controlled release of ibuprofen and mesalamine in biological fluids. The Korsmeyer–Peppas model better fits the release data indicating Fickian diffusion and zero order kinetics for synthesized mesoporous silica. The drug release rate from the modified silica was slow in simulated gastric fluid, (pH 1.2) where less than 10% of mesalamine and ibuprofen were released in initial 8 h, while comparatively high release rates were observed in simulated intestinal (pH 6.8) and simulated body fluids (pH 7.2). The preferential release of mesalamine at intestinal pH suggests that the modified silica could be a simple, efficient, inexpensive and convenient carrier for colon targeted drugs, such a mesalamine and also as a controlled drug release system. - Highlights: • Modified SBA-15 silica with long hydrophobic chains was evaluated as drug carrier. • This silica showed improved loading capacity and controlled release of ibuprofen. • Compared to gastric pH high release rate of mesalamine was observed at colonic pH. • Modified silica

  19. Effect of sodium tripolyphosphate concentration and simulated gastrointestinal fluids on release profile of paracetamol from chitosan microsphere

    Science.gov (United States)

    Mulia, Kamarza; Andrie; Krisanti, Elsa A.

    2018-03-01

    The problem to overcome in oral drug administration is the significant pH changes present in the human digestive system. In this study, ionotropic gelation method employing 2-8% (w/v) tripolyphosphate solutions were used to crosslink chitosan microspheres for a controlled release of paracetamol as a model drug. The release profiles of paracetamol from chitosan microspheres were determined using simulated gastrointestinal fluids having pH values of 1.2, 6.8, and 7.4. The results showed that the paracetamol loading and the encapsulation efficiency values increased with increasing concentration of tripolyphosphate solutions used in the preparation step. Paracetamol released at pH 1.2 and 6.8 buffer solutions was significantly higher than that at pH 7.4; also, more paracetamol was released in the presence of α-amylase and β-glucosidase enzymes. The release profiles showed zero-order release behaviour up to 8 hours where the highest drug release was 39% of the paracetamol loaded in the chitosan microspheres, indicating a strong crosslinking between chitosan and TPP anions. The relatively low accumulated drug release could be compensated by employing suitable enzymes, lower TPP solution concentration, and addition of other biodegradable polymer to reduce the TPP crosslink.

  20. [Construction and evaluation of the tissue engineered nerve of bFGF-PLGA sustained release microspheres].

    Science.gov (United States)

    Wang, Guanglin; Lin, Wei; Gao, Weiqiang; Xiao, Yuhua; Dong, Changchao

    2008-12-01

    To study the outcomes of nerve defect repair with the tissue engineered nerve, which is composed of the complex of SCs, 30% ECM gel, bFGF-PLGA sustained release microspheres, PLGA microfilaments and permeable poly (D, L-lactic acid) (PDLLA) catheters. SCs were cultured and purified from the sciatic nerves of 1-day-old neonatal SD rats. The 1st passage cells were compounded with bFGF-PLGA sustained release microspheres and ECM gel, and then were injected into permeable PDLLA catheters with PLGA microfilaments inside. In this way, the tissue engineered nerve was constructed. Sixty SD rats were included. The model of 15-mm sciatic nerve defects was made, and then the rats were randomly divided into 5 groups, with 12 rats in each. In group A, autograft was adopted. In group B, the blank PDLLA catheters with PBS inside were used. In group C, PDLLA catheters, with PLGA microfilaments and 30% ECM gel inside, were used. In group D, PDLLA catheters, with PLGA microfilaments, SCs and 30% ECM gel inside, were used. In group E, the tissue engineered nerve was applied. After the operation, observation was made for general conditions of the rats. The sciatic function index (SFI) analysis was performed at 12, 16, 20 and 24 weeks after the operation, respectively. Electrophysiological detection and histological observation were performed at 12 and 24 weeks after the operation, respectively. All rats survived to the end of the experiment. At 12 and 16 weeks after the operation, group E was significantly different from group B in SFI (P fibers in group E were significantly differents from those in groups A, B and C (P fibers in group E were smaller than those in group A (P fibers in group E was significantly different from those in groups A, B, C (P fibers in group E were bigger than those in groups B and C (P < 0.05). The tissue engineered nerve with the complex of SCs, ECM gel, bFGF-PLGA sustained release microspheres, PLGA microfilaments and permeable PDLLA catheters promote

  1. Liver cancer cells: targeting and prolonged-release drug carriers consisting of mesoporous silica nanoparticles and alginate microspheres.

    Science.gov (United States)

    Liao, Yu-Te; Liu, Chia-Hung; Yu, Jiashing; Wu, Kevin C-W

    2014-01-01

    A new microsphere consisting of inorganic mesoporous silica nanoparticles (MSNs) and organic alginate (denoted as MSN@Alg) was successfully synthesized by air-dynamic atomization and applied to the intracellular drug delivery systems (DDS) of liver cancer cells with sustained release and specific targeting properties. MSN@Alg microspheres have the advantages of MSN and alginate, where MSN provides a large surface area for high drug loading and alginate provides excellent biocompatibility and COOH functionality for specific targeting. Rhodamine 6G was used as a model drug, and the sustained release behavior of the rhodamine 6G-loaded MSN@Alg microspheres can be prolonged up to 20 days. For targeting therapy, the anticancer drug doxorubicin was loaded into MSN@Alg microspheres, and the (lysine)4-tyrosine-arginine-glycine-aspartic acid (K4YRGD) peptide was functionalized onto the surface of MSN@Alg for targeting liver cancer cells, hepatocellular carcinoma (HepG2). The results of the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay and confocal laser scanning microscopy indicate that the MSN@Alg microspheres were successfully uptaken by HepG2 without apparent cytotoxicity. In addition, the intracellular drug delivery efficiency was greatly enhanced (ie, 3.5-fold) for the arginine-glycine-aspartic acid (RGD)-labeled, doxorubicin-loaded MSN@Alg drug delivery system compared with the non-RGD case. The synthesized MSN@Alg microspheres show great potential as drug vehicles with high biocompatibility, sustained release, and targeting features for future intracellular DDS.

  2. Controlled-release and preserved bioactivity of proteins from (self-assembled core-shell double-walled microspheres

    Directory of Open Access Journals (Sweden)

    Yuan W

    2012-01-01

    Full Text Available Weien Yuan1,2, Zhenguo Liu11Department of Neurology, Xinhua Hospital, affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, 2School of Pharmacy, Shanghai Jiao Tong University, Shanghai, People’s Republic of ChinaAbstract: In order to address preserved protein bioactivities and protein sustained-release problems, a method for preparing double-walled microspheres with a core (protein-loaded nanoparticles with a polymer-suspended granule system-formed core and a second shell (a polymer-formed shell for controlled drug release and preserved protein bioactivities has been developed using (solid-in-oil phase-in-hydrophilic oil-in-water (S/O/Oh/W phases. The method, based on our previous microsphere preparation method (solid-in-oil phase-in-hydrophilic oil-in-water (S/O/Oh/W, employs different concentric poly(D,L-lactide-co-glycolide, poly(D,L-lactide, and protein-loaded nanoparticles to produce a suspended liquid which then self-assembles to form shell-core microspheres in the hydrophilic oil phase, which are then solidified in the water phase. Variations in the preparation parameters allowed complete encapsulation by the shell phase, including the efficient formation of a poly(D,L-lactide shell encapsulating a protein-loaded nanoparticle-based poly(D,L-lactide-co-glycolide core. This method produces core-shell double-walled microspheres that show controlled protein release and preserved protein bioactivities for 60 days. Based upon these results, we concluded that the core-shell double-walled microspheres might be applied for tissue engineering and therapy for chronic diseases, etc.Keywords: protein delivery, protein stability, core-shell microspheres, dextran nanoparticles

  3. In-vitro evaluation of ion-exchange microspheres for the sustained release of liposomal-adenoviral conjugates.

    Science.gov (United States)

    Steel, Jason C; Cavanagh, Heather M A; Burton, Mark A; Dingwall, Daniel; Kalle, Wouter H J

    2004-03-24

    This study looks at the development of a novel combination vector consisting of adenovirus conjugated to liposomes (AL complexes) bound to cation-exchanging microspheres (MAL complexes). With adenovirus having a net negative charge and the liposomes a net positive charge it was possible to modify the net charge of the AL complexes by varying the concentrations of adenovirus to liposomes. The modification of the net charge resulted in altered binding and release characteristics. Of the complexes tested, the 5:1 and 2:1 ratio AL complexes were able to be efficiently bound by the microspheres and exhibited sustained release over 24 h. The 1:1 and 1:2 AL complexes, however, bound poorly to the microspheres and were rapidly released. In addition the MAL complexes also were able to reduce the toxicity of the AL complexes, which was seen with the 10:1 ratio. The AL complexes showed considerably more toxicity alone than in combination with microspheres, highlighting a potential benefit of this vector.

  4. Improvement of survival in C6 rat glioma model by a sustained drug release from localized PLGA microspheres in a thermoreversible hydrogel.

    Science.gov (United States)

    Ozeki, Tetsuya; Kaneko, Daiki; Hashizawa, Kosuke; Imai, Yoshihiro; Tagami, Tatsuaki; Okada, Hiroaki

    2012-05-10

    A local drug delivery system based on sustained drug release is an attractive approach to treat brain tumors. We have developed a novel device using drug-incorporated poly(lactic-co-glycolic acid) (PLGA) microspheres embedded in thermoreversible gelation polymer (TGP) formulation (drug/PLGA/TGP formulation). TGP forms a gel at body temperature but sol at room temperature. Therefore, when this formulation is injected into the brain tumor, the PLGA microspheres in TGP gel are localized at the injection site and do not diffuse throughout the brain tissue; eventually, sustained drug release from PLGA microspheres is achieved at the target site. In this study, two chemotherapeutic drugs (camptothecin (CPT) or vincristine (VCR)) were incorporated into PLGA microspheres to prepare drug/PLGA/TGP formulations. VCR/PLGA microspheres exhibited the higher encapsulation efficiency than CPT/PLGA microspheres (70.1% versus 30.1%). In addition, VCR/PLGA microspheres showed a higher sustained release profile than CPT/PLGA microspheres (54.5% versus 72.5% release, at 28 days). Therapeutic effect (mean survival) was evaluated in the C6 rat glioma model (control group, 18 days; CPT/PLGA/TGP treatment group, 24 days; VCR/PLGA/TGP treatment group, 33 days). In particular, the VCR/PLGA/TGP formulation produced long-term survivors (>60 days). Therefore, this formulation can be therapeutically effective formulation for the glioma therapy. Copyright © 2012 Elsevier B.V. All rights reserved.

  5. Fluxgate magnetorelaxometry: a new approach to study the release properties of hydrogel cylinders and microspheres.

    Science.gov (United States)

    Wöhl-Bruhn, S; Heim, E; Schwoerer, A; Bertz, A; Harling, S; Menzel, H; Schilling, M; Ludwig, F; Bunjes, H

    2012-10-15

    Hydrogels are under investigation as long term delivery systems for biomacromolecules as active pharmaceutical ingredients. The release behavior of hydrogels can be tailored during the fabrication process. This study investigates the applicability of fluxgate magnetorelaxometry (MRX) as a tool to characterize the release properties of such long term drug delivery depots. MRX is based on the use of superparamagnetic core-shell nanoparticles as model substances. The feasibility of using superparamagnetic nanoparticles to study the degradation of and the associated release from hydrogel cylinders and hydrogel microspheres was a major point of interest. Gels prepared from two types of photo crosslinkable polymers based on modified hydroxyethylstarch, specifically hydroxyethyl starch-hydroxyethyl methacrylate (HES-HEMA) and hydroxyethyl starch-polyethylene glycol methacrylate (HES-P(EG)(6)MA), were analyzed. MRX analysis of the incorporated nanoparticles allowed to evaluate the influence of different crosslinking conditions during hydrogel production as well as to follow the increase in nanoparticle mobility as a result of hydrogel degradation during release studies. Conventional release studies with fluorescent markers (half-change method) were performed for comparison. MRX with superparamagnetic nanoparticles as model substances is a promising method to analyze pharmaceutically relevant processes such as the degradation of hydrogel drug carrier systems. In contrast to conventional release experiments MRX allows measurements in closed vials (reducing loss of sample and sampling errors), in opaque media and at low magnetic nanoparticle concentrations. Magnetic markers possess a better long-term stability than fluorescent ones and are thus also promising for the use in in vivo studies. Copyright © 2012 Elsevier B.V. All rights reserved.

  6. Composite microsphere-functionalized scaffold for the controlled release of small molecules in tissue engineering

    Directory of Open Access Journals (Sweden)

    Laura Pandolfi

    2016-01-01

    Full Text Available Current tissue engineering strategies focus on restoring damaged tissue architectures using biologically active scaffolds. The ideal scaffold would mimic the extracellular matrix of any tissue of interest, promoting cell proliferation and de novo extracellular matrix deposition. A plethora of techniques have been evaluated to engineer scaffolds for the controlled and targeted release of bioactive molecules to provide a functional structure for tissue growth and remodeling, as well as enhance recruitment and proliferation of autologous cells within the implant. Recently, novel approaches using small molecules, instead of growth factors, have been exploited to regulate tissue regeneration. The use of small synthetic molecules could be very advantageous because of their stability, tunability, and low cost. Herein, we propose a chitosan–gelatin scaffold functionalized with composite microspheres consisting of mesoporous silicon microparticles and poly(dl-lactic-co-glycolic acid for the controlled release of sphingosine-1-phospate, a small molecule of interest. We characterized the platform with scanning electron microscopy, Fourier transform infrared spectroscopy, and confocal microscopy. Finally, the biocompatibility of this multiscale system was analyzed by culturing human mesenchymal stem cells onto the scaffold. The presented strategy establishes the basis of a versatile scaffold for the controlled release of small molecules and for culturing mesenchymal stem cells for regenerative medicine applications.

  7. Controlled release system for ametryn using polymer microspheres: Preparation, characterization and release kinetics in water

    International Nuclear Information System (INIS)

    Grillo, Renato; Pereira, Anderson do Espirito Santo; Ferreira Silva de Melo, Nathalie; Porto, Raquel Martins; Feitosa, Leandro Oliveira; Tonello, Paulo Sergio; Dias Filho, Newton L.; Rosa, Andre Henrique; Lima, Renata; Fraceto, Leonardo Fernandes

    2011-01-01

    The purpose of this work was to develop a modified release system for the herbicide ametryn by encapsulating the active substance in biodegradable polymer microparticles produced using the polymers poly(hydroxybutyrate) (PHB) or poly(hydroxybutyrate-valerate) (PHBV), in order to both improve the herbicidal action and reduce environmental toxicity. PHB or PHBV microparticles containing ametryn were prepared and the efficiencies of herbicide association and loading were evaluated, presenting similar values of approximately 40%. The microparticles were characterized by scanning electron microscopy (SEM), which showed that the average sizes of the PHB and PHBV microparticles were 5.92 ± 0.74 μm and 5.63 ± 0.68 μm, respectively. The ametryn release profile was modified when it was encapsulated in the microparticles, with slower and more sustained release compared to the release profile of pure ametryn. When ametryn was associated with the PHB and PHBV microparticles, the amount of herbicide released in the same period of time was significantly reduced, declining to 75% and 87%, respectively. For both types of microparticle (PHB and PHBV) the release of ametryn was by diffusion processes due to anomalous transport (governed by diffusion and relaxation of the polymer chains), which did not follow Fick's laws of diffusion. The results presented in this paper are promising, in view of the successful encapsulation of ametryn in PHB or PHBV polymer microparticles, and indications that this system may help reduce the impacts caused by the herbicide, making it an environmentally safer alternative.

  8. In Vivo Dissolution and Systemic Absorption of Immediate Release Ibuprofen in Human Gastrointestinal Tract under Fed and Fasted Conditions.

    Science.gov (United States)

    Koenigsknecht, Mark J; Baker, Jason R; Wen, Bo; Frances, Ann; Zhang, Huixia; Yu, Alex; Zhao, Ting; Tsume, Yasuhiro; Pai, Manjunath P; Bleske, Barry E; Zhang, Xinyuan; Lionberger, Robert; Lee, Allen; Amidon, Gordon L; Hasler, William L; Sun, Duxin

    2017-12-04

    In vivo drug dissolution in the gastrointestinal (GI) tract is largely unmeasured. The purpose of this clinical study was to evaluate the in vivo drug dissolution and systemic absorption of the BCS class IIa drug ibuprofen under fed and fasted conditions by direct sampling of stomach and small intestinal luminal content. Expanding current knowledge of drug dissolution in vivo will help to establish physiologically relevant in vitro models predictive of drug dissolution. A multilumen GI catheter was orally inserted into the GI tract of healthy human subjects. Subjects received a single oral dose of ibuprofen (800 mg tablet) with 250 mL of water under fasting and fed conditions. The GI catheter facilitated collection of GI fluid from the stomach, duodenum, and jejunum. Ibuprofen concentration in GI fluid supernatant and plasma was determined by LC-MS/MS. A total of 23 subjects completed the study, with 11 subjects returning for an additional study visit (a total of 34 completed study visits). The subjects were primarily white (61%) and male (65%) with an average age of 30 years. The subjects had a median [min, max] weight of 79 [52, 123] kg and body mass index of 25.7 [19.4, 37.7] kg/m 2 . Ibuprofen plasma levels were higher under fasted conditions and remained detectable for 28 h under both conditions. The AUC 0-24 and C max were lower in fed subjects vs fasted subjects, and T max was delayed in fed subjects vs fasted subjects. Ibuprofen was detected immediately after ingestion in the stomach under fasting and fed conditions until 7 h after dosing. Higher levels of ibuprofen were detected in the small intestine soon after dosing in fasted subjects compared to fed. In contrast to plasma drug concentration, overall gastric concentrations remained higher under fed conditions due to increased gastric pH vs fasting condition. The gastric pH increased to near neutrality after feedingbefore decreasing to acidic levels after 7 h. Induction of the fed state reduced systemic

  9. Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study

    Directory of Open Access Journals (Sweden)

    Praveen Kumar Gaur

    2014-12-01

    Full Text Available The aim of this work was to design a controlled-release drug-delivery system for the angiotensin-II receptor antagonist drug telmisartan. Telmisartan was encapsulated with different EUDRAGIT polymers by an emulsion solvent evaporation technique and the physicochemical properties of the formulations were characterized. Using a solvent evaporation method, white spherical microspheres with particle sizes of 629.9–792.1 μm were produced. The in vitro drug release was studied in three different pH media (pH 1.2 for 2 hours, pH 6.8 for 4 hours, and pH 7.4 for 18 hours. The formulations were then evaluated for their pharmacokinetic parameters. The entrapment efficiency of these microspheres was between 58.6% and 90.56%. The obtained microspheres showed good flow properties, which were evaluated in terms of angle of repose (15.29–26.32, bulk and tapped densities (0.37–0.53 and 0.43–0.64, respectively, Carr indices and Hausner ratio (12.94–19.14% and 1.14–1.23, respectively. No drug release was observed in the simulated gastric medium up to 2 hours; however, a change in pH from 1.2 to 6.8 increased the drug release. At pH 7.4, formulations with EUDRAGIT RS 100 showed a steady drug release. The microsphere formulation TMRS-3 (i.e., microspheres containing 2-mg telmisartan gave the highest Cmax value (6.8641 μg/mL at 6 hours, which was three times higher than Cmax for telmisartan oral suspension (TOS. Correspondingly, the area under the curve for TMRS-3 was 8.5 times higher than TOS. Particle size and drug release depended on the nature and content of polymer used. The drug release mechanism of the TMRS-3 formulation can be explained using the Higuchi model. The controlled release of drug from TMRS-3 also provides for higher plasma drug content and improved bioavailability.

  10. In vitro Evaluation of Nateglinide-Loaded Microspheres Formulated ...

    African Journals Online (AJOL)

    Keywords: Nateglinide, Microspheres, Micromeritics, Drug release, Ionic ... Oral drug delivery systems (DDS) are commonly divided into immediate release and modified release systems. ..... Albumin Microspheres for Potential Intramuscular.

  11. Liver cancer cells: targeting and prolonged-release drug carriers consisting of mesoporous silica nanoparticles and alginate microspheres

    Directory of Open Access Journals (Sweden)

    Liao YT

    2014-06-01

    Full Text Available Yu-Te Liao,1 Chia-Hung Liu,2 Jiashing Yu,1 Kevin C-W Wu1,3 1Department of Chemical Engineering, National Taiwan University, Taipei, Taiwan; 2Department of Urology, Taipei Medical University-Shuang Ho Hospital, New Taipei City, Taiwan; 3Division of Medical Engineering Research, National Health Research Institutes, Zhunan Township, Miaoli County, Taiwan Abstract: A new microsphere consisting of inorganic mesoporous silica nanoparticles (MSNs and organic alginate (denoted as MSN@Alg was successfully synthesized by air-dynamic atomization and applied to the intracellular drug delivery systems (DDS of liver cancer cells with sustained release and specific targeting properties. MSN@Alg microspheres have the advantages of MSN and alginate, where MSN provides a large surface area for high drug loading and alginate provides excellent biocompatibility and COOH functionality for specific targeting. Rhodamine 6G was used as a model drug, and the sustained release behavior of the rhodamine 6G-loaded MSN@Alg microspheres can be prolonged up to 20 days. For targeting therapy, the anticancer drug doxorubicin was loaded into MSN@Alg microspheres, and the (lysine4-tyrosine-arginine-glycine-aspartic acid (K4YRGD peptide was functionalized onto the surface of MSN@Alg for targeting liver cancer cells, hepatocellular carcinoma (HepG2. The results of the 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT assay and confocal laser scanning microscopy indicate that the MSN@Alg microspheres were successfully uptaken by HepG2 without apparent cytotoxicity. In addition, the intracellular drug delivery efficiency was greatly enhanced (ie, 3.5-fold for the arginine-glycine-aspartic acid (RGD-labeled, doxorubicin-loaded MSN@Alg drug delivery system compared with the non-RGD case. The synthesized MSN@Alg microspheres show great potential as drug vehicles with high biocompatibility, sustained release, and targeting features for future intracellular DDS. Keywords

  12. Preparation and characterization of glycidyl methacrylate organo bridges grafted mesoporous silica SBA-15 as ibuprofen and mesalamine carrier for controlled release

    Energy Technology Data Exchange (ETDEWEB)

    Rehman, Fozia, E-mail: fozia@iqm.unicamp.br [Institute of Chemistry, University of Campinas, UNICAMP, P.O. Box 6154, 13084-971 Campinas, SP (Brazil); Interdisciplinary Research Centre in Biomedical Materials (IRCBM), COMSATS Institute of Information Technology, Lahore (Pakistan); Rahim, Abdur [Interdisciplinary Research Centre in Biomedical Materials (IRCBM), COMSATS Institute of Information Technology, Lahore (Pakistan); Airoldi, Claudio; Volpe, Pedro L.O. [Institute of Chemistry, University of Campinas, UNICAMP, P.O. Box 6154, 13084-971 Campinas, SP (Brazil)

    2016-02-01

    Mesoporous silica SBA-15 was synthesized and functionalized with bridged polysilsesquioxane monomers obtained by the reaction of 3-aminopropyltriethoxy silane with glycidyl methacrylate in 2:1 ratio. The synthesized mesoporous silica materials were characterized by elemental analysis, infrared spectroscopy, nuclear magnetic resonance spectroscopy, nitrogen adsorption, X-ray diffraction, thermogravimetry and scanning electron microscopy. The nuclear magnetic resonance in the solid state is in agreement with the sequence of carbon distributed in the attached organic chains, as expected for organically functionalized mesoporous silica. After functionalization with organic bridges the BET surface area was reduced from 1311.80 to 494.2 m{sup 2} g{sup −1} and pore volume was reduced from 1.98 to 0.89 cm{sup 3} g{sup −1}, when compared to original precursor silica. Modification of the silica surface with organic bridges resulted in high loading capacity and controlled release of ibuprofen and mesalamine in biological fluids. The Korsmeyer–Peppas model better fits the release data indicating Fickian diffusion and zero order kinetics for synthesized mesoporous silica. The drug release rate from the modified silica was slow in simulated gastric fluid, (pH 1.2) where less than 10% of mesalamine and ibuprofen were released in initial 8 h, while comparatively high release rates were observed in simulated intestinal (pH 6.8) and simulated body fluids (pH 7.2). The preferential release of mesalamine at intestinal pH suggests that the modified silica could be a simple, efficient, inexpensive and convenient carrier for colon targeted drugs, such a mesalamine and also as a controlled drug release system. - Highlights: • Modified SBA-15 silica with long hydrophobic chains was evaluated as drug carrier. • This silica showed improved loading capacity and controlled release of ibuprofen. • Compared to gastric pH high release rate of mesalamine was observed at colonic pH.

  13. Characterization of gelation process and drug release profile of thermosensitive liquid lecithin/poloxamer 407 based gels as carriers for percutaneous delivery of ibuprofen.

    Science.gov (United States)

    Djekic, Ljiljana; Krajisnik, Danina; Martinovic, Martina; Djordjevic, Dragana; Primorac, Marija

    2015-07-25

    Suitability of liquid lecithin (i.e., solution of lecithin in soy bean oil with ∼ 60% w/w of phospholipids) for formation of gels, upon addition of water solution of poloxamer 407, was investigated, and formulated systems were evaluated as carriers for percutaneous delivery of ibuprofen. Formulation study of pseudo-ternary system liquid lecithin/poloxamer 407/water at constant liquid lecithin/poloxamer 407 mass ratio (2.0) revealed that minimum concentrations of liquid lecithin and poloxamer 407 required for formation of gel like systems were 15.75% w/w and 13.13% w/w, respectively, while the maximum content of water was 60.62% w/w. The systems comprising water concentrations in a range from 55 to 60.62% w/w were soft semisolids suitable for topical application, and they were selected for physicochemical and biopharmaceutical evaluation. Analysis of conductivity results and light microscopy examination revealed that investigated systems were water dilutable dispersions of spherical oligolamellar associates of phospholipids and triglyceride molecules in the copolymer water solution. Rheological behavior evaluation results indicated that the investigated gels were thermosensitive shear thinning systems. Ibuprofen (5% w/w) was incorporated by dispersing into the previously prepared carriers. Drug-loaded systems were physically stable at storage temperature from 5 ± 3°C to 40 ± 2°C, for 30 days. In vitro ibuprofen release was in accordance with the Higuchi model (rH>0.95) and sustained for 12h. The obtained results implicated that formulated LLPBGs, optimized regarding drug release and organoleptic properties, represent promising carriers for sustained percutaneous drug delivery of poorly soluble drugs. Copyright © 2015 Elsevier B.V. All rights reserved.

  14. Setting accelerated dissolution test for PLGA microspheres containing peptide, investigation of critical parameters affecting drug release rate and mechanism.

    Science.gov (United States)

    Tomic, I; Vidis-Millward, A; Mueller-Zsigmondy, M; Cardot, J-M

    2016-05-30

    The objective of this study was development of accelerated in vitro release method for peptide loaded PLGA microspheres using flow-through apparatus and assessment of the effect of dissolution parameters (pH, temperature, medium composition) on drug release rate and mechanism. Accelerated release conditions were set as pH 2 and 45°C, in phosphate buffer saline (PBS) 0.02M. When the pH was changed from 2 to 4, diffusion controlled phases (burst and lag) were not affected, while release rate during erosion phase decreased two-fold due to slower ester bonds hydrolyses. Decreasing temperature from 45°C to 40°C, release rate showed three-fold deceleration without significant change in release mechanism. Effect of medium composition on drug release was tested in PBS 0.01M (200 mOsm/kg) and PBS 0.01M with glucose (380 mOsm/kg). Buffer concentration significantly affected drug release rate and mechanism due to the change in osmotic pressure, while ionic strength did not have any effect on peptide release. Furthermore, dialysis sac and sample-and-separate techniques were used, in order to evaluate significance of dissolution technique choice on the release process. After fitting obtained data to different mathematical models, flow-through method was confirmed as the most appropriate for accelerated in vitro dissolution testing for a given formulation. Copyright © 2016 Elsevier B.V. All rights reserved.

  15. pH- and temperature-sensitive polymeric microspheres for drug delivery: the dissolution of copolymers modulates drug release.

    Science.gov (United States)

    Fundueanu, Gheorghe; Constantin, Marieta; Stanciu, Cristina; Theodoridis, Georgios; Ascenzi, Paolo

    2009-12-01

    Most pH-/temperature-responsive polymers for controlled release of drugs are used as cross-linked hydrogels. However, the solubility properties of the linear polymers below and above the lower critical solution temperature (LCST) are not exploited. Here, the preparation and characterization of poly (N-isopropylacrylamide-co-methacrylic acid-co-methyl methacrylate) (poly (NIPAAm-co-MA-co-MM)) and poly (N-isopropylacrylamide-co-acrylamide) (poly (NIPAAm-co-AAm)), known as "smart" polymers (SP), is reported. Both poly (NIPAAm-co-MA-co-MM) and poly (NIPAAm-co-AAm) display pH- and temperature-responsive properties. Poly (NIPAAm-co-MA-co-MM) was designed to be insoluble in the gastric fluid (pH = 1.2), but soluble in the intestinal fluid (pH = 6.8 and 7.4), at the body temperature (37 degrees C). Poly (NIPAAm-co-AAm) was designed to have a lower critical solution temperature (LCST) corresponding to 37 degrees C at pH = 7.4, therefore it is not soluble above the LCST. The solubility characteristics of these copolymers were exploited to modulate the rate of release of drugs by changing pH and/or temperature. These copolymers were solubilized with hydrophobic cellulose acetate butyrate (CAB) and vitamin B(12) (taken as a water soluble drug model system) in an acetone/methanol mixture and dispersed in mineral oil. By a progressive evaporation of the solvent, the liquid droplets were transformed into loaded CAB/SP microspheres. Differential scanning calorimetric studies and scanning electron microscopy analysis demonstrated that the polymeric components of the microspheres precipitated separately during solvent evaporation forming small microdomains. Moreover, vitamin B(12) was found to be molecularly dispersed in both microdomains with no specific affinity for any polymeric component of microspheres. The release of vitamin B(12) was investigated as a function of temperature, pH, and the CAB/SP ratio.

  16. Improvement in autologous human fat transplant survival with SVF plus VEGF-PLA nano-sustained release microspheres.

    Science.gov (United States)

    Li, Liqun; Pan, Shengsheng; Ni, Binting; Lin, Yuanshao

    2014-08-01

    Early neovascularization is important for autologous fat transplant survival. SVF cells are ideal seed cells. Both vascular endothelial growth factor (VEGF) and SVF cells can promote neovascularization. However, the half-life (about 50 min) of VEGF is too short to sustain an adequate local concentration. We have investigated whether VEGF-polylactic acid (PLA) nano-sustained release microspheres plus SVF cells can improve neovascularization and survival of transplanted fat tissues. SVF cells were harvested and constructed VEGF-PLA nano-sustained release microspheres in vitro. Human fat tissues was mixed with SVF cells plus VEGF-PLA, SVF cells alone or Dulbecco's modified Eagle's medium as the control. These three mixtures were injected into random sites in 18 nude mice. Two months later, the transplants were weighed and examined histologically; and capillaries were counted to quantify neovascularization. Hematoxylin-eosin (HE) and anti-VEGF stains were applied to reveal cell infiltration. The mean wet weight of fat in the SVF plus VEGF-PLA, SVF alone, and control transplants were 0.18 ± 0.013 g, 0.16 ± 0.015 g, and 0.071 ± 0.12 g, respectively; the differences between groups were statistically significant. More vessels were present in the SVF plus VEGF-PLA transplants than in the other two types. Transplants mixed with SVF cells also had an acceptable density of capillaries. Histological analysis revealed that both the SVF plus VEGF-PLA and SVF alone transplants, but not the control transplants, were composed of adipose tissue, and had less fat necrosis and less fibrosis than control specimens. SVF plus VEGF-PLA transplants had significantly greater capillary density and VEGF expression than the other two transplant groups. Thus transplanted fat tissue survival and quality can be enhanced by the addition of VEGF-PLA nano-sustained release microspheres plus SVF cells. © 2014 International Federation for Cell Biology.

  17. Ibuprofen dosing for children

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/patientinstructions/000772.htm Ibuprofen dosing for children To use the sharing features ... much of this medicine can be harmful. How Ibuprofen can Help Your Child Ibuprofen is a type ...

  18. Incorporation of chitosan microspheres into collagen-chitosan scaffolds for the controlled release of nerve growth factor.

    Directory of Open Access Journals (Sweden)

    Wen Zeng

    Full Text Available Artifical nerve scaffold can be used as a promising alternative to autologous nerve grafts to enhance the repair of peripheral nerve defects. However, current nerve scaffolds lack efficient microstructure and neurotrophic support.Microsphere-Scaffold composite was developed by incorporating chitosan microspheres loaded with nerve growth factor (NGF-CMSs into collagen-chitosan scaffolds (CCH with longitudinally oriented microchannels (NGF-CMSs/CCH. The morphological characterizations, in vitro release kinetics study, neurite outgrowth assay, and bioactivity assay were evaluated. After that, a 15-mm-long sciatic nerve gap in rats was bridged by the NGF-CMSs/CCH, CCH physically absorbed NGF (NGF/CCH, CCH or nerve autograft. 16 weeks after implantation, electrophysiology, fluoro-gold retrograde tracing, and nerve morphometry were performed.The NGF-CMSs were evenly distributed throughout the longitudinally oriented microchannels of the scaffold. The NGF-CMSs/CCH was capable of sustained release of bioactive NGF within 28 days as compared with others in vitro. In vivo animal study demonstrated that the outcomes of NGF-CMSs/CCH were better than those of NGF/CCH or CCH.Our findings suggest that incorporation of NGF-CMSs into the CCH may be a promising tool in the repair of peripheral nerve defects.

  19. A study of chitosan hydrogel with embedded mesoporous silica nanoparticles loaded by ibuprofen as a dual stimuli-responsive drug release system for surface coating of titanium implants.

    Science.gov (United States)

    Zhao, Pengkun; Liu, Hongyu; Deng, Hongbing; Xiao, Ling; Qin, Caiqin; Du, Yumin; Shi, Xiaowen

    2014-11-01

    In this study, the complex pH and electro responsive system made of chitosan hydrogel with embedded mesoporous silica nanoparticles (MSNs) was evaluated as a tunable drug release system. As a model drug, ibuprofen (IB) was used; its adsorption in MSNs was evidenced by Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and thermogravimetric analysis (TG). In order to prepare the complex drug release system, the loaded particles IB-MSNs were dispersed in chitosan solution and then the complex IB-MSNs/chitosan film of 2mm thickness was deposited as a hydrogel on the titanium electrode. The codeposition of components was performed under a negative biasing of the titanium electrode at -0.75 mA/cm2 current density during 30 min. The IB release from the IB-MSNs/chitosan hydrogel film was studied as dependent on pH of the release media and electrical conditions applied to the titanium plate. When incubating the complex hydrogel film in buffers with different pH, the IB release followed a near zero-order profile, though its kinetics varied. Compared to the spontaneous IB release from the hydrogel in 0.9% NaCl solution (at 0 V), the application of negative biases to the coated titanium plate had profound effluences on the release behavior. The release was retarded when -1.0 V was applied, but a faster kinetics was observed at -5.0 V. These results imply that a rapid, mild and facile electrical process for covering titanium implants by complex IB-MSNs/chitosan hydrogel films can be used for controlled drug delivery applications. Copyright © 2014 Elsevier B.V. All rights reserved.

  20. Degradation and protein release properties of microspheres prepared from biodegradable poly(lactide-co-glycolide) and ABA triblock copolymers: influence of buffer media on polymer erosion and bovine serum albumin release.

    Science.gov (United States)

    Bittner, B; Witt, C; Mäder, K; Kissel, T

    1999-08-05

    The aim of the present study was to investigate the influence of the chemical insertion of poly(ethylene oxide), PEO, into a poly(lactide-co-glycolide), PLG, backbone on the mechanisms of in vitro degradation and erosion of the polymer. For this purpose microspheres prepared by a modified W/O/W double emulsion technique using ABA triblock copolymers, consisting of PLG A-blocks attached to central PEO B-blocks were compared with microspheres prepared from PLG. Due to their molecular architecture the ABA triblock copolymers differed in their erosion and degradation behavior from PLG. Degradation occurred faster in the ABA polymers by cleavage of ester bonds inside the polymer backbone. Even erosion was shown to start immediately after incubation in different buffer media. By varying pH and ionic strength of the buffer it was found that both mass loss and molecular weight decay were accelerated in alkaline and acidic pH in the case of the ABA triblock copolymers. Although the pH of the medium had a moderate influence on the degradation of PLG, the molecular weight decay was not accompanied by a mass loss during the observation time. In a second set of experiments we prepared bovine serum albumin, BSA, loaded microspheres from both polymers. The release of BSA from ABA microspheres under in vitro conditions parallels the faster swelling and erosion rates. This could be confirmed by electron paramagnetic resonance, EPR, measurements with spin labeled albumin where an influx of buffer medium into the ABA microspheres was already observed within a few minutes. In contrast, PLG microspheres revealed a burst release without any erosion. The current study shows that the environmental conditions affected the degradation and erosion of the pure polymer microspheres in the same way as the release of the model protein. This leads to the conclusion that the more favorable degradation profile of the ABA triblock copolymers was responsible for the improvement of the release profile.

  1. The influence of spray-drying parameters on phase behavior, drug distribution, and in vitro release of injectable microspheres for sustained release.

    Science.gov (United States)

    Meeus, Joke; Lenaerts, Maité; Scurr, David J; Amssoms, Katie; Davies, Martyn C; Roberts, Clive J; Van Den Mooter, Guy

    2015-04-01

    For ternary solid dispersions, it is indispensable to characterize their structure, phase behavior, and the spatial distribution of the dispersed drug as this might influence the release profile and/or stability of these formulations. This study shows how formulation (feed concentration) and process (feed rate, inlet air temperature, and atomizing air pressure) parameters can influence the characteristics of ternary spray-dried solid dispersions. The microspheres considered here consist of a poly(lactic-co-glycolic acid) (PLGA) surface layer and an underlying polyvinylpyrrolidone (PVP) phase. A poorly soluble active pharmaceutical ingredient (API) was molecularly dispersed in this matrix. Differences were observed in component miscibility, phase heterogeneity, particle size, morphology, as well as API surface coverage for selected spray-drying parameters. Observed differences are likely because of changes in the droplet generation, evaporation, and thus particle formation processes. However, varying particle characteristics did not influence the drug release of the formulations studied, indicating the robustness of this approach to produce particles of consistent drug release characteristics. This is likely because of the fact that the release is dominated by diffusion from the PVP layer through pores in the PLGA surface layer and that observed differences in the latter have no influence on the release. © 2015 Wiley Periodicals, Inc. and the American Pharmacists Association.

  2. DNA-assisted binding of microspheres on glass substrates and their laser-induced release

    International Nuclear Information System (INIS)

    Kim, Sejong; Geiss, Erik; Yu, Phillip; Papadimitrakopoulos, Fotios; Marcus, Harris L.

    2006-01-01

    DNA hybridization has been increasingly adopted in materials sciences due to its complementary nature of single stranded DNAs. This unique property could be potentially used in the realization of 2 dimensional (2D) arrays of colloidal microspheres as a precursor to further build more complicated superstructures. In order to precisely understand this DNA-assisted assembly of colloidal particles, we quantitatively assessed the surface density of grafted and hybridizing accessible DNA oligomers on both substrate and colloidal particles. The DNA grafting densities were determined by UV-Vis of dye-functionalized complementary DNA oligomers, in conjunction with theoretical models. The variations of the concentration of hybridized DNA as a function of parameters such as the number of DNA base pairs (bp), the length of spacer and the size of sphere were also investigated to determine the immobilization strength of colloidal microspheres on the substrate. Dehybridization of the particle was conducted by utilizing a focused laser beam. These results were also compared with the particle hybridization energies and modeled according to the sum of DNA bindings as a function of the number of hybridized bases

  3. Structural and morphological studies on poly(3-hydroxybutyrate acid) (PHB)/chitosan drug releasing microspheres prepared by both single and double emulsion processes

    Energy Technology Data Exchange (ETDEWEB)

    Shih, W.-J. [Department of Materials Science and Engineering, National Cheng Kung University, 1 Ta-Hsueh Road, Tainan 70101, Taiwan (China); Chen, Y.-H. [Department of Mechanical Engineering, National Kaohsiung University of Applied Sciences, 415 Chien-kung Road, Kaohsiung 80782, Taiwan (China); Shih, C.-J. [Faculty of Fragrance and Cosmetics, Kaohsiung Medical University, No. 100, Shih-Chuang 1st Rd., Sanmin District, Kaohsiung 80708, Taiwan (China); Hon, M.-H. [Department of Materials Science and Engineering, National Cheng Kung University, 1 Ta-Hsueh Road, Tainan 70101, Taiwan (China); Dayeh University, 112 Shan-Jiau Road, Da-Tsuen, Changhua 515, Taiwan (China); Wang, M.-C. [Department of Mechanical Engineering, National Kaohsiung University of Applied Sciences, 415 Chien-kung Road, Kaohsiung 80782, Taiwan (China) and Department of Materials Science and Engineering, National United University, 1 Lien-Da Road, Kung-ching Li, Miao Li 360, Taiwan (China)]. E-mail: mcwang@cc.kuas.edu.tw

    2007-05-31

    Drug releasing microspheres of poly(3-hydroxybutyric acid)/chitosan (PHB/CTS) with various compositions have been synthesized by both single and double emulsion methods, and collected by a freeze-drying process. In this study, gentamicin was used as an antibacterial medicine coated with PHB. The PHB/CTS microspheres of various compositions prepared by a single emulsion process (SEP) were identified as the major PHB phase together with a minor unknown Phase X by X-ray diffraction (XRD) and FT-IR. However, in the microspheres prepared using a double emulsion process (DEP) the dominant Phase was X and the minor phase was PHB. The size of the PHB/CTS microspheres prepared by SEP increased with the PHB/CTS ratio from 1 {mu}m for 1:1 to 2 {mu}m for 5:1. However, the size of the PHB/CTS microspheres prepared by DEP decreased with the PHB/CTS ratio from 1 {mu}m for 1:1 to 800 nm for 5:1.

  4. Structural and morphological studies on poly(3-hydroxybutyrate acid) (PHB)/chitosan drug releasing microspheres prepared by both single and double emulsion processes

    International Nuclear Information System (INIS)

    Shih, W.-J.; Chen, Y.-H.; Shih, C.-J.; Hon, M.-H.; Wang, M.-C.

    2007-01-01

    Drug releasing microspheres of poly(3-hydroxybutyric acid)/chitosan (PHB/CTS) with various compositions have been synthesized by both single and double emulsion methods, and collected by a freeze-drying process. In this study, gentamicin was used as an antibacterial medicine coated with PHB. The PHB/CTS microspheres of various compositions prepared by a single emulsion process (SEP) were identified as the major PHB phase together with a minor unknown Phase X by X-ray diffraction (XRD) and FT-IR. However, in the microspheres prepared using a double emulsion process (DEP) the dominant Phase was X and the minor phase was PHB. The size of the PHB/CTS microspheres prepared by SEP increased with the PHB/CTS ratio from 1 μm for 1:1 to 2 μm for 5:1. However, the size of the PHB/CTS microspheres prepared by DEP decreased with the PHB/CTS ratio from 1 μm for 1:1 to 800 nm for 5:1

  5. Semi-interpenetrating network of acrylamide-grafted-sodium alginate microspheres for controlled release of diclofenac sodium, preparation and characterization.

    Science.gov (United States)

    Al-Kahtani, Ahmed A; Sherigara, B S

    2014-03-01

    The semi-interpenetrating networks (semi-IPNs) of acrylamide grafted sodium alginate (AAm-g-NaAlg) microspheres (MPs) were prepared by emulsion-crosslinking method using glutaraldehyde (GA) as a crosslinking agent. The grafting of acrylamide onto sodium alginate was prepared by free-radical graft polymerization using ceric ammonium nitrate (CAN) as initiator at three acrylamide concentrations with monomer to polymer ratio of 1:1, 2:1 and 3:1, respectively. The grafting efficiency was found to be 91%. The produced MPs are almost spherical in nature with smooth surfaces. Diclofenac sodium (DS), an anti-inflammatory drug was successfully encapsulated into the MPs. The encapsulation efficiency was found to vary between 83% and 95%. The MPs were characterized by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. The diffusion coefficient (D) was dependent upon the amount of crosslinking agent (GA) and amount of grafting ratio in the matrix. The rate of release was found to be dependent on the amount of GA, AAm:NaAlg grafting ratio and % drug loading in the MPs. The release data have been fitted to an empirical equation to investigate the diffusional exponent (n), which indicated that the release mechanism from MPs follows the super Case II transport. Copyright © 2013 Elsevier B.V. All rights reserved.

  6. Solid State NMR Characterization of Ibuprofen:Nicotinamide Cocrystals and New Idea for Controlling Release of Drugs Embedded into Mesoporous Silica Particles.

    Science.gov (United States)

    Skorupska, Ewa; Kaźmierski, Sławomir; Potrzebowski, Marek J

    2017-05-01

    Grinding and melting methods were employed for synthesis of pharmaceutical cocrystals formed by racemic (R/S) and entiomeric (S) ibuprofen (IBU) and nicotinamide (NA) as coformer. Obtained (R/S)-IBU:NA and (S)-IBU:NA cocrystals were fully characterized by means of advanced one- and two-dimensional solid state nuclear magnetic resonance (SS NMR) techniques with very fast magic angle spinning (MAS) at 60 kHz. The distinction in molecular packing and specific hydrogen bonding pattern was clearly recognized by analysis of 1 H, 13 C, and 15 N spectra. It is concluded from these studies that both methods (grinding and melting) provide exactly the same, specific forms of cocrystals. Thermal solvent-free (TSF) approach was used for loading of (R/S)-IBU:NA and (S)-IBU:NA into the pores of MCM-41 mesoporous silica particle (MSP). The progress and efficiency of this process was analyzed by NMR spectroscopy. It has been confirmed that TSF method is an effective and safe technique of filling the MSP pores with active pharmaceutical ingredients (APIs). By analyzing the NMR results, it has been further proved that excess of IBU and NA components, which are not embedded into the pores during melting and cooling, crystallize on the MCM-41 walls preserving very specific arrangement, characteristic for crystalline samples. By investigating kinetic of release for (R/S)-IBU/MCM-41, (S)-IBU:NA/MCM-41, and (R/S)-IBU:NA/MCM-41 samples containing active components exclusively inside of the pores, it was revealed that release of IBU is much faster for the first of the samples compared to those containing IBU and NA inside the pores. The hypothesis that the rate of release of API can be controlled by specific composition of cocrystal embedded into the MSP pore was further supported by study of (R/S)-IBU:BA/MCM-41 sample with benzoic acid (BA) as coformer.

  7. Novel pH- and temperature-responsive blend hydrogel microspheres of sodium alginate and PNIPAAm-g-GG for controlled release of isoniazid.

    Science.gov (United States)

    Kajjari, Praveen B; Manjeshwar, Lata S; Aminabhavi, Tejraj M

    2012-12-01

    This paper reports the preparation and characterization of novel pH- and thermo-responsive blend hydrogel microspheres of sodium alginate (NaAlg) and poly(N-isopropylacrylamide)(PNIPAAm)-grafted-guar gum (GG) i.e., PNIPAAm-g-GG by emulsion cross-linking method using glutaraldehyde (GA) as a cross-linker. Isoniazid (INZ) was chosen as the model antituberculosis drug to achieve encapsulation up to 62%. INZ has a plasma half-life of 1.5 h, whose release was extended up to 12 h. Fourier transform infrared spectroscopy was used to confirm the grafting reaction and chemical stability of INZ during the encapsulation. Differential scanning calorimetry was used to investigate the drug's physical state, while powder X-ray diffraction confirmed the molecular level dispersion of INZ in the matrix. Scanning electron microscopy confirmed varying surface morphologies of the drug-loaded microspheres. Temperature- and pH-responsive nature of the blend hydrogel microspheres were investigated by equilibrium swelling, and in vitro release experiments were performed in pH 1.2 and pH 7.4 buffer media at 37°C as well as at 25°C. Kinetics of INZ release was analyzed by Ritger-Peppas empirical equation to compute the diffusional exponent parameter (n), whose value ranged between 0.27 and 0.58, indicating the release of INZ follows a diffusion swelling controlled release mechanism.

  8. Novel Fabrication of Biodegradable Superabsorbent Microspheres with Diffusion Barrier through Thermo-Chemical Modification and Their Potential Agriculture Applications for Water Holding and Sustained Release of Fertilizer.

    Science.gov (United States)

    Feng, Diejing; Bai, Bo; Wang, Honglun; Suo, Yourui

    2017-07-26

    Synergistic utilization of water and fertilizer has vital contribution to the modern production of agriculture. This work reports on a simple and facile strategy to prepare biodegradable yeast/sodium alginate/poly(vinyl alcohol) superabsorbent microspheres with a diffusion barrier merit by thermo-chemical modification route. The integrated performances, including water absorbency, water retention, water evaporation ratio, leaching loss control, sustained-release behaviors, and degradation in soil, were systematically investigated. The results revealed that the modified microspheres were a triumphant water and fertilizer manager to effectively hold water and control the unexpected leakage of fertilizer for sustained release. Therefore, this work provides a promising approach to ameliorate the utilization efficiency of water and fertilizer in potential agriculture applications.

  9. Novel therapeutic approach for pulmonary emphysema using gelatin microspheres releasing basic fibroblast growth factor in a canine model.

    Science.gov (United States)

    Chang, Sung Soo; Yokomise, Hiroyasu; Matsuura, Natsumi; Gotoh, Masashi; Tabata, Yasuhiko

    2014-08-01

    The prognosis of patients with emphysema is poor as there is no truly effective treatment. Our previous study showed that the alveolar space was smaller and the microvessel density was higher in a canine emphysema model after the intrapulmonary arterial administration of gelatin microspheres slowly releasing basic fibroblast growth factor (bFGF-GMS). In the present study, we evaluated the functional effect of injecting bFGF-GMS via the pulmonary artery in this canine pulmonary emphysema model. Using the porcine pancreatic elastase (PPE)-induced total emphysema model, we approximated the value of lung compliance with a Power Lab System, and performed blood gas analysis in a control group, a total emphysema group, and a bFGF group in which bFGF-GMS were injected toward the whole pulmonary artery via the femoral vein. Each group comprised five dogs. Lung compliance was higher in the total emphysema group than in the control group (p = 0.031), and the bFGF group showed no significant improvement of lung compliance vs. the total emphysema group (p = 0.112). PaO2 (partial pressure of oxygen in arterial blood) was improved by administering bFGF-GMS in the total emphysema model (p = 0.027). In the canine total emphysema model, blood gas parameters were improved by the whole pulmonary arterial administration of bFGF-GMS. This method has the potential to be an effective novel therapy for pulmonary emphysema.

  10. Bioavailability of ibuprofen following oral administration of standard ibuprofen, sodium ibuprofen or ibuprofen acid incorporating poloxamer in healthy volunteers

    OpenAIRE

    Dewland, Peter M; Reader, Sandie; Berry, Phillip

    2009-01-01

    Background The aim of this study was to compare the pharmacokinetic properties of sodium ibuprofen and ibuprofen acid incorporating poloxamer with standard ibuprofen acid tablets. Methods Twenty-two healthy volunteers were enrolled into this randomised, single-dose, 3-way crossover, open-label, single-centre, pharmacokinetic study. After 14 hours' fasting, participants received a single dose of 2 × 200 mg ibuprofen acid tablets (standard ibuprofen), 2 × 256 mg ibuprofen sodium dihydrate table...

  11. Ibuprofen - a Safe Analgesic During Cardiac Surgery Recovery?

    DEFF Research Database (Denmark)

    Qazi, Saddiq Mohammad; Sindby, Eske Jesper; Nørgaard, Martin Agge

    2015-01-01

    were undergoing cardiac surgery for the first time, were randomly allocated either to a regimen of slow-release oxycodone (10 mg twice daily) or slow-release ibuprofen (800 mg twice daily) combined with lansoprazole. Data relating to blood-tests, angiographies, surgical details and administered...... if short term slow release ibuprofen combined with lansoprazole treatment is used when compared to an oxycodone based regimen. Renal function should, however, be closely monitored and in the event of any decrease in renal function ibuprofen must be discontinued....

  12. Technology of stable, prolonged-release eye-drops containing Cyclosporine A, distributed between lipid matrix and surface of the solid lipid microspheres (SLM).

    Science.gov (United States)

    Wolska, Eliza; Sznitowska, Małgorzata

    2013-01-30

    The aim of this study was to prepare solid lipid microspheres (SLM) with incorporated Cyclosporine A (Cs), suitable for ocular application. For this purpose, SLM were formulated by using different lipids and three different nonionic surfactants. The SLM were produced using a hot emulsification method. The SLM dispersions contained 10, 20 or 30% of lipid (w/w) and up to 2% (w/w) of Cs. The size of the microspheres with Cs ranged from 1 to 15 μm. Physically stable SLM with Cs were prepared using Compritol, as a lipid matrix, and Tween 80, as a surfactant. In contrast, dispersion with Precirol alone, formed semi-solid gels during storage, while in formulations with Precirol and Miglyol, crystals of Cs were observed. In vitro release profile of Compritol formulations showed that 40% of Cs is released within 1h, while the release of the following 40% takes more time, depending on lipid content in the formulations. The large part of Cs, added to SLM formulations (from 45 to 80%), was found on the surface of microparticles, but no drug crystallization occurred during a long-term storage. Copyright © 2012 Elsevier B.V. All rights reserved.

  13. Yolk-Shell Porous Microspheres of Calcium Phosphate Prepared by Using Calcium L-Lactate and Adenosine 5'-Triphosphate Disodium Salt: Application in Protein/Drug Delivery.

    Science.gov (United States)

    Ding, Guan-Jun; Zhu, Ying-Jie; Qi, Chao; Sun, Tuan-Wei; Wu, Jin; Chen, Feng

    2015-06-26

    A facile and environmentally friendly approach has been developed to prepare yolk-shell porous microspheres of calcium phosphate by using calcium L-lactate pentahydrate (CL) as the calcium source and adenosine 5'-triphosphate disodium salt (ATP) as the phosphate source through the microwave-assisted hydrothermal method. The effects of the concentration of CL, the microwave hydrothermal temperature, and the time on the morphology and crystal phase of the product are investigated. The possible formation mechanism of yolk-shell porous microspheres of calcium phosphate is proposed. Hemoglobin from bovine red cells (Hb) and ibuprofen (IBU) are used to explore the application potential of yolk-shell porous microspheres of calcium phosphate in protein/drug loading and delivery. The experimental results indicate that the as-prepared yolk-shell porous microspheres of calcium phosphate have relatively high protein/drug loading capacity, sustained protein/drug release, favorable pH-responsive release behavior, and a high biocompatibility in the cytotoxicity test. Therefore, the yolk-shell porous microspheres of calcium phosphate have promising applications in various biomedical fields such as protein/drug delivery. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  14. Release and Cytokine Production of BmpB from BmpB-Loaded pH-Sensitive and Mucoadhesive Thiolated Eudragit Microspheres.

    Science.gov (United States)

    Singh, Bijay; Jiang, Tao; Kim, You-Kyoung; Kang, Sang-Kee; Choi, Yun-Jaie; Cho, Chong-Su

    2015-01-01

    Swine dysentery is a contagious mucohaemorrhagic colitis of pigs that is caused by anaerobic intestinal spirochaete Brachyspira hyodysenteriae. Recently, an outer membrane lipoprotein of B. hyodysenteriae (BmpB) has been identified, and the mice or pigs immunized with a recombinant BmpB generated antibodies recognizing the native BmpB of B. hyodysenteriae. In this study, we cloned, expressed and purified BmpB protein from E. coli and used it as a vaccine candidate for oral delivery. The BmpB was encapsulated into the pH-sensitive and thiolated Eudragit microspheres (TEMS). The sizes of the microspheres ranged from 5-20 μ. About 22-34% of BmpB were released from the BmpB-loaded TEMS within 24 h at stomach pH 2.0 whereas the release of BmpB from the BmpB-loaded TEMS was 35% in the first one hour and reached 81% within 24 h at intestinal pH 7.2. These data revealed that the BmpB could be protected in the harsh gastric condition. Mucoadhesive experiment in vitro showed that TEMS have high binding affinity with the mucin glycoproteins of porcine intestine. Finally, in vitro production of cytokines from immune cells treated with the BmpB-loaded TEMS suggested that the TEMS would be a promising approach for oral delivery of BmpB as vaccine candidate.

  15. Pelepasan Ibuprofen Dari Gel Karbomer 940 Kokristal Ibuprofen-Nikotinamida

    OpenAIRE

    Agustin, Rini; Sari, Novica; Zaini, Erizal

    2014-01-01

    Salah satu metode untuk meningkatkan kelarutan adalah co-kristalisasi. Ibuprofen dapat digunakan dalam aplikasi topikal untuk rheumatoid arthrisi, sehingga telah dilakukan sebuah studi tentang formulasi dan pelepasan kokristal ibuprofen-nikotinamida dari gel karbomer 940. Kokristal diperoleh dari metode penguapan pelarut dengan komposisi equimol (1:1). Gel terdiri dari dua formula dengan jumlah ibuprofen yang sama (5%). Formula pertama adalah gel kokristal ibuprofen-nicotinamida dan Formula d...

  16. Hydrolysis of Ibuprofen Nitrile and Ibuprofen Amide and Deracemisation of Ibuprofen Using Nocardia corallina B-276

    OpenAIRE

    Myrna Solís-Oba; Norberto Manjarrez; Aida Solís; Ricardo Lievano; Herminia Inés Pérez

    2012-01-01

    A novel application of whole cells of Nocardia corallina B-276 for the deracemisation of ibuprofen is reported. This microorganism successfully hydrolysed ibuprofen nitrile to ibuprofen amide, and ibuprofen amide to ibuprofen, using a suspension of cells in a potassium phosphate buffer solution (0.1 M, pH = 7.0). These results can be explained by the presence of NHase and amidase enzymes, but the reactions are not enantioselective and low ee values were obtained. However, (R)-ibuprofen was is...

  17. How to Safely Give Ibuprofen

    Science.gov (United States)

    ... of ibuprofen are available in similar forms. How to Give When giving ibuprofen, refer to the following dosage ... of Use Notice of Nondiscrimination Visit the Nemours Web site. Note: All information on KidsHealth® is for ...

  18. Synthesis of deuterium labelled ibuprofen

    International Nuclear Information System (INIS)

    Cappon, V.J.; Halstead, G.W.; Theis, D.L.

    1986-01-01

    The preparations of [ar- 2 H 4 ]-ibuprofen and [ar, 3,3,3- 2 H 7 ]-ibuprofen are described. The deuterium was incorporated into the aromatic ring of [ar- 2 H 4 ]-ibuprofen which is a metabolically stable position. [ar, 3,3,3- 2 H 7 ]-ibuprofen was synthesized by the same route using [ 2 H 3 ]-CH 3 I instead of CH 3 I for use as a GC/MS internal standard in stable isotope labelled bioavailability studies. (author)

  19. DEGRADATION AND INTRAHEPATIC COMPATIBILITY OF ALBUMIN-HEPARIN CONJUGATE MICROSPHERES

    NARCIS (Netherlands)

    CREMERS, HFM; WOLF, RFE; BLAAUW, EH; SCHAKENRAAD, JM; LAM, KH; NIEUWENHUIS, P; VERRIJK, R; KWON, G; BAE, YH; KIM, SW; FEIJEN, J

    The in vitro degradation properties of glutaraldehyde cross-linked albumin and albumin-heparin conjugate microspheres (AMS and AHCMS respectively) were evaluated using light microscopy, turbidity measurements and heparin release determinations, showing that the microspheres are degraded by

  20. Effect of a controlled release device containing minocycline microspheres on the treatment of chronic periodontitis: A comparative study

    Science.gov (United States)

    Gopinath, V.; Ramakrishnan, T.; Emmadi, Pamela; Ambalavanan, N.; Mammen, Biju; Vijayalakshmi

    2009-01-01

    Introduction: Adjunctive therapy with locally delivered antimicrobials has resulted in improved clinical outcomes. The aim of this study was to evaluate the efficacy and safety of locally administered minocycline microspheres (Arestin™) in the treatment of chronic periodontitis. Materials and Methods: A total of 60 sites from 15 patients in the age group of 35-50 years, who had periodontal pockets measuring 5-8 mm and had been diagnosed with chronic periodontitis, were selected for the study. The selected groups were randomly assigned to either the control group (group A) or the treatment/test group (group B). Only scaling and root planing were done at the base line visit for the control sites followed by local application of Arestin™ (1 mg). Clinical parameters such as plaque index, gingival index, and gingival bleeding index were recorded at baseline, day 30, day 90, and day 180 in the selected sites of both the groups. Probing pocket depth also was recorded at baseline, day 90, and day 180 for both the groups. Results: A statistically significant reduction was observed in both groups. Group B showed better results than Group A and these differences were statistically significant. Conclusion: The results of this study clearly indicate that treatment with scaling and root planing plus minocycline microspheres (Arestin™) is more effective and safer than scaling and root planing alone in reducing the signs of chronic periodontitis. PMID:20407655

  1. Effect of a controlled release device containing minocycline microspheres on the treatment of chronic periodontitis: A comparative study

    Directory of Open Access Journals (Sweden)

    Gopinath V

    2009-01-01

    Full Text Available Introduction: Adjunctive therapy with locally delivered antimicrobials has resulted in improved clinical outcomes. The aim of this study was to evaluate the efficacy and safety of locally administered minocycline microspheres (Arestin TM in the treatment of chronic periodontitis. Materials and Methods: A total of 60 sites from 15 patients in the age group of 35-50 years, who had periodontal pockets measuring 5-8mm and had been diagnosed with chronic periodontitis, were selected for the study. The selected groups were randomly assigned to either the control group (group A or the treatment/test group (group B. Only scaling and root planing were done at the base line visit for the control sites followed by local application of Arestin™ (1mg. Clinical parameters such as plaque index, gingival index, and gingival bleeding index were recorded at baseline, day 30, day 90, and day 180 in the selected sites of both the groups. Probing pocket depth also was recorded at baseline, day 90, and day 180 for both the groups. Results: A statistically significant reduction was observed in both groups. Group B showed better results than Group A and these differences were statistically significant. Conclusion: The results of this study clearly indicate that treatment with scaling and root planing plus minocycline microspheres (Arestin™ is more effective and safer than scaling and root planing alone in reducing the signs of chronic periodontitis.

  2. Ibuprofen: Synthesis, production and properties

    Directory of Open Access Journals (Sweden)

    Mijin Dušan Ž.

    2003-01-01

    Full Text Available Since its introduction in 1969, ibuprofen has become one of the most common painkillers in the world. Ibuprofen in an NSAID (non-steroidal anti-inflammatory drug and like other drugs of its class it possesses analgetic, antipyretic and anti-inflammatory properties. While ibuprofen is a relatively simple molecule, there is still sufficient structural complexity to ensure that a large number of different synthetic approaches are possible. Since the introduction of pharmaceutical products containing ibuprofen, industrial and academic scientists have developed many potential production processes. This paper describes the history, synthesis and production, as well as the properties and stability of ibuprofen.

  3. PLGA/alginate composite microspheres for hydrophilic protein delivery

    International Nuclear Information System (INIS)

    Zhai, Peng; Chen, X.B.; Schreyer, David J.

    2015-01-01

    Poly(lactic-co-glycolic acid) (PLGA) microspheres and PLGA/alginate composite microspheres were prepared by a novel double emulsion and solvent evaporation technique and loaded with bovine serum albumin (BSA) or rabbit anti-laminin antibody protein. The addition of alginate and the use of a surfactant during microsphere preparation increased the encapsulation efficiency and reduced the initial burst release of hydrophilic BSA. Confocal laser scanning microcopy (CLSM) of BSA-loaded PLGA/alginate composite microspheres showed that PLGA, alginate, and BSA were distributed throughout the depths of microspheres; no core/shell structure was observed. Scanning electron microscopy revealed that PLGA microspheres erode and degrade more quickly than PLGA/alginate composite microspheres. When loaded with anti-laminin antibody, the function of released antibody was well preserved in both PLGA and PLGA/alginate composite microspheres. The biocompatibility of PLGA and PLGA/alginate microspheres were examined using four types of cultured cell lines, representing different tissue types. Cell survival was variably affected by the inclusion of alginate in composite microspheres, possibly due to the sensitivity of different cell types to excess calcium that may be released from the calcium cross-linked alginate. - Highlights: • A double emulsion technique is used to prepare protein-loaded PLGA or PLGA/alginate microspheres. • PLGA, alginate and protein are distributed evenly within microsphere structure. • Addition of alginate improves loading efficiency and slows degradation and protein release. • PLGA/alginate microspheres have favorable biocompatibility

  4. PLGA/alginate composite microspheres for hydrophilic protein delivery

    Energy Technology Data Exchange (ETDEWEB)

    Zhai, Peng [Department of Anatomy and Cell Biology, University of Saskatchewan, S7N5E5 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada); Chen, X.B. [Department of Mechanical Engineering, University of Saskatchewan, S7N5A9 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada); Schreyer, David J., E-mail: david.schreyer@usask.ca [Department of Anatomy and Cell Biology, University of Saskatchewan, S7N5E5 (Canada); Division of Biomedical Engineering, University of Saskatchewan, S7N5A9 (Canada)

    2015-11-01

    Poly(lactic-co-glycolic acid) (PLGA) microspheres and PLGA/alginate composite microspheres were prepared by a novel double emulsion and solvent evaporation technique and loaded with bovine serum albumin (BSA) or rabbit anti-laminin antibody protein. The addition of alginate and the use of a surfactant during microsphere preparation increased the encapsulation efficiency and reduced the initial burst release of hydrophilic BSA. Confocal laser scanning microcopy (CLSM) of BSA-loaded PLGA/alginate composite microspheres showed that PLGA, alginate, and BSA were distributed throughout the depths of microspheres; no core/shell structure was observed. Scanning electron microscopy revealed that PLGA microspheres erode and degrade more quickly than PLGA/alginate composite microspheres. When loaded with anti-laminin antibody, the function of released antibody was well preserved in both PLGA and PLGA/alginate composite microspheres. The biocompatibility of PLGA and PLGA/alginate microspheres were examined using four types of cultured cell lines, representing different tissue types. Cell survival was variably affected by the inclusion of alginate in composite microspheres, possibly due to the sensitivity of different cell types to excess calcium that may be released from the calcium cross-linked alginate. - Highlights: • A double emulsion technique is used to prepare protein-loaded PLGA or PLGA/alginate microspheres. • PLGA, alginate and protein are distributed evenly within microsphere structure. • Addition of alginate improves loading efficiency and slows degradation and protein release. • PLGA/alginate microspheres have favorable biocompatibility.

  5. {beta}-TCP porous pellets as an orthopaedic drug delivery system: ibuprofen/carrier physicochemical interactions

    Energy Technology Data Exchange (ETDEWEB)

    Baradari, Hiba; Damia, Chantal; Dutreih-Colas, Maggy; Champion, Eric; Chulia, Dominique; Viana, Marylene, E-mail: hiva.baradari@etu.unilim.fr [SPCTS-Centre Europeen de la Ceramique, 12 Rue Atlantis, 87068 Limoges CEDEX (France)

    2011-10-15

    Calcium phosphate bone substitute materials can be loaded with active substances for in situ, targeted drug administration. In this study, porous {beta}-TCP pellets were investigated as an anti-inflammatory drug carrier. Porous {beta}-TCP pellets were impregnated with an ethanolic solution of ibuprofen. The effects of contact time and concentration of ibuprofen solution on drug adsorption were studied. The ibuprofen adsorption equilibrium time was found to be one hour. The adsorption isotherms fitted to the Freundlich model, suggesting that the interaction between ibuprofen and {beta}-TCP is weak. The physicochemical characterizations of loaded pellets confirmed that the reversible physisorption of ibuprofen on {beta}-TCP pellets is due to Van der Waals forces, and this property was associated with the 100% ibuprofen release.

  6. β-TCP porous pellets as an orthopaedic drug delivery system: ibuprofen/carrier physicochemical interactions

    International Nuclear Information System (INIS)

    Baradari, Hiba; Damia, Chantal; Dutreih-Colas, Maggy; Champion, Eric; Chulia, Dominique; Viana, Marylene

    2011-01-01

    Calcium phosphate bone substitute materials can be loaded with active substances for in situ, targeted drug administration. In this study, porous β-TCP pellets were investigated as an anti-inflammatory drug carrier. Porous β-TCP pellets were impregnated with an ethanolic solution of ibuprofen. The effects of contact time and concentration of ibuprofen solution on drug adsorption were studied. The ibuprofen adsorption equilibrium time was found to be one hour. The adsorption isotherms fitted to the Freundlich model, suggesting that the interaction between ibuprofen and β-TCP is weak. The physicochemical characterizations of loaded pellets confirmed that the reversible physisorption of ibuprofen on β-TCP pellets is due to Van der Waals forces, and this property was associated with the 100% ibuprofen release.

  7. Dissolution of ibuprofen enantiomers from coprecipitates and suspensions containing chiral excipients.

    Science.gov (United States)

    Janjikhel, R K; Adeyeye, C M

    1999-01-01

    The purpose of this research was to evaluate the stereospecific interaction of ibuprofen with chiral excipients such as hydroxypropyl-beta-cyclodextrin (HPCD), tartaric acid, sucrose, hydroxypropylmethylcellulose (HPMC), methylcellulose (MC), and a nonchiral excipient, citric acid. Coprecipitates of ibuprofen were prepared in molar ratios ranging between 1:0.5 and 1:10 by a solvent evaporation method and characterized using x-ray diffraction, Fourier-transform infrared (FTIR) spectroscopy, and dissolution testing. Phase solubility studies of ibuprofen were carried out by adding excess amount of ibuprofen to aqueous excipient solutions of varying concentrations. Interaction was studied in suspensions of ibuprofen with HPMC, MC, and sucrose stored at room temperature and 60 degrees C for 12 weeks. Solubility of ibuprofen in HPCD solutions increased 10-fold, whereas solubility decreased in the tartaric and citric acid solutions, a result of decreased pH with increased amount of the acids in which ibuprofen (pKa 4.8) is less soluble. Phase solubility diagrams of ibuprofen in aqueous HPCD, citric acid, and tartaric acid solutions showed no stereospecific differences in solubility of the two enantiomers. X-ray diffraction studies showed that ibuprofen exists in a crystalline form at low ibuprofen-to-excipient ratios, whereas at the higher ratios, it exists in an amorphous form. FTIR spectroscopy for HPCD coprecipitates showed a shift of the carbonyl stretching band of ibuprofen to a higher wavelength with a markedly decreased intensity, probably because of a breakdown in the intermolecular hydrogen bonding with ibuprofen and restriction of the drug molecule in the HPCD cavity, respectively. Dissolution profiles of the coprecipitates demonstrated higher dissolution rates than those of pure ibuprofen. The presence of chiral excipients did not appear to cause stereoselective release of the drug from the coprecipitates and the suspensions.

  8. Ibuprofen - a Safe Analgesic During Cardiac Surgery Recovery? A Randomized Controlled Trial?

    Directory of Open Access Journals (Sweden)

    Saddiq Mohammad Qazi

    2015-12-01

    Conclusion: The results of this study suggest that patients treated postoperatively, following cardiac surgery, are at no greater risk of harm if short term slow release ibuprofen combined with lansoprazole treatment is used when compared to an oxycodone based regimen. Renal function should, however, be closely monitored and in the event of any decrease in renal function ibuprofen must be discontinued.

  9. Effect of hydroxyapatite-containing microspheres embedded into three-dimensional magnesium phosphate scaffolds on the controlled release of lysozyme and in vitro biodegradation

    Directory of Open Access Journals (Sweden)

    Lee JM

    2014-09-01

    Full Text Available Jongman Lee, Hui-suk YunPowder and Ceramics Division, Korea Institute of Materials Science, Changwon, Republic of KoreaAbstract: The functionality of porous three-dimensional (3D magnesium phosphate (MgP scaffold was investigated for the development of a novel protein delivery system and biomimetic bone tissue engineering scaffold. This enhancement can be achieved by incorporation of hydroxyapatite (HA-containing polymeric microspheres (MSs into a bulk MgP matrix, and a paste-extruding deposition (PED system. In this work, the amount of MS and HA was precisely controlled when manufacturing MS-embedded MgP (MS/MgP composite scaffolds. The main influence was researched in terms of in vitro lysozyme-release, in vitro biodegradation, mechanical properties, and in vitro calcification. The controlled release of lysozyme was indicated, while showing graded release patterns according to HA content. The composite scaffolds degraded gradually with MS content and degradation time. Due to the effect of HA inclusion, the higher HA-containing MS/MgP scaffolds could, not only delay the biodegradation process but also, compensate for the possible loss of mechanical properties. In this regard, it is reasonable to confirm the inverse relationship between biodegradation and corresponding compressive properties. In order to encourage bioactivity and osteoconductivity, the MS/MgP composite scaffolds were subjected to simulated body fluid treatment. Calcium deposition was, in turn, improved with increasing MS and HA content over time. This quantitative result was also proved using morphological and elemental analysis. In summary, a significant transformation of a monolithic MgP scaffold was directed toward a multifunctional bone tissue engineering scaffold equipped with controlled protein delivery, biodegradability, and bioactivity.Keywords: protein delivery, bone tissue engineering

  10. Vincristine sulfate loaded dextran microspheres amalgamated with thermosensitive gel offered sustained release and enhanced cytotoxicity in THP-1, human leukemia cells: In vitro and in vivo study.

    Science.gov (United States)

    Thakur, Vivek; Kush, Preeti; Pandey, Ravi Shankar; Jain, Upendra Kumar; Chandra, Ramesh; Madan, Jitender

    2016-04-01

    Vincristine sulfate (VCS) is a drug of choice for the treatment of childhood and adult acute lymphocytic leukemia, Hodgkin's, non-Hodgkin's lymphoma as well as solid tumors including sarcomas. However, poor biopharmaceutical and pharmacokinetic traits of VCS like short serum half-life (12 min), high dosing frequency (1.4 mg/m(2) per week for 4 weeks) and extensive protein binding (75%) limit the clinical potential of VCS in cancer therapy. In present investigation, injectable vincristine sulfate loaded dextran microspheres (VCS-Dextran-MSs) were prepared and amalgamated with chitosan-β-glycerophosphate gel (VCS-Dextran-MSs-Gel) to surmount the biopharmaceutical and pharmacokinetic limitations of VCS that consequently induced synergistic sustained release pattern of the drug. Particle size and zeta-potential of VCS-Dextran-MSs were measured to be 6.8 ± 2.4 μm and -18.3 ± 0.11 mV along with the encapsulation efficiency of about 60.4 ± 4.5%. Furthermore, VCS-Dextran-MSs and VCS-Dextran-MSs-Gel exhibited slow release pattern and 94.7% and 95.8% of the drug was released in 72 h and 720 h, respectively. Results from cell viability assay and pharmacokinetic as well as histopathological analysis in mice indicated that VCS-Dextran-MSs-Gel offers superior therapeutic potential and higher AUClast than VCS-Dextran-MSs and drug solution. In conclusion, VCS-Dextran-MSs-Gel warrants further preclinical tumor growth study to scale up the technology. Copyright © 2015 Elsevier B.V. All rights reserved.

  11. Ibuprofen delivered by poly(lactic-co-glycolic acid) (PLGA) nanoparticles to human gastric cancer cells exerts antiproliferative activity at very low concentrations

    Science.gov (United States)

    Bonelli, Patrizia; Tuccillo, Franca M; Federico, Antonella; Napolitano, Maria; Borrelli, Antonella; Melisi, Daniela; Rimoli, Maria G; Palaia, Raffaele; Arra, Claudio; Carinci, Francesco

    2012-01-01

    Purpose Epidemiological, clinical, and laboratory studies have suggested that ibuprofen, a commonly used nonsteroidal anti-inflammatory drug, inhibits the promotion and proliferation of certain tumors. Recently, we demonstrated the antiproliferative effects of ibuprofen on the human gastric cancer cell line MKN-45. However, high doses of ibuprofen were required to elicit these antiproliferative effects in vitro. The present research compared the antiproliferative effects of ibuprofen delivered freely and released by poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) in MKN-45 cells. Methods MKN-45 human gastric adenocarcinoma cells were treated with ibuprofen-loaded PLGA NPs. The proliferation of MKN-45 cells was then assessed by cell counting. The uptake of NPs was imaged by fluorescence microscopy and flow cytometry. The release of ibuprofen from ibuprofen-loaded PLGA NPs in the cells was evaluated by gas chromatography–mass spectrometry. Results Dramatic inhibition of cellular proliferation was observed in cells treated with ibuprofen-loaded PLGA NPs versus those treated with free ibuprofen at the same concentration. The localization of NPs was cytoplasmic. The initiation of ibuprofen release was rapid, commencing within 2 hours, and then increased slowly over time, reaching a maximum concentration at 24 hours. The inhibition of proliferation was confirmed to be due to the intracellular release of ibuprofen from the NPs. Using PLGA NPs as carriers, ibuprofen exerted an antiproliferative activity at concentrations > 100 times less than free ibuprofen, suggesting greater efficiency and less cellular toxicity. In addition, when carried by PLGA NPs, ibuprofen more quickly induced the expression of transcripts involved in proliferation and invasiveness processes. Conclusion Ibuprofen exerted an antiproliferative effect on MKN-45 cells at low concentrations. This effect was achieved using PLGA NPs as carriers of low doses of ibuprofen. PMID:23180963

  12. Hydroxyapatite hierarchically nanostructured porous hollow microspheres: rapid, sustainable microwave-hydrothermal synthesis by using creatine phosphate as an organic phosphorus source and application in drug delivery and protein adsorption.

    Science.gov (United States)

    Qi, Chao; Zhu, Ying-Jie; Lu, Bing-Qiang; Zhao, Xin-Yu; Zhao, Jing; Chen, Feng; Wu, Jin

    2013-04-22

    Hierarchically nanostructured porous hollow microspheres of hydroxyapatite (HAP) are a promising biomaterial, owing to their excellent biocompatibility and porous hollow structure. Traditionally, synthetic hydroxyapatite is prepared by using an inorganic phosphorus source. Herein, we report a new strategy for the rapid, sustainable synthesis of HAP hierarchically nanostructured porous hollow microspheres by using creatine phosphate disodium salt as an organic phosphorus source in aqueous solution through a microwave-assisted hydrothermal method. The as-obtained products are characterized by powder X-ray diffraction (XRD), Fourier-transform IR (FTIR) spectroscopy, SEM, TEM, Brunauer-Emmett-Teller (BET) nitrogen sorptometry, dynamic light scattering (DLS), and thermogravimetric analysis (TGA). SEM and TEM micrographs show that HAP hierarchically nanostructured porous hollow microspheres consist of HAP nanosheets or nanorods as the building blocks and DLS measurements show that the diameters of HAP hollow microspheres are within the range 0.8-1.5 μm. The specific surface area and average pore size of the HAP porous hollow microspheres are 87.3 m(2) g(-1) and 20.6 nm, respectively. The important role of creatine phosphate disodium salt and the influence of the experimental conditions on the products were systematically investigated. This method is facile, rapid, surfactant-free and environmentally friendly. The as-prepared HAP porous hollow microspheres show a relatively high drug-loading capacity and protein-adsorption ability, as well as sustained drug and protein release, by using ibuprofen as a model drug and hemoglobin (Hb) as a model protein, respectively. These experiments indicate that the as-prepared HAP porous hollow microspheres are promising for applications in biomedical fields, such as drug delivery and protein adsorption. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  13. Implantable porous gelatin microspheres sustained release of bFGF and improved its neuroprotective effect on rats after spinal cord injury.

    Directory of Open Access Journals (Sweden)

    Li Lan

    Full Text Available In this study, porous gelatin microspheres (GMSs were constructed to improve the neuroprotective effect of basic fibroblast growth factor (bFGF on spinal cord injury. GMSs were prepared by a W/O emulsion template, followed by cross-linking, washing and drying. The particle sizes and surface porosity of the blank GMSs were carefully characterized by scan electronic microscopy. The blank GMSs have a mean particle size of 35μm and theirs surface was coarse and porous. bFGF was easily encapsulated inside the bulk GMSs through diffusion along the porous channel. 200μg of bFGF was completely encapsulated in 100mg of GMSs. The bFGF-loaded GMSs displayed a continuous drug release pattern without an obvious burst release over two weeks in vitro. Moreover, the therapeutic effects of bFGF-loaded GMSs were also evaluated in spinal cord injury rat model. After implantation of bFGF-loaded GMSs, the recovery of the motor function of SCI rats were evaluated by behavioral score and foot print experiment. The motor function of SCI rats treated with bFGF-loaded GMSs was more obvious than that treated with free bFGF solution (P<0.05. At the 28th days after treatment, rats were sacrificed and the injured spinal were removed for histopathological and apoptosis examination. Compared with treatment with free bFGF solution, treatment with bFGF-loaded GMSs resulted in a less necrosis, less infiltration of leukocytes, and a reduced the cavity ratio and less apoptotic cells in injured spinal(P<0.01, indicating its better therapeutic effect. Implantable porous GMSs may be a potential carrier to deliver bFGF for therapy of spinal cord injury.

  14. Facile fabrication of poly(L-lactic acid) microsphere-incorporated calcium alginate/hydroxyapatite porous scaffolds based on Pickering emulsion templates.

    Science.gov (United States)

    Hu, Yang; Ma, Shanshan; Yang, Zhuohong; Zhou, Wuyi; Du, Zhengshan; Huang, Jian; Yi, Huan; Wang, Chaoyang

    2016-04-01

    In this study, we develop a facile one-pot approach to the fabrication of poly(L-lactic acid) (PLLA) microsphere-incorporated calcium alginate (ALG-Ca)/hydroxyapatite (HAp) porous scaffolds based on HAp nanoparticle-stabilized oil-in-water Pickering emulsion templates, which contain alginate in the aqueous phase and PLLA in the oil phase. The emulsion aqueous phase is solidified by in situ gelation of alginate with Ca(2+) released from HAp by decreasing pH with slow hydrolysis of D-gluconic acid δ-lactone (GDL) to produce emulsion droplet-incorporated gels, followed by freeze-drying to form porous scaffolds containing microspheres. The pore structure of porous scaffolds can be adjusted by varying the HAp or GDL concentration. The compressive tests show that the increase of HAp or GDL concentration is beneficial to improve the compressive property of porous scaffolds, while the excessive HAp can lead to the decrease in compressive property. Moreover, the swelling behavior studies display that the swelling ratios of porous scaffolds reduce with increasing HAp or GDL concentration. Furthermore, hydrophobic drug ibuprofen (IBU) and hydrophilic drug bovine serum albumin (BSA) are loaded into the microspheres and scaffold matrix, respectively. In vitro drug release results indicate that BSA has a rapid release while IBU has a sustained release in the dual drug-loaded scaffolds. In vitro cell culture experiments verify that mouse bone mesenchymal stem cells can proliferate on the porous scaffolds well, indicating the good biocompatibility of porous scaffolds. All these results demonstrate that the PLLA microsphere-incorporated ALG-Ca/HAp porous scaffolds have a promising potential for tissue engineering and drug delivery applications. Copyright © 2016 Elsevier B.V. All rights reserved.

  15. Development and evaluation of ibuprofen transdermal gel formulations

    African Journals Online (AJOL)

    A commercial ibuprofen gel product (Ibutop®) was used as a reference. Results: The formulations containing 5 % of either menthol or glycerol as permeation enhancers gave drug release patterns comparable to that of the reference product. Propanol increased the apparent viscosity of the test gels to the same extent as that ...

  16. Impregnation of Ibuprofen into Polycaprolactone using supercritical carbon dioxide

    Energy Technology Data Exchange (ETDEWEB)

    Yoganathan, Roshan; Mammucari, Raffaella; Foster, Neil R, E-mail: n.foster@unsw.edu.a [Supercritical Fluids Research Group, School of Chemical Sciences and Engineering, University of New South Wales, NSW 2052 (Australia)

    2010-03-01

    Polycaprolactone (PCL) is a Food and Drug Administration (FDA) approved biodegradable polyester used in tissue engineering applications. Ibuprofen is an anti-inflammatory drug which has good solubility in supercritical CO{sub 2} (SCCO{sub 2}). The solubility of CO{sub 2} in PCL allows for the impregnation of CO{sub 2}-soluble therapeutic agents into the polymer via a supercritical fluid (SCF) process. Polymers impregnated with bio-active compounds are highly desired for medical implants and controlled drug delivery. In this study, the use of CO{sub 2} to impregnate PCL with ibuprofen was investigated. The effect of operating conditions on the impregnation of ibuprofen into PCL was investigated over two pressure and two temperature levels, 150bar and 200bar, 35{sup 0}C and 40 {sup 0}C, respectively. Polycaprolactone with drug-loadings as high as 27% w/w were obtained. Impregnated samples exhibited controlled drug release profiles over several days.

  17. Impregnation of Ibuprofen into Polycaprolactone using supercritical carbon dioxide

    International Nuclear Information System (INIS)

    Yoganathan, Roshan; Mammucari, Raffaella; Foster, Neil R

    2010-01-01

    Polycaprolactone (PCL) is a Food and Drug Administration (FDA) approved biodegradable polyester used in tissue engineering applications. Ibuprofen is an anti-inflammatory drug which has good solubility in supercritical CO 2 (SCCO 2 ). The solubility of CO 2 in PCL allows for the impregnation of CO 2 -soluble therapeutic agents into the polymer via a supercritical fluid (SCF) process. Polymers impregnated with bio-active compounds are highly desired for medical implants and controlled drug delivery. In this study, the use of CO 2 to impregnate PCL with ibuprofen was investigated. The effect of operating conditions on the impregnation of ibuprofen into PCL was investigated over two pressure and two temperature levels, 150bar and 200bar, 35 0 C and 40 0 C, respectively. Polycaprolactone with drug-loadings as high as 27% w/w were obtained. Impregnated samples exhibited controlled drug release profiles over several days.

  18. [Optimization of riboflavin sodium phosphate loading to calcium alginate floating microspheres by response surface methodology].

    Science.gov (United States)

    Zhang, An-yang; Fan, Tian-yuan

    2009-12-18

    To investigate the preparation, optimization and in vitro properties of riboflavin sodium phosphate floating microspheres. The floating microspheres composed of riboflavin sodium phosphate and calcium alginate were prepared using ion gelatin-oven drying method. The properties of the microspheres were investigated, including the buoyancy, release, appearance and entrapment efficiency. The formulation was optimized by response surface methodology (RSM). The optimized microspheres were round. The entrapment efficiency was 57.49%. All the microspheres could float on the artificial gastric juice over 8 hours. The release of the drug from the microspheres complied with Fick's diffusion.

  19. Microradiographic microsphere manipulator

    International Nuclear Information System (INIS)

    Singleton, R.M.

    1980-01-01

    A method and apparatus are provided for radiographic characterization of small hollow spherical members (microspheres), constructed of either optically transparent or opaque materials. The apparatus involves a microsphere manipulator which holds a batch of microspheres between two parallel thin plastic films for contact microradiographic characterization or projection microradiography thereof. One plastic film is translated to relative to and parallel to the other to roll the microspheres through any desired angle to allow different views of the microspheres

  20. Phospho-Ibuprofen (MDC-917) Is a Novel Agent against Colon Cancer: Efficacy, Metabolism, and Pharmacokinetics in Mouse Models

    Science.gov (United States)

    Xie, Gang; Sun, Yu; Nie, Ting; Mackenzie, Gerardo G.; Huang, Liqun; Kopelovich, Levy; Komninou, Despina

    2011-01-01

    We have developed a novel chemical modification of conventional nonsteroidal anti-inflammatory drugs to reduce their toxicity and enhance their efficacy. Phospho-ibuprofen [(PI) 2-(4-isobutyl-phenyl)-propionic acid-4-(diethoxy-phosphoryloxy)-butyl ester (MDC-917)], a novel derivative of ibuprofen, strongly inhibited the growth of human colon cancer cells in vitro and SW480 human colon cancer xenografts in nude mice. PI was metabolized minimally by cultured cells, but extensively by liver microsomes and mice, undergoing regioselective oxidation to produce 1-OH-PI and carboxyl-PI, which can be hydrolyzed to 1-OH-ibuprofen and carboxyl-ibuprofen, respectively. PI also can be hydrolyzed to release ibuprofen, which can generate 2-OH-ibuprofen, carboxyl-ibuprofen, and ibuprofen glucuronide. After a single oral administration (400 mg/kg) of PI, ibuprofen and ibuprofen glucuronide are the main plasma metabolites of PI; they have, respectively, Cmax of 530 and 215 μM, Tmax of 1 and 2 h, elimination t1/2 of 7.7 and 5.3 h, and area under the concentration-time curve (0–24 h) of 1816 and 832 μM × h. Intact PI was detected in several tissues but not in plasma; at a higher PI dose (1200 mg/kg), PI plasma levels were 12.4 μM. PI generated the same metabolites in mouse plasma as conventional ibuprofen, but with much lower levels, perhaps accounting for the enhanced safety of PI. The antitumor effect of PI was significantly associated with plasma ibuprofen levels (p = 0.016) but not with xenograft ibuprofen levels (p = 0.08), suggesting a complex anticancer effect. These results provide a pharmacological basis to explain, at least in part, the anticancer efficacy and safety of this promising compound and indicate that PI merits further evaluation as an anticancer agent. PMID:21422165

  1. Combination of calcium sulfate and simvastatin-controlled release microspheres enhances bone repair in critical-sized rat calvarial bone defects

    Directory of Open Access Journals (Sweden)

    Fu YC

    2015-12-01

    Full Text Available Yin-Chih Fu,1–4 Yan-Hsiung Wang,1,5 Chung-Hwan Chen,1,3,4 Chih-Kuang Wang,1,6 Gwo-Jaw Wang,1,3,4 Mei-Ling Ho1,3,7,8 1Orthopaedic Research Center, 2Graduate Institute of Medicine, 3Department of Orthopaedics, 4Department of Orthopaedics, College of Medicine, 5School of Dentistry, College of Dental Medicine, 6Department of Medicinal and Applied Chemistry, 7Department of Physiology, College of Medicine, Kaohsiung Medical University, Kaohsiung, Taiwan; 8Department of Marine Biotechnology and Resources, National Sun Yat-sen University, Kaohsiung, TaiwanAbstract: Most allogenic bone graft substitutes have only osteoconductive properties. Developing new strategies to improve the osteoinductive activity of bone graft substitutes is both critical and practical for clinical application. Previously, we developed novel simvastatin-encapsulating poly(lactic-co-glycolic acid microspheres (SIM/PLGA that slowly release simvastatin and enhance fracture healing. In this study, we combined SIM/PLGA with a rapidly absorbable calcium sulfate (CS bone substitute and studied the effect on bone healing in critical-sized calvarial bone defects in a rat model. The cytotoxicity and cytocompatibility of this combination was tested in vitro using lactate dehydrogenase leakage and a cell attachment assay, respectively. Combination treatment with SIM/PLGA and the CS bone substitute had no cytotoxic effect on bone marrow stem cells. Compared with the control, cell adhesion was substantially enhanced following combination treatment with SIM/PLGA and the CS bone substitute. In vivo, implantation of the combination bone substitute promoted healing of critical-sized calvarial bone defects in rats; furthermore, production of bone morphogenetic protein-2 and neovascularization were enhanced in the area of the defect. In summary, the combination of SIM/PLGA and a CS bone substitute has osteoconductive and osteoinductive properties, indicating that it could be used for regeneration

  2. Development of Risperidone PLGA Microspheres

    Directory of Open Access Journals (Sweden)

    Susan D’Souza

    2014-01-01

    Full Text Available The aim of this study was to design and evaluate biodegradable PLGA microspheres for sustained delivery of Risperidone, with an eventual goal of avoiding combination therapy for the treatment of schizophrenia. Two PLGA copolymers (50 : 50 and 75 : 25 were used to prepare four microsphere formulations of Risperidone. The microspheres were characterized by several in vitro techniques. In vivo studies in male Sprague-Dawley rats at 20 and 40 mg/kg doses revealed that all formulations exhibited an initial burst followed by sustained release of the active moiety. Additionally, formulations prepared with 50 : 50 PLGA had a shorter duration of action and lower cumulative AUC levels than the 75 : 25 PLGA microspheres. A simulation of multiple dosing at weekly or 15-day regimen revealed pulsatile behavior for all formulations with steady state being achieved by the second dose. Overall, the clinical use of Formulations A, B, C, or D will eliminate the need for combination oral therapy and reduce time to achieve steady state, with a smaller washout period upon cessation of therapy. Results of this study prove the suitability of using PLGA copolymers of varying composition and molecular weight to develop sustained release formulations that can tailor in vivo behavior and enhance pharmacological effectiveness of the drug.

  3. Compound list: ibuprofen [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available ibuprofen IBU 00072 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in..._vitro/ibuprofen.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitr...o/ibuprofen.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/...Single/ibuprofen.Rat.in_vivo.Liver.Single.zip ftp://ftp.biosciencedbc.jp/archive/

  4. IBUPROFEN IN PAIN TREATMENT IN CHILDREN

    Directory of Open Access Journals (Sweden)

    R. V. Denisova

    2012-01-01

    Full Text Available The article contains results of therapeutic efficacy of ibuprofen in pain syndrome management in children. Validity of its use is doubtless. Analgesic effect of Ibuprofen has been confirmed in clinical trials in patients with migraine and ENT-disorders. In this article we also review international experience of ibuprofen use in juvenile arthritis..

  5. Microsphere based improved sunscreen formulation of ethylhexyl methoxycinnamate.

    Science.gov (United States)

    Gogna, Deepak; Jain, Sunil K; Yadav, Awesh K; Agrawal, G P

    2007-04-01

    Polymethylmethacrylate (PMMA) microspheres of ethylhexyl methoxycinnamate (EHM) were prepared by emulsion solvent evaporation method to improve its photostability and effectiveness as sunscreening agent. Process parameters like stirring speed and aqueous polyvinyl alcohol (PVA) concentration were analyzed in order to optimize the formulations. Shape and surface morphology of the microspheres were examined using scanning electron microscopy. Particle size of the microspheres was determined using laser diffraction particle size analyzer. The PMMA microspheres of EHM were incorporated in water-removable cream base. The in vitro drug release of EHM in pH 7.4 was performed using dialysis membrane. Thin layer chromatography was performed to determine photostability of EHM inside the microspheres. The formulations were evaluated for sun protection factor (SPF) and minimum erythema dose (MED) in albino rats. Cream base formulation containing microspheres prepared using EHM:PMMA in ratio of 1:3 (C(3)) showed slowest drug (EHM) release and those prepared with EHM: PMMA in ratio of 1:1 showed fastest release. The cream base formulations containing EHM loaded microspheres had shown better SPF (more than 16.0) as compared to formulation C(d) that contained 3% free EHM as sunscreen agent and showed SPF 4.66. These studies revealed that the incorporation of EHM loaded PMMA microspheres into cream base had greatly increased the efficacy of sunscreen formulation approximately four times. Further, photostability was also shown to be improved in PMMA microspheres.

  6. Novel ionically crosslinked acrylamide-grafted poly(vinyl alcohol)/sodium alginate/sodium carboxymethyl cellulose pH-sensitive microspheres for delivery of Alzheimer's drug donepezil hydrochloride: Preparation and optimization of release conditions.

    Science.gov (United States)

    Bulut, Emine; Şanlı, Oya

    2016-01-01

    In this work, the graft copolymer, poly(vinyl alcohol)-grafted polyacrylamide (PVA-g-PAAm), was synthesized and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and elemental analysis. Microspheres of PVA-g-PAAm/sodium alginate (NaAlg)/sodium carboxymethyl cellulose (NaCMC) were prepared by the emulsion-crosslinking method and used for the delivery of an Alzheimer's drug, donepezil hydrochloride (DP). The release of DP increased with the increase in drug/polymer ratio (d/p) and PVA-g-PAAm/NaAlg/NaCMC ratio, while it decreased with the increase in the extent of crosslinking. The optimum DP release was obtained as 92.9% for a PVA-g-PAAm/NaAlg/NaCMC ratio of 1/2/1, d/p ratio of 1/8, and FeCl3 concentration of 7% (w/v).

  7. MICROSPHERE SIZE INFLUENCES THE FOREIGN BODY REACTION

    NARCIS (Netherlands)

    Zandstra, J.; Hiemstra, C.; Petersen, A. H.; Zuidema, J.; van Beuge, M. M.; Rodriguez, S.; Lathuile, A. A. R.; Veldhuis, G. J.; Steendam, R.; Bank, R. A.; Popa, E. R.

    2014-01-01

    Biodegradable poly-(DL-lactide-co-glycolide) (PLGA) microspheres (MSP) are attractive candidate vehicles for site-specific or systemic sustained release of therapeutic compounds. This release may be altered by the host's foreign body reaction (FBR), which is dependent on the characteristics of the

  8. Evaluation of a Non-aqueous Ibuprofen-Phospholipid Complex Formulation in Rats.

    Science.gov (United States)

    Li, Chunhua; Xu, Songlin; Liu, Zhidong; Ding, Lingling; Zhao, Xiaobin; Lee, Robert J

    2016-01-01

    In the present study, a non-aqueous ibuprofen-phospholipid complex was developed to reduce the gastrointestinal (GI) toxicity of ibuprofen. A non-aqueous ibuprofen-phospholipid complex (IBU-PC) was prepared by mixing phosal-35SB and ibuprofen. In vitro release behavior was studied using a dissolution apparatus. Irritation to gastrointestinal (GI) tract and pharmacokinetics of IBU-PC were studied in rats. Rapid release of drug occurred with approximately 85% of ibuprofen released from the composition within the first 30 min. The GI injury in IBU-PC-treated rats was minimal compared to those of Advil Liqui-gels-treated group. There was no significant difference between IBU-PC and Motrin-treated groups. The area under the concentration-time curve (AUC0~24) of IBU-PC and Motrin were 366±115 and 391±105 μg/h/ml, respectively. The relative bioavailability of IBU-PC was 94.2%. IBU-PC can decrease GI adverse reaction induced by ibuprofen. Copyright © 2016 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.

  9. PLGA and PHBV Microsphere Formulations and Solid-State Characterization

    DEFF Research Database (Denmark)

    Yang, Chiming; Plackett, David; Needham, David

    2009-01-01

    To develop and characterize the solid-state properties of poly(DL-lactic-co-glycolic acid) (PLGA) and poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) (PHBV) microspheres for the localized and controlled release of fusidic acid (FA). The effects of FA loading and polymer composition on the me...... of a DCM-FA-rich phase in the forming microsphere....

  10. Formulation and Evaluation of Microspheres Based on Gelatin ...

    African Journals Online (AJOL)

    Formulation and Evaluation of Microspheres Based on Gelatin-Mucin Admixtures for the Rectal Delivery of Cefuroxime Sodium. K C Ofokansi, M U Adikwu. Abstract. Purpose: Swellable microspheres based on polymers or their admixtures are frequently employed as drug delivery systems to achieve a controlled release ...

  11. Ibuprofen delivered by poly(lactic-co-glycolic acid (PLGA nanoparticles to human gastric cancer cells exerts antiproliferative activity at very low concentrations

    Directory of Open Access Journals (Sweden)

    Bonelli P

    2012-11-01

    Full Text Available Patrizia Bonelli,1 Franca M Tuccillo,1 Antonella Federico,5 Maria Napolitano,2 Antonella Borrelli,1 Daniela Melisi,6 Maria G Rimoli,6 Raffaele Palaia,3 Claudio Arra,4 Francesco Carinci71Laboratory of Molecular Biology and Viral Oncogenesis; 2Department of Clinical Immunology; 3Department of Gastrointestinal-Hepatobiliary-Pancreatic Cancer Oncology Surgery; 4Animal Facility, National Cancer Institute G Pascale, Naples, Italy; 5Microtech Laboratory, Naples, Italy; 6Pharmaceutical and Toxicological Chemistry Department, School of Pharmacy, University "Federico II", Naples, Italy; 7Department of Maxillofacial Surgery, University of Ferrara, Ferrara, ItalyPurpose: Epidemiological, clinical, and laboratory studies have suggested that ibuprofen, a commonly used nonsteroidal anti-inflammatory drug, inhibits the promotion and proliferation of certain tumors. Recently, we demonstrated the antiproliferative effects of ibuprofen on the human gastric cancer cell line MKN-45. However, high doses of ibuprofen were required to elicit these antiproliferative effects in vitro. The present research compared the antiproliferative effects of ibuprofen delivered freely and released by poly(lactic-co-glycolic acid (PLGA nanoparticles (NPs in MKN-45 cells.Methods: MKN-45 human gastric adenocarcinoma cells were treated with ibuprofen-loaded PLGA NPs. The proliferation of MKN-45 cells was then assessed by cell counting. The uptake of NPs was imaged by fluorescence microscopy and flow cytometry. The release of ibuprofen from ibuprofen-loaded PLGA NPs in the cells was evaluated by gas chromatography–mass spectrometry.Results: Dramatic inhibition of cellular proliferation was observed in cells treated with ibuprofen-loaded PLGA NPs versus those treated with free ibuprofen at the same concentration. The localization of NPs was cytoplasmic. The initiation of ibuprofen release was rapid, commencing within 2 hours, and then increased slowly over time, reaching a maximum

  12. Synthesis and characterization of magnesium gluconate contained poly(lactic-co-glycolic acid)/chitosan microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rahman, Shekh M. [Department of Chemical, Biological and Bioengineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Mahoney, Christopher [Department of Bioengineering, University of Pittsburgh, 4200 Fifth Avenue, Pittsburgh, PA 15250 (United States); Sankar, Jagannathan [NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Department of Mechanical Engineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); Marra, Kacey G. [NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States); Department of Bioengineering, University of Pittsburgh, 4200 Fifth Avenue, Pittsburgh, PA 15250 (United States); Department of Plastic Surgery, University of Pittsburgh, 200 Lothrop Street, Pittsburgh, PA 15250 (United States); McGowan Institute for Regenerative Medicine, University of Pittsburgh, 450 Technology Drive, Pittsburgh, PA 15250 (United States); Bhattarai, Narayan, E-mail: nbhattar@ncat.edu [Department of Chemical, Biological and Bioengineering, North Carolina A& T State University, 1601 East Market Street, Greensboro, NC 27411 (United States); NSF Engineering Research Center for Revolutionizing Metallic Biomaterials, North Carolina A& T State University, Greensboro, NC 27411 (United States)

    2016-01-15

    Graphical abstract: - Highlights: • Magnesium gluconate contained PLGA/chitosan microspheres were fabricated. • In vitro release of magnesium ions was performed using Xylidyl Blue assay. • Chitosan coated PLGA can significantly control the release of magnesium ions. • Cellular compatibility was tested using adipose-derived stem cells and PC12 cells. • The cells encounter acceptably low levels of damage in contact with microspheres. - Abstract: The goal of this study was to fabricate and investigate the chitosan coated poly(lactic-co-glycolic acid) (PLGA) microspheres for the development of controlled release magnesium delivery system. PLGA based microspheres are ideal vehicles for many controlled release drug delivery applications. Chitosan is a naturally occurring biodegradable and biocompatible polysaccharide, which can coat the surface of PLGA to alter the release of drugs. Magnesium gluconate (MgG) was encapsulated in the PLGA and PLGA/chitosan microspheres by utilizing the double emulsion solvent evaporation technique for controlled release study. The microspheres were tested with respect to several physicochemical and biological properties, including morphology, chemical structure, chitosan adsorption efficiency, magnesium encapsulation efficiency, in vitro release of magnesium ions, and cellular compatibility using both human adipose-derived stem cells (ASCs) and PC12 cells. Chitosan coated PLGA microspheres can significantly control the release of magnesium ions compared to uncoated PLGA microspheres. Both coated and uncoated microspheres showed good cellular compatibility.

  13. Structuring microspheres

    NARCIS (Netherlands)

    Wagdare, N.A.

    2011-01-01

    Encapsulation and use of capsules for controlled release has several applications in pharmaceuticals, foods, cosmetics, detergents and many other products for consumers. It can contribute to sustainability, since it allows an efficient use of active materials, delivery at the required site and

  14. Design of Agglomerated Crystals of Ibuprofen During Crystallization: Influence of Surfactant

    Directory of Open Access Journals (Sweden)

    Maryam Maghsoodi

    2011-01-01

    Full Text Available Objective(sIbuprofen is a problematic drug in tableting, and dissolution due to its poor solubility, hydrophobicity, and tendency to stick to surface. Because of the bad compaction behavior ibuprofen has to be granulated usually before tableting. However, it would be more satisfactory to obtain directly during the crystallization step crystalline particles that can be directly compressed and quickly dissolved. Materials and Methods Crystallization of ibuprofen was carried out using the quasi emulsion solvent diffusion method in presence of surfactant (sodium lauryl sulfate (SLS, Tween 80. The particles were characterized by differential scanning calorimetry (DSC, powder X-ray diffraction (XRPD and were evaluated for particle size, flowability, drug release and tableting behavior. ResultsIbuprofen particles obtained in the presence of surfactants consisted of numerous plate- shaped crystals which had agglomerated together as near spherical shape. The obtained agglomerates exhibited significantly improved micromeritic properties as well as tableting behavior than untreated drug crystals. The agglomerates size and size distribution was largely controlled by surfactant concentration, but there was no significant influence found on the tableting properties. The dissolution tests showed that the agglomerates obtained in presence of SLS exhibited enhanced dissolution rate while the agglomerates made in the presence of Tween 80 had no significant impact on dissolution rate of ibuprofen in comparison to untreated sample. The XRPD and DSC results showed that during the agglomeration process, ibuprofen did not undergo any polymorphic changes.Conclusion The study highlights the influence of surfactants on crystallization process leading to modified performance.

  15. Metallic coating of microspheres

    International Nuclear Information System (INIS)

    Meyer, S.F.

    1980-01-01

    Extremely smooth, uniform metal coatings of micrometer thicknesses on microscopic glass spheres (microspheres) are often needed as targets for inertial confinement fusion (ICF) experiments. The first part of this paper reviews those methods used successfully to provide metal coated microspheres for ICF targets, including magnetron sputtering, electro- and electroless plating, and chemical vapor pyrolysis. The second part of this paper discusses some of the critical aspects of magnetron sputter coating of microspheres, including substrate requirements, the sticking of microspheres during coating (preventing a uniform coating), and the difficulties in growing the desired dense, smooth, uniform microstructure on continuously moving spherical substrates

  16. Encapsulation of azithromycin into polymeric microspheres by reduced pressure-solvent evaporation method

    DEFF Research Database (Denmark)

    Li, Xiujuan; Chang, Si; Du, Guangsheng

    2012-01-01

    Azithromycin loaded microspheres with blends of poly-l-lactide and ploy-D,L-lactide-co-glycolide as matrices were prepared by the atmosphere-solvent evaporation (ASE) and reduced pressure-solvent evaporation (RSE) method. Both the X-ray diffraction spectra and DSC thermographs demonstrated...... characteristics and release profiles of microspheres. In conclusion, the overall improvement of microspheres in appearance, encapsulation efficiency and controlled drug release through the RSE method could be easily fulfilled under optimal preparation conditions....

  17. Ibuprofen-loaded poly(trimethylene carbonate-co-ε-caprolactone) electrospun fibres for nerve regeneration.

    Science.gov (United States)

    Pires, Liliana R; Guarino, Vincenzo; Oliveira, Maria J; Ribeiro, Cristina C; Barbosa, Mário A; Ambrosio, Luigi; Pêgo, Ana Paula

    2016-03-01

    The development of scaffolds that combine the delivery of drugs with the physical support provided by electrospun fibres holds great potential in the field of nerve regeneration. Here it is proposed the incorporation of ibuprofen, a well-known non-steroidal anti-inflammatory drug, in electrospun fibres of the statistical copolymer poly(trimethylene carbonate-co-ε-caprolactone) [P(TMC-CL)] to serve as a drug delivery system to enhance axonal regeneration in the context of a spinal cord lesion, by limiting the inflammatory response. P(TMC-CL) fibres were electrospun from mixtures of dichloromethane (DCM) and dimethylformamide (DMF). The solvent mixture applied influenced fibre morphology, as well as mean fibre diameter, which decreased as the DMF content in solution increased. Ibuprofen-loaded fibres were prepared from P(TMC-CL) solutions containing 5% ibuprofen (w/w of polymer). Increasing drug content to 10% led to jet instability, resulting in the formation of a less homogeneous fibrous mesh. Under the optimized conditions, drug-loading efficiency was above 80%. Confocal Raman mapping showed no preferential distribution of ibuprofen in P(TMC-CL) fibres. Under physiological conditions ibuprofen was released in 24 h. The release process being diffusion-dependent for fibres prepared from DCM solutions, in contrast to fibres prepared from DCM-DMF mixtures where burst release occurred. The biological activity of the drug released was demonstrated using human-derived macrophages. The release of prostaglandin E2 to the cell culture medium was reduced when cells were incubated with ibuprofen-loaded P(TMC-CL) fibres, confirming the biological significance of the drug delivery strategy presented. Overall, this study constitutes an important contribution to the design of a P(TMC-CL)-based nerve conduit with anti-inflammatory properties. Copyright © 2013 John Wiley & Sons, Ltd.

  18. Effect of various polymers concentrations on physicochemical properties of floating microspheres.

    Science.gov (United States)

    Jagtap, Y M; Bhujbal, R K; Ranade, A N; Ranpise, N S

    2012-11-01

    Floating microspheres have emerged as a potential candidate for gastroretentive drug delivery system. For developing a desired intragastric floatation system employing these microspheres, it is necessary to select an appropriate balance between buoyancy and drug releasing rate. These properties mainly depend on the polymers used in the formulation of the microspheres. Hence it is necessory to study the effect of these polymer concentrations on the various physicochemical properties of the microspheres. Floating microspheres were prepared by emulsion solvent evaporation technique utilising different polymers such as ethyl cellulose, Eudragit(®) RS and Eudragit(®) RL by dissolving them in a mixture of dichloromethane and methanol. Release modifiers studied were hydroxypropyl methylcellulose K4M, hydroxypropyl methylcellulose E50 LV and Eudragit(®) EPO. Prepared microspheres were analysed for particle size, surface morphology, entrapment efficiency, buoyancy, differential scanning calorimetry and in-vitro drug release. Ethyl cellulose and Eudragit(®) EPO resulted microspheres with high percentage yield, excellent spherical shape but had very less buoyancies with a high cumulative drug release. Ethyl cellulose microspheres prepared using hydroxypropyl methylcellulose K4M showed more sustained drug release and high buoyancies than that of the microspheres formulated with the hydroxypropyl methylcellulose E50 LV. Amongst these hydroxypropyl methylcellulose E50 LV showed good balance between buoyancy and the drug release.

  19. Ibuprofen loaded PLA nanofibrous scaffolds increase proliferation of human skin cells in vitro and promote healing of full thickness incision wounds in vivo.

    Science.gov (United States)

    Mohiti-Asli, M; Saha, S; Murphy, S V; Gracz, H; Pourdeyhimi, B; Atala, A; Loboa, E G

    2017-02-01

    This article presents successful incorporation of ibuprofen in polylactic acid (PLA) nanofibers to create scaffolds for the treatment of both acute and chronic wounds. Nanofibrous PLA scaffolds containing 10, 20, or 30 wt % ibuprofen were created and ibuprofen release profiles quantified. In vitro cytotoxicity to human epidermal keratinocytes (HEK) and human dermal fibroblasts (HDF) of the three scaffolds with varying ibuprofen concentrations were evaluated and compared to pure PLA nanofibrous scaffolds. Thereafter, scaffolds loaded with ibuprofen at the concentration that promoted human skin cell viability and proliferation (20 wt %) were evaluated in vivo in nude mice using a full thickness skin incision model to determine the ability of these scaffolds to promote skin regeneration and/or assist with scarless healing. Both acellular and HEK and HDF cell-seeded 20 wt % ibuprofen loaded nanofibrous bandages reduced wound contraction compared with wounds treated with Tegaderm™ and sterile gauze. Newly regenerated skin on wounds treated with cell-seeded 20 wt % ibuprofen bandages exhibited significantly greater blood vessel formation relative to acellular ibuprofen bandages. We have found that degradable anti-inflammatory scaffolds containing 20 wt % ibuprofen promote human skin cell viability and proliferation in vitro, reduce wound contraction in vivo, and when seeded with skin cells, also enhance new blood vessel formation. The approaches and results reported here hold promise for multiple skin tissue engineering and wound healing applications. © 2015 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 105B: 327-339, 2017. © 2015 Wiley Periodicals, Inc.

  20. Antibacterial activity of ciprofloxacin-loaded zein microsphere films

    International Nuclear Information System (INIS)

    Fu Jianxi; Wang Huajie; Zhou Yanqing; Wang Jinye

    2009-01-01

    Our aim was to produce an antibiotic-emitting coating composed of zein microspheres for the prevention of bacterial infection on implanted devices. Ciprofloxacin-loaded zein microspheres were prepared using a phase separation procedure, with particle sizes between 0.5 and 2 μm. Drug encapsulation and drug loading varied with the amount of both zein and ciprofloxacin, and the highest encapsulation efficiency was 8.27% (2 mg/ml ciprofloxacin and 20 mg/ml zein; n = 3). A ciprofloxacin-loaded zein microsphere film (CF-MS film) was generated via solvent evaporation. Continuous drug release from a trypsin-degraded microsphere film was observed for up to 28 days. The liberation of ciprofloxacin from the trypsin-degraded film and the biodegradation of the microsphere film were highly correlated. Proliferation assay of the growth of human umbilical vein endothelial cells (HUVECs) by the MTT method showed that the microsphere film had no toxicity when compared with cells grown on Corning culture plates alone and plates with a zein film alone. Quantification of bacteria adhesion showed that adhesion on the microsphere film is significantly suppressed. In addition, according to the results of bacterial growth tests, ciprofloxacin-loaded microsphere films maintained antibacterial activity for more than 6 days. In contrast, a control medium containing a zein film allowed constant bacterial growth. These results indicate that CF-MS films might be useful as antibacterial films on implanted devices.

  1. Antibacterial activity of ciprofloxacin-loaded zein microsphere films

    Energy Technology Data Exchange (ETDEWEB)

    Fu Jianxi [Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032 (China); Henan Normal University, 46 East Construction Road, Xinxiang, Henan 453007 (China); Wang Huajie [College of Life Science and Biotechnology, Shanghai Jiao Tong University, 1954 Huashan Road, Shanghai 200030 (China); Zhou Yanqing [Henan Normal University, 46 East Construction Road, Xinxiang, Henan 453007 (China); Wang Jinye, E-mail: jywang@mail.sioc.ac.cn [Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032 (China); College of Life Science and Biotechnology, Shanghai Jiao Tong University, 1954 Huashan Road, Shanghai 200030 (China)

    2009-05-05

    Our aim was to produce an antibiotic-emitting coating composed of zein microspheres for the prevention of bacterial infection on implanted devices. Ciprofloxacin-loaded zein microspheres were prepared using a phase separation procedure, with particle sizes between 0.5 and 2 {mu}m. Drug encapsulation and drug loading varied with the amount of both zein and ciprofloxacin, and the highest encapsulation efficiency was 8.27% (2 mg/ml ciprofloxacin and 20 mg/ml zein; n = 3). A ciprofloxacin-loaded zein microsphere film (CF-MS film) was generated via solvent evaporation. Continuous drug release from a trypsin-degraded microsphere film was observed for up to 28 days. The liberation of ciprofloxacin from the trypsin-degraded film and the biodegradation of the microsphere film were highly correlated. Proliferation assay of the growth of human umbilical vein endothelial cells (HUVECs) by the MTT method showed that the microsphere film had no toxicity when compared with cells grown on Corning culture plates alone and plates with a zein film alone. Quantification of bacteria adhesion showed that adhesion on the microsphere film is significantly suppressed. In addition, according to the results of bacterial growth tests, ciprofloxacin-loaded microsphere films maintained antibacterial activity for more than 6 days. In contrast, a control medium containing a zein film allowed constant bacterial growth. These results indicate that CF-MS films might be useful as antibacterial films on implanted devices.

  2. [Optimization of calcium alginate floating microspheres loading aspirin by artificial neural networks and response surface methodology].

    Science.gov (United States)

    Zhang, An-yang; Fan, Tian-yuan

    2010-04-18

    To investigate the preparation and optimization of calcium alginate floating microspheres loading aspirin. A model was used to predict the in vitro release of aspirin and optimize the formulation by artificial neural networks (ANNs) and response surface methodology (RSM). The amounts of the material in the formulation were used as inputs, while the release and floating rate of the microspheres were used as outputs. The performances of ANNs and RSM were compared. ANNs were more accurate in prediction. There was no significant difference between ANNs and RSM in optimization. Approximately 90% of the optimized microspheres could float on the artificial gastric juice over 4 hours. 42.12% of aspirin was released in 60 min, 60.97% in 120 min and 78.56% in 240 min. The release of the drug from the microspheres complied with Higuchi equation. The aspirin floating microspheres with satisfying in vitro release were prepared successfully by the methods of ANNs and RSM.

  3. Polymer-coated albumin microspheres as carriers for intravascular tumour targeting of cisplatin.

    Science.gov (United States)

    Verrijk, R; Smolders, I J; McVie, J G; Begg, A C

    1991-01-01

    We used a poly-lactide-co-glycolide polymer (PLAGA 50:50) to formulate cisplatin (cDDP) into microspheres designed for intravascular administration. Two systems were developed. PLAGA-coated albumin microspheres and microspheres consisting of PLAGA only. PLAGA-coated microspheres displayed a mean diameter of 31.8 +/- 0.9 microns and a payload of 7.5% cDDP (w/w). Solid PLAGA microspheres exhibited a mean diameter of 19.4 +/- 0.6 microns and a payload of 20% cDDP. Release characteristics and in vitro effects on L1210 leukemia and B16 melanoma cell lines were investigated. Both types of microsphere overcame the initial rapid release of cDDP (burst effect), and PLAGA-coated albumin microspheres also showed a lag phase of approximately 30 min before cDDP release began. PLAGA-coated albumin microspheres released most of their payload through diffusion, and the coating eventually cracked after 7 days' incubation in saline supplemented with 0.1% Tween at 37 degrees C, enabling the release of any cDDP remaining. Effects of platinum, pre-released from PLAGA-coated albumin microspheres on the in vitro growth of L1210 cells were comparable with those of standard formulations (dissolved) of cDDP. Material released from non-drug-loaded PLAGA microspheres had no effect on L1210 cell growth, suggesting the absence of cytotoxic compounds in the matrix. The colony-forming ability of B16 cells was also equally inhibited by standard cDDP and pre-released drug. These studies show that formulation of cDDP in PLAGA-based microspheres prevents the rapid burst effect of cDDP seen in previous preparations and offers an improved system of administration for hepatic artery infusion or adjuvant therapy, enabling better clinical handling and the promise of a higher ratio of tumour tissue to normal tissue.

  4. Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon.

    Science.gov (United States)

    Rai, Gopal; Yadav, Awesh K; Jain, Narendra K; Agrawal, Govind P

    2016-01-01

    Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.

  5. Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon.

    Science.gov (United States)

    Rai, Gopal; Yadav, Awesh K; Jain, Narendra K; Agrawal, Govind P

    2015-01-01

    Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.

  6. Development and Evaluation of Isoniazid Loaded Silk Fibroin Microsphere

    Directory of Open Access Journals (Sweden)

    Narinder Singh

    Full Text Available Aim: Current experimental investigation is dedicated to prepare microspheres with small size and good sphericity by Phase Separation method using Isoniazid (INH as model drug. Silk fibroin has unique intrinsic qualities like biodegradability, biocompatibility or release properties and their tunable drug loading capacity. The delivery loading proficiency of the drug molecules in silk spheres be contingent on their charge, and hydrophobicity or subsequent in altered drug release profiles. Methods: In the present work Isoniazid loaded silk fibroin microsphere was prepared by using phase separation method. Microsphere was evaluated for Ultraviolet-visible spectroscopy, Fourier Transform infrared spectroscopy, Entrapment efficiency, Scanning electron microscopy Studies. Results: Scanning electron microscopy studies revealed that Isoniazid Loaded Silk Fibroin Microspheres were spherical. Entrapment Efficiency of Isoniazid loaded Microspheres of different Formulation from F1 to F5 was in range of 53 to 68 %. F3 showed 68.47 % entrapment Efficiency and the optimized formulation drug release was 93.56 % at 24 hours. Conclusion: Experimental report disclosed a new aqueous based formulation method for silk spheres with controllable shape or size and sphere. Isoniazid loaded silk microspheres may act as ideal nano formulation with elaborated studies.

  7. Bioequivalence assessment of two formulations of ibuprofen

    KAUST Repository

    Al-Talla, Zeyad; Akrawi, Sabah H; Tolley, Luke T; Sioud, Salim H; Zaater, Mohammed F; Emwas, Abdul-Hamid M

    2011-01-01

    Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz , produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen , manufactured by Boots

  8. Glass microspheres for brachytherapy

    International Nuclear Information System (INIS)

    Prado, Miguel O.; Prastalo, Simon; Blaumann, Herman; Longhino, Juan M.; Repetto Llamazares, A.H.V.

    2007-01-01

    We developed the capacity to produce glass microspheres containing in their structure one or more radioactive isotopes useful for brachytherapy. We studied the various facts related with their production: (Rare earth) alumino silicate glass making, glass characterization, microspheres production, nuclear activation through (n,γ) nuclear reactions, mechanical characterization before and after irradiation. Corrosion tests in simulated human plasma and mechanical properties characterization were done before and after irradiation. (author) [es

  9. Development and optimization of enteric coated mucoadhesive microspheres of duloxetine hydrochloride using 3(2) full factorial design.

    Science.gov (United States)

    Setia, Anupama; Kansal, Sahil; Goyal, Naveen

    2013-07-01

    Microspheres constitute an important part of oral drug delivery system by virtue of their small size and efficient carrier capacity. However, the success of these microspheres is limited due to their short residence time at the site of absorption. The objective of the present study was to formulate and systematically evaluate in vitro performance of enteric coated mucoadhesive microspheres of duloxetine hydrochloride (DLX), an acid labile drug. DLX microspheres were prepared by simple emulsification phase separation technique using chitosan as carrier and glutaraldehyde as a cross-linking agent. Microspheres prepared were coated with eudragit L-100 using an oil-in-oil solvent evaporation method. Eudragit L-100was used as enteric coating polymer with the aim to release the drug in small intestine The microspheres prepared were characterized by particle size, entrapment efficiency, swelling index (SI), mucoadhesion time, in vitro drug release and surface morphology. A 3(2) full factorial design was employed to study the effect of independent variables polymer-to-drug ratio (X1) and stirring speed (X2) on dependent variables, particle size, entrapment efficiency, SI, in vitro mucoadhesion and drug release up to 24 h (t24). Microspheres formed were discrete, spherical and free flowing. The microspheres exhibited good mucoadhesive property and also showed high percentage entrapment efficiency. The microspheres were able to sustain the drug release up to 24 h. Thus, the prepared enteric coated mucoadhesive microspheres may prove to be a potential controlled release formulation of DLX for oral administration.

  10. Encapsulation of Liposomes within pH Responsive Microspheres for Oral Colonic Drug Delivery

    Directory of Open Access Journals (Sweden)

    M. J. Barea

    2012-01-01

    Full Text Available A novel liposome-in-microsphere (LIM formulation has been created comprising drug-loaded liposomes within pH responsive Eudragit S100 microspheres. The liposomes contained the model drug 5-ASA and were coated with chitosan in order to protect them during encapsulation within the microspheres and to improve site-specific release characteristics. In vitro drug release studies showed that LIMs prevented drug release within simulated stomach and small intestine conditions with subsequent drug release occurring in large intestine conditions. The formulation therefore has potential for oral colonic drug delivery.

  11. Ibuprofen-in-cyclodextrin-in-W/O/W emulsion - Improving the initial and long-term encapsulation efficiency of a model active ingredient.

    Science.gov (United States)

    Hattrem, Magnus N; Kristiansen, Kåre A; Aachmann, Finn L; Dille, Morten J; Draget, Kurt I

    2015-06-20

    A challenge in formulating water-in-oil-in-water (W/O/W) emulsions is the uncontrolled release of the encapsulated compound prior to application. Pharmaceuticals and nutraceuticals usually have amphipathic nature, which may contribute to leakage of the active ingredient. In the present study, cyclodextrins (CyDs) were used to impart a change in the relative polarity and size of a model compound (ibuprofen) by the formation of inclusion complexes. Various inclusion complexes (2-hydroxypropyl (HP)-β-CyD-, α-CyD- and γ-CyD-ibuprofen) were prepared and presented within W/O/W emulsions, and the initial and long-term encapsulation efficiency was investigated. HP-β-CyD-ibuprofen provided the highest encapsulation of ibuprofen in comparison to a W/O/W emulsion with unassociated ibuprofen confined within the inner water phase, with a four-fold increase in the encapsulation efficiency. An improved, although lower, encapsulation efficiency was obtained for the inclusion complex γ-CyD-ibuprofen in comparison to HP-β-CyD-ibuprofen, whereas α-CyD-ibuprofen had a similar encapsulation efficiency to that of unassociated ibuprofen. The lower encapsulation efficiency of ibuprofen in combination with α-CyD and γ-CyD was attributed to a lower association constant for the γ-CyD-ibuprofen inclusion complex and the ability of α-CyD to form inclusion complexes with fatty acids. For the W/O/W emulsion prepared with HP-β-CyD-ibuprofen, the highest encapsulation of ibuprofen was obtained at hyper- and iso-osmotic conditions and by using an excess molar ratio of CyD to ibuprofen. In the last part of the study, it was suggested that the chemical modification of the HP-β-CyD molecule did not influence the encapsulation of ibuprofen, as a similar encapsulation efficiency was obtained for an inclusion complex prepared with mono-1-glucose-β-CyD. Copyright © 2015 Elsevier B.V. All rights reserved.

  12. Hydroxyl radical induced degradation of ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Illés, Erzsébet, E-mail: erzsebet.illes@chem.u-szeged.hu [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary); Takács, Erzsébet [Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary); Dombi, András [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Gajda-Schrantz, Krisztina [Institute of Chemistry, Research Group of Environmental Chemistry, University of Szeged, Szeged (Hungary); Department of Inorganic and Analytical Chemistry, University of Szeged, Szeged (Hungary); EMPA, Laboratory for High Performance Ceramics, Duebendorf (Switzerland); Rácz, Gergely; Gonter, Katalin; Wojnárovits, László [Institute of Isotopes, Centre for Energy Research, Hungarian Academy of Sciences, Budapest (Hungary)

    2013-03-01

    Pulse radiolysis experiments were used to characterize the intermediates formed from ibuprofen during electron beam irradiation in a solution of 0.1 mmol dm{sup −3}. For end product characterization {sup 60}Co γ-irradiation was used and the samples were evaluated either by taking their UV–vis spectra or by HPLC with UV or MS detection. The reactions of {sup ·}OH resulted in hydroxycyclohexadienyl type radical intermediates. The intermediates produced in further reactions hydroxylated the derivatives of ibuprofen as final products. The hydrated electron attacked the carboxyl group. Ibuprofen degradation is more efficient under oxidative conditions than under reductive conditions. The ecotoxicity of the solution was monitored by Daphnia magna standard microbiotest and Vibrio fischeri luminescent bacteria test. The toxic effect of the aerated ibuprofen solution first increased upon irradiation indicating a higher toxicity of the first degradation products, then decreased with increasing absorbed dose. Highlights: ► In hydroxyl radical attack on the ring mainly hydroxylated products form ► The hydrated electron attacks the carboxyl group. ► Oxidative conditions are more effective in ibuprofen decomposition than reductive. ► Ecotoxicity of ibuprofen solution first increases then decreases with irradiation.

  13. Hydroxyl radical induced degradation of ibuprofen

    International Nuclear Information System (INIS)

    Illés, Erzsébet; Takács, Erzsébet; Dombi, András; Gajda-Schrantz, Krisztina; Rácz, Gergely; Gonter, Katalin; Wojnárovits, László

    2013-01-01

    Pulse radiolysis experiments were used to characterize the intermediates formed from ibuprofen during electron beam irradiation in a solution of 0.1 mmol dm −3 . For end product characterization 60 Co γ-irradiation was used and the samples were evaluated either by taking their UV–vis spectra or by HPLC with UV or MS detection. The reactions of · OH resulted in hydroxycyclohexadienyl type radical intermediates. The intermediates produced in further reactions hydroxylated the derivatives of ibuprofen as final products. The hydrated electron attacked the carboxyl group. Ibuprofen degradation is more efficient under oxidative conditions than under reductive conditions. The ecotoxicity of the solution was monitored by Daphnia magna standard microbiotest and Vibrio fischeri luminescent bacteria test. The toxic effect of the aerated ibuprofen solution first increased upon irradiation indicating a higher toxicity of the first degradation products, then decreased with increasing absorbed dose. Highlights: ► In hydroxyl radical attack on the ring mainly hydroxylated products form ► The hydrated electron attacks the carboxyl group. ► Oxidative conditions are more effective in ibuprofen decomposition than reductive. ► Ecotoxicity of ibuprofen solution first increases then decreases with irradiation

  14. Preparation of chitosan/nano hydroxyapatite organic-inorganic hybrid microspheres for bone repair.

    Science.gov (United States)

    Chen, Jingdi; Pan, Panpan; Zhang, Yujue; Zhong, Shengnan; Zhang, Qiqing

    2015-10-01

    In this work, we encapsulated icariin (ICA) into chitosan (CS)/nano hydroxyapatite (nHAP) composite microspheres to form organic-inorganic hybrid microspheres for drug delivery carrier. The composition and morphology of composite microspheres were characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and differential scanning calorimetry- thermogravimetric analysis (DSC-TGA). Moreover, we further studied the performance of swelling properties, degradation properties and drug release behavior of the microspheres. ICA, the extract of traditional Chinese medicine-epimedium, was combined to study drug release properties of the microspheres. ICA loaded microspheres take on a sustained release behavior, which can be not only ascribed to electrostatic interaction between reactive negative hydroxyl (OH) of ICA and positive amine groups (NH₂) of CS, but also depended on the homogeneous dispersion of HAP nanoparticles inside CS organic matrix. In addition, the adhesion and morphology of osteoblasts were detected by inverted fluorescence microscopy. The biocompatibility of CS/nHAP/ICA microspheres was evaluated by the MTT cytotoxicity assay, Hoechst 33258 and PI fluorescence staining. These studies demonstrate that composite microspheres provide a suitable microenvironment for osteoblast attachment and proliferation. It can be speculated that the ICA loaded CS-based organic-inorganic hybrid microspheres might have potential applications in drug delivery systems. Copyright © 2015 Elsevier B.V. All rights reserved.

  15. Insulin delivery through nasal route using thiolated microspheres.

    Science.gov (United States)

    Nema, Tarang; Jain, Ashish; Jain, Aviral; Shilpi, Satish; Gulbake, Arvind; Hurkat, Pooja; Jain, Sanjay K

    2013-01-01

    The aim of the present study was to investigate the potential of developed thiolated microspheres for insulin delivery through nasal route. In the present study, cysteine was immobilized on carbopol using EDAC. A total of 269.93 µmol free thiol groups per gram polymer were determined. The prepared nonthiolated and thiolated microspheres were studied for particle shape, size, drug content, swellability, mucoadhesion and in vitro insulin release. The thiolated microspheres exhibited higher mucoadhesion due to formation of covalent bonds via disulfide bridges with the mucus gel layer. Drug permeation through goat nasal mucosa of nonthiolated and thiolated microspheres were found as 52.62 ± 2.4% and 78.85 ± 3.1% in 6 h, respectively. Thiolated microspheres bearing insulin showed better reduction in blood glucose level (BGL) in comparison to nonthiolated microspheres as 31.23 ± 2.12% and 75.25 ± 0.93% blood glucose of initial BGL were observed at 6 h after nasal delivery of thiolated and nonthiolated microspheres in streptozotocin-induced diabetic rabbits.

  16. Current knowledge on biodegradable microspheres in drug delivery.

    Science.gov (United States)

    Prajapati, Vipul D; Jani, Girish K; Kapadia, Jinita R

    2015-08-01

    Biodegradable microspheres have gained popularity for delivering a wide variety of molecules via various routes. These types of products have been prepared using various natural and synthetic biodegradable polymers through suitable techniques for desired delivery of various challenging molecules. Selection of biodegradable polymers and technique play a key role in desired drug delivery. This review describes an overview of the fundamental knowledge and status of biodegradable microspheres in effective delivery of various molecules via desired routes with consideration of outlines of various compendial and non-compendial biodegradable polymers, formulation techniques and release mechanism of microspheres, patents and commercial biodegradable microspheres. There are various advantages of using biodegradable polymers including promise of development with different types of molecules. Biocompatibility, low dosage and reduced side effects are some reasons why usage biodegradable microspheres have gained in popularity. Selection of biodegradable polymers and formulation techniques to create microspheres is the biggest challenge in research. In the near future, biodegradable microspheres will become the eco-friendly product for drug delivery of various genes, hormones, proteins and peptides at specific site of body for desired periods of time.

  17. Nanomechanics of biocompatible hollow thin-shell polymer microspheres.

    Science.gov (United States)

    Glynos, Emmanouil; Koutsos, Vasileios; McDicken, W Norman; Moran, Carmel M; Pye, Stephen D; Ross, James A; Sboros, Vassilis

    2009-07-07

    The nanomechanical properties of biocompatible thin-shell hollow polymer microspheres with approximately constant ratio of shell thickness to microsphere diameter were measured by nanocompression tests in aqueous conditions. These microspheres encapsulate an inert gas and are used as ultrasound contrast agents by releasing free microbubbles in the presence of an ultrasound field as a result of free gas leakage from the shell. The tests were performed using an atomic force microscope (AFM) employing the force-distance curve technique. An optical microscope, on which the AFM was mounted, was used to guide the positioning of tipless cantilevers on top of individual microspheres. We performed a systematic study using several cantilevers with spring constants varying from 0.08 to 2.3 N/m on a population of microspheres with diameters from about 2 to 6 microm. The use of several cantilevers with various spring constants allowed a systematic study of the mechanical properties of the microsphere thin shell at different regimes of force and deformation. Using thin-shell mechanics theory for small deformations, the Young's modulus of the thin wall material was estimated and was shown to exhibit a strong size effect: it increased as the shell became thinner. The Young's modulus of thicker microsphere shells converged to the expected value for the macroscopic bulk material. For high applied forces, the force-deformation profiles showed a reversible and/or irreversible nonlinear behavior including "steps" and "jumps" which were attributed to mechanical instabilities such as buckling events.

  18. Method for sizing hollow microspheres

    Science.gov (United States)

    Farnum, E.H.; Fries, R.J.

    1975-10-29

    Hollow Microspheres may be effectively sized by placing them beneath a screen stack completely immersed in an ultrasonic bath containing a liquid having a density at which the microspheres float and ultrasonically agitating the bath.

  19. loaded Eudragit RL 100 Microspheres Prepared by an Emulsion

    African Journals Online (AJOL)

    Erah

    drug release profiles of the microspheres at pH 1.2 showed poor drug release characteristics while at. pH 6.8 ... drug delivery, improve bioavailability and stability and target drug to ... The factors affecting particle size, drug loading and drug.

  20. Analgesic efficacy with rapidly absorbed ibuprofen sodium dihydrate in postsurgical dental pain

    DEFF Research Database (Denmark)

    Nørholt, Sven Erik; Hallmer, F; Hartlev, Jens

    2011-01-01

    To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid).......To evaluate the onset of analgesic effect for a new formulation of ibuprofen sodium dihydrate versus conventional ibuprofen (ibuprofen acid)....

  1. Innovative hydrogen storage in hollow glass-microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Keding, M.; Schmid, G.; Tajmar, M. [Austrian Research Centers, Vienna (Austria)

    2009-07-01

    Hydrogen storage technologies are becoming increasingly important for a number of future applications. The Austrian Research Centers (ARC) are developing a unique hydrogen storage system that combines the advantages of both hollow glass microsphere and chemical compound hydrogen storage, but eliminates their respective drawbacks. Water is utilized as a functional liquid to carry the hollow glass microspheres that are loaded with up to 700 bar of hydrogen gas. Sodium borohydride (NaBH{sub 4}) is then injected together with the glass microspheres into a reaction chamber where the water reacts catalytically with the NaBH{sub 4} producing hydrogen and heat. The heat is then utilized to release the hydrogen from the hollow glass microspheres providing a double hydrogen generation process without any external energy or heat during storage or gas release. The paper described this hydrogen storage system with particular reference to microspheres, the coating process, the experimental facility and NaBH{sub 4} test results. It was concluded that hydrogen storage and production on demand is possible with microspheres and sodium borohydride solution. 9 refs., 16 figs.

  2. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2011-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  3. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2010-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  4. Ceramic microspheres for cementing applications

    NARCIS (Netherlands)

    2012-01-01

    A method and apparatus for manufacturing ceramic microspheres from industrial slag. The microspheres have a particle size of about 38 microns to about 150 microns. The microspheres are used to create a cement slurry having a density of at least about 11 lbs/g. The resultant cement slurry may then be

  5. Synovial and systemic pharmacokinetics (PK) of triamcinolone acetonide (TA) following intra-articular (IA) injection of an extended-release microsphere-based formulation (FX006) or standard crystalline suspension in patients with knee osteoarthritis (OA).

    Science.gov (United States)

    Kraus, V B; Conaghan, P G; Aazami, H A; Mehra, P; Kivitz, A J; Lufkin, J; Hauben, J; Johnson, J R; Bodick, N

    2018-01-01

    Intra-articular (IA) corticosteroids relieve osteoarthritis (OA) pain, but rapid absorption into systemic circulation may limit efficacy and produce untoward effects. We compared the pharmacokinetics (PK) of IA triamcinolone acetonide (TA) delivered as an extended-release, microsphere-based formulation (FX006) vs a crystalline suspension (TAcs) in knee OA patients. This Phase 2 open-label study sequentially enrolled 81 patients who received a single IA injection of FX006 (5 mL, 32 mg delivered dose, N = 63) or TAcs (1 mL, 40 mg, N = 18). Synovial fluid (SF) aspiration was attempted in each patient at baseline and one post-IA-injection visit (FX006: Week 1, Week 6, Week 12, Week 16 or Week 20; TAcs: Week 6). Blood was collected at baseline and multiple post-injection times. TA concentrations (validated LC-MS/MS, geometric means (GMs)), PK (non-compartmental analysis models), and adverse events (AEs) were assessed. SF TA concentrations following FX006 were quantifiable through Week 12 (pg/mL: 231,328.9 at Week 1; 3590.0 at Week 6; 290.6 at Week 12); post-TAcs, only two of eight patients had quantifiable SF TA at Week 6 (7.7 pg/mL). Following FX006, plasma TA gradually increased to peak (836.4 pg/mL) over 24 h and slowly declined to IA injection prolonged SF joint residency, diminished peak plasma levels, and thus reduced systemic TA exposure relative to TAcs. Copyright © 2017 The Authors. Published by Elsevier Ltd.. All rights reserved.

  6. Microbiological and clinical effects of enamel matrix derivative and sustained-release micro-spherical minocycline application as an adjunct to non-surgical therapy in peri-implant mucosal inflammation.

    Science.gov (United States)

    Faramarzi, Masumeh; Goharfar, Zahra; Pourabbas, Reza; Kashefimehr, Atabak; Shirmohmmadi, Adileh

    2015-08-01

    The purpose of this study was to compare the microbial and clinical effects of mechanical debridement (MD) alone or in combination with the application of enamel matrix derivative (EMD) and sustained-release micro-spherical minocycline (MSM) for treatment of peri-implant mucosal infl ammation (PIMI). Subjects with at least one implant with PIMI were included and divided into control and two different test groups. In all three groups, MD was performed. In the MSM group, following MD, MSM was placed subgingivally around the implants. In the EMD group, after MD, EMD was placed in the sulcus around the implants. Sampling of peri-implant crevicular fl uid for microbial analysis with real-time polymerase chain reaction and recording of probing depth (PD) and bleeding on probing (BOP) were performed prior to as well as two weeks and three months after treatment. Median values and interquartile range were estimated for each variable during the various assessment intervals of the study. In all groups, at two weeks and three months, the counts of Porphyromonas gingivalis decreased significantly compared to baseline. Levels of P. gingivalis were significantly reduced in MSM (P<0.001) and EMD (P=0.026) groups compared to the control group. Also, clinical parameters improved significantly at two weeks and three months. Reduction of PD was significant in MSM (P<0.001) and EMD (P<0.001) groups. The decrease in BOP in the MSM, EMD, and control groups was 60%, 50%, and 20%, respectively. The use of MSM and EMD can be an adjunctive treatment for management of PIMI and improves clinical parameters and reduces P. gingivalis burden three months after treatment.

  7. Formulation of Novel Layered Sodium Carboxymethylcellulose Film Wound Dressings with Ibuprofen for Alleviating Wound Pain

    Directory of Open Access Journals (Sweden)

    Lenka Vinklárková

    2015-01-01

    Full Text Available Effective assessment and management of wound pain can facilitate both improvements in healing rates and overall quality of life. From a pharmacological perspective, topical application of nonsteroidal anti-inflammatory drugs in the form of film wound dressings may be a good choice. Thus, the aim of this work was to develop novel layered film wound dressings containing ibuprofen based on partially substituted fibrous sodium carboxymethylcellulose (nonwoven textile Hcel NaT. To this end, an innovative solvent casting method using a sequential coating technique has been applied. The concentration of ibuprofen which was incorporated as an acetone solution or as a suspension in a sodium carboxymethylcellulose dispersion was 0.5 mg/cm2 and 1.0 mg/cm2 of film. Results showed that developed films had adequate mechanical and swelling properties and an advantageous acidic surface pH for wound application. An in vitro drug release study implied that layered films retained the drug for a longer period of time and thus could minimize the frequency of changing the dressing. Films with suspended ibuprofen demonstrated higher drug content uniformity and superior in vitro drug release characteristics in comparison with ibuprofen incorporation as an acetone solution. Prepared films could be potential wound dressings for the effective treatment of wound pain in low exuding wounds.

  8. Formulation of Novel Layered Sodium Carboxymethylcellulose Film Wound Dressings with Ibuprofen for Alleviating Wound Pain

    Science.gov (United States)

    Vinklárková, Lenka; Vetchý, David; Bernatonienė, Jurga

    2015-01-01

    Effective assessment and management of wound pain can facilitate both improvements in healing rates and overall quality of life. From a pharmacological perspective, topical application of nonsteroidal anti-inflammatory drugs in the form of film wound dressings may be a good choice. Thus, the aim of this work was to develop novel layered film wound dressings containing ibuprofen based on partially substituted fibrous sodium carboxymethylcellulose (nonwoven textile Hcel NaT). To this end, an innovative solvent casting method using a sequential coating technique has been applied. The concentration of ibuprofen which was incorporated as an acetone solution or as a suspension in a sodium carboxymethylcellulose dispersion was 0.5 mg/cm2 and 1.0 mg/cm2 of film. Results showed that developed films had adequate mechanical and swelling properties and an advantageous acidic surface pH for wound application. An in vitro drug release study implied that layered films retained the drug for a longer period of time and thus could minimize the frequency of changing the dressing. Films with suspended ibuprofen demonstrated higher drug content uniformity and superior in vitro drug release characteristics in comparison with ibuprofen incorporation as an acetone solution. Prepared films could be potential wound dressings for the effective treatment of wound pain in low exuding wounds. PMID:26090454

  9. Evaporation Behavior and Characterization of Eutectic Solvent and Ibuprofen Eutectic Solution.

    Science.gov (United States)

    Phaechamud, Thawatchai; Tuntarawongsa, Sarun; Charoensuksai, Purin

    2016-10-01

    Liquid eutectic system of menthol and camphor has been reported as solvent and co-solvent for some drug delivery systems. However, surprisingly, the phase diagram of menthol-camphor eutectic has not been reported previously. The evaporation behavior, physicochemical, and thermal properties of this liquid eutectic and ibuprofen eutectic solution were characterized in this study. Differential scanning calorimetry (DSC) analysis indicated that a eutectic point of this system was near to 1:1 menthol/camphor and its eutectic temperature was -1°C. The solubility of ibuprofen in this eutectic was 282.11 ± 6.67 mg mL(-1) and increased the drug aqueous solubility fourfold. The shift of wave number from Fourier transform infrared spectroscopy (FTIR) indicated the hydrogen bonding of each compound in eutectic mixture. The weight loss from thermogravimetric analysis of menthol and camphor related to the evaporation and sublimation, respectively. Menthol demonstrated a lower apparent sublimation rate than camphor, and the evaporation rate of eutectic solvent was lower than the sublimation rate of camphor but higher than the evaporation of menthol. The evaporation rate of the ibuprofen eutectic solution was lower than that of the eutectic solvent because ibuprofen did not sublimate. This eutectic solvent prolonged the ibuprofen release with diffusion control. Thus, the beneficial information for thermal behavior and related properties of eutectic solvent comprising menthol-camphor and ibuprofen eutectic solution was attained successfully. The rather low evaporation of eutectic mixture will be beneficial for investigation and tracking the mechanism of transformation from nanoemulsion into nanosuspension in the further study using eutectic as oil phase.

  10. Recent advances in polymeric microspheres for parenteral drug delivery--part 1.

    Science.gov (United States)

    Mao, Shirui; Guo, Chunqiang; Shi, Yi; Li, Luk Chiu

    2012-09-01

    Polymeric microspheres have been established as a valuable parenteral drug delivery system for sustained release of therapeutic agents via subcutaneous or intramuscular injection. Biodegradable polymers which are either synthetic or from natural sources are reviewed with respect to recent advances in exploring their applications for microsphere fabrications. New information on the impact of formulation variables on the properties of microspheres formed by an emulsion method was also presented. The characterization of microspheres using advanced physical analytical techniques was also reviewed and the utilization of the information in assessing in vivo performance of the product was also highlighted. The broad clinical use of microspheres for delivery of therapeutic agents in particular biologics such as proteins has not been realized commercially. The limited availability of biodegradable polymers with a long history of regulatory approval and the challenges in gaining regulatory approval of a new polymer have hindered the development of microspheres for parenteral drug delivery.

  11. Detection and Analysis of the Quality of Ibuprofen Granules

    Science.gov (United States)

    Yu-bin, Ji; Xin, LI; Guo-song, Xin; Qin-bing, Xue

    2017-12-01

    The Ibuprofen Granules comprehensive quality testing to ensure that it is in accordance with the provisions of Chinese pharmacopoeia. With reference of Chinese pharmacopoeia, the Ibuprofen Granules is tested by UV, HPLC, in terms of grain size checking, volume deviation, weight loss on drying detection, dissolution rate detection, and quality evaluation. Results indicated that Ibuprofen Granules conform to the standards. The Ibuprofen Granules are qualified and should be permitted to be marketed.

  12. Effect of Ibuprofen on masking endodontic diagnosis.

    Science.gov (United States)

    Read, Jason K; McClanahan, Scott B; Khan, Asma A; Lunos, Scott; Bowles, Walter R

    2014-08-01

    An accurate diagnosis is of upmost importance before initiating endodontic treatment; yet, there are occasions when the practitioner cannot reproduce the patient's chief complaint because the patient has become asymptomatic. Ibuprofen taken beforehand may "mask" or eliminate the patient's symptoms. In fact, 64%-83% of patients with dental pain take analgesics before seeing a dentist. The purpose of this study was to examine the possible "masking" effect of ibuprofen on endodontic diagnostic tests. Forty-two patients with endodontic pain underwent testing (cold, percussion, palpation, and bite force measurement) and then received either placebo or 800 mg ibuprofen. Both patients and operators were blinded to the medication received. One hour later, diagnostic testing was repeated and compared with pretreatment testing. Ibuprofen affected testing values for vital teeth by masking palpation 40%, percussion 25%, and cold 25% on affected teeth with symptomatic irreversible pulpitis and symptomatic apical periodontitis. There was no observed masking effect in the placebo group on palpation, percussion, or cold values. When nonvital teeth were included, the masking effect of ibuprofen was decreased. However, little masking occurred with the bite force measurement differences. Analgesics taken before the dental appointment can affect endodontic diagnostic testing results. Bite force measurements can assist in identifying the offending tooth in cases in which analgesics "mask" the endodontic diagnosis. Copyright © 2014 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  13. Bioequivalence assessment of two formulations of ibuprofen

    KAUST Repository

    Al-Talla, Zeyad

    2011-10-19

    Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz , produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen , manufactured by Boots Company, Nottingham, UK. Methods and results: A prestudy validation of ibuprofen demonstrated long-term stability, freeze-thaw stability, precision, and accuracy. Twenty-four healthy volunteers were enrolled in this study. After overnight fasting, the two formulations (test and reference) of ibuprofen (100 mg ibuprofen/5 mL suspension) were administered as a single dose on two treatment days separated by a one-week washout period. After dosing, serial blood samples were drawn for a period of 14 hours. Serum harvested from the blood samples was analyzed for the presence of ibuprofen by high-pressure liquid chromatography with ultraviolet detection. Pharmacokinetic parameters were determined from serum concentrations for both formulations. The 90% confidence intervals of the ln-transformed test/reference treatment ratios for peak plasma concentration and area under the concentration-time curve (AUC) parameters were found to be within the predetermined acceptable interval of 80%-125% set by the US Food and Drug Administration. Conclusion: Analysis of variance for peak plasma concentrations and AUC parameters showed no significant difference between the two formulations and, therefore, Doloraz was considered bioequivalent to Brufen. 2011 Al-Talla et al, publisher and licensee Dove Medical Press Ltd.

  14. Preparation of alumina microspheres

    International Nuclear Information System (INIS)

    Santos, W.R. dos; Abrao, A.

    1980-01-01

    Inorganic exchangers are widely used for adsorption and column partition chromatography. The main difficulty of using commercial alumina (in powder) for column chromatography is related to its packing, and the operations through the column become diffcult and time-consuming; also it turns to be virtually impossible to use large dimension columns. In order to eliminate these problems, a process for the preparation of alumina micro-spheres was developed as an adaptation of a similar process used to prepare nuclear fuel microspheres (UO 2 , ThO 2 ). The flowsheet of this process is presented together with the analytical results of sphericity after calcination, granulometry, density and characterization by X-ray diffractometry. Solubility tests showed that the so-prepared microspheres are well resistant to strong acids and bases; retention tests showed their efficiency, mainly to copper. (C.L.B.) [pt

  15. Silicon Microspheres Photonics

    International Nuclear Information System (INIS)

    Serpenguzel, A.

    2008-01-01

    Electrophotonic integrated circuits (EPICs), or alternatively, optoelectronic integrated circuit (OEICs) are the natural evolution of the microelectronic integrated circuit (IC) with the addition of photonic capabilities. Traditionally, the IC industry has been based on group IV silicon, whereas the photonics industry on group III-V semiconductors. However, silicon based photonic microdevices have been making strands in siliconizing photonics. Silicon microspheres with their high quality factor whispering gallery modes (WGMs), are ideal candidates for wavelength division multiplexing (WDM) applications in the standard near-infrared communication bands. In this work, we will discuss the possibility of using silicon microspheres for photonics applications in the near-infrared

  16. Formulation, evaluation and 3(2) full factorial design-based optimization of ondansetron hydrochloride incorporated taste masked microspheres.

    Science.gov (United States)

    Kharb, Vandana; Saharan, Vikas Anand; Dev, Kapil; Jadhav, Hemant; Purohit, Suresh

    2014-11-01

    Masking the bitter taste of Ondansetron hydrochloride (ONS) may improve palatability, acceptance and compliance of ONS products. ONS-loaded, taste-masked microspheres were prepared with a polycationic pH-sensitive polymer and 3(2) full factorial design (FFD) was applied to optimize microsphere batches. Solvent evaporation, in acetone--methanol/liquid paraffin system, was used to prepare taste-masked ONS microspheres. The effect of varying drug/polymer (D/P) ratios on microspheres characteristics were studied by 3(2) FFD. Desirability function was used to search the optimum formulation. Microspheres were evaluated by FTIR, XRD and DSC to examine interaction and effect of microencapsulation process. In vitro taste assessment approach based on bitterness threshold and drug release was used to assess bitterness scores. Prepared ONS microspheres were spherical and surface was wrinkled. ONS was molecularly dispersed in microspheres without any incompatibility with EE100. In hydrochloric acid buffer pH 1.2, ONS released completely from microsphere in just 10 min. Contrary to this, ONS release at initial 5 min from taste-masked microspheres was less than the bitterness threshold. Full factorial design and in vitro taste assessment approach, coupled together, was successfully applied to develop and optimize batches of ONS incorporated taste-masked microspheres.

  17. Ibuprofen in paediatrics: pharmacology, prescribing and controversies.

    Science.gov (United States)

    Moriarty, Camilla; Carroll, Will

    2016-12-01

    Ibuprofen, a propionic acid derivative, is a non-steroidal anti-inflammatory drug. The oral formulation is widely used in paediatric practice and after paracetamol it is one of the most common drugs prescribed for children in hospital. The treatment of fever with antipyretics such as ibuprofen is controversial as fever is the normal response of the body to infection and unless the child becomes distressed or symptomatic, fever alone should not be routinely treated. Combined treatment with paracetamol and ibuprofen is commonly undertaken but almost certainly is not helpful. This article aims to describe the indications and mode of action of the drug, outline its pharmacokinetics and highlight the important key messages regarding its use in clinical practice. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/.

  18. Development and optimization of enteric coated mucoadhesive microspheres of duloxetine hydrochloride using 32 full factorial design

    Science.gov (United States)

    Setia, Anupama; Kansal, Sahil; Goyal, Naveen

    2013-01-01

    Background: Microspheres constitute an important part of oral drug delivery system by virtue of their small size and efficient carrier capacity. However, the success of these microspheres is limited due to their short residence time at the site of absorption. Objective: The objective of the present study was to formulate and systematically evaluate in vitro performance of enteric coated mucoadhesive microspheres of duloxetine hydrochloride (DLX), an acid labile drug. Materials and Methods: DLX microspheres were prepared by simple emulsification phase separation technique using chitosan as carrier and glutaraldehyde as a cross-linking agent. Microspheres prepared were coated with eudragit L-100 using an oil-in-oil solvent evaporation method. Eudragit L-100was used as enteric coating polymer with the aim to release the drug in small intestine The microspheres prepared were characterized by particle size, entrapment efficiency, swelling index (SI), mucoadhesion time, in vitro drug release and surface morphology. A 32 full factorial design was employed to study the effect of independent variables polymer-to-drug ratio (X1) and stirring speed (X2) on dependent variables, particle size, entrapment efficiency, SI, in vitro mucoadhesion and drug release up to 24 h (t24). Results: Microspheres formed were discrete, spherical and free flowing. The microspheres exhibited good mucoadhesive property and also showed high percentage entrapment efficiency. The microspheres were able to sustain the drug release up to 24 h. Conclusion: Thus, the prepared enteric coated mucoadhesive microspheres may prove to be a potential controlled release formulation of DLX for oral administration. PMID:24167786

  19. Bioequivalence assessment of two formulations of ibuprofen

    Directory of Open Access Journals (Sweden)

    Al-Talla ZA

    2011-10-01

    Full Text Available Zeyad A Al-Talla1, Sabah H Akrawi2, Luke T Tolley3, Salim H Sioud1, Mohammed F Zaater4, Abdul-Hamid M Emwas1 1Analytical and NMR Core Laboratories, King Abdullah University of Science and Technology, Thuwal, Kingdom of Saudia Arabia; 2College of Pharmacy, Al-Ain University, Al-Ain, United Arab Emirates; 3Department of Chemistry and Biochemistry, Southern Illinois University Carbondale, Carbondale, IL, USA; 4Department of Chemistry, Jordan University of Science and Technology, Jordan University of Science and Technology, Irbid, Jordan Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz®, produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen®, manufactured by Boots Company, Nottingham, UK. Methods and results: A prestudy validation of ibuprofen demonstrated long-term stability, freeze-thaw stability, precision, and accuracy. Twenty-four healthy volunteers were enrolled in this study. After overnight fasting, the two formulations (test and reference of ibuprofen (100 mg ibuprofen/5 mL suspension were administered as a single dose on two treatment days separated by a one-week washout period. After dosing, serial blood samples were drawn for a period of 14 hours. Serum harvested from the blood samples was analyzed for the presence of ibuprofen by high-pressure liquid chromatography with ultraviolet detection. Pharmacokinetic parameters were determined from serum concentrations for both formulations. The 90% confidence intervals of the ln-transformed test/reference treatment ratios for peak plasma concentration and area under the concentration-time curve (AUC parameters were found to be within the predetermined acceptable interval of 80%–125% set by the US Food and Drug Administration. Conclusion: Analysis of variance for peak plasma concentrations and AUC parameters showed no significant difference between the two formulations and

  20. Dual Drug Loaded Biodegradable Nanofibrous Microsphere for Improving Anti-Colon Cancer Activity

    Science.gov (United States)

    Fan, Rangrang; Li, Xiaoling; Deng, Jiaojiao; Gao, Xiang; Zhou, Liangxue; Zheng, Yu; Tong, Aiping; Zhang, Xiaoning; You, Chao; Guo, Gang

    2016-06-01

    One of the approaches being explored to increase antitumor activity of chemotherapeutics is to inject drug-loaded microspheres locally to specific anatomic sites, providing for a slow, long term release of a chemotherapeutic while minimizing systemic exposure. However, the used clinically drug carriers available at present have limitations, such as their low stability, renal clearance and residual surfactant. Here, we report docetaxel (DOC) and curcumin (CUR) loaded nanofibrous microspheres (DOC + CUR/nanofibrous microspheres), self-assembled from biodegradable PLA-PEO-PPO-PEO-PLA polymers as an injectable drug carrier without adding surfactant during the emulsification process. The obtained nanofibrous microspheres are composed entirely of nanofibers and have an open hole on the shell without the assistance of a template. It was shown that these DOC + CUR/nanofibrous microspheres could release curcumin and docetaxel slowly in vitro. The slow, sustained release of curcumin and docetaxel in vivo may help maintain local concentrations of active drug. The mechanism by which DOC + CUR/nanofibrous microspheres inhibit colorectal peritoneal carcinomatosis might involve increased induction of apoptosis in tumor cells and inhibition of tumor angiogenesis. In vitro and in vivo evaluations demonstrated efficacious synergistic antitumor effects against CT26 of curcumin and docetaxel combined nanofibrous microspheres. In conclusion, the dual drug loaded nanofibrous microspheres were considered potentially useful for treating abdominal metastases of colorectal cancer.

  1. Carbidopa/levodopa-loaded biodegradable microspheres: in vivo evaluation on experimental Parkinsonism in rats.

    Science.gov (United States)

    Arica, Betül; Kaş, H Süheyla; Moghdam, Amir; Akalan, Nejat; Hincal, A Atilla

    2005-02-16

    The purpose of this study was to prepare and characterize injectable carbidopa (CD)/levodopa (LD)-loaded Poly(L-lactides) (L-PLA), Poly(D,L-lactides) (D,L-PLA) and Poly(D,L-lactide-co-glycolide) (PLAGA) microspheres for the intracerebral treatment of Parkinson's disease. The microspheres were prepared by solvent evaporation method. The polymers' (L-PLA, D,L-PLA and PLAGA) concentrations were 10% (w/w) in the organic phase; the emulsifiers [sodium carboxymethylcellulose (NaCMC):sodium oleate (SO) and Polyvinyl alcohol (PVA):SO mixture (4:1 w/v)] concentrations were 0.75% in the aqueous phase. Microspheres were analyzed for morphological characteristics, size distribution, drug loading and in vitro release. The release profile of CD/LD from microspheres was characterized in the range of 12-35% within the first hour of the in vitro release experiment. The efficiency of CD- and LD-encapsulated microspheres to striatal transplantation and the altering of apomorphine-induced rotational behavior in the 6-hydroxydopamine (6-OHDA) unilaterally lesioned rat model were also tested. 6-OHDA/CD-LD-loaded microsphere groups exhibited lower rotation scores than 6-OHDA/Blank microsphere groups as early as 1 week postlesion. These benefits continued throughout the entire experimental period and they were statistically significant during the 1, 2 and 8 weeks (p<0.05). CD/LD-loaded microspheres were specifically prepared to apply as an injectable dosage forms for brain implantation.

  2. 5-Fluorouracil:carnauba wax microspheres for chemoembolization: an in vitro evaluation.

    Science.gov (United States)

    Benita, S; Zouai, O; Benoit, J P

    1986-09-01

    5-Fluorouracil:carnauba wax microspheres were prepared using a meltable dispersion process with the aid of a surfactant as a wetting agent. It was noted that only hydrophilic surfactants were able to wet the 5-fluorouracil and substantially increased its content in the microspheres. No marked effect was observed in the particle size distribution of the solid microspheres as a function of the nature of the surfactant. Increasing the stirring rate in the preparation process decreased, first, the mean droplet size of the emulsified melted dispersion in the vehicle during the heating process, and, consequently, the mean particle size of the solidified microspheres during the cooling process. 5-Fluorouracil cumulative release from the microspheres followed first-order kinetics, as shown by nonlinear regression analysis. Although the kinetic results were not indicative of the true release mechanism from a single microsphere, it was believed that 5-fluorouracil release from the microspheres was probably governed by a dissolution process, rather than by a leaching process through the carnauba wax microspheres.

  3. Synthesis of carbon-13 labeled ibuprofen

    International Nuclear Information System (INIS)

    Hsi, R.S.P.; Stelzer, L.S.; Stolle, W.T.

    1989-01-01

    This report describes the synthesis of 2-[4-(2-methyl)propyl-phenyl]propionic acid (ibuprofen) labeled with carbon-13 either at the terminal methyl carbons, or at the methine carbon of the isobutyl side chain. The synthetic route involves the removal of the isopropyl group in the isobutyl side-chain of ibuprofen via 2-[4-(2-methyl-1-propenyl)phenyl]propionic acid, followed by restoration of the isopropyl group with a Wittig reaction, using appropriate carbon-13 labeled acetone as the precursor of the isopropyl group. Interesting NMR coupling data attributable to phosphorous and carbon-13 are presented in the experimental section. (author)

  4. Vapour-phase method in the synthesis of polymer-ibuprofen sodium-silica gel composites.

    Science.gov (United States)

    Kierys, Agnieszka; Krasucka, Patrycja; Grochowicz, Marta

    2017-11-01

    The study discusses the synthesis of polymer-silica composites comprising water soluble drug (ibuprofen sodium, IBS). The polymers selected for this study were poly(TRIM) and poly(HEMA- co -TRIM) produced in the form of permanently porous beads via the suspension-emulsion polymerization method. The acid and base set ternary composites were prepared by the saturation of the solid dispersions of drug (poly(TRIM)-IBS and/or poly(HEMA- co -TRIM)-IBS) with TEOS, and followed by their exposition to the vapour mixture of water and ammonia, or water and hydrochloric acid, at autogenous pressure. The conducted analyses reveal that the internal structure and total porosity of the resulting composites strongly depend on the catalyst which was used for silica precursor gelation. The parameters characterizing the porosity of both of the acid set composites are much lower than the parameters of the base set composites. Moreover, the basic catalyst supplied in the vapour phase does not affect the ibuprofen sodium molecules, whereas the acid one causes transformation of the ibuprofen sodium into the sodium chloride and a derivative of propanoic acid, which is poorly water soluble. The release profiles of ibuprofen sodium from composites demonstrate that there are differences in the rate and efficiency of drug desorption from them. They are mainly affected by the chemical character of the polymeric carrier but are also associated with the restricted swelling of the composites in the buffer solution after precipitation of silica gel.

  5. Vapour-phase method in the synthesis of polymer-ibuprofen sodium-silica gel composites

    Directory of Open Access Journals (Sweden)

    Agnieszka Kierys

    2017-11-01

    Full Text Available The study discusses the synthesis of polymer-silica composites comprising water soluble drug (ibuprofen sodium, IBS. The polymers selected for this study were poly(TRIM and poly(HEMA-co-TRIM produced in the form of permanently porous beads via the suspension-emulsion polymerization method. The acid and base set ternary composites were prepared by the saturation of the solid dispersions of drug (poly(TRIM-IBS and/or poly(HEMA-co-TRIM-IBS with TEOS, and followed by their exposition to the vapour mixture of water and ammonia, or water and hydrochloric acid, at autogenous pressure. The conducted analyses reveal that the internal structure and total porosity of the resulting composites strongly depend on the catalyst which was used for silica precursor gelation. The parameters characterizing the porosity of both of the acid set composites are much lower than the parameters of the base set composites. Moreover, the basic catalyst supplied in the vapour phase does not affect the ibuprofen sodium molecules, whereas the acid one causes transformation of the ibuprofen sodium into the sodium chloride and a derivative of propanoic acid, which is poorly water soluble. The release profiles of ibuprofen sodium from composites demonstrate that there are differences in the rate and efficiency of drug desorption from them. They are mainly affected by the chemical character of the polymeric carrier but are also associated with the restricted swelling of the composites in the buffer solution after precipitation of silica gel.

  6. Impact of Chiral Bioanalytical Methods on the Bioequivalence of Ibuprofen Products Containing Ibuprofen Lysinate and Ibuprofen Base.

    Science.gov (United States)

    García-Arieta, Alfredo; Ferrero-Cafiero, Juan Manuel; Puntes, Montse; Gich, Ignasi; Morales-Alcelay, Susana; Tarré, Maite; Font, Xavier; Antonijoan, Rosa Maria

    2016-05-01

    The purpose was to assess the impact of the use of a chiral bioanalytical method on the conclusions of a bioequivalence study that compared two ibuprofen suspensions with different rates of absorption. A comparison of the conclusion of bioequivalence between a chiral method and an achiral approach was made. Plasma concentrations of R-ibuprofen and S-ibuprofen were determined using a chiral bioanalytical method; bioequivalence was tested for R-ibuprofen and for S-ibuprofen separately and for the sum of both enantiomers as an approach for an achiral bioanalytical method. The 90% confidence interval (90% CI) that would have been obtained with an achiral bioanalytical method (90% CI: Cmax: 117.69-134.46; AUC0 (t) : 104.75-114.45) would have precluded the conclusion of bioequivalence. This conclusion cannot be generalized to the active enantiomer (90% CI: Cmax : 103.36-118.38; AUC0 (t) : 96.52-103.12), for which bioequivalence can be concluded, and/or the distomer (90% CI: Cmax : 132.97-151.33; AUC0 (t) : 115.91-135.77) for which a larger difference was observed. Chiral bioanalytical methods should be required when 1) the enantiomers exhibit different pharmacodynamics and 2) the exposure (AUC or Cmax ) ratio of enantiomers is modified by a difference in the rate of absorption. Furthermore, the bioequivalence conclusion should be based on all enantiomers, since the distomer(s) might not be completely inert, in contrast to what is required in the current regulatory guidelines. In those cases where it is unknown if the ratio between enantiomers is modified by changing the rate of absorption, chiral bioanalytical methods should be employed unless enantiomers exhibit the same pharmacodynamics. Chirality 28:429-433, 2016. © 2016 Wiley Periodicals, Inc. © 2016 Wiley Periodicals, Inc.

  7. Preparation and characterization of alginate microspheres for sustained protein delivery within tissue scaffolds

    International Nuclear Information System (INIS)

    Zhai Peng; Chen, X B; Schreyer, David J

    2013-01-01

    Tissue engineering scaffolds are designed not only to provide structural support for the repair of damaged tissue, but can also serve the function of bioactive protein delivery. Here we present a study on the preparation and characterization of protein-loaded microspheres, either alone or incorporated into mock tissue scaffolds, for sustained protein delivery. Alginate microspheres were prepared by a novel, small-scale water-in-oil emulsion technique and loaded with fluorescently labeled immunoglobulin G (IgG). Microsphere size appears to be influenced by the magnitude and distribution of force generated by mechanical stirring during emulsion. Protein release studies show that sustained IgG release from microspheres could be achieved and that application of a secondary coating of chitosan could further slow the rate of protein release. Preservation of bioactivity of released IgG protein was confirmed using an immunohistochemical assay. When IgG-loaded microspheres were incorporated into mock scaffolds, initial protein release was diminished and the overall time course of release was extended. The present study demonstrates that protein-loaded microspheres can be prepared with a controlled release profile and preserved biological activity, and can be incorporated into scaffolds to achieve sustained and prolonged protein delivery in a tissue engineering application. (paper)

  8. Cephradin-plaga microspheres for sustained delivery to cattle.

    Science.gov (United States)

    Ustariz-Peyret, C; Coudane, J; Vert, M; Kaltsatos, V; Boisramé, B

    1999-01-01

    In the field of controlled drug delivery, most of the reported work is aimed at introducing new systems, or at providing basic information on the critical parameters which affect release profiles in vitro and occasionally in vivo. The situation is totally different when one wants to fulfil the specific requirements imposed by the marketing of a sustained release device to be used in humans or in animals eaten by human beings. The control of the release characteristics is then a difficult challenge. In this work, attempts were made to combine cephradin, a hydrophilic beta-lactam antibiotic, and bioresorbable polymeric matrices of a poly(alpha-hydroxy acid) in the form of microspheres with the aim of delivering the antibiotic to cattle at a dose rate of 4-5 mg/kg/day over a 3-4 days period after i.m. injection. PLAGA aliphatic polyesters were selected because they are already FDA approved as matrices. The solvent evaporation technique using PVA as the emulsion stabilizer was selected because it is efficient and can be extended to an industrial scale. Various experimental conditions were used in order to obtain the highest encapsulation yields compatible with the desired specifications. Decreasing the volume of the aqueous phase and adding a water-miscible organic solvent/non-solvent of cephradin failed. In contrast, microspheres containing up to 30% cephradin were prepared after addition of sodium chloride to the aqueous dispersing phase. The amount of entrapped drug was raised to 40% by decreasing the temperature and the pressure. Preliminary investigations using dogs showed that 20% cephradin microspheres prepared under these conditions extended the presence of cephradin in the blood circulation up to 48 h. Increasing the load led to higher blood concentrations but shorter sustained release. The fact that the microspheres were for cattle limited the volume of the injection and thus the amount of microspheres to be administered. The other limiting factors were

  9. Preparation, Characterization and Optimization of Ibuprofen ...

    African Journals Online (AJOL)

    Purpose: To develop an ibuprofen ointment with a potential for both topical and systemic delivery of the drug. Method: A co-solvency technique with a trial and error approach was used to develop a 10% ibioprofen ointment in petrolatum base, with the entire drug dissolved in the base. An insertion cell was used to evaluate ...

  10. Polymer blends used to develop felodipine-loaded hollow microspheres for improved oral bioavailability.

    Science.gov (United States)

    Pi, Chao; Feng, Ting; Liang, Jing; Liu, Hao; Huang, Dongmei; Zhan, Chenglin; Yuan, Jiyuan; Lee, Robert J; Zhao, Ling; Wei, Yumeng

    2018-06-01

    Felodipine (FD) has been widely used in anti-hypertensive treatment. However, it has extremely low aqueous solubility and poor bioavailability. To address these problems, FD hollow microspheres as multiple-unit dosage forms were synthesized by a solvent diffusion evaporation method. Particle size of the hollow microspheres, types of ethylcellulose (EC), amounts of EC, polyvinyl pyrrolidone (PVP) and FD were investigated based on an orthogonal experiment of three factors and three levels. In addition, the release kinetics in vitro and pharmacokinetics in beagle dogs of the optimized FD hollow microspheres was investigated and compared with Plendil (commercial FD sustained-release tablets) as a single-unit dosage form. Results showed that the optimal formulation was composed of EC 10 cp :PVP:FD (0.9:0.16:0.36, w/w). The FD hollow microspheres were globular with a hollow structure and have high drug loading (17.69±0.44%) and floating rate (93.82±4.05%) in simulated human gastric fluid after 24h. Pharmacokinetic data showed that FD hollow microspheres exhibited sustained-release behavior and significantly improved relative bioavailability of FD compared with the control. Pharmacodynamic study showed that the FD hollow microspheres could effectively lower blood pressure. Therefore, these findings demonstrated that the hollow microspheres were an effective sustained-release delivery system for FD. Copyright © 2018 Elsevier B.V. All rights reserved.

  11. Pharmacodynamics of diclofenac from novel Eudragit entrapped microspheres.

    Science.gov (United States)

    Momoh, M A; Kenechukwu, F C; Adedokun, M O; Odo, C E; Attama, A A

    2014-05-01

    Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations. The objective of this study was to evaluate Eudragit® RS100/RL100 microspheres formulated by the solvent-evaporation technique for improved delivery of diclofenac. Three batches of (DF1, DF2 and DF3) microspheres were prepared using different ratios of Eudragit RS-100 and RL-100 polymers based on the solvent-evaporation method. The microspheres were characterized based on morphological properties, particle size analysis and encapsulation efficiency (EE%). In vitro release of DS was investigated in both 0.1 N HCl (pH 1.2) and phosphate-buffered saline (pH 7.4), while anti-inflammatory studies were evaluated in the rat model. Maximum EE% of 86.61 ± 0.11, 88.14 ± 0.16 and 85.50 ± 0.21 was obtained for DF1, DF2 and DF3, respectively. Discrete, smooth and brownish microspheres of size range 437 ± 0.01-479 ± 0.21 µm were obtained. Release of DS from the formulation depends on the polymer ratio. All the batches exhibited good anti-inflammatory activities. Microsphere formulations based on Eudragit® polymers would likely offer a reliable and alternative means of delivering DS orally.

  12. Formulation and evaluation of transparent ibuprofen soft gelatin capsule

    Directory of Open Access Journals (Sweden)

    A Lodha

    2012-01-01

    A medication suitable to combat acute pain is demanded to display its effects fast which action, in turn, is only achieved by a quick release and good bio-availability of the active-ingredient. It is for the commercial forms in particular that the conditions of preparation must be strictly observed, as minor alterations in production procedures such as mixing, pressure of compression and type of machine will affect the physical properties of the particles of he active ingredient and will deteriorate its bio-availability. It is an object of this presentation to provide a medicament that can be readily taken that contains an active amount of ibuprofen in a carrier, that is simple to prepare and that will quickly display a high activity.

  13. Synthesis of magnetic polymeric microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Gervald, A Yu; Gritskova, Inessa A; Prokopov, Nikolai I [M.V. Lomonosov Moscow State Academy of Fine Chemical Technology, Moscow (Russian Federation)

    2010-05-13

    The key types of magnetic polymeric microspheres are considered. Methods of synthesis of different types of magnetic nanoparticles and of preparation of stable magnetic fluids on their basis are outlined. The overview of the methods for the manufacture of magnetic polymeric microspheres is presented. The effect of the synthesis conditions on the characteristics of magnetic polymeric microspheres such as the diameter and the particle size distribution and the content of magnetic material is discussed by particular examples. The application fields of magnetic polymeric microspheres are briefly surveyed.

  14. Synthesis of magnetic polymeric microspheres

    International Nuclear Information System (INIS)

    Gervald, A Yu; Gritskova, Inessa A; Prokopov, Nikolai I

    2010-01-01

    The key types of magnetic polymeric microspheres are considered. Methods of synthesis of different types of magnetic nanoparticles and of preparation of stable magnetic fluids on their basis are outlined. The overview of the methods for the manufacture of magnetic polymeric microspheres is presented. The effect of the synthesis conditions on the characteristics of magnetic polymeric microspheres such as the diameter and the particle size distribution and the content of magnetic material is discussed by particular examples. The application fields of magnetic polymeric microspheres are briefly surveyed.

  15. Temperature and pH Responsive Microfibers for Controllable and Variable Ibuprofen Delivery

    Directory of Open Access Journals (Sweden)

    Toan Tran

    2015-01-01

    Full Text Available Electrospun microfibers (MFs composed of pH and temperature responsive polymers can be used for controllable and variable delivery of ibuprofen. First, electrospinning technique was employed to prepare poly(ε-caprolactone (PCL and poly(N-isopropylacrylamide-co-methacrylic acid (pNIPAM-co-MAA MFs containing ibuprofen. It was found that drug release rates from PCL MFs cannot be significantly varied by either temperature (22–40°C or pH values (1.7–7.4. In contrast, the ibuprofen (IP diffusion rates from pNIPAM-co-MAA MFs were very sensitive to changes in both temperature and pH. The IP release from pNIPAM-co-MAA MFs was highly linear and controllable when the temperature was above the lower critical solution temperature (LCST of pNIPAM-co-MAA (33°C and the pH was lower than the pKa of carboxylic acids (pH 2. At room temperature, however, the release rate was dramatically increased by nearly ten times compared to that at higher temperature and lower pH. Such a unique and controllable drug delivery system could be naturally envisioned to find many practical applications in biomedical and pharmaceutical sciences such as programmable transdermal drug delivery.

  16. Formulation and characterization of ketoprofen embedded polycaprolactone microspheres using solvent evaporation method

    Directory of Open Access Journals (Sweden)

    Pankaj Wagh

    2015-07-01

    Full Text Available The purpose of this study was to prepare polymeric microspheres containing Ketoprofen (KFN by single emulsion [oil-in-water (o/w] solvent evaporation method. Polycaprolactone (PCL, biocompatible polymer, was used for the preparation of sustained released microspheres of KFN. A Plackett–Burman design was employed by using the Design-Expert® software (Version- 9.0.3.1, Stat-Ease Inc., Minneapolis, MN. Eleven factors out of six processing factors were investigated in order to enhance the encapsulation efficiency (EE of the microspheres. The resultant microspheres were characterized for their size, morphology, EE, and drug release. Imaging of particles was performed by field emission scanning electron microscopy. Interaction between the drug and polymers were investigated by Fourier transform infrared (FTIR spectroscopy, X-ray powder diffractometry (XRPD and Differential Scanning Calorimetry (DSC. Graphical and mathematical analyses of the design showed that concentration of factor PCL (B and varying speed (F, revolution per minute, rpm were significant negative effect on the EE and identified as the significant factor determining the EE of the microspheres. The microspheres showed high % EE (31.18 % to 96.81 %. The microspheres were found to be discrete, oval with porous surface. The FTIR analysis confirmed no interaction of KFN with the polymer. The XRPD revealed the dispersion of drug within microspheres formulation. Sustained drug release profile over 12 h was achieved by PCL polymer. In conclusion, polymeric microspheres containing KFN can be successfully prepared using the technique of experimental design, and these results helped in finding the optimum formulation variables for EE of microspheres.

  17. Recombinant Gelatin Microspheres : Novel Formulations for Tissue Repair?

    NARCIS (Netherlands)

    Tuin, Annemarie; Kluijtmans, Sebastiaan G.; Bouwstra, Jan B.; Harmsen, Martin C.; Van Luyn, Marja J. A.

    Microspheres (MSs) can function as multifunctional scaffolds in different approaches of tissue repair (TR), as a filler, a slow-release depot for growth factors, or a delivery vehicle for cells. Natural cell adhesion-supporting extracellular matrix components like gelatin are good materials for

  18. Preparation and Characterization of Sugar Cane Wax Microspheres ...

    African Journals Online (AJOL)

    HP

    scanning calorimetry (DSC) as well as for drug loading, and in vitro and in vivo release in albino sheeps. Results: SEM images .... Rolex, India), and the sphericity factor (S) was calculated using ... using a fully validated high performance liquid ... Pharmacokinetic and data analysis ... microspheres exerts an influence on the.

  19. Formulation and evaluation of matrix microspheres for simultaneous ...

    African Journals Online (AJOL)

    The prepared microspheres were characterized for their micromeritic properties and drug loading, as well as by infrared spectroscopy (IR), differential scanning calorimetry (DSC), x-ray powder diffractometry (XRD) and scanning electron microscopy (SEM). The in vitro release studies were performed in pH 7.4, phosphate ...

  20. Effect of gamma-irradiation on biodegradable microspheres loaded with rasagiline mesylate

    International Nuclear Information System (INIS)

    Fernandez, Marcos; Barcia, Emilia; Negro, Sofia

    2016-01-01

    In the present study, the influence of gamma-irradiation was evaluated on the physicochemical characteristics and in vitro release of rasagiline mesylate (RM), a selective MAO-B inhibitor used in Parkinson's disease, from poly(D,L-lactide-co-glycolide) (PLGA) microspheres. Microspheres were prepared using PLGA 50:50 by the solvent evaporation technique (O/W emulsion). Microspheres were sterilized by gamma-irradiation and their influence was assessed by scanning electron microscopy (SEM), laser light diffraction, differential scanning calorimetry (DSC), X-ray diffraction (XRD), gel permeation chromatography (GPC), encapsulation efficiency (EE) and in vitro drug release. Gamma-irradiation of RM-loaded microspheres did not affect EE, DSC and XRD patterns. After gamma-irradiation, changes on the surface were observed by SEM, but no significant difference in mean particle size was observed. GPC measurements showed a decrease in molecular weight of the polymer after five days of in vitro release. The similarity factor value between irradiated and non-irradiates microspheres was <50, indicating the non-similarity of the release profiles. The sterilization technique had an effect on the integrity of polymeric system, significantly affecting in vitro release of RM from PLGA microspheres. Therefore, from our results we conclude that gamma-irradiation is not a suitable sterilization procedure for this formulation

  1. Development of andrographolide loaded PLGA microspheres: optimization, characterization and in vitro-in vivo correlation.

    Science.gov (United States)

    Jiang, Yunxia; Wang, Fang; Xu, Hui; Liu, Hui; Meng, Qingguo; Liu, Wanhui

    2014-11-20

    The purpose of this study was to develop a sustained-release drug delivery system based on the injectable PLGA microspheres loaded with andrographolide. The andrographolide loaded PLGA microspheres were prepared by emulsion solvent evaporation method with optimization of formulation using response surface methodology (RSM). Physicochemical characterization, in vitro release behavior and in vivo pharmacokinetics of the optimized formulation were then evaluated. The percent absorbed in vivo was determined by deconvolution using the Loo-Riegelman method, and then the in vitro-in vivo correlation (IVIVC) was established. Results showed that the microspheres were spherical with a smooth surface. Average particle size, entrapment efficiency and drug loading were found to be 53.18±2.11 μm, 75.79±3.02% and 47.06±2.18%, respectively. In vitro release study showed a low initial burst release followed by a prolonged release up to 9 days and the release kinetics followed the Korsmeyer-Peppas model. After a single intramuscular injection, the microspheres maintained relatively high plasma concentration of andrographolide over one week. A good linear relationship was observed between the in vitro and in vivo release behavior (R(2)=0.9951). These results suggest the PLGA microspheres could be developed as a potential delivery system for andrographolide with high drug loading capacity and sustained drug release. Copyright © 2014 Elsevier B.V. All rights reserved.

  2. The tritium labelling of ibuprofen by heterogeneous catalytic exchange

    International Nuclear Information System (INIS)

    Santamaria, J.; Rebollo, D.V.; Rivera, P.; Estaban, M.

    1986-01-01

    The tritium labelling of 2-(4-isobutylphenyl) propionic acid (ibuprofen) was performed. The method employed was heterogeneous catalytic exchange between ibuprofen and tritiated water. Prior to labelling, thermic stability of ibuprofen was studied. Purification was accomplished through thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Concentration, purity and specific activity of the labelled compound were determined by ultraviolet, HPLC and liquid scintillation techniques. (author)

  3. Calcium carbonate microspheres as carriers for the anticancer drug camptothecin

    Energy Technology Data Exchange (ETDEWEB)

    Qiu, Neng [Division of Biomedical Engineering, School of Engineering, University of Glasgow, Glasgow, G12 8LT (United Kingdom); State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041 (China); Department of Bio-pharmaceutical Engineering, School of Chemical Engineering, Sichuan University, Chengdu ,610065 (China); Yin, Huabing, E-mail: huabing.yin@glasgow.ac.uk [Division of Biomedical Engineering, School of Engineering, University of Glasgow, Glasgow, G12 8LT (United Kingdom); Ji, Bozhi; Klauke, Norbert; Glidle, Andrew [Division of Biomedical Engineering, School of Engineering, University of Glasgow, Glasgow, G12 8LT (United Kingdom); Zhang, Yongkui; Song, Hang [Department of Bio-pharmaceutical Engineering, School of Chemical Engineering, Sichuan University, Chengdu ,610065 (China); Cai, Lulu; Ma, Liang; Wang, Guangcheng [State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041 (China); Chen, Lijuan, E-mail: lijuan17@hotmail.com [State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041 (China); Wang, Wenwen [State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041 (China)

    2012-12-01

    Biogenic calcium carbonate has come to the attention of many researchers as a promising drug delivery system due to its safety, pH sensitivity and the large volume of information already in existence on its medical use. In this study, we employed bovine serum albumin (BSA) as an additive to synthesize a series of porous calcium carbonate microspheres (CCMS). These spheres, identified as vaterite, are stable both in aqueous solutions and organic solvents. Camptothecin, an effective anticancer agent, was loaded into the CCMS by simple diffusion and adsorption. The camptothecin loaded CCMS showed sustained cell growth inhibitory activity and a pH dependent release of camptothecin. With a few hours, the release is negligible under physiological conditions (pH = 7.4) but almost complete at pH 4 to 6 (i.e. pHs found in lysosomes and solid tumor tissue respectively). These findings suggest that porous, biogenic calcium carbonate microspheres could be promising carriers for the safe and efficient delivery of anticancer drugs of low aqueous solubility. - Highlights: Black-Right-Pointing-Pointer BSA-doped calcium carbonate microspheres with porous structure were prepared. Black-Right-Pointing-Pointer Camptothecin was encapsulated in the spherical microparticles with encapsulation efficiency up to 11%. Black-Right-Pointing-Pointer The release of encapsulated camptothecin is pH dependent Black-Right-Pointing-Pointer In vitro studies showed an effective anticancer activity of the camptothecin- microspheres.

  4. Ibuprofen regulation of microtubule dynamics in cystic fibrosis epithelial cells.

    Science.gov (United States)

    Rymut, Sharon M; Kampman, Claire M; Corey, Deborah A; Endres, Tori; Cotton, Calvin U; Kelley, Thomas J

    2016-08-01

    High-dose ibuprofen, an effective anti-inflammatory therapy for the treatment of cystic fibrosis (CF), has been shown to preserve lung function in a pediatric population. Despite its efficacy, few patients receive ibuprofen treatment due to potential renal and gastrointestinal toxicity. The mechanism of ibuprofen efficacy is also unclear. We have previously demonstrated that CF microtubules are slower to reform after depolymerization compared with respective wild-type controls. Slower microtubule dynamics in CF cells are responsible for impaired intracellular transport and are related to inflammatory signaling. Here, it is identified that high-dose ibuprofen treatment in both CF cell models and primary CF nasal epithelial cells restores microtubule reformation rates to wild-type levels, as well as induce extension of microtubules to the cell periphery. Ibuprofen treatment also restores microtubule-dependent intracellular transport monitored by measuring intracellular cholesterol transport. These effects are specific to ibuprofen as other cyclooxygenase inhibitors have no effect on these measures. Effects of ibuprofen are mimicked by stimulation of AMPK and blocked by the AMPK inhibitor compound C. We conclude that high-dose ibuprofen treatment enhances microtubule formation in CF cells likely through an AMPK-related pathway. These findings define a potential mechanism to explain the efficacy of ibuprofen therapy in CF. Copyright © 2016 the American Physiological Society.

  5. Ibuprofen plus paracetamol versus ibuprofen in acute low back pain: a randomized open label multicenter clinical study.

    Science.gov (United States)

    Ostojic, Predrag; Radunovic, Goran; Lazovic, Milica; Tomanovic-Vujadinovic, Sanja

    2017-01-01

    to estimate whether combination of ibuprofen and paracetamol is more effective than ibuprofen in monotherapy, in the treatment of acute low back pain. 80 adult patients with acute low back pain were randomized into two subgroups. In the first subgroup, 40 patients were treated with ibuprofen 400mg three times a day (TID), whilst patients in the second subgroup (n=40) were treated with a fixed-dose combination tablet of ibuprofen 200mg plus paracetamol 325mg TID, for three consecutive days. Patients were followed for another 7 days. Efficacy and tolerability of both treatment options was assessed. A statistically significant decrease in pain intensity, assessed using a visual analogue scale (pibuprofen monotherapy reported minor gastric intolerability. compared to ibuprofen monotherapy, combination of ibuprofen and paracetamol may provide faster and longer analgesia in patients with acute low back pain, with equally favorable effect on mobility and functional ability and similar tolerability.

  6. A review on target drug delivery: magnetic microspheres

    Directory of Open Access Journals (Sweden)

    Amit Chandna

    2013-01-01

    Magnetic microsphere is newer approach in pharmaceutical field. Magnetic microspheres as an alternative to traditional radiation methods which use highly penetrating radiation that is absorbed throughout the body. Its use is limited by toxicity and side effects. The aim of the specific targeting is to enhance the efficiency of drug delivery & at the same time to reduce the toxicity & side effects. This kind of delivery system is very much important which localises the drug to the disease site. In this larger amount of freely circulating drug can be replaced by smaller amount of magnetically targeted drug. Magnetic carriers receive magnetic responses to a magnetic field from incorporated materials that are used for magnetic microspheres are chitosan, dextran etc. magnetic microspheres can be prepared from a variety of carrier material. One of the most utilized is serum albumin from human or other appropriate species. Drug release from albumin microspheres can be sustained or controlled by various stabilization procedures generally involving heat or chemical cross-linking of the protein carrier matrix.

  7. Preparation and Comparative Bioavailability Studies of Indomethacin-Loaded Cetyl Alcohol Microspheres

    Directory of Open Access Journals (Sweden)

    N. Vishal Gupta

    2013-01-01

    Full Text Available The purpose of the present study was to compare the in vitro release and to find out whether the bioavailability of a 75 mg indomethacin capsule (Microcid SR was equivalent to optimized formulation (indomethacin-loaded cetyl alcohol microspheres. Indomethacin-loaded cetyl alcohol microspheres were prepared by meltable emulsified cooling-induced technique. Surface morphology of microspheres has been evaluated using scanning electron microscopy. A single dose, randomized, complete cross over study of IM microspheres was carried out on 10 healthy male and female Albino sheep’s under fasting conditions. The plasma was separated and the concentrations of the drug were determined by HPLC-UV method. Plasma indomethacin concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The SEM images revealed the spherical shape of fat microspheres, and more than 98.0% of the isolated microspheres were in the size range 12–32 μm. DSC, FTIR spectroscopy and stability studies indicated that the drug after encapsulation with fat microspheres was stable and compatible. Both formulations were found to be bioequivalent as evidenced by in vivo studies. Based on this study, it can be concluded that cetyl alcohol microspheres and Microcid SR capsule are bioequivalent in terms of the rate and extent of absorption.

  8. Preparation of grafted microspheres CPVA-g-PSSS and studies on their drug-carrying and colon-specific drug delivery properties

    International Nuclear Information System (INIS)

    Gao, Baojiao; Fang, Li; Men, Jiying; Zhang, Yanyan

    2013-01-01

    Sodium 4-styrene sulfonate (SSS) was graft-polymerized on the surfaces of crosslinked polyvinyl alcohol (CPVA) microspheres in a manner of surface-initiated graft-polymerization by using cerium salt-hydroxyl group redox initiation system, obtaining the grafted microspheres CPVA-g-PSSS. The chemical structure and physicochemical characters of CPVA-g-PSSS microspheres were fully characterized with infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and zeta potential determination. The aim of this work is to constitute a novel colon-specific drug delivery system via molecular design by using CPVA-g-PSSS microspheres as the drug-carrying material and by taking metronidazole (MTZ) as the model drug. The drug-carrying ability and mechanism of the grafted microspheres CPVA-g-PSSS for MTZ were investigated. Finally, in-vitro release tests for the drug-carrying microspheres were conducted. The experimental results show that in an acidic medium, the grafted microspheres CPVA-g-PSSS exhibit strong adsorption ability for MTZ by driving of electrostatic interaction, and have an adsorption capacity of 112 mg/g, displaying the high efficiency of drug-carrying. The in-vitro release behavior of the drug-carried microspheres is highly pH-sensitive. In the medium of pH = 1, the drug-carrying microspheres do not release the drug, whereas in the medium of pH = 7.4, a sudden delivery phenomenon of the drug will occur, displaying an excellent colon-specific drug delivery behavior. Highlights: ► A metronidazole colon-specific drug delivery was constituted using grafted polymeric microspheres. ► Grafted polymeric microspheres CPVA-g-PSSS were prepared via surface-initiated graft-polymerization. ► The release of the drug-carrying microspheres is highly pH-sensitive. ► The drug-carrying microspheres display an excellent colon-specific drug delivery behavior

  9. Preparation of grafted microspheres CPVA-g-PSSS and studies on their drug-carrying and colon-specific drug delivery properties

    Energy Technology Data Exchange (ETDEWEB)

    Gao, Baojiao, E-mail: gaobaojiao@126.com [Department of Chemical Engineering, North University of China, Taiyuan 030051, People' s Republic of China (China); Fang, Li [School of Chemistry and Chemical engineering, Shanxi University, Taiyuan 030006 (China); Men, Jiying; Zhang, Yanyan [Department of Chemical Engineering, North University of China, Taiyuan 030051, People' s Republic of China (China)

    2013-04-01

    Sodium 4-styrene sulfonate (SSS) was graft-polymerized on the surfaces of crosslinked polyvinyl alcohol (CPVA) microspheres in a manner of surface-initiated graft-polymerization by using cerium salt-hydroxyl group redox initiation system, obtaining the grafted microspheres CPVA-g-PSSS. The chemical structure and physicochemical characters of CPVA-g-PSSS microspheres were fully characterized with infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and zeta potential determination. The aim of this work is to constitute a novel colon-specific drug delivery system via molecular design by using CPVA-g-PSSS microspheres as the drug-carrying material and by taking metronidazole (MTZ) as the model drug. The drug-carrying ability and mechanism of the grafted microspheres CPVA-g-PSSS for MTZ were investigated. Finally, in-vitro release tests for the drug-carrying microspheres were conducted. The experimental results show that in an acidic medium, the grafted microspheres CPVA-g-PSSS exhibit strong adsorption ability for MTZ by driving of electrostatic interaction, and have an adsorption capacity of 112 mg/g, displaying the high efficiency of drug-carrying. The in-vitro release behavior of the drug-carried microspheres is highly pH-sensitive. In the medium of pH = 1, the drug-carrying microspheres do not release the drug, whereas in the medium of pH = 7.4, a sudden delivery phenomenon of the drug will occur, displaying an excellent colon-specific drug delivery behavior. Highlights: ► A metronidazole colon-specific drug delivery was constituted using grafted polymeric microspheres. ► Grafted polymeric microspheres CPVA-g-PSSS were prepared via surface-initiated graft-polymerization. ► The release of the drug-carrying microspheres is highly pH-sensitive. ► The drug-carrying microspheres display an excellent colon-specific drug delivery behavior.

  10. Liberação controlada da eosina impregnada em microesferas de copolímero de quitosana e poli(ácido acrílico Controlled release of eosin impregnated in microspheres of chitosan/poly(acrylic acid copolymer

    Directory of Open Access Journals (Sweden)

    Atche Josué

    2000-09-01

    Full Text Available Microesferas de quitosana com grau de desacetilação médio de 85,6% foram enxertadas com poli(ácido acrílico para aplicação como sistemas de liberação controlada de fármacos. O corante eosina impregnado nas microesferas de quitosana modificada foi utilizado como marcador para estudo in vitro de liberação de fármacos. As microesferas de quitosana foram obtidas pelo método de inversão de fases com NaOH, seguidas de reticulação com glutaraldeído, redução com cianoboroidreto de sódio e enxertia com poli(ácido acrílico na presença de uma solução de nitrato de cério (IV amoniacal como iniciador redox. Os estudos in vitro de liberação da eosina a partir de microesferas de quitosana, mostraram que o corante foi liberado em função do tempo a pH 6,8 e 9,8 que simulam as condições fisiológicas do trato gastrointestinal, enquanto que nenhuma eosina foi liberada a pH 1,2.Chitosan microspheres obtained by coacervation-phase separation, cross-linked with glutaraldehyde and grafted with poly(acrylic acid were used as the basis of in vitro studies on the controlled release of eosin. Microspheres impregnated with an aqueous solution of the dye depicted a time-dependent release of eosin at pH values of 6.8 and 9.8, typical of the gastrointestinal tract. No eosin release could be observed at 1.2 pH.

  11. Preparation of novel biodegradable ropivacaine microspheres and evaluation of their efficacy in sciatic nerve block in mice

    Directory of Open Access Journals (Sweden)

    Ni Q

    2016-08-01

    Full Text Available Qiang Ni, Wurong Chen, Lei Tong, Jue Cao, Chao Ji Department of Anesthesiology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of China Abstract: In this study, ropivacaine chitosan-loaded microspheres for subcutaneous administration were developed. The systems were characterized in terms of surface morphology, particle size, encapsulation efficiency, and in vitro release behavior. Results showed that the microspheres had drug loading rate of 7.3% and encapsulation efficiency of 91.2%, and their average diameter was 2.62±0.76 µm. The morphology study revealed that the microspheres are uniform monodispersed spheres and did not form aggregates in aqueous solution. It was clearly observed that the release profile of ropivacaine microspheres exhibited a biphasic pattern: the initial burst release within the first 2 hours and a following slower and sustained release over a long time. In vivo, a greater area under the plasma concentration–time curve from 0 to t (AUC0–t was obtained from the microspheres (4.27-fold, than from the injection group, which indicated that there was a significantly improved systemic exposure to ropivacaine. Pharmacodynamics result showed that preparing ropivacaine as microsphere preparation could not only extend the drug effect time but also decrease the administration dosage. Keywords: ropivacaine, chitosan, microspheres, in vitro release, pharmacodynamics

  12. Development and in vitro evaluation of diclofenac sodium loaded mucoadhesive microsphere with natural gum for sustained delivery.

    Science.gov (United States)

    Amin, Md Lutful; Jesmeen, Tasbira; Sutradhar, Kumar Bishwajit; Mannan, Md Abdul

    2013-12-01

    The objective of this study was to develop and evaluate mucoadhesive microsphere of diclofenac sodium with natural gums for sustained delivery. Guar gum and tragacanth were used along with sodium alginate as mucoadhesive polymers. Microspheres were formulated using orifice-ionic gelation method. Particle size, surface morphology, swelling study and drug entrapment efficiency of the prepared microspheres were determined. In vitro evaluation was carried out comprising of mucoadhesion and drug release study. The prepared microspheres were discrete and free flowing. Sodium alginate and natural gum, at a ratio of 1:0.25, showed good mucoadhesive property and they had high drug entrapment efficiencies. They also exhibited the best rate retarding effect among all the formulations. Drug entrapment efficiency of all the microspheres ranged from 80.42% to 91.67%. An inverse relationship was found between extent of crosslinking and drug release rate. Release rate was slow and extended in case of the formulations of 1:0.25 ratio (F1 and F3), releasing 68.36% and 70.56% drug respectively after 8 hours. Tragacanth-containing microspheres of F1 showed superiority over other formulations, with best mucoadhesive and rate retarding profile. The correlation value (r(2)) indicated that the drug release of all the formulations followed Higuchi's model. Overall, the results indicated that mucoadhesive microspheres containing natural gum can be promising in terms of prolonged delivery with good mucoadhesive action, targeting the absorption site to thrive oral drug delivery.

  13. In-vitro studies of enteric coated diclofenac sodium-carboxymethylcellulose microspheres.

    Science.gov (United States)

    Arica, B; Arica, M Y; Kaş, H S; Hincal, A A; Hasirci, V

    1996-01-01

    MIcrospheres containing diclofenac sodium (DS) were prepared using carboxymethylcellulose (CMC) as the main support material (1.0, 2.0, 3.0% (w/v)) and aluminum chloride as the crosslinker. Drug to polymer ratios of 1:1, 1:2 and 1:4 were used to obtain a range of microspheres. The microspheres were then coated with an enteric coating material, Eudragit S-100, efficiency, % yield value, particle sizes an in-vitro dissolution behaviour were investigated. The surface of the enteric coated microspheres seemed to be all covered with Eudragit S-100 from scanning electron microscopy observation. It was also observed that increasing the CMC concentration led to an increase in the encapsulation efficiency, % yield value and particle size and decreased the release rate. Eudragit S-100 coating did not significantly alter the size but the release rate was significantly lower even when the lower concentration solution was used.

  14. Review: microspheres for radioembolization therapy

    International Nuclear Information System (INIS)

    Zhao Mingqiang; Xu Shuhe

    2007-12-01

    Radioembolization of liver cancer has been proven to be an effective therapy in nuclear medicine. The yttrium-90 glass microspheres has been used to treat both primary and metastatic liver tumors in clinic which shown encouraging results. The preparation, stability, degradation and application for medical purpose of radioactive microspheres are reviewed. At first, the theory of radioem- bolization treating cancer is discussed; and then three major radiolabled micro- sphere materials are expounded: viz. glass, resin-based and polymer-based; Future improvements in the preparation and use of radioactive microspheres are prospected at last. (authors)

  15. Review: microspheres for radioembolization therapy

    Energy Technology Data Exchange (ETDEWEB)

    Mingqiang, Zhao; Shuhe, Xu [China Inst. of Atomic Energy, Beijing (China)

    2007-12-15

    Radioembolization of liver cancer has been proven to be an effective therapy in nuclear medicine. The yttrium-90 glass microspheres has been used to treat both primary and metastatic liver tumors in clinic which shown encouraging results. The preparation, stability, degradation and application for medical purpose of radioactive microspheres are reviewed. At first, the theory of radioem- bolization treating cancer is discussed; and then three major radiolabled micro- sphere materials are expounded: viz. glass, resin-based and polymer-based; Future improvements in the preparation and use of radioactive microspheres are prospected at last. (authors)

  16. Formulation, characterization and in vitro evaluation of theophylline-loaded Eudragit RS 100 microspheres prepared by an emulsion-solvent diffusion/evaporation technique.

    Science.gov (United States)

    Jelvehgari, Mitra; Barar, Jaleh; Valizadeh, Hadi; Shadrou, Sanam; Nokhodchi, Ali

    2011-01-01

    The aim was to prepare theophylline-loaded Eudragit RS 100 microsphere to achieve sustained release pattern with relatively high production yield. To this end, microspheres were prepared by oil/oil solvent evaporation method using an acetone-methanol mixture and liquid paraffin system containing aluminum tristearate. Drug release profiles were determined at pH 1.2 and 7.4. Morphology and solid state of microspheres were examined using SEM, DSC, X-ray powder diffraction (XRPD), and FT-IR. As the ratio of acetone/methanol increased during the preparation of microspheres the size of microsphere was reduced. The highest drug loading efficiency (87.21%) was obtained for the microsphere containing a high ratio of polymer to drug (6:1) and high volume of acetone. SEM studies showed that the microspheres are almost spherical with a few pores and cracks at surfaces. The FT-IR, XRPD and DSC results ruled out any chemical interaction between theophylline and Eudragit. The microspheres prepared with low ratio of polymer to drug (1:2) showed faster dissolution rate than those with high polymer to drug ratio. The ratio of polymer to drug and the volume of polymer solvent were found to be the key factors affecting the release profile which could lead to microspheres with desired release behavior.

  17. Mucoadhesive microspheres: a promising tool in drug delivery.

    Science.gov (United States)

    Patil, Sanjay B; Sawant, Krutika K

    2008-10-01

    Mucoadhesive polymers have recently gained interest among pharmaceutical scientists as a means of improving drug delivery by promoting the residence time and contact time of the dosage form with the mucous membranes. Mucoadhesion is the process whereby synthetic and natural polymers adhere to mucosal surfaces in the body. If these materials are then incorporated into pharmaceutical formulations, drug absorption by mucosal cells may be enhanced or the drug will be released at the site for an extended period of time. Microspheres, in general, have the potential to be used for targeted and controlled release drug delivery; however, coupling of mucoadhesive properties to microspheres has additional advantages like, a much more intimate contact with the mucus layer, efficient absorption and enhanced bioavailability of the drugs due to a high surface to volume ratio. The present review describes the potential applications of mucoadhesive microspheres as a novel carrier system to improve drug delivery by various routes of administration like buccal, oral, nasal, ocular, vaginal and rectal, either for systemic or for local effects. The mucoadhesive polymers, methods of preparation of microspheres and their in vitro and in vivo evaluation are also described.

  18. Effect Of Formulating Additives On The Properties Of Ibuprofen Tablets

    African Journals Online (AJOL)

    A study of the comparative effects of different formulating additives and film coating on the properties of ibuprofen tablets was made. The tested properties were hardeness (H), friability (F), the disintegration time (D) and dissolution characteristics of ibuprofen tablets. The hardeness, friability, the hardeness friability ratio ...

  19. Ibuprofen pharmacokinetics in preterm infants with patent ductus arteriosus

    NARCIS (Netherlands)

    Van Overmeire, B; Touw, D; Schepens, P J; Kearns, G L; van den Anker, J N

    2001-01-01

    OBJECTIVE: Our objective was to study the pharmacokinetics of ibuprofen in premature infants with patent ductus arteriosus on day 3 and day 5 after birth. METHODS: Ibuprofen was administered on days 3, 4, and 5 by a 15-minute intravenous infusion of 10, 5, and 5 mg/kg, respectively, with the aim of

  20. Polyuria, acidosis, and coma following massive ibuprofen ingestion.

    Science.gov (United States)

    Levine, Michael; Khurana, Amandeep; Ruha, Anne-Michelle

    2010-09-01

    Ibuprofen was the first over-the-counter nonsteroidal anti-inflammatory drug available in the United States. Despite being a common agent of ingestion, significant toxicity in overdose is rare. We report a case of a massive ibuprofen ingestion who developed polyuria, acidosis, and coma but survived, despite having a serum ibuprofen concentration greater than previous fatal cases. A 19-year-old man ingested 90 g (1,200 mg/kg) ibuprofen. He was initially awake and alert, but his level of consciousness deteriorated over several hours. Seven hours following the ingestion, he was intubated and mechanically ventilated secondary to loss of airway reflexes. He developed a lactic acidosis and polyuria, which lasted for nearly 24 h. His serum creatinine peaked at 1.12 mg/dL. An ibuprofen level drawn 7 h postingestion was 739.2 mg/L (therapeutic 5-49 mg/L). We describe a case of a massive ibuprofen overdose characterized by metabolic acidosis, coma, and a state of high urine output who survived with aggressive supportive care. This case is unique in several ways. First, ibuprofen levels this high have only rarely been described. Second, polyuria is very poorly described following ibuprofen ingestions.

  1. Fulvic Acid Mediated Photolysis of Ibuprofen in Water.

    Science.gov (United States)

    Photolysis of the nonsteroidal anti-inflammatory drug ibuprofen was studied in solutions of fulvic acid (FA) isolated from Pony Lake, Antarctica; Suwannee River, GA, USA; and Old Woman Creek, OH, USA. At an initial concentration of 10 µM ibuprofen degrades by direct photolysis...

  2. Biodegradable polymeric microsphere-based drug delivery for inductive browning of fat

    Directory of Open Access Journals (Sweden)

    Chunhui eJiang

    2015-11-01

    Full Text Available Brown and beige adipocytes are potent therapeutic agents to increase energy expenditure and reduce risks of obesity and its affiliated metabolic symptoms. One strategy to increase beige adipocyte content is through inhibition of the evolutionarily conserved Notch signaling pathway. However, systemic delivery of Notch inhibitors is associated with off-target effects and multiple dosages of application further faces technical and translational challenges. Here, we report the development of a biodegradable polymeric microsphere-based drug delivery system for sustained, local release of a Notch inhibitor, DBZ. The microsphere-based delivery system was fabricated and optimized using an emulsion/solvent evaporation technique to encapsulate DBZ into poly(lactide-co-glycolide (PLGA, a commonly used biodegradable polymer for controlled drug release. Release studies revealed the ability of PLGA microspheres to release DBZ in a sustained manner. Co-culture of white adipocytes with and without DBZ-loaded PLGA microspheres demonstrated that the released DBZ retained its bioactivity, and effectively inhibited Notch and promoted browning of white adipocytes. Injection of these DBZ-loaded PLGA microspheres into mouse inguinal white adipose tissue (WAT depots resulted in browning in vivo. Our results provide the encouraging proof-of-principle evidence for the application of biodegradable polymers as a controlled release platform for delivery of browning factors, and pave the way for development of new translational therapeutic strategies for treatment of obesity.

  3. Development and evaluation of intestinal targeted mucoadhesive microspheres of Bacillus coagulans.

    Science.gov (United States)

    Alli, Sk Md Athar; Ali, Sk Md Ajhar; Samanta, Amalesh

    2011-11-01

    Intestinal targeted mucoadhesive microsphere of probiotics may provide numerous associated health benefits. To develop mucoadhesive microspheres that will deliver viable probiotic cells into gut protectively against harsh environmental conditions of stomach for extended period. Core mucoadhesive microspheres of Bacillus coagulans were prepared using hypromellose, following coacervation and phase separation technique and were then coated with hypromellose phthalate to achieve their site-specific release. Microspheres were evaluated for percent yield, entrapment efficiency, surface morphology, particle size and size distribution, flow property, swelling property, mucoadhesion property by the in vitro wash-off and the ex vivo mucoadhesive strength tests, in vitro release profile and release kinetic, in vivo probiotic activity, and stability. The values for kinetic constant and regression coefficient of model-dependent approaches and the difference factor, the similarity factor, and the Rescigno index of model-independent approaches were determined for accessing and comparing in vitro performance. Microsphere formulation batches have percent yield value between 56.26% and 69.13% and entrapment efficiency value between 66.95% and 77.89%. Microspheres were coarser with spherical shape having mean particle size from 28.03 to 48.31 μm. In vitro B. coagulans release profile follows zero-order kinetics and depends on the grade of hypromellose and the B. coagulans-to-hypromellose ratio. Experimental microspheres rendered adequate stability to B. coagulans at room temperature. Microspheres had delivered B. coagulans in simulated intestinal condition following zero-order kinetics, protectively in simulated gastric condition, exhibiting appreciable mucoadhesion in intestinal condition, which could be useful to achieve site-specific delivery for extended period.

  4. [Preparation of citrulline microspheres by spray drying technique for colonic targeting].

    Science.gov (United States)

    Bahri, S; Zerrouk, N; Lassoued, M-A; Tsapis, N; Chaumeil, J-C; Sfar, S

    2014-03-01

    Citrulline is an amino acid that becomes essential in situations of intestinal insufficiency such as short bowel syndrome. It is therefore interesting to provide the patients with dosage forms for routing citrulline to the colon. The aim of this work is to formulate microspheres of citrulline for colonic targeting by the technique of spray drying. Eudragit(®) FS 30D was selected as polymer to encapsulate citrulline using the spray drying technique. Citrulline and Eudragit(®) FS 30D were dissolved in water and ethanol, respectively. The aqueous and the ethanolic solutions were then mixed in 1:2 (v/v) ratio. Microspheres were obtained by nebulizing the citrulline-Eudragit(®) FS 30D solution using a Mini spray dryer equipped with a 0.7mm nozzle. The microspheres have been formulated using citrulline and Eudragit(®) FS 30D. The size distribution of microspheres was determined by light diffraction. The morphology of the microspheres was studied by electron microscopy. Manufacturing yields, encapsulation rate and dissolution profiles were also studied. The microspheres obtained had a spherical shape with a smooth surface and a homogeneous size except for the microspheres containing the highest concentration of polymer (90 %). The formulation showed that the size and morphology of the microspheres are influenced by the polymer concentration. Manufacturing yields were about 51 % but encapsulation rate were always very high (above 90 %). The in vitro dissolution study showed that the use of the Eudragit(®) FS 30D under these conditions is not appropriate to change the dissolution profile of the citrulline. This technique has led to the formulation of microspheres with good physical properties in terms of morphology and size. The compression of the microspheres should help to control citrulline release for colonic targeting. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  5. Development of lovastatin-loaded poly(lactic acid microspheres for sustained oral delivery: in vitro and ex vivo evaluation

    Directory of Open Access Journals (Sweden)

    Guan QG

    2015-02-01

    Full Text Available Qigang Guan,1 Wei Chen,2 Xianming Hu2 1Department of Cardiology, The First Affiliated Hospital of China Medical University, Shenyang, People’s Republic of China; 2Department of Pharmaceutical, Shenyang Institute of Pharmaceutical Industry, Shenyang, People’s Republic of China Background: A novel lovastatin (LVT-loaded poly(lactic acid microsphere suitable for oral administration was developed in this study, and in vitro and in vivo characteristics were evaluated. Methods: The designed microspheres were obtained by an improved emulsion-solvent evaporation method. The morphological examination, particle size, encapsulation ratio, drug loading, and in vitro release were characterized. Pharmacokinetics studies were used to show that microspheres possess more advantages than the conventional formulations. Results: By using the emulsion-solvent evaporation method, it was simple to prepare microspheres and easy to scale up production. The morphology of formed microspheres showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the microspheres was 2.65±0.69 µm; the encapsulation efficiency was 92.5%±3.6%, and drug loading was 16.7%±2.1%. In vitro release indicated that the LVT microspheres had a well-sustained release efficacy, and ex vivo studies showed that after LVT was loaded to microspheres, the area under the plasma concentration-time curve from zero to the last measurable plasma concentration point and the extrapolation to time infinity increased significantly, which represented 2.63-fold and 2.49-fold increases, respectively, compared to suspensions. The rate of ex vivo clearance was significantly reduced. Conclusion: This research proved that poly(lactic acid microspheres can significantly prolong the drug circulation time in vivo and can also significantly increase the relative bioavailability of the drug. Keywords: lovastatin, microspheres, PLA, in vitro release, pharmacokinetics 

  6. Formulation and Evaluation of Microsphere Based Oro Dispersible Tablets of Itopride Hcl

    Directory of Open Access Journals (Sweden)

    S.S Agrawal

    2012-09-01

    Full Text Available Background The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing.Methods:With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. Results:The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8 and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. ConclusionsEffective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  7. Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl

    Directory of Open Access Journals (Sweden)

    Shah Sanjay

    2012-09-01

    Full Text Available Abstract Background The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing. Methods With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. Results The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8 and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. Conclusions Effective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  8. Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl.

    Science.gov (United States)

    Shah, Sanjay; Madan, Sarika; Agrawal, Ss

    2012-09-03

    The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT) of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing. With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8) and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. Effective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

  9. Bioactive apatite incorporated alginate microspheres with sustained drug-delivery for bone regeneration application

    Energy Technology Data Exchange (ETDEWEB)

    Li, Haibin; Jiang, Fei; Ye, Song; Wu, Yingying; Zhu, Kaiping; Wang, Deping, E-mail: wdpshk@tongji.edu.cn

    2016-05-01

    The strontium-substituted hydroxyapatite microspheres (SrHA) incorporated alginate composite microspheres (SrHA/Alginate) were prepared via adding SrHA/alginate suspension dropwise into calcium chloride solution, in which the gel beads were formed by means of crosslinking reaction. The structure, morphology and in vitro bioactivity of the composite microspheres were studied by using XRD, SEM and EDS methods. The biological behaviors were characterized and analyzed through inductively coupled plasma optical emission spectroscopy (ICP-OES), CCK-8, confocal laser microscope and ALP activity evaluations. The experimental results indicated that the synthetic SrHA/Alginate showed similar morphology to the well-known alginate microspheres (Alginate) and both of them possessed a great in vitro bioactivity. Compared with the control Alginate, the SrHA/Alginate enhanced MC3T3-E1 cell proliferation and ALP activity by releasing osteoinductive and osteogenic Sr ions. Furthermore, vancomycin was used as a model drug to investigate the drug release behaviors of the SrHA/Alginate, Alginate and SrHA. The results suggested that the SrHA/Alginate had a highest drug-loading efficiency and best controlled drug release properties. Additionally, the SrHA/Alginate was demonstrated to be pH-sensitive as well. The increase of the pH value in phosphate buffer solution (PBS) accelerated the vancomycin release. Accordingly, the multifunctional SrHA/Alginate can be applied in the field of bioactive drug carriers and bone filling materials. - Highlights: • The pH-sensitive composite alginate beads incorporating Sr-doped HA microspheres (SrHA) have been prepared. • The incorporation of the SrHA enhanced the drug loading and release properties of the alginate microspheres. • The composite microspheres showed excellent osteogenic effect by releasing osteogenic Sr ions.

  10. Serum ibuprofen levels of extremely preterm infants treated prophylactically with oral ibuprofen to prevent patent ductus arteriosus

    NARCIS (Netherlands)

    Kanmaz, Gozde; Erdeve, Omer; Canpolat, Fuat Emre; Oguz, Serife Suna; Uras, Nurdan; Altug, Nahide; Greijdanus, Ben; Dilmen, Ugur

    The aim of this study was to explore the effects of early oral ibuprofen administration on the incidence of hemodynamically significant patent ductus arteriosus (hsPDA) and define the association between serum ibuprofen levels and ductal closure. Preterm infants with a gestational age of <28 weeks

  11. IVIVC from Long Acting Olanzapine Microspheres

    Directory of Open Access Journals (Sweden)

    Susan D'Souza

    2014-01-01

    Full Text Available In this study, four PLGA microsphere formulations of Olanzapine were characterized on the basis of their in vitro behavior at 37°C, using a dialysis based method, with the goal of obtaining an IVIVC. In vivo profiles were determined by deconvolution (Nelson-Wagner method and using fractional AUC. The in vitro and in vivo release profiles exhibited the same rank order of drug release. Further, in vivo profiles obtained with both approaches were nearly superimposable, suggesting that fractional AUC could be used as an alternative to the Nelson-Wagner method. A comparison of drug release profiles for the four formulations revealed that the in vitro profile lagged slightly behind in vivo release, but the results were not statistically significant (P0.96 between in vitro release and in vivo measurements confirmed the excellent relationship between in vitro drug release and the amount of drug absorbed in vivo. The results of this study suggest that proper selection of an in vitro method will greatly aid in establishing a Level A IVIVC for long acting injectables.

  12. Microspheres for protein delivery prepared from amphiphilic multiblock copolymers. 1. Influence of preparation techniques on particle characteristics and protein delivery.

    Science.gov (United States)

    Bezemer, J M; Radersma, R; Grijpma, D W; Dijkstra, P J; van Blitterswijk, C A; Feijen, J

    2000-07-03

    The entrapment of lysozyme in amphiphilic multiblock copolymer microspheres by emulsification and subsequent solvent removal processes was studied. The copolymers are composed of hydrophilic poly(ethylene glycol) (PEG) blocks and hydrophobic poly(butylene terephthalate) (PBT) blocks. Direct solvent extraction from a water-in-oil (w/o) emulsion in ethanol or methanol did not result in the formation of microspheres, due to massive polymer precipitation caused by rapid solvent extraction in these non-solvents. In a second process, microspheres were first prepared by a water-in-oil-in-water (w/o/w) emulsion system with 4% poly(vinyl alcohol) (PVA) as stabilizer in the external phase, followed by extraction of the remaining solvent. As non-solvents ethanol, methanol and mixtures of methanol and water were employed. However, the use of alcohols in the extraction medium resulted in microspheres which gave an incomplete lysozyme release at a non-constant rate. Complete lysozyme release was obtained from microspheres prepared by an emulsification-solvent evaporation method in PBS containing poly(vinyl pyrrolidone) (PVP) or PVA as stabilizer. PVA was most effective in stabilizing the w/o/w emulsion. Perfectly spherical microspheres were produced, with high protein entrapment efficiencies. These microspheres released lysozyme at an almost constant rate for approximately 28 days. The reproducibility of the w/o/w emulsion process was demonstrated by comparing particle characteristics and release profiles of three batches, prepared under similar conditions.

  13. Influence of different structured channels of mesoporous silicate on the controlled ibuprofen delivery

    International Nuclear Information System (INIS)

    Gao, Lin; Sun, Jihong; Zhang, Li; Wang, Jinpeng; Ren, Bo

    2012-01-01

    The bimodal mesoporous silicas with short random mesoporous channels and MCM-41 with long ordered mesopores were synthesised and modified with 3-(2-aminoethylamino) propyltrimethoxysilane as ibuprofen carriers to study the influence of mesoporous structure on drug delivery property. For further comparing the different mesoporous channels, modified SBA-15 with relative large and long ordered mesopores was also synthesized as drug carriers. The resultant samples were characterized with X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectra, N 2 adsorption–desorption isotherms, thermogravimetric analyses, solid-state 29 Si NMR spectra, elemental analysis, and UV–vis spectra. Meanwhile, the Korsmeyer–Peppas equation f t = kt n was employed to analyze the drug release profile and three release mediums including simulated fluid solution, distilled water and simulated gastric fluid were used. The results indicated that the modified BMMs with the bimodal mesopores leaded to the most drug loading amount of 25.0 mg/0.1 g, while the MCM-41 with the long and one-dimensional mesopores had the least loading amount around 20.3 mg/0.1 g. Meanwhile, the easier diffusion behavior of drug molecules in the bimodal mesopore channels of BMMs resulted in relatively faster drug release properties in comparison with MCM-41, while the release time maintained in SBF for about 12 h (release percent was about 90 wt%) and corresponding release constant k obtained from Korsmeyer–Peppas equation was around 4.10. Highlights: ► BMMs, MCM-41 and SBA-15 with different mesostructure channels were modified with amino groups via post-treatment procedure. ► Loading and release profiles of ibuprofen in modified BMMs, MCM-41 and SBA-15. ► BMMs presents more drug loading amount than MCM-41 as well as better controlled release than SBA-15.

  14. Influence of different structured channels of mesoporous silicate on the controlled ibuprofen delivery

    Energy Technology Data Exchange (ETDEWEB)

    Gao, Lin [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China); Sun, Jihong, E-mail: jhsun@bjut.edu.cn [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China); Zhang, Li; Wang, Jinpeng; Ren, Bo [Department of Chemistry and Chemical Engineering, College of Environmental and Energy Engineering, Beijing University of Technology, 100 PingLeYuan, Chaoyang District, Beijing 100124 (China)

    2012-08-15

    The bimodal mesoporous silicas with short random mesoporous channels and MCM-41 with long ordered mesopores were synthesised and modified with 3-(2-aminoethylamino) propyltrimethoxysilane as ibuprofen carriers to study the influence of mesoporous structure on drug delivery property. For further comparing the different mesoporous channels, modified SBA-15 with relative large and long ordered mesopores was also synthesized as drug carriers. The resultant samples were characterized with X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectra, N{sub 2} adsorption-desorption isotherms, thermogravimetric analyses, solid-state {sup 29}Si NMR spectra, elemental analysis, and UV-vis spectra. Meanwhile, the Korsmeyer-Peppas equation f{sub t} = kt{sup n} was employed to analyze the drug release profile and three release mediums including simulated fluid solution, distilled water and simulated gastric fluid were used. The results indicated that the modified BMMs with the bimodal mesopores leaded to the most drug loading amount of 25.0 mg/0.1 g, while the MCM-41 with the long and one-dimensional mesopores had the least loading amount around 20.3 mg/0.1 g. Meanwhile, the easier diffusion behavior of drug molecules in the bimodal mesopore channels of BMMs resulted in relatively faster drug release properties in comparison with MCM-41, while the release time maintained in SBF for about 12 h (release percent was about 90 wt%) and corresponding release constant k obtained from Korsmeyer-Peppas equation was around 4.10. Highlights: Black-Right-Pointing-Pointer BMMs, MCM-41 and SBA-15 with different mesostructure channels were modified with amino groups via post-treatment procedure. Black-Right-Pointing-Pointer Loading and release profiles of ibuprofen in modified BMMs, MCM-41 and SBA-15. Black-Right-Pointing-Pointer BMMs presents more drug loading amount than MCM-41 as well as better controlled release than SBA-15.

  15. Graphene Aerogel Templated Fabrication of Phase Change Microspheres as Thermal Buffers in Microelectronic Devices.

    Science.gov (United States)

    Wang, Xuchun; Li, Guangyong; Hong, Guo; Guo, Qiang; Zhang, Xuetong

    2017-11-29

    Phase change materials, changing from solid to liquid and vice versa, are capable of storing and releasing a large amount of thermal energy during the phase change, and thus hold promise for numerous applications including thermal protection of electronic devices. Shaping these materials into microspheres for additional fascinating properties is efficient but challenging. In this regard, a novel phase change microsphere with the design for electrical-regulation and thermal storage/release properties was fabricated via the combination of monodispersed graphene aerogel microsphere (GAM) and phase change paraffin. A programmable method, i.e., coupling ink jetting-liquid marbling-supercritical drying (ILS) techniques, was demonstrated to produce monodispersed graphene aerogel microspheres (GAMs) with precise size-control. The resulting GAMs showed ultralow density, low electrical resistance, and high specific surface area with only ca. 5% diameter variation coefficient, and exhibited promising performance in smart switches. The phase change microspheres were obtained by capillary filling of phase change paraffin inside the GAMs and exhibited excellent properties, such as low electrical resistance, high latent heat, well sphericity, and thermal buffering. Assembling the phase change microsphere into the microcircuit, we found that this tiny device was quite sensitive and could respond to heat as low as 0.027 J.

  16. Gastroretentive Floating Microspheres of Silymarin: Preparation and ...

    African Journals Online (AJOL)

    Methods: Cellulose microspheres – formulated with hydroxylpropyl methylcellulose (HPMC) and ethyl cellulose (EC) – and Eudragit microspheres – formulated with Eudragit® S 100 (ES) and Eudragit® RL (ERL) - were prepared by an emulsion-solvent evaporation method. The floating microspheres were evaluated for flow ...

  17. Melatonin Nanoparticles Adsorbed to Polyethylene Glycol Microspheres as Activators of Human Colostrum Macrophages

    Directory of Open Access Journals (Sweden)

    Cristiane de Castro Pernet Hara

    2013-01-01

    Full Text Available The effectiveness of hormones associated with polymeric matrices has amplified the possibility of obtaining new drugs to activate the immune system. Melatonin has been reported as an important immunomodulatory agent that can improve many cell activation processes. It is possible that the association of melatonin with polymers could influence its effects on cellular function. Thus, this study verified the adsorption of the hormone melatonin to polyethylene glycol (PEG microspheres and analyzed its ability to modulate the functional activity of human colostrum phagocytes. Fluorescence microscopy and flow cytometry analyses revealed that melatonin was able to adsorb to the PEG microspheres. This system increased the release of superoxide and intracellular calcium. There was an increase of phagocytic and microbicidal activity by colostrum phagocytes when in the presence of melatonin adsorbed to PEG microspheres. The modified delivery of melatonin adsorbed to PEG microspheres may be an additional mechanism for its microbicidal activity and represents an important potential treatment for gastrointestinal infections of newborns.

  18. Melatonin Nanoparticles Adsorbed to Polyethylene Glycol Microspheres as Activators of Human Colostrum Macrophages

    International Nuclear Information System (INIS)

    Hara, C.D.C.P.; Honorio-Frana, A.C.; Fagundes, D.L.G.; Guimares, P.C.L.; Franca, E.L.

    2013-01-01

    The effectiveness of hormones associated with polymeric matrices has amplified the possibility of obtaining new drugs to activate the immune system. Melatonin has been reported as an important immunomodulatory agent that can improve many cell activation processes. It is possible that the association of melatonin with polymers could influence its effects on cellular function. Thus, this study verified the adsorption of the hormone melatonin to polyethylene glycol (PEG) microspheres and analyzed its ability to modulate the functional activity of human colostrum phagocytes. Fluorescence microscopy and flow cytometry analyses revealed that melatonin was able to adsorb to the PEG microspheres. This system increased the release of superoxide and intracellular calcium. There was an increase of phagocytic and microbicidal activity by colostrum phagocytes when in the presence of melatonin adsorbed to PEG microspheres. The modified delivery of melatonin adsorbed to PEG microspheres may be an additional mechanism for its microbicidal activity and represents an important potential treatment for gastrointestinal infections of newborns.

  19. A SynoviocyteModel for Osteoarthritis and Rheumatoid Arthritis: Response to Ibuprofen, Betamethasone, and Ginger Extract—A Cross-Sectional In Vitro Study

    DEFF Research Database (Denmark)

    Ribel-Madsen, Søren; Bartels, Else Marie; Stockmarr, Anders

    2012-01-01

    synovial membrane or joint fluid. Cells were cultivated and exposed to no or TNF-α stimulation without, or in the presence of, betamethasone, ibuprofen, or a standardized ginger extract. Concentrations of a panel of cytokines, growth factors, and chemokines were mapped for each culture and condition. Our......, and IL-8 release in all groups. Ibuprofen showed no effect on cytokine production, while ginger extract was similar to betamethasone. Ginger extract was as effective an anti-inflammatory agent as betamethasone in this in vitro model. Cultured fibroblast-like synoviocytes from OA and RA subjects promise...

  20. Comparative Studies on the Dissolution Profiles of Oral Ibuprofen Suspension and Commercial Tablets using Biopharmaceutical Classification System Criteria

    Science.gov (United States)

    Rivera-Leyva, J. C.; García-Flores, M.; Valladares-Méndez, A.; Orozco-Castellanos, L. M.; Martínez-Alfaro, M.

    2012-01-01

    In vitro dissolution studies for solid oral dosage forms have recently widened the scope to a variety of special dosage forms such as suspensions. For class II drugs, like Ibuprofen, it is very important to have discriminative methods for different formulations in physiological conditions of the gastrointestinal tract, which will identify different problems that compromise the drug bioavailability. In the present work, two agitation speeds have been performed in order to study ibuprofen suspension dissolution. The suspensions have been characterised relatively to particle size, density and solubility. The dissolution study was conducted using the following media: buffer pH 7.2, pH 6.8, 4.5 and 0.1 M HCl. For quantitative analysis, the UV/Vis spectrophotometry was used because this methodology had been adequately validated. The results show that 50 rpm was the adequate condition to discriminate the dissolution profile. The suspension kinetic release was found to be dependent on pH and was different compared to tablet release profile at the same experimental conditions. The ibuprofen release at pH 1.0 was the slowest. PMID:23626386

  1. P25 nanoparticles decorated on titania nanotubes arrays as effective drug delivery system for ibuprofen

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Zhang; Xie, Chunlin; Luo, Fei; Li, Ping; Xiao, Xiufeng, E-mail: xfxiao@fjnu.edu.cn

    2015-01-01

    Highlights: • P25 nanoparticles decorated on titania nanotube arrays were prepared by hydrothermal treatment. • P25 nanoparticles were conducive to improve the loading effect of ibuprofen into nanotube arrays. • The diameters of the decorated nanotubes were decrease markedly which led to an effective and prolonged drug release. - Abstract: In this study, uniformly distributed layer of P25 nanoparticles (NPs) decorated on titania (TiO{sub 2}) nanotubes (TNTs) arrays was prepared in a teflon-lined stainless steel autoclave by the hydrothermal treatment. To investigate the influence of the P25 concentration, different concentrations of P25 NPs were added into the solution to obtain the optimal decorative effect. TNTs decorated with P25 (TNTs–P25) and TNTs without P25 decorated on its surface were loaded with ibuprofen (IBU) via vacuum drying and its release properties were investigated. The samples were characterized by field emission scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectroscopy. The results indicated that P25 NPs were successfully decorated on the surface of TNTs by hydrothermal method and the optimal concentration was found to be 7.5 × 10{sup −4} M. P25 NPs decorated on TNTs led to a significant increase in the specific surface area of TNTs which was conducive to improve the loading effect of IBU. Importantly, the diameters of the decorated nanotubes were reduced to 100 ± 10 nm and the increase in roughness led to an effective and prolonged drug release.

  2. Self-Assembly of pH-Responsive Microspheres for Intestinal Delivery of Diverse Lipophilic Therapeutics.

    Science.gov (United States)

    Zhou, Xing; Zhao, Yang; Chen, Siyu; Han, Songling; Xu, Xiaoqiu; Guo, Jiawei; Liu, Mengyu; Che, Ling; Li, Xiaohui; Zhang, Jianxiang

    2016-08-08

    Targeted delivery of therapeutics to the intestine is preferred for the management of many diseases due to its diverse advantages. Currently, there are still challenges in creating cost-effective and translational pH-responsive microspheres for intestinal delivery of various hydrophobic drugs. Herein we report a multiple noncovalent interactions-mediated assembly strategy in which carboxyl-bearing compounds (CBCs) are guest molecules, while poly(N-isopropylacrylamide) (PNIPAm) serves as a host polymer. Formation of microparticles and therapeutic packaging can be achieved simultaneously by this assembly approach, leading to well-shaped microspheres with extremely higher drug loading capacity as compared to microspheres based on two FDA-approved materials of poly(d,l-lactide-co-glycolide) (PLGA) and an enteric coating polymer EudragitS 100 (S100). Also, carboxyl-deficient hydrophobic drugs can be effectively entrapped. These assembled microspheres, with excellent reconstitution capability as well as desirable scalability, could selectively release drug molecules under intestinal conditions. By significantly enhancing drug dissolution/release in the intestine, these pH-responsive assemblies may notably improve the oral bioavailability of loaded therapeutics. Moreover, the assembled microspheres possessed superior therapeutic performance in rodent models of inflammation and tumor over the control microspheres derived from PLGA and S100. Therapy with newly developed microspheres did not cause undesirable side effects. Furthermore, in vivo evaluation in mice revealed the carrier material PNIPAm was safe for oral delivery at doses as high as 10 g/kg. Collectively, our findings demonstrated that this type of pH-responsive microsphere may function as superior and translational intestine-directed delivery systems for a diverse array of therapeutics.

  3. Importance of acute renal failure with ibuprofen

    Directory of Open Access Journals (Sweden)

    Tufan F

    2014-05-01

    Full Text Available Fatih Tufan Sevket Yilmaz Training and Research Hospital, Geriatrics Unit, Yildirim, Bursa, TurkeyKuptniratsaikul et al report the efficacy of Curcuma domestica extracts in the treatment of knee osteoarthritis.1 One of my concerns about this well designed study is lack of one important adverse event assessment. One of the most important adverse effects of ibuprofen, which is a non-selective non-steroid anti-inflammatory drug, is acute renal failure.2 Although one of the exclusion criteria in this study is renal failure, especially in the elderly population, it is crucial to follow up kidney functions under non-steroid anti-inflammatory treatment.View original paper by Kuptniratsaikul and colleagues. 

  4. Layered zinc hydroxide–ibuprofen nanohybrids: synthesis and ...

    Indian Academy of Sciences (India)

    The nonsteroidal anti-inflammatory drug (NSAID), ibuprofen (IBU) anion, was intercalated into the layered zinc ... surface morphology, Fourier transform infrared (FTIR) spectrophotometer to study the chemical interactions and ..... J. Food Sci.

  5. Preparation and in vitro/in vivo characterization of curcumin microspheres intended to treat colon cancer

    Directory of Open Access Journals (Sweden)

    M Madhavi

    2012-01-01

    Full Text Available Objective: The objective of the present investigation was to prepare colon targeted curcumin microspheres using Eudragit S100 and evaluate the same for in vitro/in vivo properties. Materials and Methods: A "O/O solvent evaporation" technique was used in the preparation of microspheres. The influence of various process variables including stirring speed, drug:polymer ratio and percentage of emulsifier on the fabrication were investigated and the formulation was optimized. Prepared microspheres were evaluated for in vitro and in vivo properties. Surface morphology, particle size, percentage drug entrapment, percentage yield, drug polymer interaction, in vitro drug release in simulated gastrointestinal transit conditions and stability were the in vitro parameters investigated. Using an optimized formulation, drug release into the systemic circulation and organ distribution were investigated as in vivo parameters. In vivo parameters were estimated in male albino rats. Results: Curcumin microspheres of Eudragit S100 were successfully prepared using o/o solvent evaporation method. Microspheres prepared using 1:2 drug:polymer ratio, with a stirring speed of 1000 rpm, and using 1.0% w/v concentration of emulsifying agent was selected as an optimized formulation. The release studies with optimized formulation demonstrated that aqueous solubility of curcumin was enhanced by 8 times with the formulation. FTIR studies demonstrated no change in drug characteristics upon microsphere fabrication. The enhancement in solubility is thus due to the increase in the surface area of the drug substance and not due to a change of drug to a different physical state. This was further confirmed by scanning electron microsphere pictures. Drug release followed Korsmeyer and Peppas release model. Accelerated stability studies indicated that the drug is stable in the formulation for a period of atleast 14 weeks at room temperature. In vivo studies demonstrated a sustained

  6. Temperature influence in crystallinity of polymer microspheres

    International Nuclear Information System (INIS)

    Rezende, Cristiane de P.; Novack, Katia M.

    2011-01-01

    Drug delivery technology is evolving through the creation of new techniques of drug delivery effectively. The new methods used in drugs administration are based in microencapsulation process. Microsphere encapsulation modifies drug delivery bringing benefits and efficiency. In this work has been evaluated the influence of temperature in microspheres preparation. Microspheres were obtained by PMMA-co-PEG (COP) copolymer with indomethacin inserted in polymer matrix. Samples were characterized by SEM, DSC and XRD. SEM micrographs confirmed the formation of different sizes of microspheres and it was verified that higher temperatures make more crystalline microspheres. (author)

  7. Intracellular degradation of microspheres based on cross-linked dextran hydrogels or amphiphilic block copolymers: A comparative Raman microscopy study

    Science.gov (United States)

    van Manen, Henk-Jan; van Apeldoorn, Aart A; Verrijk, Ruud; van Blitterswijk, Clemens A; Otto, Cees

    2007-01-01

    Micro- and nanospheres composed of biodegradable polymers show promise as versatile devices for the controlled delivery of biopharmaceuticals. Whereas important properties such as drug release profiles, biocompatibility, and (bio)degradability have been determined for many types of biodegradable particles, information about particle degradation inside phagocytic cells is usually lacking. Here, we report the use of confocal Raman microscopy to obtain chemical information about cross-linked dextran hydrogel microspheres and amphiphilic poly(ethylene glycol)-terephthalate/poly(butylene terephthalate) (PEGT/PBT) microspheres inside RAW 264.7 macrophage phagosomes. Using quantitative Raman microspectroscopy, we show that the dextran concentration inside phagocytosed dextran microspheres decreases with cell incubation time. In contrast to dextran microspheres, we did not observe PEGT/PBT microsphere degradation after 1 week of internalization by macrophages, confirming previous studies showing that dextran microsphere degradation proceeds faster than PEGT/PBT degradation. Raman microscopy further showed the conversion of macrophages to lipid-laden foam cells upon prolonged incubation with both types of microspheres, suggesting that a cellular inflammatory response is induced by these biomaterials in cell culture. Our results exemplify the power of Raman microscopy to characterize microsphere degradation in cells and offer exciting prospects for this technique as a noninvasive, label-free optical tool in biomaterials histology and tissue engineering. PMID:17722552

  8. Application of guar gum biopolymer in the prescription of tablets with sodium ibuprofen--quality tests and pharmaceutical availability in vitro.

    Science.gov (United States)

    Berner-Strzelczyk, Aneta; Kołodziejska, Justyna; Zgoda, Marian Mikołaj

    2006-01-01

    The increasing interest of the technology of drug form in natural biopolymers has become the reason for undertaking investigations on the possibility of guar gum application in the prescription of oral solid form of a drug. Alternative compositions and technology of the production of tablets of regulated in time sodium ibuprofen release were worked out for children. Two series of tablets were prepared with guar gum (5 and 10% content) and a series without the biopolymer. The tablet mass in each case contained keryostatic sorbitol and bioadhesive polyvinylpyrrolidone. All tablets were tested as regards the quality of production, compliance with the requirements of Polish Pharmacopoeia VI and potential therapeutic usefulness, manifestation of which is pharmaceutical availability of the therapeutic agent (sodium ibuprofen). The tests demonstrated that the produced tablets with sodium ibuprofen have proper physicochemical properties, in compliance with Polish Pharmacopoeia VI requirements. Application of biopolymer of guar gum type as adjuvant substance contributes to the improvement of the tablet hardness parameters and prevents technological problems (lining mixture of powders to tableting machine punch). The designed tablets demonstrate proper pharmaceutical availability of over 80%. Introduction of guar gum into their prescription prolonged their disintegration time and the rate of sodium ibuprofen release, which predisposes the produced form of a drug to have the function of a tablet with slowed-down release.

  9. MODELLING DICLOFENAC AND IBUPROFEN RESIDUES IN MAJOR ESTONIAN SEASIDE CITIES

    Directory of Open Access Journals (Sweden)

    Erki Lember

    2016-06-01

    Full Text Available A theoretical model was developed to model the fate of two common pharmaceutical residues: diclofenac and ibuprofen in eight Estonian seaside cities that discharge their wastewaters directly into the Baltic Sea. The consumption rates of the active ingredients of diclofenac and ibuprofen from 2006-2014 were analysed. A decrease of 19.9% for diclofenac consumption and an increase of 14.1% for ibuprofen were found. The fate of diclofenac and ibuprofen were modelled by considering the human metabolism removal rate for pharmaceuticals, the removal rate of diclofenac and ibuprofen in activated sludge wastewater treatment plants (WWTP and annual flow rates. An average decrease from 1 to 0.8 µg/l (decrease of 20% for diclofenac and an increase from 11.4 to 13.4 µg/l (increase of 14.9% for ibuprofen for the concentration in the effluents of the WWTP were modelled. The model gives us a good overview about the theoretical concentrations of pharmaceutical residues in the environment and is helpful for evaluating environmental impacts.

  10. Ibuprofen plus paracetamol versus ibuprofen in acute low back pain: a randomized open label multicenter clinical study

    Directory of Open Access Journals (Sweden)

    Predrag Ostojic

    2017-01-01

    Full Text Available Objective: to estimate whether combination of ibuprofen and paracetamol is more effective than ibuprofen in monotherapy, in the treatment of acute low back pain. Methods: 80 adult patients with acute low back pain were randomized into two subgroups. In the first subgroup, 40 patients were treated with ibuprofen 400mg three times a day (TID, whilst patients in the second subgroup (n=40 were treated with a fixed-dose combination tablet of ibuprofen 200mg plus paracetamol 325mg TID, for three consecutive days. Patients were followed for another 7 days. Efficacy and tolerability of both treatment options was assessed. Results: A statistically significant decrease in pain intensity, assessed using a visual analogue scale (p

  11. Preparation and in vitro evaluation of xanthan gum facilitated superabsorbent polymeric microspheres.

    Science.gov (United States)

    Bhattacharya, Shiv Sankar; Mazahir, Farhan; Banerjee, Subham; Verma, Anurag; Ghosh, Amitava

    2013-10-15

    Interpenetrating polymer network (IPN) hydrogel microspheres of xanthan gum (XG) based superabsorbent polymer (SAP) and poly(vinyl alcohol) (PVA) were prepared by water-in-oil (w/o) emulsion crosslinking method for sustained release of ciprofloxacin hydrochloride (CIPRO). The microspheres were prepared with various ratios of hydrolyzed SAP to PVA and extent of crosslinking density. The prepared microspheres with loose and rigid surfaces were evidenced by scanning electron microscope (SEM). Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) analysis confirmed the IPN formation. Differential scanning calorimetry (DSC) study was performed to understand the dispersion nature of drug after encapsulation. The in vitro drug release study was extensively evaluated depending on the process variables in both acidic and alkaline media. All the formulations exhibited satisfactory physicochemical and in vitro release characteristics. Release data indicated a non-Fickian trend of drug release from the formulations. Based on the results, this study suggest that CIPRO loaded IPN microspheres were suitable for sustained release application. Copyright © 2013 Elsevier Ltd. All rights reserved.

  12. Rifapentine-linezolid-loaded PLGA microspheres for interventional therapy of cavitary pulmonary tuberculosis: preparation and in vitro characterization.

    Science.gov (United States)

    Huang, Jieyun; Chen, Zhi; Li, Ying; Li, Li; Zhang, Guangyu

    2017-01-01

    In this study, we aimed to design controlled-release microspheres for the treatment of cavitary pulmonary tuberculosis (TB) for solving the issues of poor drug delivery and short duration maintained at effective drug concentration during bronchoscopic interventional therapy. We fabricated rifapentine-linezolid-loaded poly(lactic acid-co-glycolic acid) microspheres (RLPMs) using the oil-in-water emulsion solvent evaporation method and assessed their in vitro release as well as the bronchial mucosal retention characteristics. The microspheres are spherical in shape with a circular concave on the surface. The particle size of RLPMs was 27.38±1.28 μm. The drug loading of rifapentine and linezolid was 18.51±0.26 and 8.42%±0.24%, respectively, while the encapsulation efficiencies were 55.53±0.78 and 16.87%±0.47%, respectively (n=3). During the burst release phase of the in vitro release test, 21.37%±0.68% rifapentine was released in 3 days and 43.56%±2.54% linezolid was released in 1 day. Then, both the drugs entered the sustained release phase. Finally, the cumulative percentage release of rifapentine and linezolid in 14 days was 27.61±1.52 and 51.01%±3.31%, respectively (n=3). Bronchoscopic observation revealed that the controlled-release microspheres could slowly release the drugs and retain them on the surface of bronchial mucosa of canines for 20 days. These results indicated that the fabricated microspheres exhibited a significant sustained release effect and could effectively retain the drugs on the surface of bronchial mucosa. Therefore, this study provides a theoretical and practical foundation for the development of fabricated microspheres loaded with multiple anti-TB drugs in the bronchoscopic interventional therapy of cavity pulmonary TB.

  13. Randomized comparative trial of efficacy of paracetamol, ibuprofen and paracetamol-ibuprofen combination for treatment of febrile children

    Directory of Open Access Journals (Sweden)

    Falgun Indravadan Vyas

    2014-01-01

    Full Text Available Objective: Paracetamol and ibuprofen are widely used for fever in children as monotherapy and as combined therapy. None of the treatments is proven clearly superior to others. Hence, the study was planned to compare the efficacy of paracetamol, ibuprofen and paracetamol-ibuprofen combination for treatment of febrile children. Materials and Methods: This was an investigator blind, randomized, comparative, parallel clinical trial conducted in 99 febrile children, 6 months to 12 years of age, allocated to three groups. First group received paracetamol 15 mg/kg, second group received ibuprofen 10 mg/kg and third group received both paracetamol and ibuprofen, all as a single dose by the oral route. Patients were followed-up at intervals of 1, 2, 3 and 4 h post dose by tympanic thermometry. Results: Mean tympanic temperature after 4 h of drug administration was significantly lower in the combination group compared with paracetamol group (P < 0.05; however, the difference was not clinically significant (<1΀C. The rate of fall of temperature was highest in the combination group. Number of afebrile children any time post dose until 4 h was highest in the combination group. Difference between combination and paracetamol was significant for the 1 st h (P = 0.04. Highest fall of temperature was noted in the 1 st h of drug administration in all the groups. No serious adverse events were observed in any of the groups. Conclusion: Paracetamol and ibuprofen combination caused quicker temperature reduction than either paracetamol or ibuprofen alone. If quicker reduction of body temperature is the desired goal of therapy, the use of combination of paracetamol + ibuprofen may be advocated.

  14. Drug-loaded poly (ε-caprolactone)/Fe3O4 composite microspheres for magnetic resonance imaging and controlled drug delivery

    Science.gov (United States)

    Wang, Guangshuo; Zhao, Dexing; Li, Nannan; Wang, Xuehan; Ma, Yingying

    2018-06-01

    In this study, poly (ε-caprolactone) (PCL) microspheres loading magnetic Fe3O4 nanoparticles and anti-cancer drug of doxorubicin hydrochloride (DOX) were successfully prepared by a modified solvent-evaporation method. The obtained magnetic composite microspheres exhibited dual features of magnetic resonance imaging and controlled drug delivery. The morphology, structure, thermal behavior and magnetic properties of the drug-loaded magnetic microspheres were investigated in detail by SEM, XRD, DSC and SQUID. The obtained composite microspheres showed superparamagnetic behavior and T2-weighted enhancement effect. The drug loading, encapsulation efficiency, releasing behavior and in vitro cytotoxicity of the drug-loaded composite microspheres were systematically investigated. It was found that the values of drug loading and encapsulation efficiency were 36.7% and 25.8%, respectively. The composite microspheres were sensitive to pH and released in a sustained way, and both the release curves under various pH conditions (4.0 and 7.4) were well satisfied with the biphase kinetics function. In addition, the magnetic response of the drug-loaded microspheres was studied and the results showed that the composite microspheres had a good magnetic stability and strong targeting ability.

  15. Kefiran-alginate gel microspheres for oral delivery of ciprofloxacin.

    Science.gov (United States)

    Blandón, Lina M; Islan, German A; Castro, Guillermo R; Noseda, Miguel D; Thomaz-Soccol, Vanete; Soccol, Carlos R

    2016-09-01

    Ciprofloxacin is a broad-spectrum antibiotic associated with gastric and intestinal side effects after extended oral administration. Alginate is a biopolymer commonly employed in gel synthesis by ionotropic gelation, but unstable in the presence of biological metal-chelating compounds and/or under dried conditions. Kefiran is a microbial biopolymer able to form gels with the advantage of displaying antimicrobial activity. In the present study, kefiran-alginate gel microspheres were developed to encapsulate ciprofloxacin for antimicrobial controlled release and enhanced bactericidal effect against common pathogens. Scanning electron microscopy (SEM) analysis of the hybrid gel microspheres showed a spherical structure with a smoother surface compared to alginate gel matrices. In vitro release of ciprofloxacin from kefiran-alginate microspheres was less than 3.0% and 5.0% at pH 1.2 (stomach), and 5.0% and 25.0% at pH 7.4 (intestine) in 3 and 21h, respectively. Fourier transform infrared spectroscopy (FTIR) of ciprofloxacin-kefiran showed the displacement of typical bands of ciprofloxacin and kefiran, suggesting a cooperative interaction by hydrogen bridges between both molecules. Additionally, the thermal analysis of ciprofloxacin-kefiran showed a protective effect of the biopolymer against ciprofloxacin degradation at high temperatures. Finally, antimicrobial assays of Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhymurium, and Staphylococcus aureus demonstrated the synergic effect between ciprofloxacin and kefiran against the tested microorganisms. Copyright © 2016 Elsevier B.V. All rights reserved.

  16. Ibuprofen: from invention to an OTC therapeutic mainstay.

    Science.gov (United States)

    Rainsford, K D

    2013-01-01

    The discovery of ibuprofen's anti-inflammatory activity by Dr (now Professor) Stewart Adams and colleagues (Boots Pure Chemical Company Ltd, Nottingham, UK) 50 years ago represented a milestone in the development of anti-inflammatory analgesics. Subsequent clinical studies were the basis for ibuprofen being widely accepted for treating painful conditions at high anti-rheumatic doses (≤ 2400 mg/d), with lower doses (≤ 1200 mg/d for ≤ 10 days) for mild-moderate acute pain (e.g. dental pain, headache, dysmenorrhoea, respiratory symptoms and acute injury). The early observations have since been verified in studies comparing ibuprofen with newer cyclo-oxygenase-2 selective inhibitors ('coxibs'), paracetamol and other non-steroidal anti-inflammatory drugs (NSAIDs). The use of the low-dose, non-prescription, over-the-counter (OTC) drug was based on marketing approval in 1983 (UK) and 1984 (USA); and it is now available in over 80 countries. The relative safety of OTC ibuprofen has been supported by large-scale controlled studies. It has the same low gastro-intestinal (GI) effects as paracetamol (acetaminophen) and fewer GI effects than aspirin. Ibuprofen is a racemate. Its physicochemical properties and the short plasma-elimination half-life of the R(-) isomer, together with its limited ability to inhibit cyclo-oxygenase-1 (COX-1) and thus prostaglandin (PG) synthesis, compared with that of S(+)-ibuprofen, are responsible for the relatively low GI toxicity. The R(-) isomer is then converted in the body to the S(+) isomer after absorption in the GI tract. Ex vivo inhibition of COX-1 (thromboxane A(2)) and COX-2 (PGE(2)) at the plasma concentrations of S(+)-ibuprofen corresponding to those found in the plasma following ingestion of 400 mg ibuprofen in dental and other inflammatory pain models provides evidence of the anti-inflammatory mechanism at OTC dosages. R(-)-ibuprofen has effects on leucocytes, suggesting that ibuprofen has anti-leucocyte effects, which

  17. Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

    Directory of Open Access Journals (Sweden)

    Marta Szekalska

    2016-01-01

    Full Text Available Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9 with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1 and different sodium alginate concentration (1%, 2%, and 3% were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree. In vitro drug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution. Based on glucose uptake in Saccharomyces cerevisiae cells and α-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluated in vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

  18. Dual functions of polyvinyl alcohol (PVA): fabricating particles and electrospinning nanofibers applied in controlled drug release

    Science.gov (United States)

    Qin, Xiao-Hong; Wu, De-Qun; Chu, Chih-Chang

    2013-01-01

    The fabrication of submicron size microsphere from 8-Phe-4 poly(ester amide) (PEA) using polyvinyl alcohol (PVA) as the emulsion was reported. The biodegradable microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique, and PVA was used as the emulsion. Furthermore, the emulsion PVA was electrospun into nanofibrous mats, and 8-Phe-4 PEA microspheres were entrapped in the resultant mats. The dual functions of PVA to fabricate ideal nanofibrous mats which can entrap microspheres in them and to obtain 8-Phe-4 microspheres as emulsion in their potential application were demonstrated. The anti-cancer drug doxorubicin (DOX) was encapsulated in the 8-Phe-4 amino acid-based PEA microspheres and the entrapment efficiency is almost 100 %. At the same time, the DOX can be controlled released in PBS solution and in α-chymotrypsin solution. The cytotoxicity of PVA, PVA mats-entrapped 8-Phe-4 microspheres and PVA mats-entrapped DOX-loaded 8-Phe-4 microspheres, was investigated. Hela cells were used to test the cytotoxicity of the DOX that released from the PVA mats-entrapped DOX-loaded 8-Phe-4 microspheres for 2 days, and the cell viability is below 30 % when the 8-Phe-4 microspheres concentration is 1 mg/mL. It demonstrated that the PVA mats-entrapped DOX-loaded 8-Phe-4 microspheres have a potential biomedical application.

  19. BMP2-loaded hollow hydroxyapatite microspheres exhibit enhanced osteoinduction and osteogenicity in large bone defects.

    Science.gov (United States)

    Xiong, Long; Zeng, Jianhua; Yao, Aihua; Tu, Qiquan; Li, Jingtang; Yan, Liang; Tang, Zhiming

    2015-01-01

    The regeneration of large bone defects is an osteoinductive, osteoconductive, and osteogenic process that often requires a bone graft for support. Limitations associated with naturally autogenic or allogenic bone grafts have demonstrated the need for synthetic substitutes. The present study investigates the feasibility of using novel hollow hydroxyapatite microspheres as an osteoconductive matrix and a carrier for controlled local delivery of bone morphogenetic protein 2 (BMP2), a potent osteogenic inducer of bone regeneration. Hollow hydroxyapatite microspheres (100±25 μm) with a core (60±18 μm) and a mesoporous shell (180±42 m(2)/g surface area) were prepared by a glass conversion technique and loaded with recombinant human BMP2 (1 μg/mg). There was a gentle burst release of BMP2 from microspheres into the surrounding phosphate-buffered saline in vitro within the initial 48 hours, and continued at a low rate for over 40 days. In comparison with hollow hydroxyapatite microspheres without BMP2 or soluble BMP2 without a carrier, BMP2-loaded hollow hydroxyapatite microspheres had a significantly enhanced capacity to reconstitute radial bone defects in rabbit, as shown by increased serum alkaline phosphatase; quick and complete new bone formation within 12 weeks; and great biomechanical flexural strength. These results indicate that BMP2-loaded hollow hydroxyapatite microspheres could be a potential new option for bone graft substitutes in bone regeneration.

  20. A novel NSAID derivative, phospho-ibuprofen, prevents AOM-induced colon cancer in rats

    Science.gov (United States)

    OUYANG, NENGTAI; JI, PING; WILLIAMS, JENNIE L.

    2013-01-01

    The cancer chemopreventive properties and gastrointestinal toxicity of ibuprofen are well documented. Modification of existing NSAIDs has improved on the chemopreventive efficacy of this agent and reduced its toxicity. In this study, ibuprofen and a modified derivative (phospho-modified ibuprofen or p-ibuprofen) were used in a chemically induced model of colon cancer. Fisher 344 rats were injected with azoxymethane then treated with either ibuprofen (500 ppm) or p-ibuprofen (900 ppm) for 20 weeks to observe aberrant crypt foci (ACF) or 40 weeks to evaluate tumor incidence and multiplicity. β-catenin and p65 were measured in colonic tissues by immunofluorescence staining. Equal molar doses of ibuprofen (75 and 670 mg/kg) and p-ibuprofen (135 and 1,215 mg/kg) were administered to rats for 7 days to assess acute toxicity. The in vitro effect of p-ibuprofen on COX-2 and PGE2 synthesis, β-catenin expression and NF-κB activity were examined in RAW 264.7 macrophage and HCT 116 colon cancer cells. At week 20, p-ibuprofen and ibuprofen significantly reduced the multiplicity of ACF compared with control (pibuprofen and ibuprofen reduced the multiplicity of colon tumors compared with control (pibuprofen (670 mg/kg) and p-ibuprofen (1,215 mg/kg) resulted in stomach ulceration in 85.7% (6 out of 7) and 14.3% (1 out of 7) of rats, respectively, with pibuprofen and p-ibuprofen suppressed β-catenin nuclear translocation in colon cancer cells. In addition, p-ibuprofen but not ibuprofen inhibited NF-κB activation in colon cancer cells. Collectively, these results suggest that p-ibuprofen is a potential effective novel drug for long-term use in colon cancer prevention. PMID:23291777

  1. Mucoadhesive microspheres for gastroretentive delivery of acyclovir: in vitro and in vivo evaluation.

    Science.gov (United States)

    Dhaliwal, Sumeet; Jain, Subheet; Singh, Hardevinder P; Tiwary, A K

    2008-06-01

    The aim of the present investigation was to evaluate the potential use of mucoadhesive microspheres for gastroretentive delivery of acyclovir. Chitosan, thiolated chitosan, Carbopol 71G and Methocel K15M were used as mucoadhesive polymers. Microsphere formulations were prepared using emulsion-chemical crosslinking technique and evaluated in vitro, ex-vivo and in-vivo. Gelatin capsules containing drug powder showed complete dissolution (90.5 +/- 3.6%) in 1 h. The release of drug was prolonged to 12 h (78.8 +/- 3.9) when incorporated into mucoadhesive microspheres. The poor bioavailability of acyclovir is attributed to short retention of its dosage form at the absorption sites (in upper gastrointestinal tract to duodenum and jejunum). The results of mucoadhesion study showed better retention of thiolated chitosan microspheres (8.0 +/- 0.8 h) in duodenal and jejunum regions of intestine. The results of qualitative and quantitative GI distribution study also showed significant higher retention of mucoadhesive microspheres in upper GI tract. Pharmacokinetic study revealed that administration of mucoadhesive microspheres could maintain measurable plasma concentration of acyclovir through 24 h, as compared to 5 h after its administration in solution form. Thiolated chitosan microsphere showed superiority over the other formulations as observed with nearly 4.0-fold higher AUC(0-24) value (1,090 +/- 51 ng h/ml) in comparison to drug solution (281 +/- 28 ng h/ml). Overall, the result indicated prolonged delivery with significant improvement in oral bioavailability of acyclovir from mucoadhesive microspheres due to enhanced retention in the upper GI tract.

  2. Preparation of a reproducible long-acting formulation of risperidone-loaded PLGA microspheres using microfluidic method.

    Science.gov (United States)

    Jafarifar, Elham; Hajialyani, Marziyeh; Akbari, Mona; Rahimi, Masoud; Shokoohinia, Yalda; Fattahi, Ali

    2017-09-01

    The aim of the present study is to prepare risperidone-loaded poly lactic-co-glycolic acid (PLGA) microspheres within microfluidic system and to achieve a formulation with uniform size and monotonic and reproducible release profile. In comparison to batch method, T-junction and serpentine chips were utilized and optimizing study was carried out at different processing parameters (e.g. PLGA and surfactant concentration and flow rates ratio of outer to inner phase). The computational fluid dynamic (CFD) modeling was performed, and loading and release study were carried out. CFD simulation indicates that increasing the flow rate of aqueous phase cause to decrease the droplet size, while the change in size of microspheres did not follow a specific pattern in the experimental results. The most uniform microspheres and narrowest standard deviation (66.79 μm ± 3.32) were achieved using T-junction chip, 1% polyvinylalcohol, 1% PLGA and flow rates ratio of 20. The microfluidic-assisted microspheres were more uniform with narrower size distribution. The release of risperidone from microspheres produced by the microfluidic method was more reproducible and closer to zero-order kinetic model. The release profile of formulation with 2:1 drug-to-polymer ratio was the most favorable release, in which 41.85% release could be achieved during 24 days.

  3. Preparing microspheres of actinide nitrides from carbon containing oxide sols

    International Nuclear Information System (INIS)

    Triggiani, L.V.

    1975-01-01

    A process is given for preparing uranium nitride, uranium oxynitride, and uranium carboxynitride microspheres and the microspheres as compositions of matter. The microspheres are prepared from carbide sols by reduction and nitriding steps. (Official Gazette)

  4. Investigation of emulsified, acid and acid-alkali catalyzed mesoporous bioactive glass microspheres for bone regeneration and drug delivery

    Energy Technology Data Exchange (ETDEWEB)

    Miao, Guohou [School of Materials Science and Engineering, South China University of Technology, Guangzhou 510641 China (China); National Engineering Research Center for Tissue Restoration and Reconstruction, Guangzhou 510006 China (China); Guangdong Province Key Laboratory of Biomedical Engineering, South China University of Technology, Guangzhou 510006 China (China); Chen, Xiaofeng, E-mail: chenxf@scut.edu.cn [School of Materials Science and Engineering, South China University of Technology, Guangzhou 510641 China (China); National Engineering Research Center for Tissue Restoration and Reconstruction, Guangzhou 510006 China (China); Guangdong Province Key Laboratory of Biomedical Engineering, South China University of Technology, Guangzhou 510006 China (China); Dong, Hua [National Engineering Research Center for Tissue Restoration and Reconstruction, Guangzhou 510006 China (China); Guangdong Province Key Laboratory of Biomedical Engineering, South China University of Technology, Guangzhou 510006 China (China); School of Biological Science and Engineering, South China University of Technology, Guangzhou 510006 (China); Fang, Liming; Mao, Cong; Li, Yuli; Li, Zhengmao; Hu, Qing [School of Materials Science and Engineering, South China University of Technology, Guangzhou 510641 China (China); National Engineering Research Center for Tissue Restoration and Reconstruction, Guangzhou 510006 China (China); Guangdong Province Key Laboratory of Biomedical Engineering, South China University of Technology, Guangzhou 510006 China (China)

    2013-10-15

    Acid-catalyzed mesoporous bioactive glass microspheres (MBGMs-A) and acid-alkali co-catalyzed mesoporous bioactive glass microspheres (MBGMs-B) were successfully synthesized via combination of sol-gel and water-in-oil (W/O) micro-emulsion methods. The structural, morphological and textural properties of mesoporous bioactive glass microspheres (MBGMs) were characterized by various techniques. Results show that both MBGMs-A and MBGMs-B exhibit regularly spherical shape but with different internal porous structures, i.e., a dense microstructure for MBGMs-A and internally porous structure for MBGMs-B. {sup 29}Si NMR data reveal that MGBMs have low polymerization degree of silica network. The in vitro bioactivity tests indicate that the apatite formation rate of MBGMs-B was faster than that of MBGMs-A after soaking in simulated body fluid (SBF) solution. Furthermore, the two kinds of MBGMs have similar storage capacity of alendronate (AL), and the release behaviors of AL could be controlled due to their unique porous structure. In conclusion, the microspheres are shown to be promising candidates as bone-related drug carriers and filling materials of composite scaffold for bone repair. - Graphical abstract: The morphologies and microstructures of acid-catalyzed mesoporous bioactive glass microspheres (MBGMs-A) and acid-alkali co-catalyzed mesoporous bioactive glass microspheres (MBGMs-B) were observed by scanning electron microscope and transmission electron microscope. MBGMs-A exhibits a dense structure and a porous can be observed in MBGMs-B. The microspheres have a quick inducing-apatite formation ability and show a sustained release of alendronate (AL). Highlights: • A rapid method was reported to prepare mesoporous bioactive glass microspheres. • The addition of ammonia significantly shortens the preparation time. • Acid and acid-alkali co-catalyzed microspheres were studied for the first time. • The materials exhibited excellent in vitro bioactivity and

  5. Formulation and in vitro evaluation of ibuprofen-loaded poly(D,L ...

    African Journals Online (AJOL)

    co-glycolide) (PLGA) microparticles. Methods: Ibuprofen-loaded microparticles containing PLGA were formulated using a emulsification/solvent evaporation method. Various concentrations of ibuprofen (200, 300, 400 and 0 mg) were loaded ...

  6. Facile synthesis of biphasic calcium phosphate microspheres with engineered surface topography for controlled delivery of drugs and proteins.

    Science.gov (United States)

    Zarkesh, Ibrahim; Ghanian, Mohammad Hossein; Azami, Mahmoud; Bagheri, Fatemeh; Baharvand, Hossein; Mohammadi, Javad; Eslaminejad, Mohamadreza Baghaban

    2017-09-01

    Biphasic calcium phosphate (BCP) microspheres are of great interest due to their high stability and osteoinductive properties at specific compositions. However, the need for optimal performance at a unique composition limits their flexibility for tuning drug release by modulation of bulk properties and presents the question of engineering surface topography as an alternative. It is necessary to have a facile method to control surface topography at a defined bulk composition. Here, we have produced BCP microspheres with different surface topographies that have the capability to be used as tunable drug release systems. We synthesized calcium deficient hydroxyapatite (CDHA) microparticles by precipitating calcium and phosphate ions onto ethylenediaminetetraacetic acid (EDTA) templates. The morphology and surface topography of CDHA microparticles were controlled using process parameters, which governed nucleation and growth. These parameters included template concentration, heat rate, and stirring speed. Under low heat rate and static conditions, we could obtain spherical microparticles with long and short nanosheets on their surfaces at low and high EDTA concentrations, respectively. These nanostructured microspheres were subsequently crystallized by thermal treatment to produce EDTA-free BCP microspheres with intact morphology. These biocompatible BCP microspheres were highly effective in loading and prolonged release of both small molecule [dexamethasone (Dex)] and protein [bovine serum albumin (BSA)] models. This strategy has enabled us to control the surface topography of BCP microspheres at defined compositions and holds tremendous promise for drug delivery and tissue engineering applications. Copyright © 2017 Elsevier B.V. All rights reserved.

  7. Chitosan Microspheres as Radiolabeled Delivery Devices

    International Nuclear Information System (INIS)

    Permtermsin, Chalermsin; Ngamprayad, Tippanan; Phumkhem, Sudkanung; Srinuttrakul, Wannee; Kewsuwan, Prartana

    2007-08-01

    Full text: This study optimized conditions for preparing, characterizing, radiolabeled of chitosan microspheres and the biodistribution of 99mTc-Chitosan microspheres after intravenous administration. Particle size distribution of the microspheres was determined by light scattering. Zeta potential was studied by dynamic light scattering and electrophoresis technique. Biodistribution studies were performed by radiolabeling using 99mTc. The results shown that geometric mean diameter of the microspheres was found to be 77.26?1.96 ?m. Microsphere surface charge of chitosan microspheres was positive charge and zeta potential was 25.80 ? 0.46 mV. The labeling efficiency for this condition was more than 95% and under this condition was stable for at least 6 h. Radioactivity

  8. Morpho-physiological effects of ibuprofen on Scenedesmus rubescens.

    Science.gov (United States)

    Moro, Isabella; Matozzo, Valerio; Piovan, Anna; Moschin, Emanuela; Vecchia, Francesca Dalla

    2014-09-01

    The pollution of aquatic bodies by drugs is an emerging environmental problem, because of their extensive use in animal and human context. Ibuprofen, 2-[4-(2-methylpropyl)phenyl]propanoic acid, is the non-steroidal anti-inflammatory drug mainly present both in wastewater and in rivers and lakes in Europe. Since in literature there is little information about the effects of ibuprofen on microalgae, in this paper we presented the results on the effects of this molecule at different concentrations (62.5μgL(-1), 250μgL(-1) and 1000μgL(-1)) on cultures of the freshwater microalga Scenedesmus rubescens (P.J.L. Dangeard) E. Kesslet et al. Ibuprofen effects on the alga were assayed at first through analyses of the growth curve. Moreover, analyses of cell morphology, ultrastructure, and photosynthetic pigments were additionally performed. The first negative effect of the drug was on the microalga growth, suggesting a drug action dose-dependent mechanism type, more evident at the concentration of 1000μgL(-1) ibuprofen and in the last phase of the growth curve. In support of this, following ibuprofen exposure, the cells exhibited morphological and ultrastructural alterations, mainly consisting in large cytoplasmic inclusions, probably of lipids and/or carotenoids. The decrease of chlorophyll amounts and, on the contrary, the increase of carotenoids were correlated with a stressful condition induced by drug. Copyright © 2014 Elsevier B.V. All rights reserved.

  9. APPLICATION OF POWDERY ACTIVATED CARBONS FOR REMOVAL IBUPROFEN FROM WATER

    Directory of Open Access Journals (Sweden)

    Alicja Puszkarewicz

    2017-07-01

    Full Text Available The paper presents results of studies on the use of adsorptive properties of selected powdered activated carbons (Norit SA Super and Carbopol MB5 for removal of ibuprofen from water. The tests were performed on non-flow conditions, series depending on the type and dose of powdered adsorbents. The research was carried out on a model solution of ibuprofen at initial concentration C0 = 20 mg/dm3, at 200 C. Froundlich and Langmuir adsorption isotherms were used. Lagergrene kinetic models (PFO and Ho (PSO were used to describe adsorption kinetics. Both carbons exhibited a higher affinity for the adsorbent at a pH above 7. The better adsorbent was the Norit SA Super, for which, the highest adsorption capacity q = 0.448 g/g was achieved with dose D = 35 mg/dm3. The effectiveness of adsorption (decrease of ibuprofen in water was 78%. Total removal of ibuprofen was obtained for a dose of carbon D = 200 mg/dm3. With respect to Carbopol, the highest adsorption capacity (q = 0.353 g / g was achieved at a dose of 30 mg / dm3, resulting in a 53% efficiency. Studies have shown that both tested powdered activated carbons have contributed to effective cleaning of aqueous solutions containing ibuprofen.

  10. Formulation optimization of gentamicin loaded Eudragit RS100 microspheres using factorial design study.

    Science.gov (United States)

    Singh, Deependra; Saraf, Swarnlata; Dixit, Vinod Kumar; Saraf, Shailendra

    2008-04-01

    Gentamicin-Eudragit RS100 microspheres were prepared by modified double emulsion method. A 3(2) full factorial experiment was designed to study the effects of the composition of outer aqueous phase in terms of amount of glycerol (viscosity effect) and sodium chloride (osmotic pressure gradient effect) on the entrapment efficiency and % yield and microsphere size. The results of analysis of variance test for responses measured indicated that the test is significant (p>0.05). The contribution of sodium chloride concentration was found to be higher on entrapment efficiency and % yield, whereas glycerol produced significant effect on the mean diameter of microspheres. Microspheres demonstrated spherical particles in the size range of 33.24-60.43 microm. In vitro release profile of optimized formulation demonstrated sustained release for 24 h following Higuchi kinetics. Finally, drug bioactivity was found to remain intact after microencapsulation. Response surface graphs are presented to examine the effects of independent variables on the responses studied. Thus, by formulation design important parameters affecting formulation characteristics of gentamicin loaded Eudragit RS100 microspheres can be identified for controlled delivery with desirable characters in terms of maximum entrapment and yield.

  11. Molecular Basis for Allosteric Inhibition of Acid-Sensing Ion Channel 1a by Ibuprofen

    DEFF Research Database (Denmark)

    Lynagh, Timothy; Romero-Rojo, José Luis; Lund, Camilla

    2017-01-01

    -clamp fluorometry. Our results show that ibuprofen is an allosteric inhibitor of ASIC1a, which binds to a crucial site in the agonist transduction pathway and causes conformational changes that oppose channel activation. Ibuprofen inhibits several ASIC subtypes, but certain ibuprofen derivatives show some...

  12. Evaluation of radiolabelled microspheres as digesta markers

    International Nuclear Information System (INIS)

    Young, B.A.; Turner, B.V.; Dixon, A.E.; Exley, D.M.; Young, S.B.; Abidin, Z.

    1991-01-01

    The suitability of microspheres as markers for measuring digesta kinetics in sheep was examined. Microspheres offer advantages of uniformity of size and density, and stability during passage through the gastrointestinal tract. They are commercially available labelled with the choice of one of eleven different radionuclides and can be easily measured in digesta and faecal material. Tests comparing several types of digesta markers gave different measures of kinetic parameters when the measurements were made concurrently in the same sheep. However, concurrent measurements derived from use of microspheres were consistent. Microspheres offer a new alternative for digestive studies. (author). 19 refs, 4 tabs

  13. Development and gamma-scintigraphy study of Hibiscus rosasinensis polysaccharide-based microspheres for nasal drug delivery.

    Science.gov (United States)

    Sharma, Nitin; Tyagi, Shanu; Gupta, Satish Kumar; Kulkarni, Giriraj Thirupathirao; Bhatnagar, Aseem; Kumar, Neeraj

    2016-11-01

    This work describes the application of natural plant polysaccharide as pharmaceutical mucoadhesive excipients in delivery systems to reduce the clearance rate through nasal cavity. Novel natural polysaccharide (Hibiscus rosasinensis)-based mucoadhesive microspheres were prepared by using emulsion crosslinking method for the delivery of rizatriptan benzoate (RB) through nasal route. Mucoadhesive microspheres were characterized for different parameters and nasal clearance of technetium-99m ((99m)Tc)-radiolabeled microspheres was determined by using gamma-scintigraphy. Their Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) studies showed that the drug was stable during preparation of microspheres. Aerodynamic diameter of microspheres was in the range 13.23 ± 1.83-33.57 ± 3.69 µm. Change in drug and polysaccharide ratio influenced the mucoadhesion, encapsulation efficiency and in-vitro release property. Scintigraphs taken at regular interval indicate that control solution was cleared rapidly from nasal cavity, whereas microspheres showed slower clearance (p < 0.005) with half-life of 160 min. Natural polysaccharide-based microspheres achieved extended residence by minimizing effect of mucociliary clearance with opportunity of sustained delivery for longer duration.

  14. Optimization of preparation method for ketoprofen-loaded microspheres consisting polymeric blends using simplex lattice mixture design

    Energy Technology Data Exchange (ETDEWEB)

    Das, Sanjoy Kumar, E-mail: sanjoydasju@gmail.com; Khanam, Jasmina; Nanda, Arunabha

    2016-12-01

    In the present investigation, simplex lattice mixture design was applied for formulation development and optimization of a controlled release dosage form of ketoprofen microspheres consisting polymers like ethylcellulose and Eudragit{sup ®}RL 100; when those were formed by oil-in-oil emulsion solvent evaporation method. The investigation was carried out to observe the effects of polymer amount, stirring speed and emulsifier concentration (% w/w) on percentage yield, average particle size, drug entrapment efficiency and in vitro drug release in 8 h from the microspheres. Analysis of variance (ANOVA) was used to estimate the significance of the models. Based on the desirability function approach numerical optimization was carried out. Optimized formulation (KTF-O) showed close match between actual and predicted responses with desirability factor 0.811. No adverse reaction between drug and polymers were observed on the basis of Fourier transform infrared (FTIR) spectroscopy and Differential scanning calorimetric (DSC) analysis. Scanning electron microscopy (SEM) was carried out to show discreteness of microspheres (149.2 ± 1.25 μm) and their surface conditions during pre and post dissolution operations. The drug release pattern from KTF-O was best explained by Korsmeyer-Peppas and Higuchi models. The batch of optimized microspheres were found with maximum entrapment (~ 90%), minimum loss (~ 10%) and prolonged drug release for 8 h (91.25%) which may be considered as favourable criteria of controlled release dosage form. - Graphical abstract: Optimization of preparation method for ketoprofen-loaded microspheres consisting polymeric blends using simplex lattice mixture design. - Highlights: • Simplex lattice design was used to optimize ketoprofen-loaded microspheres. • Polymeric blend (Ethylcellulose and Eudragit® RL 100) was used. • Microspheres were prepared by oil-in-oil emulsion solvent evaporation method. • Optimized formulation depicted favourable

  15. Formulation and in vitro Evaluation of Eudragit® Microspheres of ...

    African Journals Online (AJOL)

    The prepared microspheres were characterized for their micromeritic properties and drug loading, as well by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, x-ray powder diffractometry and scanning electron microscopy. The in vitro release studies were performed in pH 6.8, phosphate buffer ...

  16. Enhancement of transdermal delivery of ibuprofen using microemulsion vehicle.

    Science.gov (United States)

    Hu, Liandong; Hu, Qiaofeng; Yang, Jianxue

    2014-10-01

    The objective of this study was to find a stable microemulsion vehicle for transdermal delivery of ibuprofen to improve the skin permeability. Microemulsion was prepared using different sorts of oils, surfactants and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The effects of oleic acid and surfactant mixture on skin permeation of ibuprofen were evaluated with excised skins. The optimum formulation F3 consisting of 6% oleic acid, 30% Cremophor RH40/Transcutol P (2:1, w/w) and 59% water phase, showed a high permeation rate of 42.98 µg/cm(2)/hr. The mean droplet size of microemulsion was about 43 nm and no skin irritation signs were observed on the skin of rabbits. These results indicated that this novel microemulsion is a useful formulation for the transdermal delivery of ibuprofen.

  17. Growth, spectral and thermal studies of ibuprofen crystals

    Energy Technology Data Exchange (ETDEWEB)

    Ramukutty, S.; Ramachandran, E. [Department of Physics, Thiruvalluvar College, Papanasam (India)

    2012-01-15

    RS -Ibuprofen was crystallized for the first time in silica gel under suitable pH conditions by reduction of solubility method. The grown crystals were characterized by single crystal X-ray diffraction and density measurement. The functional groups present in the crystal were identified using Fourier transform infrared spectroscopy. Optical bandgap energy of ibuprofen was estimated as 3.19(3) eV from UV-Vis spectrum. Thermogravimetric analysis revealed that ibuprofen is thermally stable upto 102.9 C and the initial loss of mass was due to evaporation only. Morphological study showed that the growth is prominent along b-axis and the prominent face is {l_brace}100{r_brace}. (copyright 2012 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim) (orig.)

  18. Enteric coating of ibuprofen tablets (200 mg using an aqueous dispersion system

    Directory of Open Access Journals (Sweden)

    Rabia Bushra

    2010-03-01

    Full Text Available Ibuprofen is a propionic acid derivative that belongs to the class NSAIDs. Major adverse reactions associated with Ibuprofen are related to GIT and include peptic and mucosal ulcers, dyspepsia, severe gastric pain and bleeding, that results in excessive treatment failure. The goal of this study was to develop enteric coated ibuprofen tablets in order to avoid gastric mucosal irritation, diffusion of drug across mucosal lining and to let active ingredient be absorbed easily in small intestine. The formulation was developed and manufactured through the direct compression process, the simplest, easiest and most economical method of manufacturing. Enteric coating was done using an Opadry white subcoating and an aqueous coating dispersion of Acryl-Eze. Enteric coated formulation was subjected to disintegration and dissolution tests by placing in 0.1 M hydrochloric acid for 2 h and then 1 h in phosphate buffer with a pH of 6.8. About 0.04% of drug was released in the acidic phase and 99.05% in the basic medium. These results reflect that ibuprofen can be successfully enteric coated in order to prevent its release in the stomach and facilitate rapid release of the drug in the duodenum, due to the presence of superdisintegrant. Formulating this enteric coated tablets could increase patient compliance by decreasing adverse drug reactions (ADR S associated with Ibuprofen therapy.Ibuprofeno é um derivado do ácido propiônico, que pertence à classe dos fármacos não-esteróides (AINES. As principais reações adversas associadas com o ibuprofeno se referem àquelas do trato gastrintestinal (TGI, como úlceras pépticas e da mucosa, dispepsia, dor gástrica grave e sangramento, que resultam em muitas falhas de tratamento. O objetivo do estudo foi desenvolver comprimidos revestidos de ibuprofeno que impeçam a irritação da mucosa gástrica, difusão do fármaco através da mucosa e permitam, facilmente, a absorção do princípio ativo do intestino

  19. Ibuprofen Blunts Ventilatory Acclimatization to Sustained Hypoxia in Humans.

    Directory of Open Access Journals (Sweden)

    Kemal Erdem Basaran

    Full Text Available Ventilatory acclimatization to hypoxia is a time-dependent increase in ventilation and the hypoxic ventilatory response (HVR that involves neural plasticity in both carotid body chemoreceptors and brainstem respiratory centers. The mechanisms of such plasticity are not completely understood but recent animal studies show it can be blocked by administering ibuprofen, a nonsteroidal anti-inflammatory drug, during chronic hypoxia. We tested the hypothesis that ibuprofen would also block the increase in HVR with chronic hypoxia in humans in 15 healthy men and women using a double-blind, placebo controlled, cross-over trial. The isocapnic HVR was measured with standard methods in subjects treated with ibuprofen (400 mg every 8 hrs or placebo for 48 hours at sea level and 48 hours at high altitude (3,800 m. Subjects returned to sea level for at least 30 days prior to repeating the protocol with the opposite treatment. Ibuprofen significantly decreased the HVR after acclimatization to high altitude compared to placebo but it did not affect ventilation or arterial O2 saturation breathing ambient air at high altitude. Hence, compensatory responses prevent hypoventilation with decreased isocapnic ventilatory O2-sensitivity from ibuprofen at this altitude. The effect of ibuprofen to decrease the HVR in humans provides the first experimental evidence that a signaling mechanism described for ventilatory acclimatization to hypoxia in animal models also occurs in people. This establishes a foundation for the future experiments to test the potential role of different mechanisms for neural plasticity and ventilatory acclimatization in humans with chronic hypoxemia from lung disease.

  20. IBUPROFEN IN COMPLEX TREATMENT OF FEVER IN CHILDREN

    Directory of Open Access Journals (Sweden)

    А.А. Alexeeva

    2011-01-01

    Full Text Available Pain and fever are one of the most frequent conditions in pediatric practice. Frequent occurrence of fever accompanied by a pain syndrome stipulates combined antipyretic and analgesic medications. This article contains information upon ibuprofen use («Nurofen for children» in pediatric patients as an antipyretic and analgesic medication to be used as part of complex treatment of acute respiratory infections.Key words: fewer, children, ibuprofen. (Voprosy sovremennoi pediatrii — Current Pediatrics. — 2011; 10 (6: 137–140

  1. Spectral Analyses of a Novel Ibuprofen-Phillygenin Ester

    Directory of Open Access Journals (Sweden)

    FAN Hong-yu

    2018-03-01

    Full Text Available An ibuprofen-phillygenin ester was synthesized through the Schotten-Baumann reaction with ibuprofen and phillygenin as the starting materials. Ultraviolet absorption (UV spectrum, infrared absorption (IR spectrum, matrix-assisted laser desorption/ionization-mass spectra (MALDI-TOF-MS, and one-dimensional/two dimensional nuclear magnetic resonance (NMR spectra (i.e., 1H-NMR, 13C-NMR, 13C-DEPT, 1H-1H COSY, 1H-1H NOESY, 1H-13C HSQC and 1H-13C HMBC of the compound were collected. All 1H and 13C NMR signals were assigned.

  2. Cutaneous irritancy of an ibuprofen medicated plaster in healthy volunteers.

    Science.gov (United States)

    Maganji, Manisha; Connolly, Mark P; Bhatt, Aomesh

    2018-04-01

    To assess the irritation and contact sensitization potential of a 200 mg ibuprofen medicated plaster. This double-blind, phase-1 placebo controlled study had two phases; the induction phase to evaluate the irritant potential of continuous application of the plaster, and the challenge phase to assess contact sensitivity (allergy). The cumulative irritancy potential was evaluated using an adaptation of the Shelanski method. Healthy adults (≥18 years of age) (N = 210) were treated simultaneously with one ibuprofen medicated and one placebo plaster applied in a randomized fashion to either the left or right side of the lower back. During the induction phase, plasters were applied on Days 1, 3, 5, 8, 10, 12, 15, 17, and 19 and the final plaster removed on Day 22. At each scheduled visit plasters and applications sites were assessed for degree of adhesion and skin irritation (score of 1 = no irritation to 7 = strong reaction spreading beyond test sites), respectively. The challenge phase followed a two-week washout period. A plaster was applied on Day 36 for 48 h and assessment occurred on Days 38, 39, and 40. The mean cumulative irritation score during the induction phase was lower for the ibuprofen medicated plaster than the placebo plaster (0.32 vs. 1.23, respectively). Three (1.4%) subjects experience a dermal reaction of grade ≥3 for the ibuprofen medicated plaster compared with 27 (12.7%) for the placebo plaster. Following challenge with ibuprofen or placebo plasters, 12 subjects (6.2%) with the ibuprofen medicated plaster and four (2.2%) with the placebo plaster had skin reaction of assessment grade higher than the induction phase. One subject for the ibuprofen and two for the placebo plaster had reactions with grade >2. No subjects showed an increase in sensitization on Day 39 or 40 compared with Day 38. The findings indicate that the both the irritancy and contact sensitization of the ibuprofen medicated plaster is acceptable.

  3. Porous spherical shells and microspheres by electrodispersion precipitation

    International Nuclear Information System (INIS)

    Harris, M.T.; Sisson, W.G.; Basaran, O.A.; Hayes, S.M.; Bobrowski, S.J.

    1994-01-01

    The ability to reproduce the synthesis of dense- and porous-microspheres and micron-sized spherical shells is very important in (a) the development of ceramics for structural, electronic, catalyst and thermal applications; and (b) the encapsulation of products for controlled-release of drugs, flavors and perfumes, and inks and dyes, and the protection of light-sensitive components and mechanical support of fragile materials. Larger metallic- and ceramic-spherical shells have been used in inertial confinement fusion (ICF) experiments and as catalyst supports. The current paper will focus on a recent technique that has been developed for synthesizing ceramic microspheres and micro-shells. Pulsed electric fields have been used to enhance the dispersion of aqueous metal (Zr and Al) salt solutions from a nozzle and into a nonconducting liquid continuous phase that is immiscible with the aqueous phase. The diameter of the resulting microdroplets ranged in size from approximately 0.1 to 10 μm. Precipitation of hydrous metal oxides occurred as ammonia, which was dissolved in varying amounts in the continuous phase, diffused into the aqueous microdroplets. Spherical shells were formed at higher ammonia concentrations and microspheres were produced at lower ammonia concentrations. Upon drying, dimples appeared in the particles that were synthesized at higher ammonia concentrations. The latter result accords with the well known fact that under certain conditions spherical shells collapse when a fluid is extracted from the core of the particle. No dimples were observed in the microspheres that were produced at lower ammonia concentrations. Analog X-ray dot maps for aluminum and zirconium were done to determine the spatial distribution of each metal in the particles

  4. Glass microspheres for medical applications

    Science.gov (United States)

    Conzone, Samuel David

    Radioactive dysprosium lithium borate glass microspheres have been developed as biodegradable radiation delivery vehicles for the radiation synovectomy treatment of rheumatoid arthritis. Once injected into a diseased joint, the microspheres deliver a potent dose of radiation to the diseased tissue, while a non-uniform chemical reaction converts the glass into an amorphous, porous, hydrated dysprosium phosphate reaction product. The non-radioactive, lithium-borate component is dissolved from the glass (up to 94% weight loss), while the radioactive 165Dy reacts with phosphate anions in the body fluids, and becomes "chemically" trapped in a solid, dysprosium phosphate reaction product that has the same size as the un-reacted glass microsphere. Ethylene diamine tetraacetate (EDTA) chelation therapy can be used to dissolve the dysprosium phosphate reaction product after the radiation delivery has subsided. The dysprosium phosphate reaction product, which formed in vivo in the joint of a Sprague-Dawley rat, was dissolved by EDTA chelation therapy in 100 Gy) of localized beta radiation to a treatment site within the body, followed by complete biodegradability. The non-uniform reaction process is a desirable characteristic for a biodegradable radiation delivery vehicle, but it is also a novel material synthesis technique that can convert a glass to a highly porous materials with widely varying chemical composition by simple, low-temperature, glass/solution reaction. The reaction product formed by nonuniform reaction occupies the same volume as the un-reacted glass, and after drying for 1 h at 300°C, has a specific surface area of ≈200 m2/g, a pore size of ≈30 nm, and a nominal crushing strength of ≈10 MPa. Finally, rhenium glass microspheres, composed of micron-sized, metallic rhenium particles dispersed within a magnesium alumino borate glass matrix were produced by sintering ReO2 powder and glass frit at 1050°C. A 50 mg injection of radioactive rhenium glass

  5. Modeling the onset and offset of dental pain relief by ibuprofen.

    Science.gov (United States)

    Li, Hanbin; Mandema, Jaap; Wada, Russell; Jayawardena, Shyamalie; Desjardins, Paul; Doyle, Geraldine; Kellstein, David

    2012-01-01

    Onset and offset of dental pain relief by ibuprofen following third molar extraction were modeled in a randomized, double-blind, placebo-controlled, parallel-group, 8-hour study of patients receiving either a novel effervescent ibuprofen tablet (400 mg; N = 30), standard ibuprofen tablets (Nurofen(®) 2 × 200 mg; N = 22), or placebo (N = 37). An Emax model was fit to pain relief scores. Linear hazard models were used to analyze the time to first perceptible relief (TFPR), the time to meaningful pain relief (TMPR), and time to remedication (REMD). Nomograms were created to correlate TFPR, TMPR, and REMD with different ibuprofen pharmacokinetic profiles. Effervescent ibuprofen was absorbed rapidly with 95% completion within 15 minutes. Maximum pain relief score by ibuprofen was 1.8 units greater than placebo, with an EC50 (effect-site) for ibuprofen concentration of 10.2 µg·mL(-1). The likelihood to achieve TFPR and TMPR was doubled for every 10 µg·mL(-1) increase in ibuprofen plasma concentration. REMD risk decreased 40-fold as the categorical pain relief score increased from 0 to 3. Rapid absorption of ibuprofen effervescent resulted in an earlier TFPR and TMPR, and a lower REMD rate than standard ibuprofen. The nomograms may be useful in predicting the onset and offset of new faster acting ibuprofen formulations, based on pharmacokinetic profiles.

  6. In vitro evaluation and intra-articular administration of biodegradable microspheres containing naproxen sodium.

    Science.gov (United States)

    Bozdağ, S; Caliş, S; Kaş, H S; Ercan, M T; Peksoy, I; Hincal, A A

    2001-01-01

    The dispersion of non-steroidal antiinflammatory drugs (NSAIDs) into biodegradable polymeric matrices have been accepted as a good approach for obtaining a therapeutic effect in a predetermined period of time meanwhile minimizing the side effects of NSAIDs. In the present study, it was aimed to prepare Naproxen Sodium (NS), (a NSAID) loaded microsphere formulation using natural Bovine Serum Albumin (BSA) and synthetic biodegradable polymers such as poly(lactide-co-glycolic acid) (PLGA) (50:50 MW 34,000 and 88,000 Da) for intra-articular administration, and to study the retention of the drug at the site of injection in the knee joint. NS incorporated microspheres were evaluated in vitro for particle size (the mean particle size; for BSA microspheres, 10.0 +/- 0.3 microm, for PLGA microspheres, 9.0 +/- 0.2 and 5.0 +/- 0.1 microm for MW 34,000 and 88,000 Da, respectively), yield value, drug loading, surface morphology and drug release. For in vivo studies, monoarticular arthritis was induced in the left knee joints of rabbits by using ovalbumin and Freund's Complete Adjuvant as antigen and adjuvant. A certain time (4 days) is allowed for the formation of arthritis in the knee joints, then the NS loaded microspheres were injected directly into the articular cavity. At specific time points, gamma scintigrams were obtained to determine the residence time of the microspheres in knee joints, in order to determine the most suitable formulation. This study indicated that PLGA, a synthetic polymer, is more promising than the natural type BSA microspheres for an effective cure of mono-articular arthritis in rabbits.

  7. Preparation And Biodistribution Study Of 153sm-Albumin Microspheres As Radiosynovectomy Agent

    International Nuclear Information System (INIS)

    W, Widyatuti; Tamat, Swasono R.; Indrawati, Teti; Fatimah; Aulya, Anna

    2003-01-01

    Treatment of rheumatics arthritis previously was done by inflamed synovial membrane surgery called synovectomy. The conventional synovectomy was costly and inconvenient method for the patients, therefore alternative method using radiation synovectomy was considered. Preparation of 153 Sm albumin microspheres as radio synovectomy agent has been candied out. Experiments have been carried out to decide optimal conditions of preparation, such as speed and time of stirring to form microspheres, and to find optimal condition in labelling the microspheres, such as pH, content of sodium citrate, samarium oxide and the amount of microspheres. The albumin particles were expected as spheres with 15-50 μm in diameter, high labelling efficiency and 153 Sm is strongly bound to the microspheres. In-vitro and in-vivo stability were tested by observing 153 Sm released from the particles after incubating the labelled particles in saline and human serum albumin solution for one week, and after administration of labelled particles into Wistar rats via intraarticular injection through one of its knee joint. The result shows the optimal speed and time of stirring to obtain desired shape and size of the particles was 750 rpm in 15 minutes, while the optimal formulation to obtain high labelling efficiency was at pH 5-6, containing 10 μg/mL of sodium citrate, 125 μg/mL of samarium oxide and 10 mg of albumin microspheres. The preparation was stable up to 5 days. In conclusion the 153 Sm-albumin microspheres can be produced and is ready for clinical trial

  8. Microsphere estimates of blood flow: Methodological considerations

    International Nuclear Information System (INIS)

    von Ritter, C.; Hinder, R.A.; Womack, W.; Bauerfeind, P.; Fimmel, C.J.; Kvietys, P.R.; Granger, D.N.; Blum, A.L.

    1988-01-01

    The microsphere technique is a standard method for measuring blood flow in experimental animals. Sporadic reports have appeared outlining the limitations of this method. In this study the authors have systematically assessed the effect of blood withdrawals for reference sampling, microsphere numbers, and anesthesia on blood flow estimates using radioactive microspheres in dogs. Experiments were performed on 18 conscious and 12 anesthetized dogs. Four blood flow estimates were performed over 120 min using 1 x 10 6 microspheres each time. The effects of excessive numbers of microspheres pentobarbital sodium anesthesia, and replacement of volume loss for reference samples with dextran 70 were assessed. In both conscious and anesthetized dogs a progressive decrease in gastric mucosal blood flow and cardiac output was observed over 120 min. This was also observed in the pancreas in conscious dogs. The major factor responsible for these changes was the volume loss due to the reference sample withdrawals. Replacement of the withdrawn blood with dextran 70 led to stable blood flows to all organs. The injection of excessive numbers of microspheres did not modify hemodynamics to a greater extent than did the injection of 4 million microspheres. Anesthesia exerted no influence on blood flow other than raising coronary flow. The authors conclude that although blood flow to the gastric mucosa and the pancreas is sensitive to the minor hemodynamic changes associated with the microsphere technique, replacement of volume loss for reference samples ensures stable blood flow to all organs over a 120-min period

  9. Thermal analysis of iron hydroxide microspheres

    International Nuclear Information System (INIS)

    Turcanu, C.N.; Cornescu, M.

    1979-03-01

    The thermal treatment is an important step in the preparative technology of the iron oxids microspheres with well established mechanical, physical and chemical characteristics. The first indications on the heating procedure have been obtained from the thermal analysis on iron hydroxide microspheres prepared by the support precipitation and internal gelification methods. (author)

  10. Encapsulated PDMS microspheres with reactive handles

    DEFF Research Database (Denmark)

    Gonzalez, Lidia; Ma, Baoguang; Li, Li

    2014-01-01

    , cured PDMS microspheres are coated with poly(methyl methacrylate) using a chemical process (solvent evaporation technique). Three solvents are used in three different experiments: dichloromethane, tetrahydrofuran, and acetone. The composition and morphology of the cured PDMS microspheres and PMMA coated...

  11. Microencapsulation and microspheres for food applications

    NARCIS (Netherlands)

    Sagis, L.M.C.

    2015-01-01

    This book provides an update on the latest developments, challenges, and opportunities in the highly expanding field of microencapsulation and microspheres for food applications, examining the various types of microspheres and microcapsules essential to those who need to develop stable and

  12. Radioiodination of ibuprofen with 125I and its biological behavior in mice

    International Nuclear Information System (INIS)

    Amin, A. M.; Abd El-bary, A.; Shoukry, M. and other

    2012-12-01

    A procedure for radioiodination of Ibuprofen with iodine-125 is carried out via an electrophilic substitution reaction. The reaction parameters were studied Ibuprofen concentration, pH of the reaction mixture, reaction time temperature, and different oxidizing agents to optimize the conditions for the labeling of Ibuprofen to abstain a high radiochemical yield of 1 25I -Ibuprofen (1 25I -Ib up). Using 3.7 MBq of of Na 1 25I , 100μg of ibuprofen as substrate and 100μg of iodogen as oxidizing agent in ethanol at 60 O C for 10 min, a maximum radiochemical yield of 1 25I -Ib up (78%) was obtained. The labeled compound was separated and purified from inactive Ibuprofen by means of high-pressure liquid chromatography (HPLC). The biological distribution in normal and inflamed mice indicates the suitability of radioiodinated Ibuprofen for imaging of inflammation only induced with turpentine oil. (Author)

  13. In vitro and in vivo therapeutic activity of ibuprofen against dermatophytes

    International Nuclear Information System (INIS)

    AlJanabi, Ali S

    2009-01-01

    To evaluate the in vitro and in vivo therapeutic activity of ibuprofen against dermatophytes. The period of study ranged from June to September 2008. For in vitro investigation of ibuprofen activity, measurement of colony diameter, and dry weight were employed against 4 isolated strains of dermatophytes from 46 patients (30-43 years) suffering from dermatophytoses at Morgan Hospital, Hilla City, Iraq in June 2008. For the in vivo evaluation of ibuprofen, rabbits as the main subjects, were infected with dermatophytes and treated with prepared ibuprofen cream (15mg/gm). In vitro application of ibuprofen showed cidal activity on 4 strains of dermatophytes at minimum inhibitory concentrations of 200 ug/ml. The infected rabbits were successfully cured of dermatophytoses after treatment with ibuprofen cream. Based on in vitro and in vivo application, Ibuprofen can be used as a short-term cure for dermatophytoses. (author)

  14. U3O8 microspheres sintering kinetics

    International Nuclear Information System (INIS)

    Godoy, A.L.E.

    1986-01-01

    U 3 O 8 microspheres sintering kinetics was determined using a hot-stage optical microscopy apparatus, able to reach temperature up to 1350 0 C in controlled atmospheres. The sintered material had its microstructure analysed by optical and electron microscopy. The microspheres were characterized initialy utilizing X-ray diffractometry and thermogravimetry. The equation which describes the microspheres shrinkage in function of the time was obtained using finite difference analysis X-ray diffractometry indicated hexagonal structure for the microspheres main starting material, ammonium diuranate thermogravimetric analysis showed reduction of this material to U 3 O 8 at 600 0 C. Ceramography results showed 5 hours sintered microspheres grain sizes G vary with the temperature. Sintered U 3 O 8 micrographs compared with published results for UO 2 , indicate similar homogeneity microstructural characteristics and suggest the processed micorspheres to be potentially useful as nuclear fuels. (Author) [pt

  15. Magnetic susceptibility characterisation of superparamagnetic microspheres

    Science.gov (United States)

    Grob, David Tim; Wise, Naomi; Oduwole, Olayinka; Sheard, Steve

    2018-04-01

    The separation of magnetic materials in microsystems using magnetophoresis has increased in popularity. The wide variety and availability of magnetic beads has fuelled this drive. It is important to know the magnetic characteristics of the microspheres in order to accurately use them in separation processes integrated on a lab-on-a-chip device. To investigate the magnetic susceptibility of magnetic microspheres, the magnetic responsiveness of three types of Dynabeads microspheres were tested using two different approaches. The magnetophoretic mobility of individual microspheres is studied using a particle tracking system and the magnetization of each type of Dynabeads microsphere is measured using SQUID relaxometry. The magnetic beads' susceptibility is obtained at four different applied magnetic fields in the range of 38-70 mT for both the mobility and SQUID measurements. The susceptibility values in both approaches show a consistent magnetic field dependence.

  16. Physico-mechanical and dissolution behaviours of ibuprofen crystals crystallized in the presence of various additives

    Directory of Open Access Journals (Sweden)

    A Nokhodchi

    2010-06-01

    Full Text Available "n  "n Background and the purpose of the study: The success of any direct-tableting procedure is strongly affected by the quality of the crystals used in the process. Ibuprofen is a poorly compactible drug with a high tendency for capping. In order to use ibuprofen in direct compression formulations, physico-mechanical properties of ibuprofen should be improved considerably. The aim of the present investigation was to employ crystallization techniques in order to improve the physico-mechanical properties of ibuprofen for direct compression. "nMethods:The experimental methods involved the preparation of ibuprofen crystals by solvent change technique. Ibuprofen was dissolved in ethanol and crystallized out with water in the absence or presence of various hydrophilic additives (PEG 6000, 8000, Brij 98P and polyvinyl alcohol 22000, PVA 22000 with different concentrations. The physico-mechanical properties of the ibuprofen crystals were studied in terms of flow, density, tensile strength and dissolution behaviour. Morphology of ibuprofen crystals was studied by scanning electron microscopic (SEM. Solid state of the recrystallized particles was also investigated using differential scanning calorimeter (DSC and FT-IR. "nResults:Ibuprofen samples crystallized in the presence of PEG 6000 and 8000 and PVA showed remarkable increase in the tensile strengths of the directly compressed tablets, while some other additives, i.e. Brij 98P did not produce improved ibuprofen crystals. Ibuprofen powders made from particles obtained in the presence of PVA and Brij 98P showed similar dissolution profiles to the commercial ibuprofen particles. DSC and FT-IR results ruled out any significant interaction between ibuprofen and additives except for the samples crystallized in the presence of PEG 8000. Conclusion:The crystal habit of ibuprofen can be altered successfully by the crystallization technique which was developed in this study. The crystals developed in the

  17. Silver-functionalized carbon nanofiber composite electrodes for ibuprofen detection

    NARCIS (Netherlands)

    Manea, F.; Motoc, S.; Pop, A.; Remes, A.; Schoonman, J.

    2012-01-01

    The aim of this study is to prepare and characterize two types of silver-functionalized carbon nanofiber (CNF) composite electrodes, i.e., silver-decorated CNF-epoxy and silver-modified natural zeolite-CNF-epoxy composite electrodes suitable for ibuprofen detection in aqueous solution. Ag carbon

  18. Premarketing surveillance of ibuprofen suppositories in febrile children.

    Science.gov (United States)

    Hadas, Dan; Youngster, Ilan; Cohen, Avner; Leibovitch, Eugene; Shavit, Itai; Erez, Ilan; Uziel, Yosef; Berkovitch, Matitiahu

    2011-03-01

    In many countries, ibuprofen is available only in oral formulations. The authors aimed to investigate parental satisfaction and possible adverse reactions among children receiving newly marketed ibuprofen suppositories, prior to their arrival at the pharmaceutical points of distribution. Children needing antipyretic medication were recruited from 11 pediatric wards and clinics in Israel. Each patient received ibuprofen suppositories (5-10 mg/kg/dose) after completing a data collection form. After 3 to 7 days of treatment, information regarding parent satisfaction, possible adverse reactions, and concomitant use of drugs was obtained. Overall, 490 children completed the study. Parents' satisfaction was high (4.5 ± 0.47 on a scale of 1-5), and 92.2% reported that they would use the medication in the future. Adverse reactions were reported in 8 patients (1.63%, 95% confidence interval = 1.77-3.25), the most common being diarrhea. Rectal administration of ibuprofen suppositories is well tolerated and overall satisfaction and the repeated expected use were high.

  19. Jejunal perforation by swallowed ibuprofen caplet | Njoku | Nigerian ...

    African Journals Online (AJOL)

    We present a case of jejunal perforation caused by an unusual foreign body, an ibuprofen caplet in its blister packing believed to be the first of its kind, perforation of the intestine caused by an ingested medication. The patient eventually developed an enterocutaneous fistula through the weak wall of a preexisting incisional ...

  20. Synthesis of Ibuprofen in the Introductory Organic Laboratory

    Science.gov (United States)

    Kjonaas, Richard A.; Williams, Peggy E.; Counce, David A.; Crawley, Lindsey R.

    2011-01-01

    A method for the synthesis of ibuprofen in introductory organic chemistry laboratory courses is reported. This experiment requires two 3-h lab sessions. All of the reactions and techniques are a standard part of any introductory organic chemistry course. In the first lab session, students reduce p-isobutylacetophenone to an alcohol and then…

  1. A sonochemical route for the encapsulation of drug in magnetic microspheres

    International Nuclear Information System (INIS)

    Wu Shixi; Jiang Wei; Zhang Xiaojuan; Sun Huan; Zhang Wenyao; Dai Junjun; Liu Li; Chen Xiaolong; Li Fengsheng

    2012-01-01

    This study focused on the preparation and characterization of magnetic targeted antibiotic microspheres (MTAMs). MTAMs were prepared by a sonochemical method in the presence of hydrophobic Fe 3 O 4 nanoparticles and tetracycline. The properties of MTAMs were characterized by transmission electron microscopy, Fourier-transform infrared spectrum, thermogravimetric analysis, vibration sample magnetometry, and bacteriostatic experiment. The results indicated that the superparamagnetic microspheres have ultrafine size (below 230 nm), high saturation magnetization (80.90 emu/g), high biocompatibility, biodegradability, controlled-release, and antibiotic effect. It has been proved that MTAMs can carry out the function of magnetic targeted drugs delivery system by putting together magnetic materials and antibiotics. The possible formation mechanism of MTAMs was also discussed. In summary, MTAMs had potential in medical imaging, drug targeting, and catalysis. - Highlights: → Microspheres carry out the function of magnetic targeted drugs delivery system. → Microspheres exhibit high saturation magnetization and antibiotic effect. → Microspheres have a potential application in the biomedical field. → The sonochemical method is well controlled for the synthesis.

  2. Enhancing Photocatalytic Performance through Tuning the Interfacial Process between -Assembled and Pt-Loaded Microspheres

    Directory of Open Access Journals (Sweden)

    Jun Zhang

    2012-01-01

    Full Text Available This work reports on a simple two-step approach to rutile TiO2-assembled microspheres loaded by Pt with an aim to tune semiconductor-metal interfacial processes for enhancing the photocatalytic performance. Systematic sample characterizations and structural analysis indicate that Pt loading did not produce any significant influences on the lattice structure of TiO2-assembled microspheres. Instead, upon Pt loading, Schottky barrier was formed in the interfaces between microspheres and Pt nanoparticles, which inhabited efficiently the recombination of photo-generated electron-hole pairs essential for the photocatalytic activities. In addition, TiO2 microspheres also showed a capacity of electrons storage and releasing as represented by a high dielectric constant, which increased the utility rate of photogenerated electrons. All these structural advantages contribute to the excellent photocatalytic activity under ultraviolet light irradiation. The interfacial process between microspheres and Pt nanoparticles was further tuned through adjusting the loading Pt content of metal Pt. As a consequence, the best photocatalytic activity on TiO2 was obtained at 0.85 wt% Pt loading, above or below which photocatalytic activity was apparently decreased.

  3. Pharmacokinetics of Cromolyn and Ibuprofen in Healthy Elderly Volunteers.

    Science.gov (United States)

    Brazier, David; Perry, Robert; Keane, Jim; Barrett, Katie; Elmaleh, David R

    2017-11-01

    BACKGROUND AND OBJECTIVES: The combination of cromolyn and ibuprofen is being investigated as a treatment for early Alzheimer's disease (AD). This study investigated the pharmacokinetics, safety, and tolerability of cromolyn and ibuprofen co-administration in healthy elderly adult volunteers. In this open-labeled study, 26 subjects, aged 55-75 years, received co-administration of inhaled cromolyn (single dose 17.1 mg; double dose 34.2 mg total) and oral ibuprofen (single dose 10 mg; double dose 20 mg total). Blood sampling was performed for 6 h after co-administration in all subjects; cerebrospinal fluid (CSF) was collected in three to four subjects per cohort for 4 h following co-administration. Safety parameters, including adverse events (AEs), were monitored throughout the study. For cromolyn, the mean (±SD) maximum observed concentration (C max ) in plasma was 46.69 ± 32.97 and 96.75 ± 46.22 ng/ml after single- and double-dose inhalation, respectively [time to C max (t max ) ~22 min for each; terminal elimination half-life (t ½ ) ~1.8 h for each]. For ibuprofen, the plasma C max was 1090.98 ± 474.64 ng/ml and 2062.96 ± 655.13 ng/ml after single- and double-dose oral administration, respectively (t max ~1.6-1.8 h; t ½ ~1.9 h for each). For cromolyn, the CSF C max was 0.24 ± 0.08 ng/ml at 3.72 ± 0.70 h after single-dose administration and 0.34 ± 0.17 ng/ml at 3.45 ± 0.95 h after double-dose administration, and for ibuprofen, the CSF C max was 3.94 ± 1.29 ng/ml at 2.55 ± 0.96 h after single-dose administration and 8.93 ± 3.29 ng/ml at 3.15 ± 1.05 h after double-dose administration. Three (12%) subjects reported mild or moderate AEs which were unlikely to be related to study drug. The combination of cromolyn and ibuprofen was safe and well tolerated. The concentrations of cromolyn and ibuprofen observed in the CSF are considered sufficient to titrate the estimated daily amyloid production and the associated inflammatory response

  4. Rifapentine-linezolid-loaded PLGA microspheres for interventional therapy of cavitary pulmonary tuberculosis: preparation and in vitro characterization

    Directory of Open Access Journals (Sweden)

    Huang J

    2017-03-01

    Full Text Available Jieyun Huang,1,* Zhi Chen,2,* Ying Li,3 Li Li,2 Guangyu Zhang2 1The Second Clinical Medical College, Shanxi Medical University, Taiyuan, People’s Republic of China; 2Institute for Tuberculosis Research, The 309th Hospital of Chinese PLA, Beijing, People’s Republic of China; 3Department of Drug Delivery Research Center, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, People’s Republic of China *These authors contributed equally to this work Abstract: In this study, we aimed to design controlled-release microspheres for the treatment of cavitary pulmonary tuberculosis (TB for solving the issues of poor drug delivery and short duration maintained at effective drug concentration during bronchoscopic interventional therapy. We fabricated rifapentine-linezolid-loaded poly(lactic acid-co-glycolic acid microspheres (RLPMs using the oil-in-water emulsion solvent evaporation method and assessed their in vitro release as well as the bronchial mucosal retention characteristics. The microspheres are spherical in shape with a circular concave on the surface. The particle size of RLPMs was 27.38±1.28 µm. The drug loading of rifapentine and linezolid was 18.51±0.26 and 8.42%±0.24%, respectively, while the encapsulation efficiencies were 55.53±0.78 and 16.87%±0.47%, respectively (n=3. During the burst release phase of the in vitro release test, 21.37%±0.68% rifapentine was released in 3 days and 43.56%±2.54% linezolid was released in 1 day. Then, both the drugs entered the sustained release phase. Finally, the cumulative percentage release of rifapentine and linezolid in 14 days was 27.61±1.52 and 51.01%±3.31%, respectively (n=3. Bronchoscopic observation revealed that the controlled-release microspheres could slowly release the drugs and retain them on the surface of bronchial mucosa of canines for 20 days. These results indicated that the fabricated microspheres exhibited

  5. Thermodynamic study of ibuprofen by adiabatic calorimetry and thermal analysis

    International Nuclear Information System (INIS)

    Xu Fen; Sun Lixian; Tan Zhicheng; Liang Jianguo; Li Ruilian

    2004-01-01

    Molar heat capacities of ibuprofen were precisely measured with a small sample precision automated adiabatic calorimeter over the temperature range from 80 to 400 K. The polynomial functions of C p,m (J K -1 mol -1 ) versus T were established on the heat capacity measurements by means of the least fitting square method. The functions are as follows: for solid ibuprofen, at the temperature range of 79.105 K≤T≤333.297 K, C p,m =144.27+77.046X+3.5171X 2 +10.925X 3 +11.224X 4 , where X=(T-206.201)/127.096; for liquid ibuprofen, at the temperature range of 353.406 K≤T≤378.785 K, C p,m =325.79+8.9696X-1.6073X 2 -1.5145X 3 , where X=(T-366.095)/12.690. A fusion transition at T=348.02 K was found from the C p -T curve. The molar enthalpy and entropy of the fusion transition were determined to be 26.65 kJ mol -1 and 76.58 J mol -1 K -1 , respectively. The thermodynamic functions on the base of the reference temperature of 298.15 K, (H T -H 298.15 ) and (S T -S 298.15 ), were derived. Thermal characteristic of ibuprofen was studied by thermo-gravimetric analysis (TG-DTG) and differential scanning calorimeter (DSC). The temperature of fusion, the molar enthalpy and entropy of fusion obtained by DSC were well consistent with those obtained by adiabatic calorimeter. The evaporation process of ibuprofen was investigated further by TG and DTG, and the activation energy of the evaporation process was determined to be 80.3±1.4 kJ mol -1

  6. Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation.

    Science.gov (United States)

    Sharma, Neelam; Arora, Sandeep; Madan, Jitender

    2018-02-01

    Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management. Microspheres were synthesized using poly-3-hydroxybutyrate and poly-(ɛ-caprolactone) by double emulsion solvent evaporation technique. NPH-MS were characterized through FTIR, PXRD and SEM. In-vitro drug release study revealed sustained behavior till 24 h. Haemolysis was pain model, reversal of mechanical allodynia and thermal hyperalgesia by NPH-MS was statistically significant (p < .001) as compared with NPH till 24 h post-dose.

  7. Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

    OpenAIRE

    Szekalska, Marta; Wróblewska, Magdalena; Sosnowska, Katarzyna; Winnicka, Katarzyna

    2016-01-01

    Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9) with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1) and different sodium alginate concentration (1%, 2%, and 3%) were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree. In vitro drug release, mathematical release profile, and physical state of microspheres were also evaluated. Op...

  8. Novel local drug delivery system using thermoreversible gel in combination with polymeric microspheres or liposomes.

    Science.gov (United States)

    Arai, Takao; Benny, Ofra; Joki, Tatsuhiro; Menon, Lata G; Machluf, Marcelle; Abe, Toshiaki; Carroll, Rona S; Black, Peter M

    2010-04-01

    The purpose of our study was to evaluate the application of thermoreversible gelation polymer (TGP) as a local drug delivery system for malignant glioma. Polymeric microspheres or liposomes loaded with doxorubicin (sphere-dox or lipo-dox) were combined with TGP to provide continuous drug delivery of doxorubicin (dox) for kinetic release studies and cell viability assays on glioma cell lines in vitro. For in vivo studies, TGP loaded with dox alone (TGP-dox) was combined with sphere-dox or lipo-dox. Their antitumor effects on subcutaneous human glioma xenografts were evaluated in nude mice. In vitro, TGP combined with sphere-dox or lipo-dox released dox for up to 30 days. In vivo, TGP-dox combined with sphere-dox or lipo-dox inhibited subcutaneous glioma tumor growth until day 32 and day 38, respectively. TGP in combination with microspheres or liposomes successfully prolonged the release of dox and its antitumor effects.

  9. Thermodynamic study of complex formation of β-cyclodextrin with ibuprofen by conductometric method and determination of ibuprofen in pharmaceutical drugs

    Directory of Open Access Journals (Sweden)

    Somayeh Heydari

    2017-02-01

    Based on the obtained results, a conductometric method for the determination of ibuprofen in the presence of β-CD at 25 °C was developed in the range of 10−3–10−5 mol dm−1. The method was satisfactorily applied to the quantification of ibuprofen in pharmaceutical preparations.

  10. Progress in Preparation of Monodisperse Polymer Microspheres

    Science.gov (United States)

    Zhang, Hongyan

    2017-12-01

    The monodisperse crosslinked polymer microspheres have attracted much attention because of their superior thermal and solvent resistance, mechanical strength, surface activity and adsorption properties. They are of wide prospects for using in many fields such as biomedicine, electronic science, information technology, analytical chemistry, standard measurement and environment protection etc. Functional polymer microspheres prepared by different methods have the outstanding surface property, quantum size effect and good potential future in applications with its designable structure, controlled size and large ratio of surface to volume. Scholars of all over the world have focused on this hot topic. The preparation method and research progress in functional polymer microspheres are addressed in the paper.

  11. Acetaminophen versus Ibuprofen in Young Children with Mild Persistent Asthma.

    Science.gov (United States)

    Sheehan, William J; Mauger, David T; Paul, Ian M; Moy, James N; Boehmer, Susan J; Szefler, Stanley J; Fitzpatrick, Anne M; Jackson, Daniel J; Bacharier, Leonard B; Cabana, Michael D; Covar, Ronina; Holguin, Fernando; Lemanske, Robert F; Martinez, Fernando D; Pongracic, Jacqueline A; Beigelman, Avraham; Baxi, Sachin N; Benson, Mindy; Blake, Kathryn; Chmiel, James F; Daines, Cori L; Daines, Michael O; Gaffin, Jonathan M; Gentile, Deborah A; Gower, W Adam; Israel, Elliot; Kumar, Harsha V; Lang, Jason E; Lazarus, Stephen C; Lima, John J; Ly, Ngoc; Marbin, Jyothi; Morgan, Wayne J; Myers, Ross E; Olin, J Tod; Peters, Stephen P; Raissy, Hengameh H; Robison, Rachel G; Ross, Kristie; Sorkness, Christine A; Thyne, Shannon M; Wechsler, Michael E; Phipatanakul, Wanda

    2016-08-18

    Studies have suggested an association between frequent acetaminophen use and asthma-related complications among children, leading some physicians to recommend that acetaminophen be avoided in children with asthma; however, appropriately designed trials evaluating this association in children are lacking. In a multicenter, prospective, randomized, double-blind, parallel-group trial, we enrolled 300 children (age range, 12 to 59 months) with mild persistent asthma and assigned them to receive either acetaminophen or ibuprofen when needed for the alleviation of fever or pain over the course of 48 weeks. The primary outcome was the number of asthma exacerbations that led to treatment with systemic glucocorticoids. Children in both groups received standardized asthma-controller therapies that were used in a simultaneous, factorially linked trial. Participants received a median of 5.5 doses (interquartile range, 1.0 to 15.0) of trial medication; there was no significant between-group difference in the median number of doses received (P=0.47). The number of asthma exacerbations did not differ significantly between the two groups, with a mean of 0.81 per participant with acetaminophen and 0.87 per participant with ibuprofen over 46 weeks of follow-up (relative rate of asthma exacerbations in the acetaminophen group vs. the ibuprofen group, 0.94; 95% confidence interval, 0.69 to 1.28; P=0.67). In the acetaminophen group, 49% of participants had at least one asthma exacerbation and 21% had at least two, as compared with 47% and 24%, respectively, in the ibuprofen group. Similarly, no significant differences were detected between acetaminophen and ibuprofen with respect to the percentage of asthma-control days (85.8% and 86.8%, respectively; P=0.50), use of an albuterol rescue inhaler (2.8 and 3.0 inhalations per week, respectively; P=0.69), unscheduled health care utilization for asthma (0.75 and 0.76 episodes per participant, respectively; P=0.94), or adverse events. Among

  12. [Plasma ibuprofen enantiomers and their pharmacokinetics in Beagle dogs determined by HPLC].

    Science.gov (United States)

    Wang, Hong-yan; Kong, Ai-ying; Yang, Bo; Yan, Liang-ping; Di, Xin

    2015-12-01

    A chiral high-performance liquid chromatography method was developed for the simultaneous determination of ibuprofen enantiomers in dog plasma. It was used to study the pharmacokinetics in the Beagle dog after intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen. Ketoprofen was chosen as the internal standard. After a simple precipitation using methanol as the precipitating solvent, both analytes and IS were separated on a Kromasil 100-5CHI-TBB chiral column (250 mm x4.6 mm, 5 μm) with isocratic elution using acetonitrile - 20 mmol x L(-1) phosphate buffer (pH 3.0, containing 5% methanol) (6 : 4) as the mobile phase. The detection wavelength was 220 nm. Liner calibration curves for both of the ibuprofen enantiomers were over the concentration range from 0.5 to 50 μg x mL(-1) with a lower limit of quantification of 0.5 μg x mL(-1), the accuracies were all in standard ranges. The intra- and inter- assay precisions were all below 7%. The recovery rate was 93.1% to 100.4%. The experiments proved that the method was simple, rapid and sensitive. It can be used in the quantitative determination of ibuprofen enantiomers in dog plasma. The method was used to determine the concentration of ibuprofen enantiomers in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen (9 mg x kg(-1)) and the pharmacokinetics parameters were calculated based on the concentration-time curves. The C(max) of S-ibuprofen in Beagle dog plasma after a single intravenous administration of racemic-ibuprofen, S-ibuprofen and R-ibuprofen were 30.8 ± 4.7, 46.1 ± 5.9 and 20.0 ± 2.6 μg x mL(-1), respectively. In terms of the exposure of active ingredient, it revealed a significant difference between the administration of S-ibuprofen and the other two groups. The systematical R- to S- chiral inversion was discussed. Comparing the pharmacokinetic parameters at different doses, chiral inversion were 70.1% ± 36.6% and 76

  13. Co-delivery of ibuprofen and gentamicin from nanoporous anodic titanium dioxide layers.

    Science.gov (United States)

    Pawlik, Anna; Jarosz, Magdalena; Syrek, Karolina; Sulka, Grzegorz D

    2017-04-01

    Although single-drug therapy may prove insufficient in treating bacterial infections or inflammation after orthopaedic surgeries, complex therapy (using both an antibiotic and an anti-inflammatory drug) is thought to address the problem. Among drug delivery systems (DDSs) with prolonged drug release profiles, nanoporous anodic titanium dioxide (ATO) layers on Ti foil are very promising. In the discussed research, ATO samples were synthesized via a three-step anodization process in an ethylene glycol-based electrolyte with fluoride ions. The third step lasted 2, 5 and 10min in order to obtain different thicknesses of nanoporous layers. Annealing the as-prepared amorphous layers at the temperature of 400°C led to obtaining the anatase phase. In this study, water-insoluble ibuprofen and water-soluble gentamicin were used as model drugs. Three different drug loading procedures were applied. The desorption-desorption-diffusion (DDD) model of the drug release was fitted to the experimental data. The effects of crystalline structure, depth of TiO 2 nanopores and loading procedure on the drug release profiles were examined. The duration of the drug release process can be easily altered by changing the drug loading sequence. Water-soluble gentamicin is released for a long period of time if gentamicin is loaded in ATO as the first drug. Additionally, deeper nanopores and anatase phase suppress the initial burst release of drugs. These results confirm that factors such as morphological and crystalline structure of ATO layers, and the procedure of drug loading inside nanopores, allow to alter the drug release performance of nanoporous ATO layers. Copyright © 2017 Elsevier B.V. All rights reserved.

  14. The Evidence Base on the Efficacy and Safety of Ibuprofen in Pediatrics

    Directory of Open Access Journals (Sweden)

    Yu.V. Marushko

    2013-10-01

    Full Text Available The article deals with an analysis of the world literature of recent years, the aim of which was to study the efficacy and safety of ibuprofen use as first-line antipyretic in pediatric practice. Special attention was paid to researches on the study the pharmacokinetics, efficacy and safety of ibuprofen in fever in children of all ages, as well as the use of different forms of ibuprofen (suspension, suppositories.

  15. Pilot monitoring study of ibuprofen in surface waters of north of Portugal

    OpenAIRE

    Paíga, Paula; Santos, Lúcia; Amorim, Célia G.; Araújo, Alberto N.; Montenegro, M. Conceição B. S. M.; Pena, Angelina; Delerue-Matos, Cristina

    2013-01-01

    Ibuprofen is amongst the most worldwide consumed pharmaceuticals. The present work presents the first data in the occurrence of ibuprofen in Portuguese surface waters, focusing in the north area of the country, which is one of the most densely populated areas of Portugal. Analysis of ibuprofen is based on pre-concentration of the analyte with solid phase extraction and subsequent determination with liquid chromatography coupled to fluorescence detection. A total of 42 ...

  16. Comparative study of anti-inflammatory, ulcerogenic and cytotoxic activities of racemate and S-ibuprofen

    Directory of Open Access Journals (Sweden)

    Flavio Henrique Nuevo Benez

    2013-08-01

    Full Text Available Ibuprofen is widely commercialized in racemic form. Although metabolic chiral inversion occurs through the conversion of R(--ibuprofen to S(+-ibuprofen and the latter enantiomer is considered the active form, clinical trials involving the administration of a racemate to S-enantiomer dosage ratio of 1:0.5 have demonstrated that S(+-ibuprofen is as efficacious as the racemic formulation. Moreover, the R(--enantiomer has been implicated in adverse gastrointestinal effects found with the racemic form, but the mechanisms involved in this process are not yet fully understood. The aim of the present study was to evaluate the anti-inflammatory activity of a racemate to S(+-ibuprofen dosage ratio of 1:0.5 using the carrageenan air pouch model of inflammation and determine both ulcerogenic activity and the chiral conversion rate in rats. An in vitro study of the cytotoxicity of racemate and S(+-ibuprofen in gastric cells was also performed. Although the plasma level of S(+-ibuprofen was raised after racemate administration, no significant difference was found in anti-inflammatory activity, as assessed by exudate formation, PGE2 production and leukocyte migration to the air pouches. Fewer gastric lesions were found after S(+-ibuprofen administration, despite the low gastric PGE2 content. In the in vitro study, the racemic compound proved more cytotoxic than S(+-ibuprofen. The present findings suggest that the S-enantiomer of ibuprofen could be considered a therapeutic alternative to minimize gastrointestinal side effects, since the chiral inversion of R(--ibuprofen to S(+-ibuprofen did not result in an improved anti-inflammatory response.

  17. Formulation and delivery strategies of ibuprofen: challenges and opportunities.

    Science.gov (United States)

    Irvine, Jake; Afrose, Afrina; Islam, Nazrul

    2018-02-01

    Ibuprofen, a non-steroidal anti-inflammatory drug (NSAID), is mostly administered orally and topically to relieve acute pain and fever. Due to its mode of action this drug may be useful in the treatment regimens of other, more chronic conditions, like cystic fibrosis. This drug is poorly soluble in aqueous media and thus the rate of dissolution from the currently available solid dosage forms is limited. This leads to poor bioavailability at high doses after oral administration, thereby increasing the risk of unwanted adverse effects. The poor solubility is a problem for developing injectable solution dosage forms. Because of its poor skin permeability, it is difficult to obtain an effective therapeutic concentration from topical preparations. This review aims to give a brief insight into the status of ibuprofen dosage forms and their limitations, particle/crystallization technologies for improving formulation strategies as well as suggesting its incorporation into the pulmonary drug delivery systems for achieving better therapeutic action at low dose.

  18. Effect of amine functionalization of spherical MCM-41 and SBA-15 on controlled drug release

    International Nuclear Information System (INIS)

    Szegedi, A.; Popova, M.; Goshev, I.; Mihaly, J.

    2011-01-01

    MCM-41 and SBA-15 silica materials with spherical morphology and different particle sizes were synthesized and modified by post-synthesis method with 3-aminopropyltriethoxysilane (APTES). A comparative study of the adsorption and release of a model drug, ibuprofen, were carried out. The modified and drug loaded mesoporous materials were characterized by XRD, TEM, N 2 physisorption, thermal analysis, elemental analysis and FT-IR spectroscopy. Surface modification with amino groups resulted in high degree of ibuprofen loading and slow rate of release for MCM-41, whereas it was the opposite for SBA-15. The adsorbed drug content and the delivery rate can be predetermined by the choice of mesoporous material with the appropriate structural characteristics and surface functionality. -- Graphical Abstract: Ibuprofen delivery from the parent and amino-modified spherical MCM-41 materials with 100 nm (small) and 500 nm (large) particle sizes. Display Omitted Highlights: → Spherical type MCM-41 and SBA-15 with different particle sizes were modified by APTES. → Adsorption and release rate of ibuprofen were compared. → High degree of ibuprofen loading, slow release rate for MCM-41, the opposite for SBA-15. → MCM-41 with 100 nm particles was more stable and showed slower release rate

  19. Optimization of Process Variables for Grinding of Ibuprofen using Response Surface Methodology

    Energy Technology Data Exchange (ETDEWEB)

    Sim, Chol-Ho [Sangji University, Wonju (Korea, Republic of)

    2013-12-15

    Ibuprofen, non-steroidal anti-inflammatory drugs; NSAIDs, is a highly crystalline substance with the pharmaceutical properties of poor solubility and low bioavailability. The size reduction of ibuprofen is needed to improve the solubility. The objective of this study is to optimize the grinding condition of ibuprofen. Grinding of ibuprofen was carried out using a planetary mill. Grinding parameters were optimized using Box-Behnken experimental design method. The physical characteristics of ground ibuprofen were investigated for the particle size by particle size analyzer, for the crystal size by X-ray diffraction (XRD), and for the tensile strength by tensile/compression tester. The optimum conditions for the milling of ibuprofen were 290 rpm of the revolution number of mill, 24.6 g of the weight of sample, and 10minutes of grinding time. The measured value of the particle size of ground ibuprofen at these optimum conditions was 13.5 µm. The results showed that the crystal size of ibuprofen was reduced by the planetary milling process. In case the relative density of the tablets formulated of ground ibuprofen was range of 0.85-0.90, the tensile strength of them was range of 12-14 Kg{sub f}/cm{sup 2}.

  20. Optimization of Process Variables for Grinding of Ibuprofen using Response Surface Methodology

    International Nuclear Information System (INIS)

    Sim, Chol-Ho

    2013-01-01

    Ibuprofen, non-steroidal anti-inflammatory drugs; NSAIDs, is a highly crystalline substance with the pharmaceutical properties of poor solubility and low bioavailability. The size reduction of ibuprofen is needed to improve the solubility. The objective of this study is to optimize the grinding condition of ibuprofen. Grinding of ibuprofen was carried out using a planetary mill. Grinding parameters were optimized using Box-Behnken experimental design method. The physical characteristics of ground ibuprofen were investigated for the particle size by particle size analyzer, for the crystal size by X-ray diffraction (XRD), and for the tensile strength by tensile/compression tester. The optimum conditions for the milling of ibuprofen were 290 rpm of the revolution number of mill, 24.6 g of the weight of sample, and 10minutes of grinding time. The measured value of the particle size of ground ibuprofen at these optimum conditions was 13.5 µm. The results showed that the crystal size of ibuprofen was reduced by the planetary milling process. In case the relative density of the tablets formulated of ground ibuprofen was range of 0.85-0.90, the tensile strength of them was range of 12-14 Kg f /cm 2

  1. Does ibuprofen treatment in patent ductus arteriosus alter oxygen free radicals in premature infants?

    Science.gov (United States)

    Akar, Melek; Yildirim, Tulin G; Sandal, Gonca; Bozdag, Senol; Erdeve, Omer; Altug, Nahide; Uras, Nurdan; Oguz, Serife S; Dilmen, Ugur

    2017-04-01

    Introduction Ibuprofen is used widely to close patent ductus arteriosus in preterm infants. The anti-inflammatory activity of ibuprofen may also be partly due to its ability to scavenge reactive oxygen species and reactive nitrogen species. We evaluated the interaction between oxidative status and the medical treatment of patent ductus arteriosus with two forms of ibuprofen. Materials and methods This study enrolled newborns of gestational age ⩽32 weeks, birth weight ⩽1500 g, and postnatal age 48-96 hours, who received either intravenous or oral ibuprofen to treat patent ductus arteriosus. Venous blood was sampled before ibuprofen treatment from each patient to determine antioxidant and oxidant concentrations. Secondary samples were collected 24 hours after the end of the treatment. Total oxidant status and total antioxidant capacity were measured using Erel's method. This prospective randomised study enrolled 102 preterm infants with patent ductus arteriosus. The patent ductus arteriosus closure rate was significantly higher in the oral ibuprofen group (84.6 versus 62%) after the first course of treatment (p=0.011). No significant difference was found between the pre- and post-treatment total oxidant status and total antioxidant capacity in the groups. Discussion Ibuprofen treatment does not change the total oxidant status or total antioxidant capacity. We believe that the effect of ibuprofen treatment in inducing ischaemia overcomes the scavenging effect of ibuprofen.

  2. Ibuprofen versus steroids: risk and benefit, efficacy and safety

    Directory of Open Access Journals (Sweden)

    M. Giovannini

    2013-10-01

    Full Text Available In the last few years we have observed an upward trend in the employment of ibuprofen as anti-inflammatory and antipyretic therapy. Therefore the pediatrician has often a precious option in the anti-inflammatory and antipyretic treatment in children instead of using steroids and paracetamol. In clinical practice ibuprofen can be used in the treatment of headache, toothache, otalgy, dysmenorrhea, neuralgia, arthralgia, myalgia, abdominal pain and fever: it is the first choice for these common diseases. However, the use of steroids is a routine, even if non-corticosteroid anti-inflammatory molecules could be useful. Certainly steroids are powerful anti-inflammatory, indicated for the treatment of chronic inflammatory disorders and in acute respiratory and allergic diseases. Beside, thanks to their chemical and pharmacological profile, they also provide patients with an antipyretic effect. However, the use of steroids must be reserved to cases in which other classical antipyretics such as non-steroidal anti-inflammatory drugs are not effective. The possible side effects and risks associated with stepping down steroids must be considered. Although “steroids-phobia” should be discouraged, steroids are to be reserved only as the first indication. In all other cases the pediatrician can use ibuprofen, whose efficacy and safety are widely demonstrated by now.

  3. Formulation and evaluation of Bacillus coagulans-loaded hypromellose mucoadhesive microspheres

    Directory of Open Access Journals (Sweden)

    Alli SMA

    2011-03-01

    Full Text Available Sk Md Athar AlliDepartment of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, IndiaAbstract: Development of a novel delivery system has been attempted to deliver viable probiotic cells into the gut for a prolonged period of time while maintaining high numbers of viable cells within the formulation throughout the shelf-life of the product and during the gastrointestinal transit. Core mucoadhesive microspheres of Bacillus coagulans were developed employing several grades of hypromellose, a mucoadhesive polymer, following coacervation and phase separation technique and were subsequently enteric-coated with hypromellose phthalate. Microspheres were evaluated for percent yield; entrapment efficiency; in vitro swelling; surface morphology; particle size, size distribution, and zeta potential; flow property, mucoadhesion property by the ex vivo mucoadhesive strength test and the in vitro wash off test; in vitro release profile and release kinetic; in vivo probiotic activity; and stability. The values for the kinetic constant and regression coefficient of model-dependent approaches and the difference factor ( ƒ1, the similarity factor (ƒ2, and the Rescigno index (ξ1 and ξ 2 of model independent approaches were determined for comparing in vitro dissolution profiles. Freeze dried B. coagulans cells were successfully formulated as enteric-coated mucoadhesive microspheres with satisfactory physical structure and yield. The viability of B. coagulans was maintained in the simulated gastric conditions and during processing; in simulated intestinal conditions exhibiting mucoadhesion, and controlling and extending the viable cell release following zero-order; and was satisfactorily stable at room temperature. Test results depict statistically significant effects of the hypromellose grade and their concentration on the performance and release profile of formulations.Keywords: probiotics, B. coagulans, mucoadhesive, microspheres, extended-release

  4. Formulation and evaluation of Bacillus coagulans-loaded hypromellose mucoadhesive microspheres.

    Science.gov (United States)

    Alli, Sk Md Athar

    2011-01-01

    Development of a novel delivery system has been attempted to deliver viable probiotic cells into the gut for a prolonged period of time while maintaining high numbers of viable cells within the formulation throughout the shelf-life of the product and during the gastrointestinal transit. Core mucoadhesive microspheres of Bacillus coagulans were developed employing several grades of hypromellose, a mucoadhesive polymer, following coacervation and phase separation technique and were subsequently enteric-coated with hypromellose phthalate. Microspheres were evaluated for percent yield; entrapment efficiency; in vitro swelling; surface morphology; particle size, size distribution, and zeta potential; flow property, mucoadhesion property by the ex vivo mucoadhesive strength test and the in vitro wash off test; in vitro release profile and release kinetic; in vivo probiotic activity; and stability. The values for the kinetic constant and regression coefficient of model-dependent approaches and the difference factor (f(1)), the similarity factor (f(2)), and the Rescigno index (ξ(1) and ξ(2)) of model independent approaches were determined for comparing in vitro dissolution profiles. Freeze dried B. coagulans cells were successfully formulated as enteric-coated mucoadhesive microspheres with satisfactory physical structure and yield. The viability of B. coagulans was maintained in the simulated gastric conditions and during processing; in simulated intestinal conditions exhibiting mucoadhesion, and controlling and extending the viable cell release following zero-order; and was satisfactorily stable at room temperature. Test results depict statistically significant effects of the hypromellose grade and their concentration on the performance and release profile of formulations.

  5. Release and Degradation of Microencapsulated Spinosad and Emamectin Benzoate.

    Science.gov (United States)

    Huang, Bin Bin; Zhang, Shao Fei; Chen, Peng Hao; Wu, Gang

    2017-09-07

    The dynamics of release and degradation of the microencapsulation formulation containing spinosad (SP) and emamectin benzoate (EM) were evaluated in the present study. SP and EM were microencapsulated using biodegradable poly-lactic acid (PLA) as the wall material. Their release from and degradation within the prepared SP and EM microspheres (SP-EM-microspheres) were studied. It was found that the encapsulation significantly prolonged the insecticide release. The release could be further extended if the external aqueous phase was pre-saturated with the insecticides and the microspheres were additionally coated with gelatin. On the other hand, increasing the water content of the emulsion or the hydrophilic polycaprolactone (PCL) content in the PLA/PCL mixture accelerated the release. Due to the photolysis and hydrolysis of SP and EM by sunlight, the toxicity of the non-encapsulated insecticides in water declined continuously from 0 through the 9 th day (d), and dissipated in 13 d. In contrast, an aqueous suspension containing 5% SP-EM-microspheres maintained a mostly constant toxicity to Plutella xylostella for 17 d. The biodegradable SP-EM-microspheres showed significantly higher long-term toxicity to P. xylostella due to lower release, reduced photolysis and hydrolysis of the encapsulated insecticides, which were affected by the varied preparation conditions.

  6. Thermodynamic study of ibuprofen by adiabatic calorimetry and thermal analysis

    Energy Technology Data Exchange (ETDEWEB)

    Xu Fen; Sun Lixian; Tan Zhicheng; Liang Jianguo; Li Ruilian

    2004-03-23

    Molar heat capacities of ibuprofen were precisely measured with a small sample precision automated adiabatic calorimeter over the temperature range from 80 to 400 K. The polynomial functions of C{sub p,m} (J K{sup -1} mol{sup -1}) versus T were established on the heat capacity measurements by means of the least fitting square method. The functions are as follows: for solid ibuprofen, at the temperature range of 79.105 K{<=}T{<=}333.297 K, C{sub p,m}=144.27+77.046X+3.5171X{sup 2}+10.925X{sup 3}+11.224X{sup 4}, where X=(T-206.201)/127.096; for liquid ibuprofen, at the temperature range of 353.406 K{<=}T{<=}378.785 K, C{sub p,m}=325.79+8.9696X-1.6073X{sup 2}-1.5145X{sup 3}, where X=(T-366.095)/12.690. A fusion transition at T=348.02 K was found from the C{sub p}-T curve. The molar enthalpy and entropy of the fusion transition were determined to be 26.65 kJ mol{sup -1} and 76.58 J mol{sup -1} K{sup -1}, respectively. The thermodynamic functions on the base of the reference temperature of 298.15 K, (H{sub T}-H{sub 298.15}) and (S{sub T}-S{sub 298.15}), were derived. Thermal characteristic of ibuprofen was studied by thermo-gravimetric analysis (TG-DTG) and differential scanning calorimeter (DSC). The temperature of fusion, the molar enthalpy and entropy of fusion obtained by DSC were well consistent with those obtained by adiabatic calorimeter. The evaporation process of ibuprofen was investigated further by TG and DTG, and the activation energy of the evaporation process was determined to be 80.3{+-}1.4 kJ mol{sup -1}.

  7. Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres: State-of-the-art and challenges

    NARCIS (Netherlands)

    Ramazani, F.; Chen, Weiluan; van Nostrum, C.F.; Storm, Gerrit; Kiessling, F.; Lammers, Twan Gerardus Gertudis Maria; Hennink, W.E.; Kok, R.J.

    2016-01-01

    Poly(lactide-co-glycolide) (PLGA) microspheres are efficient delivery systems for controlled release of low molecular weight drugs as well as therapeutic macromolecules. The most common microencapsulation methods are based on emulsification procedures, in which emulsified droplets of polymer and

  8. Encapsulation of Ibuprofen in CD-MOF and Related Bioavailability Studies.

    Science.gov (United States)

    Hartlieb, Karel J; Ferris, Daniel P; Holcroft, James M; Kandela, Irawati; Stern, Charlotte L; Nassar, Majed S; Botros, Youssry Y; Stoddart, J Fraser

    2017-05-01

    Although ibuprofen is one of the most widely used nonsteroidal anti-inflammatory drugs (NSAIDs), it exhibits poor solubility in aqueous and physiological environments as a free acid. In order to improve its oral bioavailability and rate of uptake, extensive research into the development of new formulations of ibuprofen has been undertaken, including the use of excipients as well as ibuprofen salts, such as ibuprofen lysinate and ibuprofen, sodium salt. The ultimate goals of these studies are to reduce the time required for maximum uptake of ibuprofen, as this period of time is directly proportional to the rate of onset of analgesic/anti-inflammatory effects, and to increase the half-life of the drug within the body; that is, the duration of action of the effects of the drug. Herein, we present a pharmaceutical cocrystal of ibuprofen and the biocompatible metal-organic framework called CD-MOF. This metal-organic framework (MOF) is based upon γ-cyclodextrin (γ-CD) tori that are coordinated to alkali metal cations (e.g., K + ions) on both their primary and secondary faces in an alternating manner to form a porous framework built up from (γ-CD) 6 cubes. We show that ibuprofen can be incorporated within CD-MOF-1 either by (i) a crystallization process using the potassium salt of ibuprofen as the alkali cation source for production of the MOF or by (ii) absorption and deprotonation of the free-acid, leading to an uptake of 23-26 wt % of ibuprofen within the CD-MOF. In vitro viability studies revealed that the CD-MOF is inherently not affecting the viability of the cells with no IC 50 value determined up to a concentration of 100 μM. Bioavailability investigations were conducted on mice, and the ibuprofen/CD-MOF pharmaceutical cocrystal was compared to control samples of the potassium salt of ibuprofen in the presence and absence of γ-CD. From these animal studies, we observed that the ibuprofen/CD-MOF-1 cocrystal exhibits the same rapid uptake of ibuprofen as the

  9. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model.

    Science.gov (United States)

    Rooney, Sarah Ilkhanipour; Baskin, Rachel; Torino, Daniel J; Vafa, Rameen P; Khandekar, Pooja S; Kuntz, Andrew F; Soslowsky, Louis J

    2016-09-01

    Previous studies have shown that ibuprofen is detrimental to tissue healing after acute injury; however, the effects of ibuprofen when combined with noninjurious exercise are debated. Administration of ibuprofen to rats undergoing a noninjurious treadmill exercise protocol will abolish the beneficial adaptations found with exercise but will have no effect on sedentary muscle and tendon properties. Controlled laboratory study. A total of 167 male Sprague-Dawley rats were divided into exercise or cage activity (sedentary) groups and acute (a single bout of exercise followed by 24 hours of rest) and chronic (2 or 8 weeks of repeated exercise) response times. Half of the rats were administered ibuprofen to investigate the effects of this drug over time when combined with different activity levels (exercise and sedentary). Supraspinatus tendons were used for mechanical testing and histologic assessment (organization, cell shape, cellularity), and supraspinatus muscles were used for morphologic (fiber cross-sectional area, centrally nucleated fibers) and fiber type analysis. Chronic intake of ibuprofen did not impair supraspinatus tendon organization or mechanical adaptations (stiffness, modulus, maximum load, maximum stress, dynamic modulus, or viscoelastic properties) to exercise. Tendon mechanical properties were not diminished and in some instances increased with ibuprofen. In contrast, total supraspinatus muscle fiber cross-sectional area decreased with ibuprofen at chronic response times, and some fiber type-specific changes were detected. Chronic administration of ibuprofen does not impair supraspinatus tendon mechanical properties in a rat model of exercise but does decrease supraspinatus muscle fiber cross-sectional area. This fundamental study adds to the growing literature on the effects of ibuprofen on musculoskeletal tissues and provides a solid foundation on which future work can build. The study findings suggest that ibuprofen does not detrimentally affect

  10. Synthesis, characterisation and biomedical applications of curcumin conjugated chitosan microspheres.

    Science.gov (United States)

    Saranya, T S; Rajan, V K; Biswas, Raja; Jayakumar, R; Sathianarayanan, S

    2018-04-15

    Curcumin is a diaryl heptanoid of curcuminoids class obtained from Curcuma longa. It possesses various biological activities like anti-inflammatory, hypoglycemic, antioxidant, wound-healing, and antimicrobial activities. Chitosan is a biocompatible, biodegradable and non-toxic natural polymer which enhances the adhesive property of the skin. Chemical conjugation will leads to sustained release action and to enhance the bioavailability. This study aims to synthesis and characterize biocompatible curcumin conjugated chitosan microspheres for bio-medical applications. The Schiff base reaction was carried out for the preparation of curcumin conjugated chitosan by microwave method and it was characterised using FTIR and NMR. Curcumin conjugated chitosan microspheres (CCCMs) were prepared by wet milling solvent evaporation method. SEM analysis showed these CCCMs were 2-5μm spherical particles. The antibacterial activities of the prepared CCCMs were studied against Staphylococcus aureus and Escherichia coli, the zone of inhibition was 28mm and 23mm respectively. Antioxidant activity of the prepared CCCMs was also studied by DPPH and H 2 O 2 method it showed IC 50 esteem value of 216μg/ml and 228μg/ml, and anti-inflammatory activity results showed that CCCMs having IC 50 value of 45μg/ml. The results conclude that the CCCMs having a good antibacterial, antioxidant and anti-inflammatory activities. This, the prepared CCCMs have potential application in preventing skin infections. Copyright © 2017. Published by Elsevier B.V.

  11. Biocompatibility of Polyhydroxybutyrate Microspheres: in vitro and in vivo Evaluation

    OpenAIRE

    Shishatskaya, Ekaterina I.; Voinova, Olga N.; Goreva, Anastasya V.; Mogilnaya, Olga A.; Volova, Tatiana G.

    2008-01-01

    Microspheres have been prepared from the resorbable linear polyester of β-hydroxybutyric acid (polyhydroxybutyrate, PHB) by the solvent evaporation technique and investigated in vitro and in vivo. Biocompatibility of the microspheres has been proved in tests in the culture of mouse fibroblast cell line NIH 3Т3 and in experiments on intramuscular implantation of the microspheres to Wistar rats for 3 months. Tissue response to the implantation of polymeric microspheres has been found to consist...

  12. Synthesis and characterization of pH-sensitive drinkable nanoparticles for oral delivery of ibuprofen

    Science.gov (United States)

    Agostini, Azzurra; Capasso Palmiero, Umberto; Barbieri, Sara D. A.; Lupi, Monica; Moscatelli, Davide

    2018-06-01

    Ibuprofen (IBU) is a widespread drug used to treat both acute and chronic disorders. It is generally taken orally but the free drug can induce the irritation of the gastric mucosa due to its acid nature. In literature, different approaches have been adopted to prevent the release in the stomach, such as physical entrapment with film-coated tablets and drug-conjugates. Nevertheless, these solutions have many disadvantages, including the fast release of the drug and the difficulty to swallow the tablet, especially for children who may vomit or refuse the tablet. For this reason, in this work, novel formulations are proposed that do not require the encapsulation of the drug into a solid form and, in turn, their assumption as a pill. IBU has been linked to different types of methacrylates via ester bond in order to produce pH-responsive macromolecular monomers. The novelty is related to the use of these drug-conjugates macromonomer for the production of nanoparticles (NPs) via emulsion polymerization (EP), using water as solvent. The final emulsion is able to load up to 30 mg ml‑1 of IBU, so less than 10 ml is required to be assumed to reach the minimum therapeutic dose of the drug (200 mg). Finally, the release of IBU from these novel drinkable formulations has been investigated in the gastric and intestinal simulated fluids to show the preferential release of IBU from the NPs in basic conditions. A comparison with an existing oral suspension has been performed to highlight the slower release in acid environment of these new formulations. Afterwards, the IBU loaded NPs were tested in vitro showing lower toxicity compared to the free drug.

  13. VEGF-incorporated biomimetic poly(lactide-co-glycolide) sintered microsphere scaffolds for bone tissue engineering.

    Science.gov (United States)

    Jabbarzadeh, Ehsan; Deng, Meng; Lv, Qing; Jiang, Tao; Khan, Yusuf M; Nair, Lakshmi S; Laurencin, Cato T

    2012-11-01

    Regenerative engineering approaches utilizing biomimetic synthetic scaffolds provide alternative strategies to repair and restore damaged bone. The efficacy of the scaffolds for functional bone regeneration critically depends on their ability to induce and support vascular infiltration. In the present study, three-dimensional (3D) biomimetic poly(lactide-co-glycolide) (PLAGA) sintered microsphere scaffolds were developed by sintering together PLAGA microspheres followed by nucleation of minerals in a simulated body fluid. Further, the angiogenic potential of vascular endothelial growth factor (VEGF)-incorporated mineralized PLAGA scaffolds were examined by monitoring the growth and phenotypic expression of endothelial cells on scaffolds. Scanning electron microscopy micrographs confirmed the growth of bone-like mineral layers on the surface of microspheres. The mineralized PLAGA scaffolds possessed interconnectivity and a compressive modulus of 402 ± 61 MPa and compressive strength of 14.6 ± 2.9 MPa. Mineralized scaffolds supported the attachment and growth and normal phenotypic expression of endothelial cells. Further, precipitation of apatite layer on PLAGA scaffolds resulted in an enhanced VEGF adsorption and prolonged release compared to nonmineralized PLAGA and, thus, a significant increase in endothelial cell proliferation. Together, these results demonstrated the potential of VEGF-incorporated biomimetic PLAGA sintered microsphere scaffolds for bone tissue engineering as they possess the combined effects of osteointegrativity and angiogenesis. Copyright © 2012 Wiley Periodicals, Inc.

  14. Extraction and encapsulation of prodigiosin in chitosan microspheres for targeted drug delivery

    Energy Technology Data Exchange (ETDEWEB)

    Dozie-Nwachukwu, S.O. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Biotechnology and Genetic Engineering Advanced Laboratory, Sheda Science and Technology Complex (SHESTCO), P.M.B 186, Garki, Abuja, Federal Capital Territory (Nigeria); Danyuo, Y. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Materials Science and Engineering, Kwara State University, Malete (Nigeria); Obayemi, J.D. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Odusanya, O.S. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Biotechnology and Genetic Engineering Advanced Laboratory, Sheda Science and Technology Complex (SHESTCO), P.M.B 186, Garki, Abuja, Federal Capital Territory (Nigeria); Malatesta, K. [Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Soboyejo, W.O., E-mail: soboyejo@princeton.edu [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Princeton Institute of Science and Technology of Materials (PRISM), Bowen Hall, 70 Prospect Street, Princeton, NJ 08544 (United States)

    2017-02-01

    The encapsulation of drugs in polymeric materials has brought opportunities to the targeted delivery of chemotherapeutic agents. These polymeric delivery systems are capable of maximizing the therapeutic activity, as well as reducing the side effects of anti-cancer agents. Prodigiosin, a secondary metabolite extracted from the bacteria, Serratia marcescens, exhibits anti-cancer properties. Prodigiosin-loaded chitosan microspheres were prepared via water-in-oil (w/o) emulsion technique, using glutaraldehyde as a cross-linker. The morphologies of the microspheres were studied using scanning electron microscopy. The average sizes of the microspheres were between 40 μm and 60 μm, while the percentage yields ranged from 42 ± 2% to 55.5 ± 3%. The resulting encapsulation efficiencies were between 66.7 ± 3% and 90 ± 4%. The in-vitro drug release from the microspheres was characterized by zeroth order, first order and Higuchi and Korsmeyer-Peppas models. - Highlights: • Prodigiosin of ~ 92.8% purity was extracted from locally isolated Serratia marcescens. • This approach reduces the cost and ensure availability of drugs for cancer treatment. • High encapsulation efficiency which increased with increasing drug:polymer ratio • The percentage yield was generally poor due to the recovery process. • Prodigiosin greatly reduced the viability of the breast cancer cell line (MDA-MB-231).

  15. K88 Fimbrial Adhesin Targeting of Microspheres Containing Gentamicin Made with Albumin Glycated with Lactose

    Directory of Open Access Journals (Sweden)

    Andre-i Sarabia-Sainz

    2015-09-01

    Full Text Available The formulation and characterization of gentamicin-loaded microspheres as a delivery system targeting enterotoxigenic Escherichia coli K88 (E. coli K88 was investigated. Glycated albumin with lactose (BSA-glucose-β (4-1 galactose was used as the microsphere matrix (MS-Lac and gentamicin included as the transported antibiotic. The proposed target strategy was that exposed galactoses of MS-Lac could be specifically recognized by E. coli K88 adhesins, and the delivery of gentamicin would inhibit bacterial growth. Lactosylated microspheres (MS-Lac1, MS-Lac2 and MS-Lac3 were obtained using a water-in-oil emulsion, containing gentamicin, followed by crosslinking with different concentrations of glutaraldehyde. Electron microscopy displayed spherical particles with a mean size of 10–17 µm. In vitro release of gentamicin from MS-Lac was best fitted to a first order model, and the antibacterial activity of encapsulated and free gentamicin was comparable. MS-Lac treatments were recognized by plant galactose-specific lectins from Ricinus communis and Sophora japonica and by E. coli K88 adhesins. Results indicate MS-Lac1, produced with 4.2 mg/mL of crosslinker, as the best treatment and that lactosylated microsphere are promising platforms to obtain an active, targeted system against E. coli K88 infections.

  16. Enhanced in vitro dissolution of Iloperidone using Caesalpinia Pulcherrima mucoadhesive microspheres

    Directory of Open Access Journals (Sweden)

    Pradum Pundlikrao Ige

    2015-03-01

    Full Text Available The aim of the present investigation was to improve the solubility and dissolution rate of Iloperidone. Microspheres containing Iloperidone were prepared by spray drying using mucilage extracted from seeds of Caesalpinia pulcherrima. The novelty of this work is that, the extraction of mucilage and its usage for preparation of drug loaded microspheres. The prepared microspheres were characterized by SEM, DSC, XRPD, FTIR, 1H-NMR, particle size, drug content, entrapment efficiency, in vitro dissolution and ex vivo mucoadhesion. Based on particle size, drug content, ex vivo mucoadhesive strength and in vitro drug release, the best formulation was optimized. Percent entrapment efficiency and mean particle size for optimized formulation was found to be 73.49 and 3.27 ± 1.23 μm, respectively. More precisely, mucilage of C. pulcherrima could be significant carrier of (drug and polymer ratio 1:5 microspheres for the development of oral drug delivery.

  17. Extraction and encapsulation of prodigiosin in chitosan microspheres for targeted drug delivery

    International Nuclear Information System (INIS)

    Dozie-Nwachukwu, S.O.; Danyuo, Y.; Obayemi, J.D.; Odusanya, O.S.; Malatesta, K.; Soboyejo, W.O.

    2017-01-01

    The encapsulation of drugs in polymeric materials has brought opportunities to the targeted delivery of chemotherapeutic agents. These polymeric delivery systems are capable of maximizing the therapeutic activity, as well as reducing the side effects of anti-cancer agents. Prodigiosin, a secondary metabolite extracted from the bacteria, Serratia marcescens, exhibits anti-cancer properties. Prodigiosin-loaded chitosan microspheres were prepared via water-in-oil (w/o) emulsion technique, using glutaraldehyde as a cross-linker. The morphologies of the microspheres were studied using scanning electron microscopy. The average sizes of the microspheres were between 40 μm and 60 μm, while the percentage yields ranged from 42 ± 2% to 55.5 ± 3%. The resulting encapsulation efficiencies were between 66.7 ± 3% and 90 ± 4%. The in-vitro drug release from the microspheres was characterized by zeroth order, first order and Higuchi and Korsmeyer-Peppas models. - Highlights: • Prodigiosin of ~ 92.8% purity was extracted from locally isolated Serratia marcescens. • This approach reduces the cost and ensure availability of drugs for cancer treatment. • High encapsulation efficiency which increased with increasing drug:polymer ratio • The percentage yield was generally poor due to the recovery process. • Prodigiosin greatly reduced the viability of the breast cancer cell line (MDA-MB-231).

  18. Preparation and Characterization of Sugar Cane Wax Microspheres ...

    African Journals Online (AJOL)

    ... and characterize indomethacin (IM) microspheres prepared with sugar cane wax microsperes. Methods: Microspheres were prepared by melt-emulsified dispersion and cooling-induced solidification method. The microspheres were characterized by scanning electron microscopy (SEM) and differntial scanning calorimetry ...

  19. Preparation of polymer microspheres by radiation-induced polymerization

    International Nuclear Information System (INIS)

    Naka, Y.; Yamamoto, Y.; Yoshida, Y.; Tagawa, S.

    1995-01-01

    Cross-liking monomer, diethylene glycol dimethacrylate gives microspheres from organic solution by radiation-induced polymerization. /One of the remarkable result is that the number of the microspheres is not changing during the polymerization. Ethyl methacrylate, maleic anhydride, styrene and acrylamide are used as comonomers. These comonomers give the microspheres in the range of 0 to 0.4 as mol fractions. (author)

  20. Controlled drug release on amine functionalized spherical MCM-41

    Energy Technology Data Exchange (ETDEWEB)

    Szegedi, Agnes, E-mail: szegedi@chemres.hu [Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences, Hungarian Academy of Sciences, 1025 Budapest, Pusztaszeri ut 59-67 (Hungary); Popova, Margarita; Goshev, Ivan [Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Sofia (Bulgaria); Klebert, Szilvia [Institute of Materials and Environmental Chemistry, Research Centre for Natural Sciences, Hungarian Academy of Sciences, 1025 Budapest, Pusztaszeri ut 59-67 (Hungary); Mihaly, Judit [Institute of Molecular Pharmacology, Research Centre for Natural Sciences, Hungarian Academy of Sciences, 1025 Budapest, Pusztaszeri ut 59-67 (Hungary)

    2012-10-15

    MCM-41 silica with spherical morphology and small particle sizes (100 nm) was synthesized and modified by post-synthesis method with different amounts of 3-aminopropyltriethoxysilane (APTES). A comparative study of the adsorption and release of a model drug, ibuprofen, was carried out. The modified and drug loaded mesoporous materials were characterized by XRD, TEM, N{sub 2} physisorption, elemental analysis, thermal analysis and FT-IR spectroscopy. A new method was developed for the quantitative determination of amino groups in surface modified mesoporous materials by the ninhydrin reaction. Good correlation was found between the amino content of the MCM-41 materials determined by the ninhydrin method and their ibuprofen adsorption capacity. Amino modification resulted in high degree of ibuprofen loading and slow release rate in comparison to the parent non-modified MCM-41. - Graphical abstract: Determination of surface amino groups by ninhidrin method. Highlights: Black-Right-Pointing-Pointer Spherical MCM-41 modified by different amounts of APTES was studied. Black-Right-Pointing-Pointer Ibuprofen (IBU) adsorption and release characteristics was tested. Black-Right-Pointing-Pointer The ninhydrin reaction was used for the quantitative determination of amino groups. Black-Right-Pointing-Pointer Stoichiometric amount of APTES is enough for totally covering the surface with amino groups. Black-Right-Pointing-Pointer Good correlation was found between the amino content and IBU adsorption capacity.

  1. Controlled drug release on amine functionalized spherical MCM-41

    International Nuclear Information System (INIS)

    Szegedi, Agnes; Popova, Margarita; Goshev, Ivan; Klébert, Szilvia; Mihály, Judit

    2012-01-01

    MCM-41 silica with spherical morphology and small particle sizes (100 nm) was synthesized and modified by post-synthesis method with different amounts of 3-aminopropyltriethoxysilane (APTES). A comparative study of the adsorption and release of a model drug, ibuprofen, was carried out. The modified and drug loaded mesoporous materials were characterized by XRD, TEM, N 2 physisorption, elemental analysis, thermal analysis and FT-IR spectroscopy. A new method was developed for the quantitative determination of amino groups in surface modified mesoporous materials by the ninhydrin reaction. Good correlation was found between the amino content of the MCM-41 materials determined by the ninhydrin method and their ibuprofen adsorption capacity. Amino modification resulted in high degree of ibuprofen loading and slow release rate in comparison to the parent non-modified MCM-41. - Graphical abstract: Determination of surface amino groups by ninhidrin method. Highlights: ► Spherical MCM-41 modified by different amounts of APTES was studied. ► Ibuprofen (IBU) adsorption and release characteristics was tested. ► The ninhydrin reaction was used for the quantitative determination of amino groups. ► Stoichiometric amount of APTES is enough for totally covering the surface with amino groups. ► Good correlation was found between the amino content and IBU adsorption capacity.

  2. Effect of Multimodal Pore Channels on Cargo Release from Mesoporous Silica Nanoparticles

    Directory of Open Access Journals (Sweden)

    Sushilkumar A. Jadhav

    2016-01-01

    Full Text Available Mesoporous silica nanoparticles (MSNs with multimodal pore channels were fully characterized by TEM, nitrogen adsorption-desorption, and DLS analyses. MSNs with average diameter of 200 nm with dual pore channel zones with pore diameters of 1.3–2.6 and 4 nm were tested for their use in drug delivery application. Important role of the multimodal pore systems present on MSNs on the quantitative release of model drug ibuprofen was investigated. The results obtained revealed that the release profile for ibuprofen clearly shows distinct zones which can be attributed to the respective porous channel zones present on the particles. The fluctuations in the concentration of ibuprofen during the prolonged release from MSNs were caused by the multimodal pore channel systems.

  3. Porous PLGA microspheres tailored for dual delivery of biomolecules via layer-by-layer assembly.

    Science.gov (United States)

    Go, Dewi P; Palmer, Jason A; Mitchell, Geraldine M; Gras, Sally L; O'Connor, Andrea J

    2015-05-01

    Tissue engineering is a complex and dynamic process that requires varied biomolecular cues to promote optimal tissue growth. Consequently, the development of delivery systems capable of sequestering more than one biomolecule with controllable release profiles is a key step in the advancement of this field. This study develops multilayered polyelectrolyte films incorporating alpha-melanocyte stimulating hormone (α-MSH), an anti-inflammatory molecule, and basic fibroblast growth factor (bFGF). The layers were successfully formed on macroporous poly lactic-co-glycolic acid microspheres produced using a combined inkjet and thermally induced phase separation technique. Release profiles could be varied by altering layer properties including the number of layers and concentrations of layering molecules. α-MSH and bFGF were released in a sustained manner and the bioactivity of α-MSH was shown to be preserved using an activated macrophage cell assay in vitro. The system performance was also tested in vivo subcutaneously in rats. The multilayered microspheres reduced the inflammatory response induced by a carrageenan stimulus 6 weeks after implantation compared to the non-layered microspheres without the anti-inflammatory and growth factors, demonstrating the potential of such multilayered constructs for the controlled delivery of bioactive molecules. © 2014 Wiley Periodicals, Inc.

  4. Influence of acidic beverage (Coca-Cola) on pharmacokinetics of ibuprofen in healthy rabbits.

    Science.gov (United States)

    Kondal, Amit; Garg, S K

    2003-11-01

    The study was aimed at determining the effect of Coca-Cola on the pharmacokinetics of ibuprofen in rabbits. In a cross-over study, ibuprofen was given orally in a dose of 56 mg/kg, prepared as 0.5% suspension in carboxymethyl cellulose (CMC) and blood samples (1 ml) were drawn at different time intervals from 0-12 hr. After a washout period of 7 days, Coca-Cola in a dose of (5 ml/kg) was administered along with ibuprofen (56 mg/kg) and blood samples were drawn from 0-12 hr. To these rabbits, 5 ml/kg Coca-Cola was administered once daily for another 7 days. On 8th day, Coca-Cola (5 ml/kg) along with ibuprofen (56 mg/kg), prepared as a suspension was administered and blood samples (1 ml each) were drawn at similar time intervals. Plasma was separated and assayed for ibuprofen by HPLC technique and various pharmacokinetic parameters were calculated. The Cmax and AUC0-alpha of ibuprofen were significantly increased after single and multiple doses of Coca-Cola, thereby indicating increased extent of absorption of ibuprofen. The results warrant the reduction of ibuprofen daily dosage, frequency when administered with Coca-Cola.

  5. CLINICAL EFFICACY OF IBUPROFEN IN THERAPY FOR VIRAL UPPER RESPIRATORY TRACT INFECTIONS IN INFANTS

    Directory of Open Access Journals (Sweden)

    I.O. Skugarevskaya

    2006-01-01

    Full Text Available A study of use of ibuprofen in cases of viral upper respiratory tract infections (Vuri in children of early childhood has proved its' safety and efficacy. This medical agent has not only terminate fever but also diminished some other symptoms of Vuri.Key words: ibuprofen, viral upper respiratory tract infections, children.

  6. Effects of constructed wetland design on ibuprofen removal – A mesocosm scale study

    DEFF Research Database (Denmark)

    Zhang, Liang; Lyu, Tao; Zhang, Yang

    2017-01-01

    This study aimed to investigate the effects of constructed wetland design (unsaturated, saturated and aerated saturated) and plant species (Juncus, Typha, Berula, Phragmites and Iris) on the mass removal and removal kinetics of the pharmaceutical ibuprofen. Planted systems had higher ibuprofen...

  7. Selective degradation of ibuprofen and clofibric acid in two model river biofilm systems.

    Science.gov (United States)

    Winkler, M; Lawrence, J R; Neu, T R

    2001-09-01

    A field survey indicated that the Elbe and Saale Rivers were contaminated with both clofibric acid and ibuprofen. In Elbe River water we could detect the metabolite hydroxy-ibuprofen. Analyses of the city of Saskatoon sewage effluent discharged to the South Saskatchewan river detected clofibric acid but neither ibuprofen nor any metabolite. Laboratory studies indicated that the pharmaceutical ibuprofen was readily degraded in a river biofilm reactor. Two metabolites were detected and identified as hydroxy- and carboxy-ibuprofen. Both metabolites were observed to degrade in the biofilm reactors. However, in human metabolism the metabolite carboxy-ibuprofen appears and degrades second whereas the opposite occurs in biofilm systems. In biofilms the pharmacologically inactive stereoisomere of ibuprofen is degraded predominantly. In contrast, clofibric acid was not biologically degraded during the experimental period of 21 days. Similar results were obtained using biofilms developed using waters from either the South Saskatchewan or Elbe River. In a sterile reactor no losses of ibuprofen were observed. These results suggested that abiotic losses and adsorption played only a minimal role in the fate of the pharmaceuticals in the river biofilm reactors.

  8. Thermodynamics of chiral selectivity in capillary electrophoresis : separation of ibuprofen enantiomers with beta-cyclodextrin

    NARCIS (Netherlands)

    Reijenga, J.C.; Ingelse, B.A.; Everaerts, F.M.

    1997-01-01

    The effect of temperature on the electrophoretic chiral separation of ibuprofen with ß-CD was investigated. Background electrolytes with sodium acetate or formate were chosen because of their constant pK within 0.03 units in the temperature range 25–50°C. Ibuprofen has a temperature independent pK

  9. EFFICACY OF IBUPROFEN IN TREATMENT OF PAIN IN CHILDREN: SYSTEMATIC REVIEW OF RANDOMIZED CONTROLLED STUDIES

    Directory of Open Access Journals (Sweden)

    R.T. Saygitov

    2010-01-01

    Full Text Available The article presents results of systematic review of data on prophylactic and therapeutic efficacy of ibuprofen. Data search was performed by PubMed database and Google search. 27 publications for analysis were available. Prophylactic efficacy of ibuprofen was studied in 14 studies. Summarizing of the results showed that ibuprofen prevents pain and decreases its following intensity after different surgical or dental operations. There is no significant difference in prophylactic efficacy of single dose ibuprofen and acetaminophen. Therapeutic efficacy of ibuprofen was described in 13 studies. Administration of the drug for pain stopping in children is reasonable. The analgesic effect of ibuprofen compared to placebo was shown in all studies of patients with migraine and diseases of ENT-organs. 5 studies performed in last 5 years showed efficacy of ibuprofen in trauma patients, including children with non-complicated fractures of extremities.Key words: children, pain, ibuprofen, prophylaxis, treatment.(Voprosy sovremennoi pediatrii — Current Pediatrics. 2010;9(6:52-62

  10. Ibuprofen and/or paracetamol (acetaminophen) for pain relief after surgical removal of lower wisdom teeth

    NARCIS (Netherlands)

    Bailey, E.; Worthington, H.V.; van Wijk, A.; Yates, J.M.; Coulthard, P.; Afzal, Z.

    2013-01-01

    Background Both paracetamol and ibuprofen are commonly used analgesics for the relief of pain following the surgical removal of lower wisdom teeth (third molars). In 2010, a novel analgesic (marketed as Nuromol) containing both paracetamol and ibuprofen in the same tablet was launched in the United

  11. 75 FR 48352 - Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn...

    Science.gov (United States)

    2010-08-10

    ... DEPARTMENT OF HEALTH AND HUMAN SERVICES Food and Drug Administration [Docket No. FDA-2010-N-0391] Determination That MOTRIN (Ibuprofen) Tablets and Four Other Drug Products Were Not Withdrawn From Sale for... Applicant NDA 17-463 MOTRIN (ibuprofen) Tablets, 300 milligrams (mg), McNeil Consumer Healthcare, 7050 Camp...

  12. Flexible Microsphere-Embedded Film for Microsphere-Enhanced Raman Spectroscopy.

    Science.gov (United States)

    Xing, Cheng; Yan, Yinzhou; Feng, Chao; Xu, Jiayu; Dong, Peng; Guan, Wei; Zeng, Yong; Zhao, Yan; Jiang, Yijian

    2017-09-27

    Dielectric microspheres with extraordinary microscale optical properties, such as photonic nanojets, optical whispering-gallery modes (WGMs), and directional antennas, have drawn interest in many research fields. Microsphere-enhanced Raman spectroscopy (MERS) is an alternative approach for enhanced Raman detection by dielectric microstructures. Unfortunately, fabrication of microsphere monolayer arrays is the major challenge of MERS for practical applications on various specimen surfaces. Here we report a microsphere-embedded film (MF) by immersing a highly refractive microsphere monolayer array in the poly(dimethylsiloxane) (PDMS) film as a flexible MERS sensing platform for one- to three-dimensional (1D to 3D) specimen surfaces. The directional antennas and wave-guided whispering-gallery modes (WG-WGMs) contribute to the majority of Raman enhancement by the MFs. Moreover, the MF can be coupled with surface-enhanced Raman spectroscopy (SERS) to provide an extra >10-fold enhancement. The limit of detection is therefore improved for sensing of crystal violet (CV) and Sudan I molecules in aqueous solutions at concentrations down to 10 -7 M. A hybrid dual-layer microsphere enhancer, constructed by depositing a MF onto a microsphere monolayer array, is also demonstrated, wherein the WG-WGMs become dominant and boost the enhancement ratio >50-fold. The present work opens up new opportunities for design of cost-effective and flexible MERS sensing platforms as individual or associated techniques toward practical applications in ultrasensitive Raman detection.

  13. Quantitative proteomic analysis of ibuprofen-degrading Patulibacter sp. strain I11

    DEFF Research Database (Denmark)

    Almeida, Barbara; Kjeldal, Henrik; Lolas, Ihab Bishara Yousef

    2013-01-01

    was identified and quantified by gel based shotgun-proteomics. In total 251 unique proteins were quantitated using this approach. Biological process and pathway analysis indicated a number of proteins that were up-regulated in response to active degradation of ibuprofen, some of them are known to be involved...... in the degradation of aromatic compounds. Data analysis revealed that several of these proteins are likely involved in ibuprofen degradation by Patulibacter sp. strain I11.......Ibuprofen is the third most consumed pharmaceutical drug in the world. Several isolates have been shown to degrade ibuprofen, but very little is known about the biochemistry of this process. This study investigates the degradation of ibuprofen by Patulibacter sp. strain I11 by quantitative...

  14. Disposable screen printed graphite electrode for the direct electrochemical determination of ibuprofen in surface water

    KAUST Repository

    Amin, Sidra

    2014-08-01

    The potential of square wave voltammetry (SWV) for the determination of ibuprofen in aqueous solution, applying baseline correction, is reported. A screen printed graphite electrodes (SPGEs), especially pretreated for this purpose, were used to investigate the electrochemical oxidation and detection of ibuprofen. After optimization of SWV parameters, measurements were carried out at 200 Hz modulation frequency, 4 mV step potential and 40 mV pulse amplitude for the determination of ibuprofen. The surfaces of both untreated and pretreated SPGEs were characterized by scanning electron microscopy (SEM) and electrochemical impedance spectroscopy (EIS). The electro-catalytic properties of both the electrodes were correlated with the surface treatment. The pretreated screen printed graphite electrode exhibited a high sensitivity toward ibuprofen even in low concentration. The developed method was found rapid, cost-effective and reproducible for in-field ibuprofen detection.

  15. Disposable screen printed graphite electrode for the direct electrochemical determination of ibuprofen in surface water

    KAUST Repository

    Amin, Sidra; Soomro, M. Tahir; Memon, Najma; Solangi, Amber R.; Sirajuddin; Qureshi, Tahira; Behzad, Ali Reza

    2014-01-01

    The potential of square wave voltammetry (SWV) for the determination of ibuprofen in aqueous solution, applying baseline correction, is reported. A screen printed graphite electrodes (SPGEs), especially pretreated for this purpose, were used to investigate the electrochemical oxidation and detection of ibuprofen. After optimization of SWV parameters, measurements were carried out at 200 Hz modulation frequency, 4 mV step potential and 40 mV pulse amplitude for the determination of ibuprofen. The surfaces of both untreated and pretreated SPGEs were characterized by scanning electron microscopy (SEM) and electrochemical impedance spectroscopy (EIS). The electro-catalytic properties of both the electrodes were correlated with the surface treatment. The pretreated screen printed graphite electrode exhibited a high sensitivity toward ibuprofen even in low concentration. The developed method was found rapid, cost-effective and reproducible for in-field ibuprofen detection.

  16. SIMULTANEOUS DETERMINATION OF PARACETAMOL AND IBUPROFENE MIXTURES BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

    Directory of Open Access Journals (Sweden)

    Sophi Damayanti

    2010-06-01

    Full Text Available Analytical method for the determination of paracetamol and ibuprofene mixtures has been developed by High Performance Liquid Chromatography using C-18 column and acetinitrile - phosphate buffer pH = 4.5 (75:25 containing 0.075% sodium hexanesulfunate as a mobile phase. The detector was set at 215 nm. Using such conditions, retention time for paracetamol and ibuprofen was 4.89 and 7.11 min, respectively. The recovery for paracetamol and ibuprofen was found to be 101.07± 0.73% and 102.02 ± 1.58%, respectively. The detector limits of the method was 1.30 and 1.60 μg/mL with the relative standard deviation (RSD 0.74 and 1.52% for paracetamol and ibuprofen, respectively.   Keywords: paracetamol, ibuprofen, multi-component, validation, HPLC.

  17. A comparative study of ibuprofen with paracetamol versus oxyphenbutazone with analgin combination in ophthalmic practice

    Directory of Open Access Journals (Sweden)

    Roy I

    1988-01-01

    Full Text Available A total of 200 patients of either sex with various ophthalmic inflammatory disorders of surgical and non-surgical types were treated with ibuprofen with paracetamol 1 tablet tid. or a combination of oxyphenbutazone and analgin-1 tablet t. i. d. for 7 days/ Patients in the ibuprofen with Paracetamol group recorded a signifi-cantly greater reduction in pain scores; on day 1 and 2 and in swelling scores on day 2, 5 and 7 as compared to patients receiving the combination of ox yphenbutazone and analgin. A significantly lesserr number of patients in the ibuprofen with paraeetamol group required escape analgesics. Seventy six per cent of patients in the Ibuprofen with paracetamol group were judged as showing a Very good - Good, response to treatment as against 55 per cent in the oxvphenbutazone-analgin group. It is concluded that ibuprofen with Paracetamol is superior in efficacy and a safer alternative to a combination of oxyphenbutazone and analgin.

  18. Biosensing by WGM Microspherical Resonators

    Directory of Open Access Journals (Sweden)

    Giancarlo C. Righini

    2016-06-01

    Full Text Available Whispering gallery mode (WGM microresonators, thanks to their unique properties, have allowed researchers to achieve important results in both fundamental research and engineering applications. Among the various geometries, microspheres are the simplest 3D WGM resonators; the total optical loss in such resonators can be extremely low, and the resulting extraordinarily high Q values of 108–109 lead to high energy density, narrow resonant-wavelength lines and a lengthy cavity ringdown. They can also be coated in order to better control their properties or to increase their functionality. Their very high sensitivity to changes in the surrounding medium has been exploited for several sensing applications: protein adsorption, trace gas detection, impurity detection in liquids, structural health monitoring of composite materials, detection of electric fields, pressure sensing, and so on. In the present paper, after a general introduction to WGM resonators, attention is focused on spherical microresonators, either in bulk or in bubble format, to their fabrication, characterization and functionalization. The state of the art in the area of biosensing is presented, and the perspectives of further developments are discussed.

  19. [Recurrent aseptic meningitis secondary to taking ibuprofen and ketorolac].

    Science.gov (United States)

    Cano Vargas-Machuca, E; Mondéjar-Marín, B; Navarro-Muñoz, S; Pérez-Molina, I; Garrido-Robres, J A; Alvarez-Tejerina, A

    Aseptic meningitis is a process that is characterised by an inflammatory reaction of the meninges that is not due to any infectious agent. Its aetiology is varied and is most frequently caused by rheumatologic and/or autoimmune processes, chemical or medication-induced meningitis, the most notable drugs involved being antibiotics and non-steroidal anti-inflammatory drugs (NSAI). We report the case of a 70-year-old male, with no relevant history, who was admitted to hospital five times over a period of 16 months because of acute meningitis with polymorphonuclear pleocytosis, high protein levels in cerebrospinal fluid and normal glucose in cerebrospinal fluid. No evidence of an infectious causation, chemical meningitis, carcinomatosis or autoimmune disease was found and the patient was diagnosed with recurrent aseptic meningitis. It was found that the patient had taken ibuprofen or ketorolac on several occasions, a few hours before the appearance of symptoms. These episodes were quickly resolved after withdrawal of this medication. A number of NSAI have been reported as inducers of aseptic meningitis, one of the most notable being ibuprofen. We report the case of a patient who, as a consequence of taking ibuprofen and ketorolac, presented episodes of recurrent aseptic meningitis. To our knowledge this side effect of ketorolac has not been reported before. Its clinical features are impossible to differentiate from those of infectious meningitis. Diagnosis is reached by exclusion and a careful pharmacological study, including over-the-counter drugs like some of the NSAI, must be performed in patients with this condition, since it is a problem that can easily be solved by withdrawing the drug that causes it.

  20. Scalable and sustainable synthesis of carbon microspheres via a purification-free strategy for sodium-ion capacitors

    Science.gov (United States)

    Wang, Shijie; Wang, Rutao; Zhang, Yabin; Jin, Dongdong; Zhang, Li

    2018-03-01

    Sodium-based energy storage receives a great deal of interest due to the virtually inexhaustible sodium reserve, while the scalable and sustainable strategies to synthesize carbon-based materials with suitable interlayer spaces and large sodium storage capacities are yet to be fully investigated. Carbon microspheres, with regular geometry, non-graphitic characteristic, and stable nature are promising candidates, yet the synthetic methods are usually complex and energy consuming. In this regard, we report a scalable purification-free strategy to synthesize carbon microspheres directly from 5 species of fresh juice. As-synthesized carbon microspheres exhibit dilated interlayer distance of 0.375 nm and facilitate Na+ uptake and release. For example, such carbon microsphere anodes have a specific capacity of 183.9 mAh g-1 at 50 mA g-1 and exhibit ultra-stability (99.0% capacity retention) after 10000 cycles. Moreover, via facile activation, highly porous carbon microsphere cathodes are fabricated and show much higher energy density at high rate than commercial activated carbon. Coupling the compelling anodes and cathodes above, novel sodium-ion capacitors show the high working potential up to 4.0 V, deliver a maximum energy density of 52.2 Wh kg-1, and exhibit an acceptable capacity retention of 85.7% after 2000 cycles.

  1. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1995-04-18

    New, high strength glass microspheres filled with pressurized hydrogen exhibit densities which make them attractive for bulk hydrogen storage and transport. The membrane tensile stress at failure for our engineered glass microspheres is about 150,000 psi, permitting a threefold increase in pressure limit and storage capacity above commercial microspheres, which have been studied a decade ago and have been shown to fail at membrane stresses of 50,000 psi. Our analysis relating glass microspheres for hydrogen transport with infrastructure and economics, indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as pressurized tube transports and liquid hydrogen trailers.

  2. Use of Novel Polyurethane Microspheres in a Curcumin Delivery System

    Directory of Open Access Journals (Sweden)

    Yongmei Hu

    2014-01-01

    Full Text Available Despite having a wide range of beneficial pharmacological effects, curcumin is characterized by poor water solubility and absorption. In this study, novel polyurethane microspheres containing curcumin (Cur-PUMs were prepared using carboxymethyl cellulose sodium to improve the bioavailability and prolong the retention time of curcumin. The prepared Cur-PUMs were characterized by Fourier transform infrared spectroscopy, scanning electron microscope, and ultraviolet spectrophotometer. The sustained-release effects of Cur-PUMs were demonstrated using stability tests in vitro and in vivo pharmacokinetic studies following oral administration. We found that the stability of Cur-PUMs was strongly affected by pH variation. Further, compared with free curcumin, Cur-PUMs showed significantly improved maximum concentration and half-life.

  3. Controlled drug delivery for glaucoma therapy using montmorillonite/Eudragit microspheres as an ion-exchange carrier

    Directory of Open Access Journals (Sweden)

    Tian SY

    2018-01-01

    Full Text Available Shuangyan Tian,1 Juan Li,1 Qi Tao,2,3 Yawen Zhao,1 Zhufen Lv,4 Fan Yang,1 Haoyun Duan,5 Yanzhong Chen,4 Qingjun Zhou,5 Dongzhi Hou1 1Guangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Department of Pharmaceutics, Guangdong Pharmaceutical University, 2CAS Key Laboratory of Mineralogy and Metallogeny, 3Guangdong Provincial Key Laboratory of Mineral Physics and Materials, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, 4Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, 5State Key Laboratory Cultivation Base, Shandong Provincial Key Laboratory of Ophthalmology, Shandong Eye Institute, Shandong Academy of Medical Sciences, Qingdao, China Background: Glaucoma is a serious eye disease that can lead to loss of vision. Unfortunately, effective treatments are limited by poor bioavailability of antiglaucoma medicine due to short residence time on the preocular surface. Materials and methods: To solve this, we successfully prepared novel controlled-release ion-exchange microparticles to deliver betaxolol hydrochloride (BH. Montmorillonite/BH complex (Mt-BH was prepared by acidification-intercalation, and this complex was encapsulated in microspheres (Mt-BH encapsulated microspheres [BMEMs] by oil-in-oil emulsion–solvent evaporation method. The BH loaded into ion-exchange Mt was 47.45%±0.54%. After the encapsulation of Mt-BH into Eudragit microspheres, the encapsulation efficiency of BH into Eudragit microspheres was 94.35%±1.01% and BH loaded into Eudragit microspheres was 14.31%±0.47%. Results: Both Fourier transform infrared spectra and X-ray diffraction patterns indicated that BH was successfully intercalated into acid-Mt to form Mt-BH and then Mt-BH was encapsulated into Eudragit microspheres to obtain BMEMs. Interestingly, in vitro release duration of the prepared BMEMs was extended to 12 hours

  4. A microsphere suspension model of metamaterial fluids

    Directory of Open Access Journals (Sweden)

    Qian Duan

    2017-05-01

    Full Text Available Drawing an analogy to the liquid phase of natural materials, we theoretically propose a microsphere suspension model to realize a metamaterial fluid with artificial electromagnetic indexes. By immersing high-ε, micrometer-sized dielectric spheres in a low-ε insulating oil, the structured fluid exhibits liquid-like properties from dispersing phase as well as the isotropic negative electromagnetic parameters caused by Mie resonances from dispersed microspheres. The work presented here will benefit the development of structured fluids toward metamaterials.

  5. Albumin microspheres labeled with Ga-67 by chelation: concise communication

    International Nuclear Information System (INIS)

    Hnatowich, D.J.; Schlegel, P.

    1981-01-01

    Albumin microspheres have been synthesized with EDTA and DTPA chelating groups covalently bound to their surface. The microspheres may be labeled with Ga-67 at high yield (97 +- 2%) by transcomplexation from a 0.1 M Ga-67 acetate solution. With EDTA microspheres the resulting label dissociates only slightly after 24 hr in 50% plasma at 37 0 C, whereas with DTPA microspheres the label shows no detectable dissociation over this period. By contrast, microspheres without chelating groups lose their label virtually completely under these conditions. Following intravenous administration of sized Ga-67 DTPA microspheres in mice, about (84 +- 16)% of the activity localizes in the lungs at 5 min, with (60 +- 7)% remaining after 2 h. Since labeling is by chelation, the microspheres may also be tagged with other metallic radionuclides

  6. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model

    Science.gov (United States)

    Rooney, Sarah Ilkhanipour; Baskin, Rachel; Torino, Daniel J.; Vafa, Rameen P.; Khandekar, Pooja S.; Kuntz, Andrew F.; Soslowsky, Louis J.

    2017-01-01

    Background Previous studies have shown that ibuprofen is detrimental to tissue healing following acute injury; however, the effects of ibuprofen when combined with non-injurious exercise are debated. Hypothesis We hypothesized that administration of ibuprofen to rats undergoing a non-injurious treadmill exercise protocol would abolish the beneficial adaptations found with exercise but have no effect on sedentary muscle and tendon properties. Study Design Controlled laboratory study Methods Rats were divided into exercise or cage activity (sedentary) groups and acute (a single bout of exercise followed by 24 hours of rest) and chronic (2 or 8 weeks of repeated exercise) time points. Half of the rats received ibuprofen to investigate the effects of this drug over time when combined with different activity levels (exercise and sedentary). Supraspinatus tendons were used for mechanical testing and histology (organization, cell shape, cellularity), and supraspinatus muscles were used for morphological (fiber CSA, centrally nucleated fibers) and fiber type analysis. Results Chronic intake of ibuprofen did not impair supraspinatus tendon organization or mechanical adaptations (stiffness, modulus, max load, max stress, dynamic modulus, or viscoelastic properties) to exercise. Tendon mechanical properties were not diminished and in some instances increased with ibuprofen. In contrast, total supraspinatus muscle fiber cross-sectional area decreased with ibuprofen at chronic time points, and some fiber type-specific changes were detected. Conclusions Chronic administration of ibuprofen does not impair supraspinatus tendon mechanical properties in a rat model of exercise but does decrease supraspinatus muscle fiber cross-sectional area. Clinically, these findings suggest that ibuprofen does not detrimentally affect regulation of supraspinatus tendon adaptions to exercise but does decrease muscle growth. Individuals should be advised on the risk of decreased muscle hypertrophy

  7. Active self-healing encapsulation of vaccine antigens in PLGA microspheres

    Science.gov (United States)

    Desai, Kashappa-Goud H.; Schwendeman, Steven P.

    2013-01-01

    Herein, we describe the detailed development of a simple and effective method to microencapsulate vaccine antigens in poly(lactic-co-glycolic acid) (PLGA) by simple mixing of preformed active self-microencapsulating (SM) PLGA microspheres in a low concentration aqueous antigen solution at modest temperature (10-38 °C). Co-encapsulating protein-sorbing vaccine adjuvants and polymer plasticizers were used to “actively” load the protein in the polymer pores and facilitate polymer self-healing at temperature > hydrated polymer glass transition temperature, respectively. The microsphere formulation parameters and loading conditions to provide optimal active self-healing microencapsulation of vaccine antigen in PLGA was investigated. Active self-healing encapsulation of two vaccine antigens, ovalbumin and tetanus toxoid (TT), in PLGA microspheres was adjusted by preparing blank microspheres containing different vaccine adjuvant (aluminum hydroxide (Al(OH)3) or calcium phosphate). Active loading of vaccine antigen in Al(OH)3-PLGA microspheres was found to: a) increase proportionally with an increasing loading of Al(OH)3 (0.88-3 wt%) and addition of porosigen, b) decrease when the inner Al(OH)3/trehalose phase to 1 mL outer oil phase and size of microspheres was respectively > 0.2 mL and 63 μm, and c) change negligibly by PLGA concentration and initial incubation (loading) temperature. Encapsulation of protein sorbing Al(OH)3 in PLGA microspheres resulted in suppression of self-healing of PLGA pores, which was then overcome by improving polymer chain mobility, which in turn was accomplished by coincorporating hydrophobic plasticizers in PLGA. Active self-healing microencapsulation of manufacturing process-labile TT in PLGA was found to: a) obviate micronization- and organic solvent-induced TT degradation, b) improve antigen loading (1.4-1.8 wt% TT) and encapsulation efficiency (~ 97%), c) provide nearly homogeneous distribution and stabilization of antigen in polymer

  8. Development and evaluation of chitosan microspheres for tetanus, diphtheria and divalent vaccines: a comparative study of subcutaneous and intranasal administration in mice.

    Science.gov (United States)

    Hashem, Fahima M; Fahmy, Sahar A; El-Sayed, Aly M; Al-Sawahli, Majid M

    2013-01-01

    There is a need to use the new technologies to induce immunity with minimum number of vaccination sessions to ensure compliance with reducing cost. To develop single shot vaccines of tetanus, diphtheria and divalent toxoids microsphere's formulations and to induce their immune response after intranasal and subcutaneous administration in mice. The microspheres were prepared using different concentrations of chitosan. Microsphere's morphology, particle size analysis, encapsulation efficiency and antigen integrity were performed and the best formulations were selected for in vitro and in vivo testing in mice. The developed microspheres have a yield percent of 70.3-91.5%. In vitro release of antigens indicated that tetanus release was increased up to 75 and 81% post T5 and TD5 formulations respectively, whereas diphtheria cumulative release increased up to 74 and 69% post D3 and TD5, respectively. Antibody levels produced were lower than that obtained from alum adsorbed vaccine but higher than the minimum level required to induce immunogenicity (>0.01 IU/mL). The subcutaneous route of administration was superior over the intranasal route in producing higher antibody levels. Chitosan microspheres were developed successfully and prove that chitosan represents a good candidate for vaccines delivery.

  9. Thiolated Chitosan Masked Polymeric Microspheres with Incorporated Mesocellular Silica Foam (MCF for Intranasal Delivery of Paliperidone

    Directory of Open Access Journals (Sweden)

    Stavroula Nanaki

    2017-11-01

    Full Text Available In this study, mesocellular silica foam (MCF was used to encapsulate paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. MCF with the drug adsorbed was further encapsulated into poly(lactic acid (PLA and poly(lactide-co-glycolide (PLGA 75/25 w/w microspheres and these have been coated with thiolated chitosan. As found by TEM analysis, thiolated chitosan formed a thin layer on the polymeric microspheres’ surface and was used in order to enhance their mucoadhesiveness. These microspheres aimed at the intranasal delivery of paliperidone. The DSC and XRD studies showed that paliperidone was encapsulated in amorphous form inside the MCF silica and for this reason its dissolution profile was enhanced compared to the neat drug. In coated microspheres, thiolated chitosan reduced the initial burst effect of the paliperidone dissolution profile and in all cases sustained release formulations have been prepared. The release mechanism was also theoretically studied and three kinetic models were proposed and successfully fitted for a dissolution profile of prepared formulations to be found.

  10. Alternating ibuprofen and acetaminophen in the treatment of febrile children: a pilot study [ISRCTN30487061

    Directory of Open Access Journals (Sweden)

    Sabra Ramzi

    2006-03-01

    Full Text Available Abstract Background Alternating ibuprofen and acetaminophen for the treatment of febrile children is a prevalent practice among physicians and parents, despite the lack of evidence on effectiveness or safety. This randomized, double-blind and placebo-controlled clinical trial aims at comparing the antipyretic effectiveness and safety of a single administration of alternating ibuprofen and acetaminophen doses to that of ibuprofen mono-therapy in febrile children. Methods Seventy febrile children were randomly allocated to receive either a single oral dose of 10 mg/kg ibuprofen and 15 mg/kg oral acetaminophen after 4 hours, or a similar dose of ibuprofen and placebo at 4 hours. Rectal temperature was measured at baseline, 4, 5, 6, 7 and 8 hours later. Endpoints included proportions of afebrile children at 6, 7 and 8 hours, maximum decline in temperature, time to recurrence of fever, and change in temperature from baseline at each time point. Intent-to-treat analysis was planned with statistical significance set at P Results A higher proportion of subjects in the intervention group (83.3% became afebrile at 6 hours than in the control group (57.6%; P = 0.018. This difference was accentuated at 7 and 8 hours (P Conclusion A single dose of alternating ibuprofen and acetaminophen appears to be a superior antipyretic regimen than ibuprofen mono-therapy. Further studies are needed to confirm these findings.

  11. Single dose oral ibuprofen plus paracetamol (acetaminophen) for acute postoperative pain.

    Science.gov (United States)

    Derry, Christopher J; Derry, Sheena; Moore, R Andrew

    2013-06-24

    Combining two different analgesics in fixed doses in a single tablet can provide better pain relief than either drug alone in acute pain. This appears to be broadly true across a range of different drug combinations, in postoperative pain and migraine headache. Some combinations of ibuprofen and paracetamol are available for use without prescription in some acute pain situations. To assess the efficacy and adverse effects of single dose oral ibuprofen plus paracetamol for acute postoperative pain using methods that permit comparison with other analgesics evaluated in standardised trials using almost identical methods and outcomes. We searched the Cochrane Central Register of Controlled Trials (CENTRAL) on The Cochrane Library (Issue 4 of 12, 2013), MEDLINE (1950 to May 21st 2013), EMBASE (1974 to May 21st 2013), the Oxford Pain Database, ClinicalTrials.gov, and reference lists of articles. Randomised, double-blind clinical trials of single dose, oral ibuprofen plus paracetamol compared with placebo or the same dose of ibuprofen alone for acute postoperative pain in adults. Two review authors independently considered trials for inclusion in the review, assessed quality, and extracted data. We used validated equations to calculate the area under the pain relief versus time curve and derive the proportion of participants with at least 50% of maximum pain relief over six hours. We calculated relative risk (RR) and number needed to treat to benefit (NNT) for ibuprofen plus paracetamol, ibuprofen alone, or placebo. We used information on use of rescue medication to calculate the proportion of participants requiring rescue medication and the weighted mean of the median time to use. We also collected information on adverse events. Searches identified three studies involving 1647 participants. Each of them examined several dose combinations. Included studies provided data from 508 participants for the comparison of ibuprofen 200 mg + paracetamol 500 mg with placebo, 543

  12. Effects of acetaminophen and ibuprofen in children with migraine receiving preventive treatment with magnesium.

    Science.gov (United States)

    Gallelli, Luca; Avenoso, Tiziana; Falcone, Daniela; Palleria, Caterina; Peltrone, Francesco; Esposito, Maria; De Sarro, Giovambattista; Carotenuto, Marco; Guidetti, Vincenzo

    2014-02-01

    The purpose of this study was to evaluate both the effects of ibuprofen and/or acetaminophen for the acute treatment of primary migraine in children in or out prophylactic treatment with magnesium. Children ranging from the ages of 5 to 16 years with at least 4 attack/month of primary migraine were eligible for participation the study. A visual analog scale was used to evaluate pain intensity at the moment of admission to the study (start of the study) and every month up to 18 months later (end of the study). One hundred sixty children of both sexes aged 5-16 years were enrolled and assigned in 4 groups to receive a treatment with acetaminophen or ibuprofen without or with magnesium. Migraine pain endurance and monthly frequency were similar in the 4 groups. Both acetaminophen and ibuprofen induced a significant decrease in pain intensity (P < .01), without a time-dependent correlation, but did not modify its frequency. Magnesium pretreatment induced a significant decrease in pain intensity (P < .01) without a time-dependent correlation in both acetaminophen- and ibuprofen-treated children and also significantly reduced (P < .01) the pain relief timing during acetaminophen but not during ibuprofen treatment (P < .01). In both acetaminophen and ibuprofen groups, magnesium pretreatment significantly reduced the pain frequency (P < .01). Magnesium increased the efficacy of ibuprofen and acetaminophen with not age-related effects. © 2013 American Headache Society.

  13. Characteristics and clinical implications of the pharmacokinetic profile of ibuprofen in patients with knee osteoarthritis.

    Science.gov (United States)

    Gallelli, L; Galasso, O; Urzino, A; Saccà, S; Falcone, D; Palleria, C; Longo, P; Corigliano, A; Terracciano, R; Savino, R; Gasparini, G; De Sarro, G; Southworth, S R

    2012-12-01

    Ibuprofen is a non-selective cyclo-oxygenase (COX)-1/COX-2 inhibitor used to treat pain conditions and inflammation. Limited data have been published concerning the pharmacokinetic profile and clinical effects of ibuprofen in patients with osteoarthritis (OA). In this paper we compared the pharmacokinetic and clinical profile of ibuprofen (at a dosage of from 800 mg/day to 1800 mg/day) administered in patients affected by severe knee OA. Ibuprofen was administered for 7 days to patients who were scheduled to undergo knee arthroplasty due to OA. After 7 days, the ibuprofen concentration in plasma and synovial fluid was measured through both high-performance liquid chromatography (HPLC)-UV and gas chromatography-mass spectroscopy (GC/MS), while clinical effects were evaluated through both visual analogue scale (VAS) and Western Ontario and McMaster Universities (WOMAC) scores. The Naranjo scale and the WHO causality assessment scale were used for estimating the probability of adverse drug reactions (ADRs). The severity of ADRs was assessed by the modified Hartwig and Siegel scale. Ibuprofen showed a dose-dependent diffusion in both plasma and synovial fluid, which was related to the reduction of pain intensity and improvement of health status, without the development of ADRs. Ibuprofen at higher dosages can be expected to provide better control of OA symptoms as a result of higher tissue distribution.

  14. Treatment of ibuprofen intoxication in a dog via therapeutic plasma exchange.

    Science.gov (United States)

    Walton, Stuart; Ryan, Kirk A; Davis, Jennifer L; Acierno, Mark

    2017-07-01

    To describe the treatment of ibuprofen intoxication with therapeutic plasma exchange in a dog (TPE). A 13-year-old male neutered mixed breed dog presented after ingesting approximately 200 mg/kg of ibuprofen. Treatment consisted of supportive medical therapy with IV fluids, gastrointestinal protectants, antiemetics and prostaglandin analogs, and TPE. A cycle of TPE was performed over 180 minutes, achieving 1.5 plasma volume exchanges. During therapy, heparinized blood and effluent samples were collected. Ibuprofen concentrations were determined in the samples by high-pressure liquid chromatography. Post TPE, the dog was continued on supportive medical therapy and was discharged 96 hours after the overdose. This report describes the use of TPE as an adjunct for ibuprofen intoxication. An 85% reduction in plasma ibuprofen concentration occurred and recovery from a potentially lethal ingestion of ibuprofen was achieved with TPE and supportive care. TPE should be considered when presented with acute ibuprofen intoxication due to the rapid and efficacious nature of therapy. © Veterinary Emergency and Critical Care Society 2017.

  15. Mechanistic studies of the metabolic chiral inversion of (R)-ibuprofen in humans

    International Nuclear Information System (INIS)

    Baillie, T.A.; Adams, W.J.; Kaiser, D.G.; Olanoff, L.S.; Halstead, G.W.; Harpootlian, H.; Van Giessen, G.J.

    1989-01-01

    The metabolic chiral inversion of R-(-)-ibuprofen has been studied in human subjects by means of specific deuterium labeling and stereoselective gas chromatography-mass spectrometry methodology. After simultaneous p.o. administration of a mixture of R-(-)-ibuprofen (300 mg) and R-(-)-[3,3,3-2H3]ibuprofen (304 mg) to four adult male volunteers, the enantiomeric composition and deuterium content of the drug in serum, and of the drug and its principal metabolites in urine, were followed over a period of 24 hr. The results of these analyses indicated that: (1) conversion of R-(-)- to S-(+)-ibuprofen takes place with complete retention of deuterium at the beta-methyl (C-3) position; (2) chiral inversion of R-(-)-[2H3]ibuprofen is not subject to a discernible deuterium isotope effect; and (3) replacement of the beta-methyl hydrogen atoms by deuterium has no effect on any of the serum pharmacokinetic parameters for R-(-)- or S-(+)-ibuprofen. These data indicate that the process whereby R-(-)-ibuprofen undergoes metabolic inversion in human subjects does not involve 2,3-dehydroibuprofen as an intermediate, and that the underlying mechanism cannot, therefore, entail a desaturation/reduction sequence

  16. Physical state of poorly water soluble therapeutic molecules loaded into SBA-15 ordered mesoporous silica carriers: a case study with itraconazole and ibuprofen.

    Science.gov (United States)

    Mellaerts, Randy; Jammaer, Jasper A G; Van Speybroeck, Michiel; Chen, Hong; Van Humbeeck, Jan; Augustijns, Patrick; Van den Mooter, Guy; Martens, Johan A

    2008-08-19

    The ordered mesoporous silica material SBA-15 was loaded with the model drugs itraconazole and ibuprofen using three different procedures: (i) adsorption from solution, (ii) incipient wetness impregnation, and (iii) heating of a mixture of drug and SBA-15 powder. The location of the drug molecules in the SBA-15 particles and molecular interactions were investigated using nitrogen adsorption, TGA, DSC, DRS UV-vis, and XPS. The in vitro release of hydrophobic model drugs was evaluated in an aqueous environment simulating gastric fluid. The effectiveness of the loading method was found to be strongly compound dependent. Incipient wetness impregnation using a concentrated itraconazole solution in dichloromethane followed by solvent evaporation was most efficient for dispersing itraconazole in SBA-15. The itraconazole molecules were located on the mesopore walls and inside micropores of the mesopore walls. When SBA-15 was loaded by slurrying it in a diluted itraconazole solution from which the solvent was evaporated, the itraconazole molecules ended up in the mesopores that they plugged locally. At a loading of 30 wt %, itraconazole exhibited intermolecular interactions inside the mesopores revealed by UV spectroscopy and endothermic events traced with DSC. The physical mixing of itraconazole and SBA-15 powder followed by heating above the itraconazole melting temperature resulted in formulations in which glassy itraconazole particles were deposited externally on the SBA-15 particles. Loading with ibuprofen was successful with each of the three loading procedures. Ibuprofen preferably is positioned inside the micropores. In vitro release experiments showed fast release kinetics provided the drug molecules were evenly deposited over the mesoporous surface.

  17. Ibuprofen and Diclofenac Restrict Migration and Proliferation of Human Glioma Cells by Distinct Molecular Mechanisms

    Science.gov (United States)

    Leidgens, Verena; Seliger, Corinna; Jachnik, Birgit; Welz, Tobias; Leukel, Petra; Vollmann-Zwerenz, Arabel; Bogdahn, Ulrich; Kreutz, Marina; Grauer, Oliver M.; Hau, Peter

    2015-01-01

    Background Non-steroidal anti-inflammatory drugs (NSAIDs) have been associated with anti-tumorigenic effects in different tumor entities. For glioma, research has generally focused on diclofenac; however data on other NSAIDs, such as ibuprofen, is limited. Therefore, we performed a comprehensive investigation of the cellular, molecular, and metabolic effects of ibuprofen and diclofenac on human glioblastoma cells. Methods Glioma cell lines were treated with ibuprofen or diclofenac to investigate functional effects on proliferation and cell motility. Cell cycle, extracellular lactate levels, lactate dehydrogenase-A (LDH-A) expression and activity, as well as inhibition of the Signal Transducer and Activator of Transcription 3 (STAT-3) signaling pathway, were determined. Specific effects of diclofenac and ibuprofen on STAT-3 were investigated by comparing their effects with those of the specific STAT-3 inhibitor STATTIC. Results Ibuprofen treatment led to a stronger inhibition of cell growth and migration than treatment with diclofenac. Proliferation was affected by cell cycle arrest at different checkpoints by both agents. In addition, diclofenac, but not ibuprofen, decreased lactate levels in all concentrations used. Both decreased STAT-3 phosphorylation; however, diclofenac led to decreased c-myc expression and subsequent reduction in LDH-A activity, whereas treatment with ibuprofen in higher doses induced c-myc expression and less LDH-A alteration. Conclusions This study indicates that both ibuprofen and diclofenac strongly inhibit glioma cells, but the subsequent metabolic responses of both agents are distinct. We postulate that ibuprofen may inhibit tumor cells also by COX- and lactate-independent mechanisms after long-term treatment in physiological dosages, whereas diclofenac mainly acts by inhibition of STAT-3 signaling and downstream modulation of glycolysis. PMID:26485029

  18. Acute pain management: acetaminophen and ibuprofen are often under-dosed.

    Science.gov (United States)

    Milani, Gregorio P; Benini, Franca; Dell'Era, Laura; Silvagni, Davide; Podestà, Alberto F; Mancusi, Rossella Letizia; Fossali, Emilio F

    2017-07-01

    Most children with pain are managed by either acetaminophen or ibuprofen. However, no study has so far investigated if children are prescribed adequate doses of acetaminophen or ibuprofen in emergency department. Aim of this retrospective study was to investigate the prevalence of under-dosage of these drugs in children presenting with pain in emergency department. Children initially prescribed with acetaminophen or ibuprofen for pain management were included. The χ 2 automatic interaction detection method was used considering the percentage variation from the minimum of the appropriate dose as dependent variable while prescribed drug, age, gender, body weight, type of hospital (pediatric or general), and availability of internal guidelines on pediatric pain management in the emergency department as independent variables. Data on 1471 children managed for pain were available. Under-dosage was prescribed in 893 subjects (61%), of whom 577 were prescribed acetaminophen and 316 ibuprofen. The use of acetaminophen suppositories, body weight 40 kg, and the use of oral ibuprofen identified clusters of children associated with under-dosage prescription. Prescription of acetaminophen and ibuprofen was frequently under-dosed. The use of suppositories, lower and higher body weight, and the use of ibuprofen were associated with under-dosage. Under-dosing may reflect prescription of anti-pyretic doses. Agenzia Italiana del Farmaco-Observational Study Register (RSO). Registration code: PIERRE/1 What is Known: • Pain is frequent in children presented to emergency department. • International recommendations on pain management are often not implemented. What is New: • Acetaminophen and ibuprofen were frequently underdosed in children prescribed for pain in the Italian emergency departments. • Under-dosage may be related to the habit of using acetaminophen and ibuprofen in the recommended range for fever treatment.

  19. A Randomized Placebo Controlled Trial of Ibuprofen for Respiratory Syncytial Virus Infection in a Bovine Model.

    Directory of Open Access Journals (Sweden)

    Paul Walsh

    Full Text Available Respiratory syncytial virus (RSV is the most common cause of bronchiolitis and hospital admission in infants. An analogous disease occurs in cattle and costs US agriculture a billion dollars a year. RSV causes much of its morbidity indirectly via adverse effects of the host response to the virus. RSV is accompanied by elevated prostaglandin E2 (PGE2 which is followed by neutrophil led inflammation in the lung. Ibuprofen is a prototypical non-steroidal anti-inflammatory drug that decreases PGE2 levels by inhibiting cyclooxygenase.We hypothesized that treatment of RSV with ibuprofen would decrease PGE2 levels, modulate the immune response, decrease clinical illness, and decrease the histopathological lung changes in a bovine model of RSV. We further hypothesized that viral replication would be unaffected.We performed a randomized placebo controlled trial of ibuprofen in 16 outbred Holstein calves that we infected with RSV. We measured clinical scores, cyclooxygenase, lipoxygenase and endocannabinoid products in plasma and mediastinal lymph nodes and interleukin (Il-4, Il-13, Il-17 and interferon-γ in mediastinal lymph nodes. RSV shedding was measured daily and nasal Il-6, Il-8 and Il-17 every other day. The calves were necropsied on Day 10 post inoculation and histology performed.One calf in the ibuprofen group required euthanasia on Day 8 of infection for respiratory distress. Clinical scores (p<0.01 and weight gain (p = 0.08 seemed better in the ibuprofen group. Ibuprofen decreased cyclooxygenase, lipoxygenase, and cytochrome P450 products, and increased monoacylglycerols in lung lymph nodes. Ibuprofen modulated the immune response as measured by narrowed range of observed Il-13, Il-17 and IFN-γ gene expression in mediastinal lymph nodes. Lung histology was not different between groups, and viral shedding was increased in calves randomized to ibuprofen.Ibuprofen decreased PGE2, modulated the immune response, and improved clinical outcomes

  20. Efficacy of ibuprofen on prevention of high altitude headache: A systematic review and meta-analysis.

    Directory of Open Access Journals (Sweden)

    Juan Xiong

    Full Text Available Ibuprofen is used to prevent high altitude headache (HAH but its efficacy remains controversial. We conducted a systematic review and meta-analysis of randomized, placebo-controlled trials (RCTs of ibuprofen for the prevention of HAH.Studies reporting efficacy of ibuprofen for prevention of HAH were identified by searching electronic databases (until December 2016. The primary outcome was the difference in incidence of HAH between ibuprofen and placebo groups. Risk ratios (RR were aggregated using a Mantel-Haenszel random effect model. Heterogeneity of included trials was assessed using the I2 statistics.In three randomized-controlled clinical trials involving 407 subjects, HAH occurred in 101 of 239 subjects (42% who received ibuprofen and 96 of 168 (57% who received placebo (RR = 0.79, 95% CI 0.66 to 0.96, Z = 2.43, P = 0.02, I2 = 0%. The absolute risk reduction (ARR was 15%. Number needed to treat (NNT to prevent HAH was 7. Similarly, The incidence of severe HAH was significant in the two groups (RR = 0.40, 95% CI 0.17 to 0.93, Z = 2.14, P = 0.03, I2 = 0%. Severe HAH occurred in 3% treated with ibuprofen and 10% with placebo. The ARR was 8%. NNT to prevent severe HAH was 13. Headache severity using a visual analogue scale was not different between ibuprofen and placebo. Similarly, the difference between the two groups in the change in SpO2 from baseline to altitude was not different. One included RCT reported one participant with black stools and three participants with stomach pain in the ibuprofen group, while seven participants reported stomach pain in the placebo group.Based on a limited number of studies ibuprofen seems efficacious for the prevention of HAH and may therefore represent an alternative for preventing HAH with acetazolamide or dexamethasone.

  1. Gastroretentive Floating Microspheres of Silymarin: Preparation and ...

    African Journals Online (AJOL)

    Erah

    simulated gastric fluid for at least 12 h, and, therefore, could potentially ... systems (GRFDDS) have a bulk density ... The objective of this work was to develop and characterise gastroretentive floating microspheres of silymarin which, following oral administration, would exhibit .... hydrochloric acid to maintain sink conditions.

  2. Structuring of diamond films using microsphere lithography

    Czech Academy of Sciences Publication Activity Database

    Domonkos, Mária; Ižák, Tibor; Štolcová, L.; Proška, J.; Demo, Pavel; Kromka, Alexander

    2014-01-01

    Roč. 54, č. 5 (2014), s. 320-324 ISSN 1210-2709 R&D Projects: GA ČR(CZ) GBP108/12/G108 Institutional support: RVO:68378271 Keywords : nanostructuring * diamond thin films * polystyrene microspheres * reactive ion etching * scanning electron microscopy Subject RIV: BM - Solid Matter Physics ; Magnetism

  3. Method and apparatus for producing microspherical particles

    International Nuclear Information System (INIS)

    Egli, W.; Bailey, W.H.; Leary, D.F.; Lansley, R.J.

    1979-01-01

    This invention relates generally to a method and apparatus for producing microspherical particles and more particularly to a method and apparatus which are particularly useful in connection with the sol-gel process for the production of nuclear fuel kernels. (U.K.)

  4. Beat-Frequency/Microsphere Medical Ultrasonic Imaging

    Science.gov (United States)

    Yost, William T.; Cantrell, John H.; Pretlow, Robert A., III

    1995-01-01

    Medical ultrasonic imaging system designed to provide quantitative data on various flows of blood in chambers, blood vessels, muscles, and tissues of heart. Sensitive enough to yield readings on flows of blood in heart even when microspheres used as ultrasonic contrast agents injected far from heart and diluted by circulation of blood elsewhere in body.

  5. Tabletted guar gum microspheres of piroxicam for targeted adjuvant therapy for colonic adenocarcinomas.

    Science.gov (United States)

    Vats, Anima; Pathak, Kamla

    2012-11-01

    In recent years, nonsteroidal anti-inflammatory drugs have been found to be cogent as an adjuvant therapeutic agent in mitigating colorectal cancer. Thus, this present investigation was aimed to formulate an oral, targeted tablet of piroxicam microspheres for sustained and targeted adjuvant therapy for colonic adenocarcinomas. Crosslinked guar gum microspheres of piroxicam were directly compressed into matrix tablet and coated with Eudragit S100. The optimized tablet that displayed 0% release in simulated gastric fluid, 15% in simulated intestinal fluid and 97.1% in simulated colonic fluid underwent roentgenographic study in rabbits to check its safe transit to the colon. x-ray images revealed intactness of the tablet until it reached the colon where the tablet matrix eroded. The designed, conceptual formulation emerged as potential carrier for targeted adjuvant therapy of piroxicam.

  6. Akut pankreatitis hos en 16-årig dreng efter indtag af ibuprofen

    DEFF Research Database (Denmark)

    Bruusgaard-Mouritsen, Mads Emil; Leerhøy, Bonna; Hansen, Mark Berner

    2015-01-01

    This is a case report of a 16-year-old boy with possible drug-induced pancreatitis (DIP) caused by ibuprofen. The patient had a history of psychiatric, but no somatic, disease, and he was admitted with a clinical presentation consistent with acute pancreatitis after a bolus ingestion of 10 g...... of ibuprofen in a suicidal attempt. No evidence of other causality for acute pancreatitis was identified. The patient was treated with a standard pancreatitis treatment regime and was discharged against medical advice after four days. The case represents a possible causality between ibuprofen and DIP....

  7. IBUPROFEN AS A MEDICATION FOR A CORRECTION OF SYMPTOMS OF NORMAL VACCINAL PROCESS IN CHILDREN

    Directory of Open Access Journals (Sweden)

    T.A. Chebotareva

    2008-01-01

    Full Text Available The pathogenetic approach to treatment of symptoms of normal vaccinal process in children after standard vaccination, based on the results of application of anti9inflammatory medications — ibuprofen (nurofen for children and paracetamol is presented in this article. Clinical activity of ibuprofen was established on the basis of clinica catamnestic observation of 856 vaccinated children aged from 3 months to 3 years. recommendations for application of these medications as a treatment for a correction of vaccinal reactions are given.Key words: children, ibuprofen, paracetamol, vaccination.

  8. Resolution of ibuprofen: a project for an experimental organic chemistry course

    International Nuclear Information System (INIS)

    Romero, Adriano L.; Baptistella, Lucia H.B.; Coelho, Fernando; Imamura, Paulo M.

    2012-01-01

    A practical and didactic sequence of experiments was proposed to illustrate the stereochemistry concept, optically active compounds, resolution of racemates, and use of the NMR technique, including 2D-COSY for identification of organic compounds, on a laboratory course for undergraduate students. The sequence was: extractions of racemic ibuprofen and chiral naproxen from commercial tablets; syntheses of diastereoisomeric amides reacting chiral (S)-(-)-α-methylbenzylamine with (+-)-ibuprofen; separation and determination of absolute configuration of amides by 1 H NMR spectroscopy and GC analysis, and hydrolysis of amides to obtain (+)- and (-)-ibuprofen. (author)

  9. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1994-04-20

    New, high-strength, hollow, glass microspheres filled with pressurized hydrogen exhibit storage densities which make them attractive for bulk hydrogen storage and transport. The hoop stress at failure of our engineered glass microspheres is about 150,000 psi, permitting a three-fold increase in pressure limit and storage capacity above commercial microspheres, which fail at wall stresses of 50,000 psi. For this project, microsphere material and structure will be optimized for storage capacity and charge/discharge kinetics to improve their commercial practicality. Microsphere production scale up will be performed, directed towards large-scale commercial use. Our analysis relating glass microspheres for hydrogen transport with infrastructure and economics` indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as hydride beds, cryocarbons and pressurized tube transports. For microspheres made from advanced materials and processes, analysis will also be performed to identify the appropriate applications of the microspheres considering property variables, and different hydrogen infrastructure, end use, production and market scenarios. This report presents some of the recent modelling results for large beds of glass microspheres in hydrogen storage applications. It includes plans for experiments to identify the properties relevant to large-bed hydrogen transport and storage applications, of the best, currently producible, glass microspheres. This work began in March, 1994. Project successes will be manifest in the matching of cur-rent glass microspheres with a useful application in hydrogen bulk transport and storage, and in developing microsphere materials and processes that increase the storage density and reduce the storage energy requirement.

  10. Self-templated Synthesis of Nickel Silicate Hydroxide/Reduced Graphene Oxide Composite Hollow Microspheres as Highly Stable Supercapacitor Electrode Material.

    Science.gov (United States)

    Zhang, Yanhua; Zhou, Wenjie; Yu, Hong; Feng, Tong; Pu, Yong; Liu, Hongdong; Xiao, Wei; Tian, Liangliang

    2017-12-01

    Nickel silicate hydroxide/reduced graphene oxide (Ni 3 Si 2 O 5 (OH) 4 /RGO) composite hollow microspheres were one-pot hydrothermally synthesized by employing graphene oxide (GO)-wrapped SiO 2 microspheres as the template and silicon source, which were prepared through sonication-assisted interfacial self-assembly of tiny GO sheets on positively charged SiO 2 substrate microspheres. The composition, morphology, structure, and phase of Ni 3 Si 2 O 5 (OH) 4 /RGO microspheres as well as their electrochemical properties were carefully studied. It was found that Ni 3 Si 2 O 5 (OH) 4 /RGO microspheres featured distinct hierarchical porous morphology with hollow architecture and a large specific surface area as high as 67.6 m 2  g -1 . When utilized as a supercapacitor electrode material, Ni 3 Si 2 O 5 (OH) 4 /RGO hollow microspheres released a maximum specific capacitance of 178.9 F g -1 at the current density of 1 A g -1 , which was much higher than that of the contrastive bare Ni 3 Si 2 O 5 (OH) 4 hollow microspheres and bare RGO material developed in this work, displaying enhanced supercapacitive behavior. Impressively, the Ni 3 Si 2 O 5 (OH) 4 /RGO microsphere electrode exhibited outstanding rate capability and long-term cycling stability and durability with 97.6% retention of the initial capacitance after continuous charging/discharging for up to 5000 cycles at the current density of 6 A g -1 , which is superior or comparable to that of most of other reported nickel-based electrode materials, hence showing promising application potential in the energy storage area.

  11. Removal of the pharmaceuticals ibuprofen and iohexol by four wetland plant species in hydroponic culture: plant uptake and microbial degradation.

    Science.gov (United States)

    Zhang, Yang; Lv, Tao; Carvalho, Pedro N; Arias, Carlos A; Chen, Zhanghe; Brix, Hans

    2016-02-01

    We aimed at assessing the effects of four wetland plant species commonly used in constructed wetland systems: Typha, Phragmites, Iris and Juncus for removing ibuprofen (IBU) and iohexol (IOH) from spiked culture solution and exploring the mechanisms responsible for the removal. IBU was nearly completely removed by all plant species during the 24-day experiment, whereas the IOH removal varied between 13 and 80 %. Typha and Phragmites were the most efficient in removing IBU and IOH, respectively, with first-order removal rate constants of 0.38 and 0.06 day(-1), respectively. The pharmaceuticals were taken up by the roots and translocated to the aerial tissues. However, at the end of the experiment, plant accumulation constituted only up to 1.1 and 5.7 % of the amount of IBU and IOH spiked initially. The data suggest that the plants mainly function by facilitating pharmaceutical degradation in the rhizosphere through release of root exudates.

  12. In vitro evaluation of biodegradable microspheres with surface-bound ligands.

    Science.gov (United States)

    Keegan, Mark E; Royce, Sara M; Fahmy, Tarek; Saltzman, W Mark

    2006-02-21

    Protein ligands were conjugated to the surface of biodegradable microspheres. These microsphere-ligand conjugates were then used in two in vitro model systems to evaluate the effect of conjugated ligands on microsphere behavior. Microsphere retention in agarose columns was increased by ligands on the microsphere surface specific for receptors on the agarose matrix. In another experiment, conjugating the lectin Ulex europaeus agglutinin 1 to the microsphere surface increased microsphere adhesion to Caco-2 monolayers compared to control microspheres. This increase in microsphere adhesion was negated by co-administration of l-fucose, indicating that the increase in adhesion is due to specific interaction of the ligand with carbohydrate receptors on the cell surface. These results demonstrate that the ligands conjugated to the microspheres maintain their receptor binding activity and are present on the microsphere surface at a density sufficient to target the microspheres to both monolayers and three-dimensional matrices bearing complementary receptors.

  13. Modification of crystal habit of ibuprofen using the phase partition technique: effect of aerosil and tween 80 in binding solvent.

    Science.gov (United States)

    Umprayn, K; Luengtummuen, A; Kitiyadisai, C; Pornpiputsakul, T

    2001-11-01

    A ternary diagram, representing the solubility of binding solvent (chloroform) in a mixture of ethanol and water, was constructed. For this study, the solvent mixture that gave the best ibuprofen pellets (IPs) was composed of chloroform.ethanol:water at a ratio of 1.5%:8%:90.5%. The suitable agitator speed, temperature, and mixing time were found to be 1,500 rpm, 25 degrees C +/- 2 degrees C, and 20 min, respectively. In addition, suitable stirring time when the phase partition process of IPs began was 15 min. IPs obtained from these conditions were small and round, approximately 1 mm; surface determination by scanning electron microscopy (SEM) indicated that the IPs were composed of drug microcrystals rearranged on the surface. For the dissolution, IPs showed lower drug release when compared with pure ibuprofen crystal (IC) (f2 analysis). An attempt to modify the dissolution property of IP by incorporating various concentrations of Aerosil and Tween 80 in the binding solvent was made. Microscopic appearance showed that both Aerosil and Tween 80 gave less spherical pellets when compared with the use of binding solvent alone. For both the Aerosil and Tween 80 employed, the results indicated a change in rearrangement of drug microcrystals and a change in crystal habit. However, Tween 80 gave more change of the crystallographic direction of drug microcrystals than Aerosil. In term of dissolution, the results showed that employing Tween 80 at 1.2% gave the highest drug release compared to the use of Aerosil and IC alone (f2 analysis). These pellets had a good flow property, as indicated by Carr's compressibility, flow rate, and angle of repose, and they can be compressed into a tablet, encapsulated by suitable polymer, or pulverized to obtain micronized crystals. In the case of compression into tablets, the dissolution profiles of these tablets compared with those of commercial product meet the USP 24 requirement (Q > or = 80% at 60 min).

  14. Phytoextraction, phytotransformation and rhizodegradation of ibuprofen associated with Typha angustifolia in a horizontal subsurface flow constructed wetland.

    Science.gov (United States)

    Li, Yifei; Zhang, Jiefeng; Zhu, Guibing; Liu, Yu; Wu, Bing; Ng, Wun Jern; Appan, Adhityan; Tan, Soon Keat

    2016-10-01

    Widespread occurrence of trace pharmaceutical residues in aquatic environments is of great concerns due to the potential chronic toxicity of certain pharmaceuticals including ibuprofen on aquatic organisms even at environmental levels. In this study, the phytoextraction, phytotransformation and rhizodegradation of ibuprofen associated with Typha angustifolia were investigated in a horizontal subsurface flow constructed wetland system. The experimental wetland system consisted of a planted bed with Typha angustifolia and an unplanted bed (control) to treat ibuprofen-loaded wastewater (∼107.2 μg L(-1)). Over a period of 342 days, ibuprofen was accumulated in leaf sheath and lamina tissues at a mean concentration of 160.7 ng g(-1), indicating the occurrence of the phytoextraction of ibuprofen. Root-uptake ibuprofen was partially transformed to ibuprofen carboxylic acid, 2-hydroxy ibuprofen and 1-hydroxy ibuprofen which were found to be 1374.9, 235.6 and 301.5 ng g(-1) in the sheath, respectively, while they were 1051.1, 693.6 and 178.7 ng g(-1) in the lamina. The findings from pyrosequencing analysis of the rhizosphere bacteria suggest that the Dechloromonas sp., the Clostridium sp. (e.g. Clostridium saccharobutylicum), the order Sphingobacteriales, and the Cytophaga sp. in the order Cytophagales were most probably responsible for the rhizodegradation of ibuprofen. Copyright © 2016 Elsevier Ltd. All rights reserved.

  15. From Single Microparticles to Microfluidic Emulsification: Fundamental Properties (Solubility, Density, Phase Separation from Micropipette Manipulation of Solvent, Drug and Polymer Microspheres

    Directory of Open Access Journals (Sweden)

    Koji Kinoshita

    2016-11-01

    Full Text Available The micropipette manipulation technique is capable of making fundamental single particle measurements and analyses. This information is critical for establishing processing parameters in systems such as microfluidics and homogenization. To demonstrate what can be achieved at the single particle level, the micropipette technique was used to form and characterize the encapsulation of Ibuprofen (Ibp into poly(lactic-co-glycolic acid (PLGA microspheres from dichloromethane (DCM solutions, measuring the loading capacity and solubility limits of Ibp in typical PLGA microspheres. Formed in phosphate buffered saline (PBS, pH 7.4, Ibp/PLGA/DCM microdroplets were uniformly solidified into Ibp/PLGA microparticles up to drug loadings (DL of 41%. However, at DL 50 wt% and above, microparticles showed a phase separated pattern. Working with single microparticles, we also estimated the dissolution time of pure Ibp microspheres in the buffer or in detergent micelle solutions, as a function of the microsphere size and compare that to calculated dissolution times using the Epstein-Plesset (EP model. Single, pure Ibp microparticles precipitated as liquid phase microdroplets that then gradually dissolved into the surrounding PBS medium. Analyzing the dissolution profiles of Ibp over time, a diffusion coefficient of 5.5 ± 0.2 × 10−6 cm2/s was obtained by using the EP model, which was in excellent agreement with the literature. Finally, solubilization of Ibp into sodium dodecyl sulfate (SDS micelles was directly visualized microscopically for the first time by the micropipette technique, showing that such micellization could increase the solubility of Ibp from 4 to 80 mM at 100 mM SDS. We also introduce a particular microfluidic device that has recently been used to make PLGA microspheres, showing the importance of optimizing the flow parameters. Using this device, perfectly smooth and size-homogeneous microparticles were formed for flow rates of 0.167 mL/h for

  16. Thermodynamic and Calorimetric Study of Acetylsalicylic Acid (Aspirin and Ibuprofen

    Directory of Open Access Journals (Sweden)

    Juan Carlos Moreno-Piraján

    2011-01-01

    Full Text Available Enthalpies of solution and dilution of aqueous solutions of sodium acetylsalicylic acid salt and ibuprofen salt were measured with an isoperibolic calorimeter at 293.15 K, 298.15 K, 303.15 K, 308.15 K and 318.15 K. The concentration of the electrolyte was restricted to the solubility of the salt at various temperatures and did not exceed 0.035–0.057 mol kg-1, depending on the temperature studied. The Virial coefficients were derived from Pitzer's model and the excess thermodynamic functions of both the solution and the components of the solution were calculated. An analysis of the thermodynamic characteristics of the solution in terms of concentration and temperature interval was carried out and discussed. Additionally, an analysis was performed by differential scanning calorimetry (DSC.

  17. Optically Levitated Microspheres as a Probe for New Interactions

    Science.gov (United States)

    Rider, Alexander; Moore, David; Blakemore, Charles; Lu, Marie; Gratta, Giorgio

    2016-03-01

    We are developing novel techniques to probe new interactions at micron distances using optically levitated dielectric microspheres. Levitated microspheres are an ideal probe for short-range interactions because they are suspended using the radiation pressure at the focus of a laser beam, which means that the microspheres can be precisely manipulated and isolated from the surrounding environment at high vacuum. We have performed a search for unknown charged particles bound within the bulk of the microspheres. Currently, we are searching for the presence of a Chameleon field postulated to explain the presence of dark energy in the universe. In the future we plan to use optically levitated microspheres to search for micron length-scale gravity like interactions that could couple between a microsphere and another mass. We will present resent results from these experiments and plans for future searches for new interactions.

  18. Hydrogen transport and storage in engineered glass microspheres

    Energy Technology Data Exchange (ETDEWEB)

    Rambach, G.D.

    1995-02-28

    New, high strength glass microspheres filled with pressurized hydrogen exhibit densities which make them attractive for bulk hydrogen storage and transport. The membrane tensile stress at failure for engineered glass microspheres is about 150,000 psi, permitting a three-fold increase in pressure limit and storage capacity above commercial microspheres, which have been studied a decade ago and have been shown to fail at membrane stresses of 50,000 psi. This analysis relating glass microspheres for hydrogen transport with infrastructure and economics, indicate that pressurized microspheres can be economically competitive with other forms of bulk rail and truck transport such as pressurized tube transports and liquid hydrogen trailers. This paper will describe the matching of current glass microspheres with the useful application in commercial hydrogen bulk transport and storage.

  19. Application of SeDeM expert systems in preformulation studies of pediatric ibuprofen ODT tablets

    Directory of Open Access Journals (Sweden)

    Sipos Emese

    2017-06-01

    Full Text Available Pediatric, ibuprofen containing orodispersible tablets (ODTs were prepared using the SeDeM expert system methodology. In order to facilitate formulation, directly compressible ibuprofen was employed (Ibuprofen DC 8TM and characterized using its SeDeM profile. The mannitol based superdisintegrant Ludiflash® was characterized by the SeDeM-ODT expert system, which also allowed calculation of the optimal excipient concentration in order to obtain suitable tablet hardness and disintegration time. After adding a sweetener and a standard combination of lubricants, the optimized formulation was directly compressed into tablets and evaluated in terms of tablet hardness, friability, disintegration time and dissolution profile. The SeDeM method was applied to determine the amount of corrective excipient (Ludiflash® required for the compression of Ibuprofen DC 85TM in order to achieve suitable ODTs. Adequate tablet hardness, disintegration time, friability and dissolution profiles were found during tablet evaluation.

  20. Microbial Removal of the Pharmaceutical Compounds Ibuprofen and Diclofenac from Wastewater

    NARCIS (Netherlands)

    Langenhoff, A.A.M.; Inderfurth, N.S.; Veuskens, T.; Schraa, G.; Blokland, M.; Kujawa-Roeleveld, K.; Rijnaarts, H.H.M.

    2013-01-01

    Studies on the occurrence of pharmaceuticals show that the widely used pharmaceuticals ibuprofen and diclofenac are present in relevant concentrations in the environment. A pilot plant treating hospital wastewater with relevant concentrations of these pharmaceuticals was evaluated for its

  1. Enantioselective analysis of ibuprofen and its biotransformation products in water/sediment systems,

    DEFF Research Database (Denmark)

    Sundström, Maria; Escola, Monica; Radke, Michael

    2015-01-01

    of the sediments in the aquatic systems has neither been taken in account previously. In this study, four water-sediment systems were chosen according to anthropogenic exposure and sediment conditions. A low anthropogenic impact lake (Largen), a river receiving wastewater (Fyrisån) and two sediments (anoxic......As ibuprofen degrades enantioselectively in activated sludge, the same process is assumed to occur in surface lake-water and in river-water based biofilms. Yet, the effects of the wastewater inflow, containing non-racemic ibuprofen, into natural systems have never been studied. The role......-7 days in Tvären and B1 respectively. Largen sediments, not impacted by wastewater, degraded ibuprofen faster than Fyrisån sediments did. Yet, these two sediments sediments showed no significant difference with respect to the degradation rates of the ibuprofen enantiomers. A connection between wastewater...

  2. Application of SeDeM expert systems in preformulation studies of pediatric ibuprofen ODT tablets.

    Science.gov (United States)

    Sipos, Emese; Oltean, Andrea Ramona; Szabó, Zoltán-István; Rédai, Emőke-Margit; Nagy, Gabriella Dónáth

    2017-06-27

    Pediatric, ibuprofen containing orodispersible tablets (ODTs) were prepared using the SeDeM expert system methodology. In order to facilitate formulation, directly compressible ibuprofen was employed (Ibuprofen DC 8TM) and characterized using its SeDeM profile. The mannitol based superdisintegrant Ludiflash® was characterized by the SeDeM-ODT expert system, which also allowed calculation of the optimal excipient concentration in order to obtain suitable tablet hardness and disintegration time. After adding a sweetener and a standard combination of lubricants, the optimized formulation was directly compressed into tablets and evaluated in terms of tablet hardness, friability, disintegration time and dissolution profile. The SeDeM method was applied to determine the amount of corrective excipient (Ludiflash®) required for the compression of Ibuprofen DC 85TM in order to achieve suitable ODTs. Adequate tablet hardness, disintegration time, friability and dissolution profiles were found during tablet evaluation.

  3. Drug release control in delivery system for biodegradable polymer drugs by γ-radiation

    International Nuclear Information System (INIS)

    Yoshioka, Sumie; Azo, Yukio; Kojima, Shigeo

    1997-01-01

    Characterizations of the drug release from microsphere and hydrogel preparation made from biodegradable polymers were investigated aiming at development of a drug delivery system which allows an optimum drug delivery and the identification of the factors which control its delivery. Poly-lactic acid microspheres containing 10% of progesterone were produced from poly DL-lactic acid and exposed to γ-ray at 5-1000 kGy. And its glass transition temperature (Tg) was determined by differential scanning calorimetry. The temperature was gradually lowered with an increase in the dose of radiation. Tg of the microsphere exposed at 1000 kGy was lower by 10degC compared with the untreated one, showing that Tg control is possible without changing the size distribution of microsphere. Then, the amount of progesterone released from microsphere was determined. The release rate of the drug linearly increased with a square root of radiation time. These results indicate that the control of drug release rate is possible through controling the microsphere's Tg by γ-ray radiation. (M.N.)

  4. Cyclodextrin Controlled Release of Poorly Water-Soluble Drugs from Hydrogels

    DEFF Research Database (Denmark)

    Woldum, Henriette Sie; Madsen, Flemming; Larsen, Kim Lambertsen

    2008-01-01

    The effect of 2-hydroxypropyl- -cyclodextrin and -cyclodextrin on the release of ibuprofen, ketoprofen and prednisolone was studied. Stability constants calculated for inclusion complexes show size dependence for complexes with both cyclodextrins. Hydrogels were prepared by ultraviolet irradiation...... and release of each model drug was studied. For drugs formulated using cyclodextrins an increase in the achievable concentration and in the release from hydrogels was obtained due to increased solubility, although the solubility of all -cyclodextrin complexes was limited. The load also was increased...

  5. Differential renal adverse effects of ibuprofen and indomethacin in preterm infants: a review

    Directory of Open Access Journals (Sweden)

    Pacifici GM

    2014-07-01

    Full Text Available Gian Maria Pacifici Medical School, Department of Translational Research and New Technologies in Medicine and Surgery, Section of Pharmacology, University of Pisa, Pisa, Italy Objective: The objective of this study was to evaluate the extent of renal adverse effects caused by ibuprofen or indomethacin in order to choose the safer drug to administer to preterm infants. Methods: The following three parameters of renal function were taken into consideration: 1 the urine output; 2 the serum creatinine concentration; and 3 the frequency of oliguria. The bibliographic search was performed using PubMed and Embase databases as search engines. Results: Urine output ranged from 3.5±1.2 to 4.0±1.4 mL/kg/h after ibuprofen treatment, and from 2.8±1.1 to 3.6±1.4 mL/kg/h after indomethacin treatment. The values for ibuprofen are significantly (P<0.05 higher than those for indomethacin. The serum creatinine concentrations ranged from 0.98±0.24 to 1.48±0.2 mg/dL after ibuprofen treatment, and from 1.06±0.24 and 2.03±2.10 mg/dL after indomethacin treatment. The values for ibuprofen are significantly (P<0.05 lower than those for indomethacin. The frequency of oliguria ranged from 1.0% to 9.6% (ibuprofen and from 14.8% to 40.0% (indomethacin, and was significantly lower following ibuprofen than indomethacin administration. In infants with body weight lower than 1,000 g, oliguria appeared in 5% (ibuprofen and 40% (indomethacin; P=0.02. Conclusion: Indomethacin is associated with more severe renal adverse effects than ibuprofen. Ibuprofen is less nephrotoxic than indomethacin and should be used to treat patent ductus arteriosus in preterm infants. Immaturity increases the frequency of adverse effects of indomethacin. Keywords: ibuprofen, indomethacin, patent-ductus-arteriosus, renal-side-effects

  6. From harmful Microcystis blooms to multi-functional core-double-shell microsphere bio-hydrochar materials.

    Science.gov (United States)

    Bi, Lei; Pan, Gang

    2017-11-13

    Harmful algal blooms (HABs) induced by eutrophication is becoming a serious global environmental problem affecting public health and aquatic ecological sustainability. A novel strategy for the utilization of biomass from HABs was developed by converting the algae cells into hollow mesoporous bio-hydrochar microspheres via hydrothermal carbonization method. The hollow microspheres were used as microreactors and carriers for constructing CaO 2 core-mesoporous shell-CaO 2 shell microspheres (OCRMs). The CaO 2 shells could quickly increase dissolved oxygen to extremely anaerobic water in the initial 40 min until the CaO 2 shells were consumed. The mesoporous shells continued to act as regulators restricting the release of oxygen from CaO 2 cores. The oxygen-release time using OCRMs was 7 times longer than when directly using CaO 2 . More interestingly, OCRMs presented a high phosphate removal efficiency (95.6%) and prevented the pH of the solution from rising to high levels in comparison with directly adding CaO 2 due to the OH - controlled-release effect of OCRMs. The distinct core-double-shell micro/nanostructure endowed the OCRMs with triple functions for oxygen controlled-release, phosphorus removal and less impact on water pH. The study is to explore the possibility to prepare smarter bio-hydrochar materials by utilizing algal blooms.

  7. Beat frequency ultrasonic microsphere contrast agent detection system

    Science.gov (United States)

    Pretlow, III, Robert A. (Inventor); Yost, William T. (Inventor); Cantrell, Jr., John H. (Inventor)

    1997-01-01

    A system for and method of detecting and measuring concentrations of an ultrasonically-reflective microsphere contrast agent involving detecting non-linear sum and difference beat frequencies produced by the microspheres when two impinging signals with non-identical frequencies are combined by mixing. These beat frequencies can be used for a variety of applications such as detecting the presence of and measuring the flow rates of biological fluids and industrial liquids, including determining the concentration level of microspheres in the myocardium.

  8. Microsphere formation in droplets using antisolvent vapour precipitation technique

    OpenAIRE

    Chew, Sean Jun Liang

    2017-01-01

    In previous studies, the antisolvent vapour precipitation method has been proven to produce uniformly sized lactose microspheres (1.0 µm) from a single droplet (1.2 mm diameter) at atmospheric pressure. These types of particles have potential applications in the pharmaceutical industry, especially due to their high dissolution rate. This project looked into the possibility of using antisolvent vapour precipitation to produce microspheres from finely atomised droplets. Microspheres in the sub-...

  9. Comparison of Analgesic Effects of Novafen and Ibuprofen after Periodontal Surgeries

    Directory of Open Access Journals (Sweden)

    Amirreza Babaloo

    2017-01-01

    Full Text Available Introduction: Management of pain after dental procedures is one of the most important issues for dentists. Non-steroidal antiinflammatory agents, such as ibuprofen, are one of the most commonly used medications to relieve pain. Recently a new medication, Novafen, has been introduced into the Iranian pharmaceutical market, which is a combination of ibuprofen, acetaminophen and caffeine. Considering the importance of management of pain after periodontal surgeries and a paucity of studies in this respect, the present study was undertaken to compare the analgesic efficacy of Novafen and ibuprofen in alleviating pain after periodontal surgeries. Materials and methods: In the present controlled randomized clinical trial, 30 systemically healthy subjects with moderate to severe generalized chronic periodontitis, who were candidates for flap surgeries were evaluated in two groups with 30 areas in each group (two areas in each patient. After the periodontal surgical procedures, the subjects in group 1 received Novafen capsules (containing 325 mg of acetaminophen, 200 mg of ibuprofen and 40 mg of caffeine and the subjects in group 2 received ibuprofen (400 mg. The medications were selected from one pharmaceutical company and the patients only used the medications they received. The severity of pain was determined and compared at 3-minute, 1-hour and 3-hour intervals using VAS and 1, 2 and 3 days postoperatively using VRS. Results: Severity of pain at 30-minute interval in the Novafen group was significantly less than that in the ibuprofen group, with no significant differences at 1- and 3-hour intervals. However, VRS revealed significantly less pain 1, 2 and 3 days postoperatively in the Novafen group compared to the ibuprofen group. Conclusion: Based on the results of the present study, it can be concluded than Novafen can be more effective after periodontal surgeries in alleviating pain. However, its pain control capacity was similar to that of

  10. Maternal use of acetaminophen, ibuprofen, and acetylsalicylic acid during pregnancy and risk of cryptorchidism

    DEFF Research Database (Denmark)

    Jensen, Morten Søndergaard; Rebordosa, Cristina; Thulstrup, Ane Marie

    2010-01-01

    Cyclooxygenase (COX) inhibitors-acetaminophen, ibuprofen and acetylsalicylic acid-have endocrine-disruptive properties in the rainbow trout. In humans, aspirin blocks the androgen response to human chorionic gonadotropin (hCG), and, because hCG-stimulated androgen production in utero is crucial...... for normal testicular descent, exposure to COX inhibitors at vulnerable times during gestation may impair testicular descent. We examined whether prenatal exposure to acetaminophen, ibuprofen, and acetylsalicylic acid was associated with increased occurrence of cryptorchidism....

  11. The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol

    OpenAIRE

    Tanner, Trevor; Aspley, Sue; Munn, Andrew; Thomas, Tracy

    2010-01-01

    Background Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of two studies on the pharmacokinetic properties of a novel ibuprofen (200 mg) and paracetamol (500 mg) fixed-dose combination tablet. Methods Both studies were open-label, randomised studies in healthy volunteers: Study 1 was a four-way crossover, single-dose study; Study 2 was a two-way cross-...

  12. Ibuprofen Ameliorates Fatigue- and Depressive-like Behavior in Tumor-bearing Mice

    Science.gov (United States)

    Norden, Diana M.; McCarthy, Donna O.; Bicer, Sabahattin; Devine, Raymond; Reiser, Peter J.; Godbout, Jonathan P.; Wold, Loren E.

    2015-01-01

    Aims Cancer-related fatigue (CRF) is often accompanied by depressed mood, both of which reduce functional status and quality of life. Research suggests that increased expression of pro-inflammatory cytokines are associated with skeletal muscle wasting and depressive- and fatigue- like behaviors in rodents and cancer patients. We have previously shown that treatment with ibuprofen, a nonsteroidal anti-inflammatory drug, preserved muscle mass in tumor-bearing mice. Therefore, the purpose of the present study was to determine the behavioral effects of ibuprofen in a mouse model of CRF. Main Methods Mice were injected with colon-26 adenocarcinoma cells and treated with ibuprofen (10mg/kg) in the drinking water. Depressive-like behavior was determined using the forced swim test (FST). Fatigue-like behaviors were determined using voluntary wheel running activity (VWRA) and grip strength. The hippocampus, gastrocnemius muscle, and serum were collected for cytokine analysis. Key Findings Tumor-bearing mice showed depressive-like behavior in the FST, which was not observed in mice treated with ibuprofen. VWRA and grip strength declined in tumor-bearing mice, and ibuprofen attenuated this decline. Tumor-bearing mice had decreased gastrocnemius muscle mass and increased expression of IL-6, MAFBx and MuRF mRNA, biomarkers of protein degradation, in the muscle. Expression of IL-1β and IL-6 was also increased in the hippocampus. Treatment with ibuprofen improved muscle mass and reduced cytokine expression in both the muscle and hippocampus of tumor-bearing mice. Significance Ibuprofen treatment reduced skeletal muscle wasting, inflammation in the brain, and fatigue- and depressive-like behavior in tumor-bearing mice. Therefore, ibuprofen warrants evaluation as an adjuvant treatment for CRF. PMID:26498217

  13. A Randomized Placebo Controlled Trial of Ibuprofen for Respiratory Syncytial Virus Infection in a Bovine Model

    Science.gov (United States)

    Walsh, Paul; Behrens, Nicole; Carvallo Chaigneau, Francisco R.; McEligot, Heather; Agrawal, Karan; Newman, John W.; Anderson, Mark; Gershwin, Laurel J.

    2016-01-01

    Background Respiratory syncytial virus (RSV) is the most common cause of bronchiolitis and hospital admission in infants. An analogous disease occurs in cattle and costs US agriculture a billion dollars a year. RSV causes much of its morbidity indirectly via adverse effects of the host response to the virus. RSV is accompanied by elevated prostaglandin E2 (PGE2) which is followed by neutrophil led inflammation in the lung. Ibuprofen is a prototypical non-steroidal anti-inflammatory drug that decreases PGE2 levels by inhibiting cyclooxygenase. Hypotheses We hypothesized that treatment of RSV with ibuprofen would decrease PGE2 levels, modulate the immune response, decrease clinical illness, and decrease the histopathological lung changes in a bovine model of RSV. We further hypothesized that viral replication would be unaffected. Methods We performed a randomized placebo controlled trial of ibuprofen in 16 outbred Holstein calves that we infected with RSV. We measured clinical scores, cyclooxygenase, lipoxygenase and endocannabinoid products in plasma and mediastinal lymph nodes and interleukin (Il)-4, Il-13, Il-17 and interferon-γ in mediastinal lymph nodes. RSV shedding was measured daily and nasal Il-6, Il-8 and Il-17 every other day. The calves were necropsied on Day 10 post inoculation and histology performed. Results One calf in the ibuprofen group required euthanasia on Day 8 of infection for respiratory distress. Clinical scores (pibuprofen group. Ibuprofen decreased cyclooxygenase, lipoxygenase, and cytochrome P450 products, and increased monoacylglycerols in lung lymph nodes. Ibuprofen modulated the immune response as measured by narrowed range of observed Il-13, Il-17 and IFN-γ gene expression in mediastinal lymph nodes. Lung histology was not different between groups, and viral shedding was increased in calves randomized to ibuprofen. Conclusions Ibuprofen decreased PGE2, modulated the immune response, and improved clinical outcomes. However lung

  14. Phase III study of ibuprofen versus placebo for radiation-induced genitourinary side effects

    International Nuclear Information System (INIS)

    Coleman, C. Norman; Kelly, Laura; Riese Daly, Nancy; Beard, Clair; Kaplan, Irving; Lamb, Carolyn; Propert, Kathleen; Manola, Judith

    2002-01-01

    Purpose: On the basis of our anecdotal clinical observations that nonsteroidal anti-inflammatory agents relieved dysuria during radiotherapy for patients with prostate cancer, we conducted a Phase III randomized trial of ibuprofen vs. placebo for patients who had an increase in acute urinary symptoms. Our in vitro and in vivo laboratory data with a higher concentration of ibuprofen than achievable in this study demonstrated radiosensitization. This study examined whether the inflammatory response within the prostate during radiotherapy would respond to the standard dose of ibuprofen as assessed by a symptom score. Methods and Materials: Patients were registered to the study and were followed weekly with a formal symptom assessment. A double-blind randomization to ibuprofen, 400 mg q.i.d., vs. placebo for 7 days was done at a time when the severity score increased. The symptom response was evaluated at the end of the week. Results: Between 1995 and 1998, 100 patients were entered, 28 did not have a sufficient change in symptom score to be randomized, and 19 were either unable to take ibuprofen or withdrew before randomization. Of the 53 patients randomized, 27 received placebo and 26 ibuprofen. No statistically significant differences were found between the placebo and ibuprofen groups between baseline and randomization or between randomization and the 1-week posttreatment assessment. Neither group had a change in symptom severity between randomization and the 1-week posttreatment evaluation. Conclusion: The standard anti-inflammatory dose of ibuprofen did not relieve the acute urinary or rectal symptoms during radiotherapy for prostate cancer. The nonsteroidal anti-inflammatory drugs are potential radiation sensitizers with the mechanism of action as yet unknown. Clinical trials of the cyclooxygenase inhibitors as radiation sensitizers should explore a range of doses and evaluate potential mechanisms of action, including cyclooxygenase inhibition and other non

  15. Preparation of polystyrene microsphere with emulsion microencapsulation method

    International Nuclear Information System (INIS)

    Li Bo Zhang Lin; Zhang Zhganwen; You Dan; Wei Yun; Wang Chaoyang; Lin Bo; Shi Tao; Chu Qiaomei

    2003-01-01

    The preparation of hollow polystyrene microspheres that are used as inner shell of multi-shell plastic microspheres in the ICF experiments is focused on. The effects of surfactants, water-soluble polymer and electrolyte on the properties of resultant microspheres are studied. Based on these experiments, a fabricating procedure was established with which hollow microspheres were prepared with diameter about 150-3000 μm, wall thickness 0.8-15 μm and toughness Ra less than 4 nm. (authors)

  16. Intestinal absorption of PLAGA microspheres in the rat.

    Science.gov (United States)

    Damgé, C; Aprahamian, M; Marchais, H; Benoit, J P; Pinget, M

    1996-12-01

    Rhodamine B-labelled poly (DL-lactide-co-glycolide) (PLAGA) microspheres of 2 different sizes, 1-5 microns and 5-10 microns, were administered as a single dose (1.44 x 10(9) and 1.83 x 10(8) particles, respectively) into the ileal lumen of adult rats. The content of rhodamine in the mesenteric vein and ileal lumen was analysed periodically from 10 min to 48 h as well as the distribution of microspheres in the intestinal mucosa and various other tissues. The concentration of rhodamine decreased progressively in the intestinal lumen and was negligible after 24 h. The number of microspheres in the mesenteric vein increased rapidly and reached a maximum after 4 h whatever the size of the particles. It then decreased progressively, but more rapidly with microspheres > 5 microns than with microspheres PLAGA microspheres mainly crossed the intestinal mucosa at the site of Peyer's patches where microspheres of 5 microns were retained in the ileal lumen. A few small microspheres were occasionally observed in the epithelial cells. Only the smallest particles were recovered in the liver, lymph nodes and spleen while basement membranes were always labelled. It is concluded that PLAGA microspheres could be useful for the oral delivery of antigens if their size is between 1 and 5 microns.

  17. Preparation of porous zirconia microspheres by internal gelation method

    International Nuclear Information System (INIS)

    Pathak, Sachin S.; Pius, I.C.; Bhanushali, R.D.; Rao, T.V. Vittal; Mukerjee, S.K.

    2008-01-01

    A modified internal gelation process for the preparation of porous zirconia microspheres has been developed. The conventional method has been modified by adding a surfactant in the feed broth. The effects of variation of surfactant concentration, washing techniques and temperature of calcination on the pore volume and the surface area of the microspheres have been studied. The conditions were optimized to obtain porous stable microspheres suitable for various applications. The microspheres were characterized by surface area analysis, pore volume analysis, thermogravimetric analysis and X-ray diffraction. The ion exchange behavior was studied using pH titration

  18. Photoluminescence and lasing in whispering gallery mode glass microspherical resonators

    Energy Technology Data Exchange (ETDEWEB)

    Ristić, D. [Ruđer Bošković Institute, Division of Materials Physics, Laboratory for Molecular Physics, Bijenička c. 54, Zagreb (Croatia); Center of Excellence for Advanced Materials and Sensing Devices, Research unit New Functional Materials, Bijenička c. 54, Zagreb (Croatia); Berneschi, S.; Camerini, M. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Farnesi, D.; Pelli, S. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy); Trono, C. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Chiappini, A.; Chiasera, A.; Ferrari, M. [CSMFO Group, Istituto di Fotonica e Nanotecnologie, IFN-CNR, Via alla Cascata 56/C, 38050 Povo-Trento (Italy); Lukowiak, A. [Institute of Low Temperature and Structure Research, PAS, ul. Okolna 2, Wroclaw 50-950 (Poland); Dumeige, Y.; Féron, P. [Laboratoire d' Optronique, (CNRS-UMR 6082-Foton), ENSSAT, 6 rue de Kérampont, 22300 Lannion (France); Righini, G.C. [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy); Soria, S., E-mail: s.soria@ifac.cnr.it [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Conti, G. Nunzi [IFAC-CNR Istituto di Fisica Applicata, Via Madonna del Piano 10, 50019 Sesto Fiorentino (Italy); Centro Studi e Ricerche ' E. Fermi' , Piazza del Viminale 2, 00184 Roma (Italy)

    2016-02-15

    We report experimental results regarding the development of Er{sup 3+}-doped glass microspherical cavities for the fabrication of compact sources at 1.55 μm. We investigate several different approaches in order to fabricate the microspheres including direct melting of Er{sup 3+}-doped glass powders, synthesis of Er{sup 3+}-doped monolithic microspheres by drawing Er{sup 3+}-doped glass, and coating of silica microspheres with an Er{sup 3+}-doped sol–gel layer. Details of the different fabrication processes are presented together with the photoluminescence characterization in free space configuration of the microspheres and of the glass precursor. We have analyzed the photoluminescence spectra of the whispering gallery modes of the microspheres excited using evanescent coupling and we demonstrate tunable laser action in a wide range of wavelengths around 1.55 μm. As much as 90 μW of laser output power was measured in Er{sup 3+}-doped glass microspheres. - Highlights: • Different approaches in microsphere fabrication and various types of post-processing. • Trimming of photorefractive glass microsphere lasers with UV light. • Peak power record of 90 μW by pumping at 1480 nm.

  19. Low pressure gas filling of laser fusion microspheres

    International Nuclear Information System (INIS)

    Koo, J.C.; Dressler, J.L.; Hendricks, C.D.

    1979-01-01

    In our laser fusion microsphere production, large, thin gel-microspheres are formed before the chemicals are fused into glass. In this transient stage,, the gel-microspheres are found to be highly permeable to argon and many other inert gases. When the gel transforms to glass, the argon gas, for example, is trapped within to form argon filled, fusion target quality, glass microspheres. On the average, the partial pressure of the argon fills attained in this process is around 2 x 10 4 Pa at room temperature

  20. Characterization and Compatibility Studies of Different Rate Retardant Polymer Loaded Microspheres by Solvent Evaporation Technique: In Vitro-In Vivo Study of Vildagliptin as a Model Drug

    Directory of Open Access Journals (Sweden)

    Irin Dewan

    2015-01-01

    Full Text Available The present study has been performed to microencapsulate the antidiabetic drug of Vildagliptin to get sustained release of drug. The attempt of this study was to formulate and evaluate the Vildagliptin loaded microspheres by emulsion solvent evaporation technique using different polymers like Eudragit RL100, Eudragit RS100, Ethyl cellulose, and Methocel K100M. In vitro dissolution studies were carried out in 0.1 N HCl for 8 hours according to USP paddle method. The maximum and minimum drug release were observed as 92.5% and 68.5% from microspheres, respectively, after 8 hours. Release kinetics were studied in different mathematical release models to find out the linear relationship and release rate of drug. The SEM, DSC, and FTIR studies have been done to confirm good spheres and smooth surface as well as interaction along with drug and polymer. In this experiment, it is difficult to explain the exact mechanism of drug release. But the drug might be released by both diffusion and erosion as the correlation coefficient (R2 best fitted with Korsmeyer model and release exponent (n was 0.45–0.89. At last it can be concluded that all in vitro and in vivo experiments exhibited promising result to treat type II diabetes mellitus with Vildagliptin microspheres.

  1. Core/shell cellulose-based microspheres for oral administration of Ketoprofen Lysinate.

    Science.gov (United States)

    Guarino, Vincenzo; Caputo, Tania; Calcagnile, Paola; Altobelli, Rosaria; Demitri, Christian; Ambrosio, Luigi

    2018-01-26

    Herein, we propose the fabrication of a new carrier with core/shell structure-inner core of cellulose acetate (CA) coated by a micrometric layer of chitosan (CS)-fabricated through an integrated process, which combines Electro Dynamic Atomization (EDA) and layer-by-layer (LbL) technique. We demonstrate that CA based microspheres possess a unique capability to relevantly retain the drugs-that is, Ketoprofen Lysinate (KL)-along the gastric tract, while providing a massive release along the intestine. CS shell slightly influences the morphology and water retention under different pH conditions, improving drug encapsulation without compromising drug release kinetics. In vitro studies in simulated gastric and intestine fluids (SGF, SIF) with physiological enzymes, show a moderate release of LSK during the first 2 h (ca. 20% at pH 2), followed by a sustained release during the next 6 h (ca. 80% at pH 7). The obtained results demonstrate that CA-based microspheres hold strong potential to be used as carriers for a delayed oral administration of anti-inflammatory drugs. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2018. © 2018 Wiley Periodicals, Inc.

  2. Characteristics and degradation of chitosan/cellulose acetate microspheres with different model drugs

    Science.gov (United States)

    Zhou, Hui-yun; Chen, Xi-guang

    2008-12-01

    In this study, chitosan/cellulose acetate microspheres (CCAM) were prepared by W/O/W emulsification and solvent evaporation as a drug delivery system. The microspheres were spherical, free-flowing and non-aggregated. The CCAM had good flow and suspension ability. The loading efficiency of different model drugs increased with the increasing hydrophobicity of the drug. The loading efficiency of 6-mercaptopurine (6-MP) was more than 30% whereas that of ranitidine hydrochloride (RT) or acetaminophen (ACP) was only 10%. The pH values of solution affected the swelling ability of CCAM and the relative humidity had little effect on the characteristics of CCAM when it was not more than 75%. The CCAM system had a good effect on the controlled release of different model drugs. However, the release rate became slower with the increase of the hydrophobicity of drugs. The release rate of CCAM loaded with hydrophilic RT was almost 60% during 48 h and the release rate of CCAM loaded with hydrophobic drug of 6-MP was not more than 30%. In the meantime, the CCAM system was degradable in vitro and the degradation rate was faster in lysozyme solution than that in the medium of PBS. So the CCAM system was a degradable promising drug delivery system especially for hydrophobic drugs.

  3. Pilot monitoring study of ibuprofen in surface waters of north of Portugal.

    Science.gov (United States)

    Paíga, Paula; Santos, Lúcia H M L M; Amorim, Célia G; Araújo, Alberto N; Montenegro, M Conceição B S M; Pena, Angelina; Delerue-Matos, Cristina

    2013-04-01

    Ibuprofen is amongst the most worldwide consumed pharmaceuticals. The present work presents the first data in the occurrence of ibuprofen in Portuguese surface waters, focusing in the north area of the country, which is one of the most densely populated areas of Portugal. Analysis of ibup