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Sample records for albumin-stabilized nanoparticle formulation

  1. Paclitaxel Albumin-stabilized Nanoparticle Formulation

    Science.gov (United States)

    This page contains brief information about paclitaxel albumin-stabilized nanoparticle formulation and a collection of links to more information about the use of this drug, research results, and ongoing clinical trials.

  2. Pertuzumab, Trastuzumab, and Paclitaxel Albumin-Stabilized Nanoparticle Formulation in Treating Patients With HER2-Positive Advanced Breast Cancer

    Science.gov (United States)

    2016-06-23

    HER2-positive Breast Cancer; Recurrent Breast Cancer; Stage IIA Breast Cancer; Stage IIB Breast Cancer; Stage IIIA Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Stage IV Breast Cancer; Breast Adenocarcinoma; Inflammatory Breast Carcinoma

  3. Paclitaxel Albumin-Stabilized Nanoparticle Formulation and Carboplatin Followed By Chemoradiation in Treating Patients With Recurrent Head and Neck Cancer

    Science.gov (United States)

    2016-03-30

    Recurrent Salivary Gland Cancer; Recurrent Squamous Cell Carcinoma of the Hypopharynx; Recurrent Squamous Cell Carcinoma of the Larynx; Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity; Recurrent Squamous Cell Carcinoma of the Nasopharynx; Recurrent Squamous Cell Carcinoma of the Oropharynx; Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity; Recurrent Verrucous Carcinoma of the Larynx; Recurrent Verrucous Carcinoma of the Oral Cavity; Salivary Gland Squamous Cell Carcinoma; Tongue Cancer

  4. Paclitaxel Albumin-Stabilized Nanoparticle Formulation in Treating Older Patients With Locally Advanced or Metastatic Breast Cancer

    Science.gov (United States)

    2016-02-09

    Male Breast Cancer; Recurrent Breast Cancer; Stage IV Breast Cancer; Estrogen Receptor-negative Breast Cancer; Estrogen Receptor-positive Breast Cancer; HER2-negative Breast Cancer; HER2-positive Breast Cancer; Progesterone Receptor-negative Breast Cancer; Progesterone Receptor-positive Breast Cancer; Stage IIIA Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Triple-negative Breast Cancer

  5. Doxorubicin Hydrochloride, Cyclophosphamide, and Filgrastim Followed By Paclitaxel Albumin-Stabilized Nanoparticle Formulation With or Without Trastuzumab in Treating Patients With Breast Cancer Previously Treated With Surgery

    Science.gov (United States)

    2013-05-07

    Estrogen Receptor-positive Breast Cancer; HER2-positive Breast Cancer; Stage IA Breast Cancer; Stage IB Breast Cancer; Stage II Breast Cancer; Stage IIIA Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Stage IV Breast Cancer

  6. Carboplatin and Paclitaxel Albumin-Stabilized Nanoparticle Formulation Before Surgery in Treating Patients With Locally Advanced or Inflammatory Triple Negative Breast Cancer

    Science.gov (United States)

    2016-07-14

    Inflammatory Breast Cancer; Stage IIA Breast Cancer; Stage IIIA Breast Cancer; Stage IIIB Breast Cancer; Stage IIIC Breast Cancer; Triple-negative Breast Cancer; Stage IIB Breast Cancer; Estrogen Receptor Negative; Progesterone Receptor Negative; HER2/Neu Negative

  7. Paclitaxel Albumin-Stabilized Nanoparticle Formulation and Bevacizumab in Treating Patients With Stage IV Melanoma That Cannot Be Removed by Surgery or Gynecological Cancers

    Science.gov (United States)

    2016-06-09

    Cervical Adenosarcoma; Cervical Adenosquamous Carcinoma; Cervical Carcinosarcoma; Cervical Squamous Cell Carcinoma; Endometrial Clear Cell Adenocarcinoma; Endometrial Endometrioid Adenocarcinoma; Endometrial Mixed Adenocarcinoma; Endometrial Mucinous Adenocarcinoma; Endometrial Squamous Cell Carcinoma; Endometrial Transitional Cell Carcinoma; Endometrial Undifferentiated Carcinoma; Fallopian Tube Adenocarcinoma; Fallopian Tube Clear Cell Adenocarcinoma; Fallopian Tube Mucinous Adenocarcinoma; Fallopian Tube Serous Adenocarcinoma; Fallopian Tube Transitional Cell Carcinoma; Malignant Ovarian Epithelial Tumor; Malignant Peritoneal Neoplasm; Ovarian Carcinosarcoma; Ovarian Clear Cell Adenocarcinoma; Ovarian Endometrioid Adenocarcinoma; Ovarian Mucinous Adenocarcinoma; Ovarian Serous Adenocarcinoma; Ovarian Transitional Cell Carcinoma; Primary Peritoneal Serous Adenocarcinoma; Recurrent Fallopian Tube Carcinoma; Recurrent Melanoma; Recurrent Ovarian Carcinoma; Recurrent Primary Peritoneal Carcinoma; Stage IV Skin Melanoma; Undifferentiated Fallopian Tube Carcinoma; Undifferentiated Ovarian Carcinoma; Uterine Corpus Carcinosarcoma

  8. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

    Directory of Open Access Journals (Sweden)

    Kunikazu Moribe

    2011-01-01

    Full Text Available Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs or carrier components. Ascorbyl n-alkyl fatty acid derivatives have been formulated as antioxidants or anticancer drugs for nanoparticle formulations such as micelles, microemulsions, and liposomes. ASC-P vesicles called aspasomes are submicron-sized particles that can encapsulate hydrophilic drugs. Several transdermal and injectable formulations of ascorbyl n-alkyl fatty acid derivatives were used, including ascorbyl palmitate.

  9. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

    OpenAIRE

    Kunikazu Moribe; Waree Limwikrant; Kenjirou Higashi; Keiji Yamamoto

    2011-01-01

    Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs...

  10. Nanoparticle formulations of cisplatin for cancer therapy.

    Science.gov (United States)

    Duan, Xiaopin; He, Chunbai; Kron, Stephen J; Lin, Wenbin

    2016-09-01

    The genotoxic agent cisplatin, used alone or in combination with radiation and/or other chemotherapeutic agents, is an important first-line chemotherapy for a broad range of cancers. The clinical utility of cisplatin is limited both by intrinsic and acquired resistance and dose-limiting normal tissue toxicity. That cisplatin shows little selectivity for tumor versus normal tissue may be a critical factor limiting its value. To overcome the low therapeutic ratio of the free drug, macromolecular, liposomal, and nanoparticle drug delivery systems have been explored toward leveraging the enhanced permeability and retention effect and promoting delivery of cisplatin to tumors. Here, we survey recent advances in nanoparticle formulations of cisplatin, focusing on agents that show promise in preclinical or clinical settings. WIREs Nanomed Nanobiotechnol 2016, 8:776-791. doi: 10.1002/wnan.1390 For further resources related to this article, please visit the WIREs website. PMID:26848041

  11. Nanoparticle formulation of ormeloxifene for pancreatic cancer

    Science.gov (United States)

    Khan, Sheema; Chauhan, Neeraj; Yallapu, Murali M.; Ebeling, Mara C.; Balakrishna, Swathi; Ellis, Robert T.; Thompson, Paul A.; Balabathula, Pavan; Behrman, Stephen W.; Zafar, Nadeem; Singh, Man Mohan; Halaweish, Fathi T.; Jaggi, Meena; Chauhan, Subhash C.

    2015-01-01

    Pancreatic cancer is the fourth most prevalent cancer with about an 85% mortality rate; thus, an utmost need exists to discover new therapeutic modalities that would enhance therapy outcomes of this disease with minimal or no side effects. Ormeloxifene (ORM), a synthetic molecule, has exhibited potent anti-cancer effects through inhibition of important oncogenic and proliferation signaling pathways. However, the anti-cancer efficacy of ORM can be further improved by developing its nanoformulation, which will also offer tumor specific targeted delivery. Therefore, we have developed a novel ORM encapsulated poly(lactic-co-glycolic acid) nanoparticle (NP) formulation (PLGA-ORM NP). This formulation was characterized for particle size, chemical composition, and drug loading efficiency, using various physico-chemical methods (TEM, FT-IR, DSC, TGA, and HPLC). Because of its facile composition, this novel formulation is compatible with antibody/aptamer conjugation to achieve tumor specific targeting. The particle size analysis of this PLGA-ORM formulation (~ 100 nm) indicates that this formulation can preferentially reach and accumulate in tumors by the Enhanced Permeability and Retention (EPR) effect. Cellular uptake and internalization studies demonstrate that PLGA-ORM NPs escape lysosomal degradation, providing efficient endosomal release to cytosol. PLGA-ORM NPs showed remarkable anti-cancer potential in various pancreatic cancer cells (HPAF-II, BxPC-3, Panc-1, MiaPaca) and a BxPC-3 xenograft mice model resulting in increased animal survival. PLGA-ORM NPs suppressed pancreatic tumor growth via suppression of Akt phosphorylation and expression of MUC1, HER2, PCNA, CK19 and CD31. This study suggests that the PLGA-ORM formulation is highly efficient for the inhibition of pancreatic tumor growth and thus can be valuable for the treatment of pancreatic cancer in the future. PMID:25890768

  12. Formulation design and evaluation of amorphous ABT-102 nanoparticles.

    Science.gov (United States)

    Jog, Rajan; Kumar, Sumit; Shen, Jie; Jugade, Nital; Tan, David Cheng Thiam; Gokhale, Rajeev; Burgess, Diane J

    2016-02-10

    Amorphous nanoparticles are able to enhance the kinetic solubility and concomitant dissolution rates of BCS class II and BCS class II/IV molecules due to their characteristic increased supersaturation levels, smaller particle size and greater surface area. A DoE approach was applied to investigate formulation and spray drying process parameters for the preparation of spray dried amorphous ABT-102 nanoparticles. Stability studies were performed on the optimized formulations to monitor physical and chemical changes under different temperature and humidity conditions. SLS/soluplus and SLS/PVP K25 were the best stabilizer combinations. Trehalose was used to prevent nanoparticle aggregation during spray drying. Particle size distribution, moisture content, PXRD, PLM, FTIR and in vitro dissolution were utilized to characterize the spray dried nanoparticle formulations. The formulations prepared using soluplus showed enhanced dissolution rate compared to those prepared using PVP K25. Following three months storage, it was observed that the formulations stored at 4°C were stable in terms of particle size distribution, moisture content, and crystallinity, whereas those stored at 25°C/60%RH and 40°C/75%RH were unstable. A predictive model to prepare stable solid spray dried amorphous ABT-102 nanoparticles, incorporating both formulation and process parameters, was successfully developed using multiple linear regression analysis. PMID:26705150

  13. Formulation and evaluation of novel aspirin nanoparticles loaded suppositories

    Institute of Scientific and Technical Information of China (English)

    Ravi Sankar V.; Dhachinamoorthi D.; Chandra Shekar K.B.

    2013-01-01

    The main objective of the present work is to design aspirin nanoparticles loaded suppositories which will reduce the side effects caused by aspirin suppositories.Aspirin nanoparticles were prepared initially based on ionic-gelation mechanism and lyophilized.The prepared nanoparticles were evaluated,and the results confirmed that Fa9 formulation was the best with greater drug entrapment efficiency.Aspirin suppositories were prepared in order to investigate the best base composition.The prepared suppositories were evaluated and FS1,FS3,FS4,FS8,FS11,and FS12 were proved to be the best base compositions based on dissolution performed.The lyophilized aspirin nanoparticles of Fa9 were used to prepare aspirin nanoparticles loaded suppositories.The in vitro results revealed that Fas 11 was the best formulation.

  14. Cream Formulation Impact on Topical Administration of Engineered Colloidal Nanoparticles

    Science.gov (United States)

    Marzi, Roberta; Cigni, Clara; Bedoni, Marzia; Gramatica, Furio; Palugan, Luca; Corsi, Fabio; Granucci, Francesca; Colombo, Miriam

    2015-01-01

    In order to minimize the impact of systemic toxicity of drugs in the treatment of local acute and chronic inflammatory reactions, the achievement of reliable and efficient delivery of therapeutics in/through the skin is highly recommended. While the use of nanoparticles is now an established practice for drug intravenous targeted delivery, their transdermal penetration is still poorly understood and this important administration route remains almost unexplored. In the present study, we have synthesized magnetic (iron oxide) nanoparticles (MNP) coated with an amphiphilic polymer, developed a water-in-oil emulsion formulation for their topical administration and compared the skin penetration routes with the same nanoparticles deposited as a colloidal suspension. Transmission and scanning electron microscopies provided ultrastructural evidence that the amphiphilic nanoparticles (PMNP) cream formulation allowed the efficient penetration through all the skin layers with a controllable kinetics compared to suspension formulation. In addition to the preferential follicular pathway, also the intracellular and intercellular routes were involved. PMNP that crossed all skin layers were quantified by inductively coupled plasma mass spectrometry. The obtained data suggests that combining PMNP amphiphilic character with cream formulation improves the intradermal penetration of nanoparticles. While PMNP administration in living mice via aqueous suspension resulted in preferential nanoparticle capture by phagocytes and migration to draining lymph nodes, cream formulation favored uptake by all the analyzed dermis cell types, including hematopoietic and non-hematopoietic. Unlike aqueous suspension, cream formulation also favored the maintenance of nanoparticles in the dermal architecture avoiding their dispersion and migration to draining lymph nodes via afferent lymphatics. PMID:25962161

  15. Cream formulation impact on topical administration of engineered colloidal nanoparticles.

    Directory of Open Access Journals (Sweden)

    Benedetta Santini

    Full Text Available In order to minimize the impact of systemic toxicity of drugs in the treatment of local acute and chronic inflammatory reactions, the achievement of reliable and efficient delivery of therapeutics in/through the skin is highly recommended. While the use of nanoparticles is now an established practice for drug intravenous targeted delivery, their transdermal penetration is still poorly understood and this important administration route remains almost unexplored. In the present study, we have synthesized magnetic (iron oxide nanoparticles (MNP coated with an amphiphilic polymer, developed a water-in-oil emulsion formulation for their topical administration and compared the skin penetration routes with the same nanoparticles deposited as a colloidal suspension. Transmission and scanning electron microscopies provided ultrastructural evidence that the amphiphilic nanoparticles (PMNP cream formulation allowed the efficient penetration through all the skin layers with a controllable kinetics compared to suspension formulation. In addition to the preferential follicular pathway, also the intracellular and intercellular routes were involved. PMNP that crossed all skin layers were quantified by inductively coupled plasma mass spectrometry. The obtained data suggests that combining PMNP amphiphilic character with cream formulation improves the intradermal penetration of nanoparticles. While PMNP administration in living mice via aqueous suspension resulted in preferential nanoparticle capture by phagocytes and migration to draining lymph nodes, cream formulation favored uptake by all the analyzed dermis cell types, including hematopoietic and non-hematopoietic. Unlike aqueous suspension, cream formulation also favored the maintenance of nanoparticles in the dermal architecture avoiding their dispersion and migration to draining lymph nodes via afferent lymphatics.

  16. Cream formulation impact on topical administration of engineered colloidal nanoparticles.

    Science.gov (United States)

    Santini, Benedetta; Zanoni, Ivan; Marzi, Roberta; Cigni, Clara; Bedoni, Marzia; Gramatica, Furio; Palugan, Luca; Corsi, Fabio; Granucci, Francesca; Colombo, Miriam

    2015-01-01

    In order to minimize the impact of systemic toxicity of drugs in the treatment of local acute and chronic inflammatory reactions, the achievement of reliable and efficient delivery of therapeutics in/through the skin is highly recommended. While the use of nanoparticles is now an established practice for drug intravenous targeted delivery, their transdermal penetration is still poorly understood and this important administration route remains almost unexplored. In the present study, we have synthesized magnetic (iron oxide) nanoparticles (MNP) coated with an amphiphilic polymer, developed a water-in-oil emulsion formulation for their topical administration and compared the skin penetration routes with the same nanoparticles deposited as a colloidal suspension. Transmission and scanning electron microscopies provided ultrastructural evidence that the amphiphilic nanoparticles (PMNP) cream formulation allowed the efficient penetration through all the skin layers with a controllable kinetics compared to suspension formulation. In addition to the preferential follicular pathway, also the intracellular and intercellular routes were involved. PMNP that crossed all skin layers were quantified by inductively coupled plasma mass spectrometry. The obtained data suggests that combining PMNP amphiphilic character with cream formulation improves the intradermal penetration of nanoparticles. While PMNP administration in living mice via aqueous suspension resulted in preferential nanoparticle capture by phagocytes and migration to draining lymph nodes, cream formulation favored uptake by all the analyzed dermis cell types, including hematopoietic and non-hematopoietic. Unlike aqueous suspension, cream formulation also favored the maintenance of nanoparticles in the dermal architecture avoiding their dispersion and migration to draining lymph nodes via afferent lymphatics. PMID:25962161

  17. FORMULATION DEVELOPMENT AND EVALUATION OF ABACAVIR LOADED POLYMETHACRYLIC ACID NANOPARTICLES

    Directory of Open Access Journals (Sweden)

    S.L. Dheivanai

    2012-03-01

    Full Text Available Nanoparticles render a promising drug delivery system of controlled and targeted drug release. These are specially designed to release the drug in the vicinity of target tissue. The aim of this present study was to develop and evaluate polymethacrylic acid nanoparticles containing nanoparticles abacavir in different drug to polymer ratio by nanoprecipitation method. SEM indicates that nanoparticles have a discrete spherical structure without aggregation. The average particle size was accurately found to be 120 ±9 - 403 ±3 nm. The particle size of the nanoparticles was gradually increased with increase in the proportion of polymethacrylic acid polymer. The drug containing nanoparticles was increasing on increasing polymer concentration up to a particular concentration ratio. No difference was observed in the extent of degradation of product during sixty days in which, nanoparticles were stored at various temperatures. FT-IR studies indicated that there were no chemical interaction between drug and polymer and stability of drug. The in-vitro release character from all the drug loaded batches was found to be zero order and rendered sustained release over a period of 24 h. The prepared formulations overcome and breakup the drawbacks and limitations of abacavir sustained release formulations and could possibility be advantageous in terms of increased bioavailability and efficacy of abacavir.

  18. Influence of formulation factors on the preparation of zein nanoparticles.

    Science.gov (United States)

    Podaralla, Satheesh; Perumal, Omathanu

    2012-09-01

    The main objective of the present study was to investigate the influence of various formulation parameters on the preparation of zein nanoparticles. 6,7-dihydroxycoumarin (DHC) was used as a model hydrophobic compound. The influence of pH of the aqueous phase, buffer type, ionic strength, surfactant, and zein concentration on particle size, polydispersity index, and zeta potential of DHC-loaded zein nanoparticles were studied. Smaller nanoparticles were formed when the pH was close to the isoelectric point of zein. DHC-loaded zein nanoparticles prepared using citrate buffer (pH 7.4) was better than phosphate buffer in preventing particle aggregation during lyophilization. The ionic strength did not have a significant influence on the particle size of DHC-loaded zein nanoparticles. A combination of Pluronic F68 and lecithin in 2:1 ratio stabilized the zein nanoparticles. An increase in zein concentration led to increase in particle size of DHC-loaded zein nanoparticles. The use of optimal conditions produced DHC-loaded nanoparticles of 256 ± 30 nm and an encapsulation efficiency of 78 ± 7%. Overall, the study demonstrated the optimal conditions to prepare zein nanoparticles for drug encapsulation.

  19. Sargramostim and Paclitaxel Albumin-Stabilized Nanoparticle Formulation in Treating Patients With Advanced Ovarian Cancer, Fallopian Tube Cancer, or Primary Peritoneal Cancer That Did Not Respond to Previous Chemotherapy

    Science.gov (United States)

    2014-01-15

    Brenner Tumor; Fallopian Tube Cancer; Ovarian Clear Cell Cystadenocarcinoma; Ovarian Endometrioid Adenocarcinoma; Ovarian Mixed Epithelial Carcinoma; Ovarian Mucinous Cystadenocarcinoma; Ovarian Serous Cystadenocarcinoma; Ovarian Undifferentiated Adenocarcinoma; Peritoneal Cavity Cancer; Recurrent Ovarian Epithelial Cancer; Stage III Ovarian Epithelial Cancer; Stage IV Ovarian Epithelial Cancer

  20. Nanoparticles containing curcuminoids (Curcuma longa: development of topical delivery formulation

    Directory of Open Access Journals (Sweden)

    Cristina M. Zamarioli

    2015-02-01

    Full Text Available Solid lipid nanoparticles incorporating Curcuma longa L., Zingiberaceae, curcuminoids were produced by the hot melt emulsion method. A Box–Behnken factorial design was adopted to study the nanoparticles production at different levels of factors such as the percentage of curcuminoids, time of homogenization and surfactant ratio. The optimized nanoparticles were incorporated into hydrogels for stability, drug release and skin permeation tests. The average nanoparticle sizes were 210.4 nm; the zeta potential of −30.40 ± 4.16; the polydispersivity was 0.222 ± 0.125. The average encapsulation efficiency of curcumin and curcuminoids was 52.92 ± 5.41% and 48.39 ± 6.62%, respectively. Solid lipid nanocapsules were obtained with curcumin load varying from 14.2 to 33.6% and total curcuminoids load as high as 47.7%. The topical formulation containing SLN-Curcuminoids showed good spreadability and stability when subjected to mechanical stress test remained with characteristic color, showed no phase separation and no significant change in pH. As a result of slow release, the nanoparticles were able to avoid permeation or penetration in the pig ear epidermis/dermis during 18 h. The topical formulation is stable and can be used in further in vivo studies for the treatment of inflammatory reactions, in special for radiodermitis.

  1. Docetaxel loaded chitosan nanoparticles: formulation, characterization and cytotoxicity studies.

    Science.gov (United States)

    Jain, Ankit; Thakur, Kanika; Kush, Preeti; Jain, Upendra K

    2014-08-01

    The primary objective of the present investigation was to explore biodegradable chitosan as a polymeric material for formulating docetaxel nanoparticles (DTX-NPs) to be used as a delivery system for breast cancer treatment. Docetaxel loaded chitosan nanoparticles were formulated by water-in-oil nanoemulsion system and characterized in terms of particle size, zeta potential, polydispersity index, drug entrapment efficiency (EE), loading capacity (LC), scanning electron microscopy (SEM), in vitro release study and drug release kinetics. Further, to evaluate the potential anticancer efficacy of docetaxel loaded chitosan nanoparticulate system, in vitro cytotoxicity studies on human breast cancer cell line (MDA-MB-231) were carried out. The morphological studies revealed the spherical shape of docetaxel loaded chitosan nanoparticles having an average size of 170.1±5.42-227.6±7.87nm, polydispersity index in the range of 0.215±0.041-0.378±0.059 and zeta potential between 28.3 and 31.4mV. Nanoparticles exhibited 65-76% of drug entrapment and 8-12% loading capacity releasing about 68-83% of the drug within 12h following Higuchi's square-root kinetics. An increase of 20% MDA-MB-231 cell line growth inhibition was determined by docetaxel loaded chitosan nanoparticles with respect to the free drug after 72h incubation.

  2. EXPLOITING THE VERSATILITY OF CHOLESTEROL IN NANOPARTICLES FORMULATION.

    Science.gov (United States)

    Belletti, D; Grabrucker, A M; Pederzoli, F; Menrath, I; Cappello, V; Vandelli, M A; Forni, F; Tosi, G; Ruozi, B

    2016-09-10

    The biocompatibility of polymers, lipids and surfactants used to formulate is crucial for the safe and sustainable development of nanocarriers (nanoparticles, liposomes, micelles, and other nanocarriers). In this study, Cholesterol (Chol), a typical biocompatible component of liposomal systems, was formulated in Chol-based solid nanoparticles (NPs) stabilized by the action of surfactant and without the help of any other formulative component. Parameters as type (Solutol HS 15, cholic acid sodium salt, poly vinyl alcohol and Pluronic-F68), concentration (0.2; 0.5 and 1% w/v) of surfactant and working temperature (r.t. and 45°C) were optimized and all samples characterized in terms of size, zeta potential, composition, thermal behavior and structure. Results demonstrated that only Pluronic-F68 (0.5% w/v) favors the organization of Chol chains in structured NPs with mean diameter less than 400nm. Moreover, we demonstrated the pivotal role of working temperature on surfactant aggregation state/architecture/stability of Chol-based nanoparticles. At room temperature, Pluronic-F68 exists in solution as individual coils. In this condition, nanoprecipitation of Chol formed the less stable NPs with a 14±3% (w/w) of Pluronic-F68 prevalently on surface (NP-Chol/0.5). On the contrary, working near the critical micelle temperature (CMT) of surfactant (45°C), Chol precipitates with Pluronic-F68 (9±5% w/w) in a compact stable matricial structure (NP-Chol/0.5-45). In vitro studies highlight the low toxicity and the affinity of NP-Chol/0.5-45 for neuronal cells suggesting their potential applicability in pathologies with a demonstrated alteration of neuronal plasticity and synaptic communication (i.e. Huntington's disease).

  3. Formulation and Characterization of Acetaminophen Nanoparticles in Orally Disintegrating Films

    Science.gov (United States)

    AI-Nemrawi, Nusaiba K.

    The purpose of this study is to prepare acetaminophen loaded nanoparticles to be cast directly, while still in the emulsion form, into Orally Disintegrating Films (ODF). By casting the nanoparticles in the films, we expected to keep the particles in a stable form where the nanoparticles would be away from each other to prevent their aggregation. Once the films are applied on the buccal mucosa, they are supposed to dissolve within seconds, releasing the nanoparticles. Then the nanoparticles could be directly absorbed through the mucosa to the blood stream and deliver acetaminophen there. The oral cavity mucosa is one of the most attractive sites for systemic drug delivery due to its high permeability and blood supply. Furthermore, it is robust and shows short recovery times after stress or damage, and the drug bypasses first pass effect and avoids presystemic elimination in the GI tract. Nanoencapsulation increases drug efficacy, specificity, tolerability and therapeutic index. These Nanocapsules have several advantages in the protection of premature degradation and interaction with the biological environment, enhancement of absorption into a selected tissue, bioavailability, retention time and improvement of intracellular penetration. The most important characteristics of nanoparticles are their size, encapsulation efficiency (EE), zeta potential (surface charge), and the drug release profiles. Unfortunately, nanoparticles tend to precipitate or aggregate into larger particles within a short time after preparation or during storage. Some solutions for this problem were mentioned in literature including lyophilization and spray drying. These methods are usually expensive and give partial solutions that might have secondary problems; such as low re-dispersion efficacy of the lyophilized NPs. Furthermore, most of the formulations of NPs are invasive or topical. Few formulas are available to be given orally. Fast disintegrating films (ODFs) are rapidly gaining interest

  4. FORMULATION AND CHARACTERIZATION OF SOLID LIPID NANOPARTICLES FOR TRANSDERMAL DELIVERY OF TESTOSTERONE

    Directory of Open Access Journals (Sweden)

    L. K. Omray

    2014-07-01

    Full Text Available Present study deals with the formulation and characterization of testosterone bearing solid lipid nanoparticles for transdermal drug delivery. Solid lipid nanoparticles of testosterone were prepared by ether injection method. Solid lipid nanoparticles were prepared by testosterone, glyceryl mono stearate, brij 35, propylene glycol and double distilled water. Four different formulations i.e. F1 to F4 were prepared in different quantity of brij 35. All the solid lipid nanoparticles formulations were characterized on the basis of electron microscopy, particle size by zeta sizer, polydispersity index, encapsulation efficiency, viscosity and in vitro drug release study. Average size and polydispersity index of developed formulation F3 found to have 298 nm and 0.328 respectively, determined by zeta sizer. Encapsulation efficiency of formulation F3 was found to have 54.16%. Viscosity of formulation was also enough to handle for transdermal application. All the formulations followed zero order release profile.

  5. Formulation and Characterization of Acetaminophen Nanoparticles in Orally Disintegrating Films

    Science.gov (United States)

    AI-Nemrawi, Nusaiba K.

    The purpose of this study is to prepare acetaminophen loaded nanoparticles to be cast directly, while still in the emulsion form, into Orally Disintegrating Films (ODF). By casting the nanoparticles in the films, we expected to keep the particles in a stable form where the nanoparticles would be away from each other to prevent their aggregation. Once the films are applied on the buccal mucosa, they are supposed to dissolve within seconds, releasing the nanoparticles. Then the nanoparticles could be directly absorbed through the mucosa to the blood stream and deliver acetaminophen there. The oral cavity mucosa is one of the most attractive sites for systemic drug delivery due to its high permeability and blood supply. Furthermore, it is robust and shows short recovery times after stress or damage, and the drug bypasses first pass effect and avoids presystemic elimination in the GI tract. Nanoencapsulation increases drug efficacy, specificity, tolerability and therapeutic index. These Nanocapsules have several advantages in the protection of premature degradation and interaction with the biological environment, enhancement of absorption into a selected tissue, bioavailability, retention time and improvement of intracellular penetration. The most important characteristics of nanoparticles are their size, encapsulation efficiency (EE), zeta potential (surface charge), and the drug release profiles. Unfortunately, nanoparticles tend to precipitate or aggregate into larger particles within a short time after preparation or during storage. Some solutions for this problem were mentioned in literature including lyophilization and spray drying. These methods are usually expensive and give partial solutions that might have secondary problems; such as low re-dispersion efficacy of the lyophilized NPs. Furthermore, most of the formulations of NPs are invasive or topical. Few formulas are available to be given orally. Fast disintegrating films (ODFs) are rapidly gaining interest

  6. Formulation and Evaluation of Morin-Loaded Solid Lipid Nanoparticles.

    Science.gov (United States)

    Ikeuchi-Takahashi, Yuri; Ishihara, Chizuko; Onishi, Hiraku

    2016-09-01

    In this study, solid lipid nanoparticle (SLN) suspensions were prepared using a base of hard fat with or without ethylcellulose (EC) and polyvinyl alcohols (PVA) and polysorbate (Tween) 60 surfactants. Commercially available PVAs vary in their degree of saponification and polymerization, and the appropriate PVAs to form SLNs from hard fat with or without EC were investigated. A relatively low-saponification-degree PVA was required to reproducibly form SLN suspensions without EC and relatively high-saponification-degree PVAs were suitable for SLNs with EC. The release of morin from SLNs with EC was more sustained than that from SLNs without EC. The maximum plasma concentration (Cmax) of SLNs with and without EC were almost the same, and both were higher than that of a morin suspension. The area under the curve for 0 to 360 min (AUC0-360) of SLNs with EC was increased compared with those of a morin suspension and SLNs without EC. The median diameter of SLNs with EC and a very low-saponification-degree PVA was decreased compared to other formulation, and morin release was more sustained for this formulation. SLNs with EC and a very low-saponification-degree PVA showed higher Cmax and AUC0-360 than SLNs with EC lacking a very low-saponification-degree PVA. The optimized SLNs with EC and a very low-saponification-degree PVA improved bioavailability via increased accessibility to the enterocyte surface by decreased particle size and increased permeation of SLN encapsulated morin through the intestinal membrane by sustained release properties.

  7. Solid Lipid Nanoparticles Formulated for Transdermal Aconitine Administration and Evaluated In Vitro and In Vivo.

    Science.gov (United States)

    Zhang, Yong-Tai; Han, Meng-Qing; Shen, Li-Na; Zhao, Ji-Hui; Feng, Nian-Ping

    2015-02-01

    In this study, solid lipid nanoparticles were formulated for transdermal delivery of aconitine to improve its safety and permeability. Aconitine-loaded solid lipid nanoparticles were formulated as an oil-in-water microemulsion. Drug encapsulation efficiencies for these formulations were higher than 85%, and correlated positively with levels of surfactant and oil matrix. The size of the solid lipid nanoparticles was increased with an increase of the oil matrix, and reduction of the surfactant levels. Compared with an ethanol tincture, all the tested solid lipid nanoparticle formulations achieved improved transdermal fluxes and drug deposition in skin in vitro. Real-time monitoring of drug distribution in rat dermis using in vivo microdialysis showed that aconitine concentration was markedly higher following application of solid lipid nanoparticles, compared to tincture, throughout the experimental period. A regional comparison of rat skin found that application of solid lipid nanoparticles to the scapular region resulted in higher AUC(0-t) and C(max), compared to those achieved with application to the abdomen or chest (p nanoparticles contributed to stronger anti-inflammatory and analgesic effects on mouse in vivo models of pain than the tincture (p in vivo studies indicated that smaller particle sizes of solid lipid nanoparticles enhanced the transdermal permeability of aconitine, which can promote drug efficacy, reduce administration time, and improve medication safety.

  8. FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF A POORLY WATER SOLUBLE MODEL DRUG, IBUPROFEN

    OpenAIRE

    De Pintu Kumar; Dinda Subas C; Chakraborty Subrata; Rakshit Soumen

    2012-01-01

    Approximately 40% of lipophilic drug candidates fail to comply the commercial requirements of solubility and formulation stability, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle (SLN) technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles typically are spherical with average diameters between 1 to 1000 nanometers. SLNs possess a solid lipid core matrix that can solubilize lipophilic m...

  9. Simvastatin-loaded PLGA nanoparticles for improved oral bioavailability and sustained release: Effect of formulation variables

    Directory of Open Access Journals (Sweden)

    Aman Soni

    2011-01-01

    Full Text Available The objective of this study was to prepare a nanoparticulate formulation of simvastatin (SV for improving oral bioavailability and sustaining the drug release while investigating the effect of various formulation parameters on characteristics of nanoparticles. Nanoparticles containing SV were prepared by a modified emulsification solvent evaporation technique using a biodegradable polymer, poly(d,l-lactide-coglycolide (PLGA as a sustained release carrier. The effect of various formulation parameters such as drug polymer ratios (SV:PLGA, 1:4 to 1:1, organic solvents (methanol/dichloromethane, and surfactants (PVA/polysorbate-80 in a fixed concentration (0.5%, w/v were studied for particle size, drug loading, and entrapment efficiency. Nanoparticles were characterized by differential scanning calorimetry (DSC and their shapes were observed by scanning electron microscopy (SEM. An aqueous solubility study indicated that the dissolution rates were remarkably increased for nanoparticles compared with the drug alone. The in vitro drug release study of the nanoparticles showed a biphasic release pattern: one initial burst release of 40.56% in the first 4 h which can be helpful to improve the penetration of drug followed by a second slow-release phase (extended release consistent with a Higuchi diffusion mechanism. The hypolipidemic activity of nanoparticles was determined in comparison with SV in male Wistar rats for changes in total cholesterol (CH and triglyceride (TG levels in blood. Nanoparticles showed a significantly better in vivo performance than SV in reducing total CH and TG levels which is primarily attributed to the improved solubility and dissolution of nanoparticles. Together, these results indicate that nanoparticulate formulations are ideal carriers for oral administration of SV having great potential to improve the oral bioavailability and sustain the drug release, thereby minimizing the dose-dependent adverse effects and maximizing

  10. Early development drug formulation on a chip: fabrication of nanoparticles using a microfluidic spray dryer.

    Science.gov (United States)

    Thiele, Julian; Windbergs, Maike; Abate, Adam R; Trebbin, Martin; Shum, Ho Cheung; Förster, Stephan; Weitz, David A

    2011-07-21

    Early development drug formulation is exacerbated by increasingly poor bioavailability of potential candidates. Prevention of attrition due to formulation problems necessitates physicochemical analysis and formulation studies at a very early stage during development, where the availability of a new substance is limited to small quantities, thus impeding extensive experiments. Miniaturization of common formulation processes is a strategy to overcome those limitations. We present a versatile technique for fabricating drug nanoformulations using a microfluidic spray dryer. Nanoparticles are formed by evaporative precipitation of the drug-loaded spray in air at room temperature. Using danazol as a model drug, amorphous nanoparticles of 20-60 nm in diameter are prepared with a narrow size distribution. We design the device with a geometry that allows the injection of two separate solvent streams, thus enabling co-spray drying of two substances for the production of drug co-precipitates with tailor-made composition for optimization of therapeutic efficiency. PMID:21617823

  11. Effect of formulation variables on preparation of celecoxib loaded polylactide-co-glycolide nanoparticles.

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    Dustin L Cooper

    Full Text Available Polymer based nanoparticle formulations have been shown to increase drug bioavailability and/or reduce drug adverse effects. Nonsteroidal anti-inflammatory drugs (e.g. celecoxib reduce prostaglandin synthesis and cause side effects such as gastrointestinal and renal complications. The aim of this study was to formulate celecoxib entrapped poly lactide-co-glycolide based nanoparticles through a solvent evaporation process using didodecyldimethylammonium bromide or poly vinyl alcohol as stabilizer. Nanoparticles were characterized for zeta potential, particle size, entrapment efficiency, and morphology. Effects of stabilizer concentration (0.1, 0.25, 0.5, and 1% w/v, drug amount (5, 10, 15, and 20 mg, and emulsifier (lecithin on nanoparticle characterization were examined for formula optimization. The use of 0.1, 0.25, and 0.5% w/v didodecyldimethylammonium bromide resulted in a more than 5-fold increase in zeta potential and a more than 1.5-fold increase in entrapment efficiency with a reduction in particle size over 35%, when compared to stabilizer free formulation. Nanoparticle formulations were also highly influenced by emulsifier and drug amount. Using 0.25% w/v didodecyldimethylammonium bromide NP formulations, peak zeta potential was achieved using 15 mg celecoxib with emulsifier (17.15±0.36 mV and 20 mg celecoxib without emulsifier (25.00±0.18 mV. Peak NP size reduction and entrapment efficiency was achieved using 5 mg celecoxib formulations with (70.87±1.24 nm and 95.55±0.66%, respectively and without (92.97±0.51 nm and 95.93±0.27%, respectively emulsifier. In conclusion, formulations using 5 mg celecoxib with 0.25% w/v didodecyldimethylammonium bromide concentrations produced nanoparticles exhibiting enhanced size reduction and entrapment efficiency. Furthermore, emulsifier free formulations demonstrated improved zeta potential when compared to formulations containing emulsifier (p<0.01. Therefore, our results suggest the use of

  12. FORMULATION AND OPTIMIZATION OF CEFPODOXIME PROXETIL LOADED SOLID LIPID NANOPARTICLES BY BOX-BEHNKEN DESIGN

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    Umesh A. Nimbalkar

    2011-06-01

    Full Text Available The objective of this study was to develop and evaluate solid lipid nanoparticles of Cefpodoxime Proxetil for enhancement of bioavailability via its lymphatic absorption. The solid lipid nanoparticles (SLNs were prepared by solvent evaporation method using Precirol as a lipid carrier. A Box Behnken design has been applied to study the effect of independent variables i.e. lipid concentration, span 60 concentration and stirring speed on dependent variables i.e. particle size and entrapment efficiency. Response surface plots and counter plots were drawn and optimum formulations were selected based on feasibility search method. Validation of optimized study performed using four confirmatory runs indicated very high degree of prognostic ability of response surface methodology, with mean percentage error as +0.02. Optimized SLN formulations were freeze dried and its effect on particle size was evaluated. Optimized solid lipid nanoparticles were evaluated for EE, Drug content, FTIR, DSC, SEM and in vitro drug release study.

  13. FORMULATION AND EVALUATION OF CURCUMIN LOADED MAGNETIC NANOPARTICLES FOR CANCER THERAPY

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    T. Silambarasi, S. Latha*, M. Thambidurai and P. Selvamani

    2012-05-01

    Full Text Available The conventional chemotherapeutic agents in oncology drug discovery still exhibit poor specificity in reaching tumor site and often restricted by dose-limiting toxicity. The combination of developing drug formulation by utilizing both controlled release technology and drug targeting technology may provide a more efficient and less harmful solution to conquer the limitations found in conventional chemotherapy. In this study, the anticancer drug curcumin was encapsulated in a polymeric magnetic nanoparticle which was synthesized with polymers β-cyclodextrin cross linked with epichlorhydrin, hydrophobically modified dextran byoleoylchloride and magnetite as magnetic material. Particle size, surface morphology, zeta potential and magnetic measurements were used to characterize the developed drug formulations. The developed drug-iron conjugated nanoparticles were found to be within the size range of 100nm with excellent negative surface charge (>-30eV and spherical in shape. The magnetic susceptibility and magnetization curve substantiate the super paramagnetic property of the developed drug formulation. Furthermore, the drug content and encapsulation efficiency found was directly proportional to epichlorhydrin β-cyclodextrin concentration in the developed formulation. The in-vitro release profile of curcumin loaded magnetic nanoparticles exhibited biphasic initial release first 24 hours and release extended upto 72 hours. The drug release kinetics indicated that drug release from drug formulations were best explained by Higuchi’s equation, as these plots showed the highest linearity but a close relationship was also noted with first-order kinetics.

  14. Formulation and evaluation of dorzolamide hydrochloride-loaded nanoparticles as controlled release drug delivery system

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    Azza A Hasan

    2012-01-01

    Full Text Available This study aimed to prepare anti-glaucomatous dorzolamide hydrochloride-(Dorzo loaded nanoparticles as a controlled release system. Eudragit RS 100 (RS and/or RL 100 (RL were used in formulations by an opportunely adapted Quasi-emulsion solvent diffusion technique. The formulations were evaluated in terms of particle size, zeta potential, drug entrapment, and release profile. All formulations showed tiny particle size varying from 114 to 395 nm for RS and 65 to 277 nm for RL. Positive zeta potential was +19 to +32 mV for RS and +23 to +42 mV for RL formulations. It was demonstrated that increasing polymer concentration lead to increase the percentage of drug entrapped in all batches, to a certain extent (drug: polymer 1:4. Nanoparticles prepared using RL showed lower entrapment efficiency than RS. In contrast, increasing the stirring rate resulted in an increase in the percentage of Dorzo entrapped. A prolonged drug release was shown by all the formulations. Increasing the polymer concentration caused a decrease in the release rate. Moreover, it was evident that increasing RL content increased the amount of Dorzo released. Dorzo-loaded nanoparticles could represent promising drug ophthalmic carriers, due to small particle size, positive zeta potential, and sustained release profile; hence, expecting prolonged corneal contact time, more therapeutically efficient, decreased frequency of administration per day, and better patient compliance.

  15. Ag85A DNA Vaccine Delivery by Nanoparticles: Influence of the Formulation Characteristics on Immune Responses.

    Science.gov (United States)

    Poecheim, Johanna; Barnier-Quer, Christophe; Collin, Nicolas; Borchard, Gerrit

    2016-01-01

    The influence of DNA vaccine formulations on immune responses in combination with adjuvants was investigated with the aim to increase cell-mediated immunity against plasmid DNA (pDNA) encoding Mycobacterium tuberculosis antigen 85A. Different ratios of pDNA with cationic trimethyl chitosan (TMC) nanoparticles were characterized for their morphology and physicochemical characteristics (size, zeta potential, loading efficiency and pDNA release profile) applied in vitro for cellular uptake studies and in vivo, to determine the dose-dependent effects of pDNA on immune responses. A selected pDNA/TMC nanoparticle formulation was optimized by the incorporation of muramyl dipeptide (MDP) as an immunostimulatory agent. Cellular uptake investigations in vitro showed saturation to a maximum level upon the increase in the pDNA/TMC nanoparticle ratio, correlating with increasing Th1-related antibody responses up to a definite pDNA dose applied. Moreover, TMC nanoparticles induced clear polarization towards a Th1 response, indicated by IgG2c/IgG1 ratios above unity and enhanced numbers of antigen-specific IFN-γ producing T-cells in the spleen. Remarkably, the incorporation of MDP in TMC nanoparticles provoked a significant additional increase in T-cell-mediated responses induced by pDNA. In conclusion, pDNA-loaded TMC nanoparticles are capable of provoking strong Th1-type cellular and humoral immune responses, with the potential to be further optimized by the incorporation of MDP. PMID:27626449

  16. Formulation and characterization of pyrazinamide polymeric nanoparticles for pulmonary tuberculosis: Efficiency for alveolar macrophage targeting

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    J N Ravi Varma

    2015-01-01

    Full Text Available Pyrazinamide, a highly specific agent against Mycobacterium tuberculosis is used as first-line drug to treat tuberculosis. The current work aims to formulate polymeric nanoparticles based drug delivery system to sustain the release profile and reduce the dosing frequency of pyrazinamide. Further aim was to target the macrophages within body fluid. These polymeric nanoparticles were prepared by simultaneous double-emulsion (W/O/W solvent evaporation/diffusion technique. The prepared dispersions were characterized for various biopharmaceutical parameters such as particle size, zeta potential, polydispersity index, drug loading capacity, entrapment efficiency and targeting to alveolar macrophages. The formulated polymeric nanoparticles were in the particle size range of 45.51 to 300.4 nm with a maximum drug entrapment efficiency of 80.9%. The stability study of optimized batch conducted at 40±2°/75±5% relative humidity showed no significant changes up to 90 days. X-Ray Diffraction spectrum exhibits the transformation of crystalline form of drug to amorphous in the formulation. Scanning Electron Microscope image showed nanoparticles spherical in shape with smooth surface. In vitro release profiles were biphasic in nature with burst release followed by controlled release over a period of 24 h obeying diffusion mechanism. In vivo and ex vivo studies results of the study show significant uptake of the nanoparticles by alveolar macrophages through fluorescent micrograph. Polymeric nanoparticles formulation of pyrazinamide could encompass significant uptake by alveolar macrophages, the high first-pass metabolism, sustain the release of drug leading to reduction in dose, toxicity and improvement of patient compliance.

  17. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies.

    Science.gov (United States)

    Bhaskar, Kesavan; Anbu, Jayaraman; Ravichandiran, Velayutham; Venkateswarlu, Vobalaboina; Rao, Yamsani Madhusudan

    2009-01-01

    The aim of the study is to prepare aqueous dispersions of lipid nanoparticles--flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 +/- 2.77 microg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 +/- 2.96 microg/ml). The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel. PMID:19243632

  18. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies

    Science.gov (United States)

    Bhaskar, Kesavan; Anbu, Jayaraman; Ravichandiran, Velayutham; Venkateswarlu, Vobalaboina; Rao, Yamsani Madhusudan

    2009-01-01

    The aim of the study is to prepare aqueous dispersions of lipid nanoparticles – flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 ± 2.77 μg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 ± 2.96 μg/ml). The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel PMID:19243632

  19. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies

    Directory of Open Access Journals (Sweden)

    Venkateswarlu Vobalaboina

    2009-02-01

    Full Text Available Abstract The aim of the study is to prepare aqueous dispersions of lipid nanoparticles – flurbiprofen solid lipid nanoparticles (FLUSLN and flurbiprofen nanostructured lipid carriers (FLUNLC by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1 and NLC gel (B1 for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 ± 2.77 μg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 ± 2.96 μg/ml. The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel

  20. FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION OF NOVEL THIENOPYRIMIDINES AND TRIAZOLOTHIENOPYRIMIDINES LOADED SOLID LIPID NANOPARTICLES

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    Mulla Jameel Ahmed S.

    2010-09-01

    Full Text Available Thienopyrimidines and triazolothienopyrimidines loaded solid lipid nanoparticles (SLNs were produced by microemulsion method. All the formulations were subjected to particle size analysis, zeta potential, compound entrapment efficiency and in vitro release studies. The SLNs formed were in nano-size range with maximum entrapment efficiency. Formulation with 195 nm in particle size and 84.20% of compound entrapment was subjected to scanning electron microscopy (SEM for surface morphology, differential scanning calorimetry (DSC for thermal analysis and short term stability studies. SEM confirms that the SLNs are circular in shape. The compound release behavior from SLN suspension exhibited biphasic pattern with an initial burst and prolonged release over 24 h.

  1. Drug/polymer nanoparticles prepared using unique spray nozzles and recent progress of inhaled formulation

    OpenAIRE

    Tetsuya Ozeki; Tatsuaki Tagami

    2014-01-01

    Inhaled formulations are promising for pulmonary and systemic non-pulmonary diseases. Functional engineered particles including drugs and drug-loaded nanocarriers have been anticipated because they can improve drug delivery efficacy against target sites in the lungs or blood. In this review, unique spray nozzles (e.g., four-fluid spray nozzle and two-solution mixing type nozzle) for the preparation of nanocomposite particles which mean microparticles containing drug nanoparticles are describe...

  2. Polymer Stabilized Nanosuspensions Formed via Flash Nanoprecipitation: Nanoparticle Formation, Formulation, and Stability

    Science.gov (United States)

    Zhu, ZhengXi

    Nanoparticles loaded with hydrophobic components (e.g., active pharmaceutical ingredients, medical diagnostic agents, nutritional or personal care chemicals, catalysts, dyes/pigments, and substances with exceptional magnetic/optical/electronic/thermal properties) have tremendous industrial applications. The common desire is to efficiently generate nanoparticles with a desired size, size distribution, and size stability. Recently, Flash NanoPrecipition (FNP) technique with a fast, continuous, and easily scalable process has been developed to efficiently generate hydrophobe-loaded nanoparticles. This dissertation extended this technique, optimized process conditions and material formulations, and gave new insights into the mechanism and kinetics of nanoparticle formation. This dissertation demonstrated successful generation of spherical beta-carotene nanoparticles with an average diameter of 50--100 nm (90 wt% nanoparticles below 200 nm), good size stability (maintained an average diameter below 200 nm for at least one week in saline), and much higher loading (80--90 wt%) than traditional carriers, such as micelles and polymersomes (typically FNP were proposed. To optimize the material formulations, either polyelectrolytes (i.e., epsilon-polylysine, branched and linear poly(ethylene imine), and chitosan) or amphiphilic diblock copolymers (i.e., polystyrene-b-poly(ethylene glycol) (PS-b-PEG), polycarprolactone-b-poly(ethylene glycol) (PCL-b-PEG), poly(lactic acid)-b-poly(ethylene glycol) (PLA-b-PEG), and poly(lactic-co-glycolic acid)-b-poly(ethylene glycol) (PLGA-b-PEG)) were selectively screened to study the nanoparticle size, distribution, and stability. The effect of the molecular weight of the polymers and pH were also studied. Chitosan and PLGA-b-PEG best stabilized the beta-carotene nanoparticles. Solubility of the hydrophobic drug solute in the aqueous mixture was considered to dominate the nanoparticle stability (i.e., size and morphology) in terms of Ostwald

  3. Engineering novel targeted nanoparticle formulations to increase the therapeutic efficacy of conventional chemotherapeutics against multiple myeloma

    Science.gov (United States)

    Ashley, Jonathan D.

    Multiple myeloma (MM) is a hematological malignancy which results from the uncontrolled clonal expansion of plasma cells within the body. Despite recent medical advances, this disease remains largely incurable, with a median survival of ˜7 years, owing to the development of drug resistance. This dissertation will explore new advances in nanotechnology that will combine the cytotoxic effects of small molecule chemotherapeutics with the tumor targeting capabilities of nanoparticles to create novel nanoparticle formulations that exhibit enhanced therapeutic indices in the treatment of MM. First, doxorubicin was surfaced conjugated onto micellar nanoparticles via an acid labile hydrazone bond to increase the drug accumulation at the tumor. The cell surface receptor Very Late Antigen-4 (VLA-4; alpha4beta1) is expressed on cancers of hematopoietic origin and plays a vital role in the cell adhesion mediated drug resistance (CAM-DR) in MM. Therefore, VLA-4 antagonist peptides were conjugated onto the nanoparticles via a multifaceted procedure to actively target MM cells and simultaneously inhibit CAM-DR. The micellar doxorubicin nanoparticles were able to overcome CAM-DR and demonstrated improved therapeutic index relative to free doxorubicin. In addition to doxorubicin, other classes of therapeutic agents, such as proteasome inhibitors, can be incorporated in nanoparticles for improved therapeutic outcomes. Utilizing boronic acid chemistry, bortezomib prodrugs were synthesized using a reversible boronic ester bond and then incorporated into liposomes. The different boronic ester bonds that could be potentially used in the synthesis of bortezomib prodrugs were screened based on stability using isobutylboronic acid. The liposomal bortezomib nanoparticles demonstrated significant proteasome inhibition and cytotoxicity in MM cells in vitro, and dramatically reduced the non-specific toxicities associated with free bortezomib while maintaining significant tumor growth

  4. FORMULATION AND EVALUATION OF SOLID LIPID NANOPARTICLES OF A POORLY WATER SOLUBLE MODEL DRUG, IBUPROFEN

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    De Pintu Kumar

    2012-12-01

    Full Text Available Approximately 40% of lipophilic drug candidates fail to comply the commercial requirements of solubility and formulation stability, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle (SLN technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles typically are spherical with average diameters between 1 to 1000 nanometers. SLNs possess a solid lipid core matrix that can solubilize lipophilic molecules. The lipid core is stabilized by surfactants. Primary objective of this study is to enhance the solubility and dissolution rate of Ibuprofen by formulation into SLN using hot homogenization method. Further, this study also investigates the effect of various formulation parameters like stabilizer concentration, surfactant ratio, Lipid ratio and drug loading. SLNs were characterized for size distribution, entrapment efficiency, drug release and stability. SLN of Ibuprofen was prepared using stearic acid (lipid Phospholipon 80 H (surfactant and Tween-80 as stabilizer. The FTIR study shows no major interaction of Ibuprofen with other formulation ingredients, and the Differential Scanning Calorimetry (DSC study revealed that the drug is molecularly dispersed into the lipid. The particle size determinations confirm the particle size distribution in the nanoparticular range (27% Volume to 56% volume. In-vitro drug release through the dialysis membrane from the prepared SLNs is much higher than the pure drug. The stability study indicates the stability of the formulations without changing its performance on storage. Hence formulation of Ibuprofen in SLN enhances the dissolution rate as well as it will enhance the bioavailability of the drug which could be stabilized during storage.

  5. Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

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    Ahmed TA

    2016-02-01

    Full Text Available Tarek A Ahmed1,2 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt Abstract: In this study, optimized freeze-dried finasteride nanoparticles (NPs were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM. Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD. Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful

  6. Physical-Chemical Characterization and Formulation Considerations for Solid Lipid Nanoparticles.

    Science.gov (United States)

    Chauhan, Harsh; Mohapatra, Sarat; Munt, Daniel J; Chandratre, Shantanu; Dash, Alekha

    2016-06-01

    Pure glyceryl mono-oleate (GMO) (lipid) and different batches of GMO commonly used for the preparation of GMO-chitosan nanoparticles were characterized by modulated differential scanning calorimetry (MDSC), cryo-microscopy, and cryo-X-ray powder diffraction techniques. GMO-chitosan nanoparticles containing poloxamer 407 as a stabilizer in the absence and presence of polymers as crystallization inhibitors were prepared by ultrasonication. The effect of polymers (polyvinyl pyrrolidone (PVP), Eudragits, hydroxyl propyl methyl cellulose (HPMC), polyethylene glycol (PEG)), surfactants (poloxamer), and oils (mineral oil and olive oil) on the crystallization of GMO was investigated. GMO showed an exothermic peak at around -10°C while cooling and another exothermic peak at around -12°C while heating. It was followed by two endothermic peaks between 15 and 30 C, indicative of GMO melting. The results are corroborated by cryo-microscopy and cryo-X-ray. Significant differences in exothermic and endothermic transition were observed between different grades of GMO and pure GMO. GMO-chitosan nanoparticles resulted in a significant increase in particle size after lyophilization. MDSC confirmed that nanoparticles showed similar exothermic crystallization behavior of lipid GMO. MDSC experiments showed that PVP inhibits GMO crystallization and addition of PVP showed no significant increase in particle size of solid lipid nanoparticle (SLN) during lyophilization. The research highlights the importance of extensive physical-chemical characterization for successful formulation of SLN.

  7. Physical-Chemical Characterization and Formulation Considerations for Solid Lipid Nanoparticles.

    Science.gov (United States)

    Chauhan, Harsh; Mohapatra, Sarat; Munt, Daniel J; Chandratre, Shantanu; Dash, Alekha

    2016-06-01

    Pure glyceryl mono-oleate (GMO) (lipid) and different batches of GMO commonly used for the preparation of GMO-chitosan nanoparticles were characterized by modulated differential scanning calorimetry (MDSC), cryo-microscopy, and cryo-X-ray powder diffraction techniques. GMO-chitosan nanoparticles containing poloxamer 407 as a stabilizer in the absence and presence of polymers as crystallization inhibitors were prepared by ultrasonication. The effect of polymers (polyvinyl pyrrolidone (PVP), Eudragits, hydroxyl propyl methyl cellulose (HPMC), polyethylene glycol (PEG)), surfactants (poloxamer), and oils (mineral oil and olive oil) on the crystallization of GMO was investigated. GMO showed an exothermic peak at around -10°C while cooling and another exothermic peak at around -12°C while heating. It was followed by two endothermic peaks between 15 and 30 C, indicative of GMO melting. The results are corroborated by cryo-microscopy and cryo-X-ray. Significant differences in exothermic and endothermic transition were observed between different grades of GMO and pure GMO. GMO-chitosan nanoparticles resulted in a significant increase in particle size after lyophilization. MDSC confirmed that nanoparticles showed similar exothermic crystallization behavior of lipid GMO. MDSC experiments showed that PVP inhibits GMO crystallization and addition of PVP showed no significant increase in particle size of solid lipid nanoparticle (SLN) during lyophilization. The research highlights the importance of extensive physical-chemical characterization for successful formulation of SLN. PMID:26292931

  8. Formulation of novel lipid-coated magnetic nanoparticles as the probe for in vivo imaging

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    Mou Chung-Yuan

    2009-09-01

    Full Text Available Abstract Background Application of superparamagnetic iron oxide nanoparticles (SPIOs as the contrast agent has improved the quality of magnetic resonance (MR imaging. Low efficiency of loading the commercially available iron oxide nanoparticles into cells and the cytotoxicity of previously formulated complexes limit their usage as the image probe. Here, we formulated new cationic lipid nanoparticles containing SPIOs feasible for in vivo imaging. Methods Hydrophobic SPIOs were incorporated into cationic lipid 1,2-dioleoyl-3-(trimethylammonium propane (DOTAP and polyethylene-glycol-2000-1,2-distearyl-3-sn-phosphatidylethanolamine (PEG-DSPE based micelles by self-assembly procedure to form lipid-coated SPIOs (L-SPIOs. Trace amount of Rhodamine-dioleoyl-phosphatidylethanolamine (Rhodamine-DOPE was added as a fluorescent indicator. Particle size and zeta potential of L-SPIOs were determined by Dynamic Light Scattering (DLS and Laser Doppler Velocimetry (LDV, respectively. HeLa, PC-3 and Neuro-2a cells were tested for loading efficiency and cytotoxicity of L-SPIOs using fluorescent microscopy, Prussian blue staining and flow cytometry. L-SPIO-loaded CT-26 cells were tested for in vivo MR imaging. Results The novel formulation generates L-SPIOs particle with the average size of 46 nm. We showed efficient cellular uptake of these L-SPIOs with cationic surface charge into HeLa, PC-3 and Neuro-2a cells. The L-SPIO-loaded cells exhibited similar growth potential as compared to unloaded cells, and could be sorted by a magnet stand over ten-day duration. Furthermore, when SPIO-loaded CT-26 tumor cells were injected into Balb/c mice, the growth status of these tumor cells could be monitored using optical and MR images. Conclusion We have developed a novel cationic lipid-based nanoparticle of SPIOs with high loading efficiency, low cytotoxicity and long-term imaging signals. The results suggested these newly formulated non-toxic lipid-coated magnetic

  9. Statistical design for formulation optimization of hydrocortisone butyrate-loaded PLGA nanoparticles.

    Science.gov (United States)

    Yang, Xiaoyan; Patel, Sulabh; Sheng, Ye; Pal, Dhananjay; Mitra, Ashim K

    2014-06-01

    The aim of this investigation was to develop hydrocortisone butyrate (HB)-loaded poly(D,L-lactic-co-glycolic acid) (PLGA) nanoparticles (NP) with ideal encapsulation efficiency (EE), particle size, and drug loading (DL) under emulsion solvent evaporation technique utilizing various experimental statistical design modules. Experimental designs were used to investigate specific effects of independent variables during preparation of HB-loaded PLGA NP and corresponding responses in optimizing the formulation. Plackett-Burman design for independent variables was first conducted to prescreen various formulation and process variables during the development of NP. Selected primary variables were further optimized by central composite design. This process leads to an optimum formulation with desired EE, particle size, and DL. Contour plots and response surface curves display visual diagrammatic relationships between the experimental responses and input variables. The concentration of PLGA, drug, and polyvinyl alcohol and sonication time were the critical factors influencing the responses analyzed. Optimized formulation showed EE of 90.6%, particle size of 164.3 nm, and DL of 64.35%. This study demonstrates that statistical experimental design methodology can optimize the formulation and process variables to achieve favorable responses for HB-loaded NP.

  10. Formulation, Optimization and In vitro Characterization of Letrozole Loaded Solid Lipid Nanoparticles

    Directory of Open Access Journals (Sweden)

    Archana Nerella

    2014-07-01

    Full Text Available Letrozole (LTZ is an oral non-steroidal aromatase inhibitor for the treatment of hormonally responsive breast cancer after surgery. The objective of the current study is to prepare and evaluate Solid lipid nanoparticles (SLN of LTZ. SLNs were prepared by hot homogenization followed by ultrasonication. Trimyristin was used as solid lipid core, Soyphosphatidyl choline, Tween 80 as surfactant mixture. Process and formulation variables were studied and optimized. LTZ-SLN were characterized for mean particle size, polydispersity index (PDI and zeta potential for all the formulations. The mean particles size, PDI, zeta potential and entrapment efficiency of optimized LTZ-SLN optimized formulation was found to be 28.54 nm, 0.162, 11.80 mV, 85.64 %, respectively. In vitro release profiles are performed in 0.1N HCl using modified franz diffusion cell showed controlled drug release behavior over a period of 24h. LTZ-SLN formulations are subjected to stability study over a period of 1 month in terms of particle size, zeta potential, PDI, entrapment efficiency and are found to be stable. Differential scanning calorimetry (DSC and transmission electron microscopy (TEM analysis was performed to characterize the state of drug, lipid modification, shape and surface morphology of prepared LTZ-SLN formulations.

  11. An efficient and low immunostimulatory nanoparticle formulation for systemic siRNA delivery to the tumor.

    Science.gov (United States)

    Chono, Sumio; Li, Shyh-Dar; Conwell, Christine C; Huang, Leaf

    2008-10-01

    We have developed a nanoparticle formulation [liposomes-protamine-hyaluronic acid nanoparticle (LPH-NP)] for systemically delivering siRNA into the tumor. The LPH-NP was prepared in a self-assembling process. Briefly, protamine and a mixture of siRNA and hyaluronic acid were mixed to prepare a negatively charged complex. Then, cationic liposomes were added to coat the complex with lipids via charge-charge interaction to prepare the LPH-NP. The LPH-NP was further modified by DSPE-PEG or DSPE-PEG-anisamide by the post-insertion method. Anisamide is a targeting ligand for the sigma receptor over-expressed in the B16F10 melanoma cells. The particle size, zeta potential and siRNA encapsulation efficiency of the formulation were approximately 115 nm, +25 mV and 90%, respectively. Luciferase siRNA was used to evaluate the gene silencing activity in the B16F10 cells, which were stably transduced with a luciferase gene. The targeted LPH-NP (PEGylated with ligand) silenced 80% of luciferase activity in the metastatic B16F10 tumor in the lung after a single i.v. injection (0.15 mg siRNA/kg). The targeted LPH-NP also showed very little immunotoxicity in a wide dose range (0.15-1.2 mg siRNA/kg), while the previously published formulation, LPD-NP (liposome-protamine-DNA nanoparticle), had a much narrow therapeutic window (0.15-0.45 mg/kg).

  12. Effect of different lipids and surfactants on formulation of solid lipid nanoparticles incorporating tamoxifen citrate.

    Science.gov (United States)

    Upadhyay, S U; Patel, J K; Patel, V A; Saluja, A K

    2012-03-01

    Tamoxifen Citrate (TC) is an estrogen receptor antagonist and drug of choice for hormone sensitive breast cancer. Solid Lipid Nanoparticles loaded with TC were prepared by High Shear Homogenization followed by Ultrasonication. The aim of the present work is to study the effect of four different Solid Lipids and three Surfactants on Formulation and Stability of SLN. They were characterized for Particle size, Polydispersity Index and Zeta Potential by Zetasizer Nano. SLN prepared by Solid Lipid Compritol 888 (Glyceryldibehenate) and Tween 80 (1%) showed desired Particle Size of 206.9 nm, PDI of 0.046 and Zeta Potential of 9.32 mV. PMID:23066183

  13. Effect of different lipids and surfactants on formulation of solid lipid nanoparticles incorporating tamoxifen citrate

    Directory of Open Access Journals (Sweden)

    S U Upadhyay

    2012-01-01

    Full Text Available Tamoxifen Citrate (TC is an estrogen receptor antagonist and drug of choice for hormone sensitive breast cancer. Solid Lipid Nanoparticles loaded with TC were prepared by High Shear Homogenization followed by Ultrasonication. The aim of the present work is to study the effect of four different Solid Lipids and three Surfactants on Formulation and Stability of SLN. They were characterized for Particle size, Polydispersity Index and Zeta Potential by Zetasizer Nano. SLN prepared by Solid Lipid Compritol 888 (Glyceryldibehenate and Tween 80 (1% showed desired Particle Size of 206.9 nm, PDI of 0.046 and Zeta Potential of 9.32 mV.

  14. Drug/polymer nanoparticles prepared using unique spray nozzles and recent progress of inhaled formulation

    Directory of Open Access Journals (Sweden)

    Tetsuya Ozeki

    2014-10-01

    Full Text Available Inhaled formulations are promising for pulmonary and systemic non-pulmonary diseases. Functional engineered particles including drugs and drug-loaded nanocarriers have been anticipated because they can improve drug delivery efficacy against target sites in the lungs or blood. In this review, unique spray nozzles (e.g., four-fluid spray nozzle and two-solution mixing type nozzle for the preparation of nanocomposite particles which mean microparticles containing drug nanoparticles are described. These nozzles can produce nanocomposite particles in one-step and their spray drying system is suitable for scaling-up. Nanocomposite particles are useful in improving drug absorption and delivery efficacy against alveolar macrophages. In addition, recent studies on several pulmonary diseases (tuberculosis, lung cancer, cystic fibrosis, pneumonia, vaccine and others and related inhaled formulations were also reviewed.

  15. Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation.

    Science.gov (United States)

    Ahmed, Tarek A

    2016-01-01

    In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom-up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability. PMID:26893559

  16. CHEMICAL MODIFICATION OF CHITOSAN AND FORMULATION OF ITS NANOPARTICLES FOR PROTEIN DRUG DELIVERY SYSTEM

    Directory of Open Access Journals (Sweden)

    Swastika Karwani

    2013-06-01

    Full Text Available The most common route of administration of proteins has been parenterals using invasive ways of administration but this route has many side effects like lack of patient compliance, cost, high drug levels etc. The development of an oral dosage form that improves the absorption of protein drugs is the most desirable formulation but one of the greatest challenges in the pharmaceutical field. The major barriers in developing oral formulations for peptides and proteins include poor intrinsic permeability, luminal and cellular enzymatic degradation and chemical and conformational stability. A number of innovative oral drug delivery approaches have been recently developed, including the drug entrapment within polymer nanoparticles. The various advantages of oral delivery of proteins are like ease of administration, can be used as cure in primary stages of disease eg. Thrombosis, no internal bleeding, patient compliance and economical Our formulation development approach is to develop the formulations targeted to bypass the stomach with an aim to release the drug in the intestine; with extended residence time in the GIT and for this polymer like Chitosan is used. To improve the lipophillic property of chitosan, to modify biodegradation pattern of polymer and for oral delivery of proteins (Insulin and serratiopeptidase, modification is done using lactic-acid and polyethyleneglycol by copolymerization.

  17. Efficient gene silencing in metastatic tumor by siRNA formulated in surface-modified nanoparticles.

    Science.gov (United States)

    Li, Shyh-Dar; Chono, Sumio; Huang, Leaf

    2008-02-18

    We have developed a nanoparticle (NP) formulation for systemically delivering siRNA into metastatic tumors. The NP, composed of nucleic acids, a polycationic peptide and cationic liposome, was prepared in a self-assembling process. The NP was then modified by PEG-lipid containing a targeting ligand, anisamide, and thus was decorated for targeting sigma receptor expressing B16F10 tumor. The activity of the targeted NP was compared with the naked NP (no PEGylation) and non-targeted NP (no ligand). The delivery efficiency of the targeted NP was 4-fold higher than the non-targeted NP and could be competed by excess free ligand. Luciferase siRNA was used to evaluate the gene silencing activity in the B16F10 cells, which were stably transduced with a luciferase gene. The gene silencing activity of the targeted NP was significantly higher than the other formulations and lasted for 4 days. While confocal microscopy showed that the naked NP provided no tissue selectivity and non-targeted NP was ineffective for tumor uptake, the targeted NP effectively penetrated the lung metastasis, but not the liver. It resulted in 70-80% gene silencing in the metastasis model after a single i.v. injection (150 microg siRNA/kg). This effective formulation also showed very little immunotoxicity.

  18. Sucrose ester stabilized solid lipid nanoparticles and nanostructured lipid carriers: II. Evaluation of the imidazole antifungal drug-loaded nanoparticle dispersions and their gel formulations

    Science.gov (United States)

    Das, Surajit; Kiong Ng, Wai; Tan, Reginald B. H.

    2014-03-01

    This study focused on: (i) feasibility of the previously developed sucrose ester stabilized SLNs and NLCs to encapsulate different imidazole antifungal drugs and (ii) preparation and evaluation of topical gel formulations of those SLNs and NLCs. Three imidazole antifungal drugs; clotrimazole, ketoconazole and climbazole were selected for this study. The results suggested that size, size distribution and drug encapsulation efficiency depend on the drug molecule and type of nanoparticles (SLN/NLC). The drug release experiment always showed faster drug release from NLCs than SLNs when the same drug molecule was loaded in both nanoparticles. However, drug release rate from both SLNs and NLCs followed the order of climbazole > ketoconazole > clotrimazole. NLCs demonstrated better physicochemical stability than SLNs in the case of all drugs. The drug release rate from ketoconazole- and clotrimazole-loaded SLNs became faster after three months than a fresh formulation. There was no significant change in drug release rate from climbazole-loaded SLNs and all drug-loaded NLCs. Gel formulations of SLNs and NLCs were prepared using polycarbophil polymer. Continuous flow measurements demonstrated non-Newtonian flow with shear-thinning behavior and thixotropy. Oscillation measurements depicted viscoelasticity of the gel formulations. Similar to nanoparticle dispersion, drug release rate from SLN- and NLC-gel was in the order of climbazole > ketoconazole > clotrimazole. However, significantly slower drug release was noticed from all gel formulations than their nanoparticle counterparts. Unlike nanoparticle dispersions, no significant difference in drug release from gel formulations containing SLNs and NLCs was observed for each drug. This study concludes that gel formulation of imidazole drug-loaded SLNs and NLCs can be used for sustained/prolonged topical delivery of the drugs.

  19. Sucrose ester stabilized solid lipid nanoparticles and nanostructured lipid carriers: II. Evaluation of the imidazole antifungal drug-loaded nanoparticle dispersions and their gel formulations

    International Nuclear Information System (INIS)

    This study focused on: (i) feasibility of the previously developed sucrose ester stabilized SLNs and NLCs to encapsulate different imidazole antifungal drugs and (ii) preparation and evaluation of topical gel formulations of those SLNs and NLCs. Three imidazole antifungal drugs; clotrimazole, ketoconazole and climbazole were selected for this study. The results suggested that size, size distribution and drug encapsulation efficiency depend on the drug molecule and type of nanoparticles (SLN/NLC). The drug release experiment always showed faster drug release from NLCs than SLNs when the same drug molecule was loaded in both nanoparticles. However, drug release rate from both SLNs and NLCs followed the order of climbazole > ketoconazole > clotrimazole. NLCs demonstrated better physicochemical stability than SLNs in the case of all drugs. The drug release rate from ketoconazole- and clotrimazole-loaded SLNs became faster after three months than a fresh formulation. There was no significant change in drug release rate from climbazole-loaded SLNs and all drug-loaded NLCs. Gel formulations of SLNs and NLCs were prepared using polycarbophil polymer. Continuous flow measurements demonstrated non-Newtonian flow with shear-thinning behavior and thixotropy. Oscillation measurements depicted viscoelasticity of the gel formulations. Similar to nanoparticle dispersion, drug release rate from SLN- and NLC-gel was in the order of climbazole > ketoconazole > clotrimazole. However, significantly slower drug release was noticed from all gel formulations than their nanoparticle counterparts. Unlike nanoparticle dispersions, no significant difference in drug release from gel formulations containing SLNs and NLCs was observed for each drug. This study concludes that gel formulation of imidazole drug-loaded SLNs and NLCs can be used for sustained/prolonged topical delivery of the drugs. (paper)

  20. Formulation and in vitro characterization of domperidone loaded solid lipid nanoparticles and nanostructured lipid carriers

    Directory of Open Access Journals (Sweden)

    RP Thatipamula

    2011-03-01

    Full Text Available Background and the purpose of the study: Domperidone (DOM is a dopamine- receptor (D2 antagonist, widely used in the treatment of motion-sickness. The pharmacokinetic parameters of DOM make it a suitable candidate for development of Solid Lipid Nanoparticle (SLN and Nanostructured Lipide Carrier (NLC. The purpose of the present investigation was to prepare and evaluate DOM loaded solid lipid nanoparticles (DOM-SLN and DOM loaded nanostructured lipid carriers (DOM-NLC. Methods: DOM loaded SLN and NLC were prepared by hot homogenization followed by ultrasonication technique, using trimyristin as solid lipid, cetyl recinoleate as liquid lipid and a mixture of soy phosphatidylcholine (99% and tween 80 as surfactant. SLN and NLC were characterized for particle size, polydispersity index (PDI, zeta potential and entrapment efficiency. The effects of composition of lipid materials and surfactant mixture on the particle size, PDI, zeta potential, drug entrapment efficiency, and in vitro drug release behavior were investigated. DSC analysis was performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by transmission electron microscopy (TEM. SLN and NLC formulations were subjected to stability study over a period of 40 days. Results: The mean particle size, PDI, zeta potential and entrapment efficiency of optimized SLN (SLN1 and NLC were found to be 30.45 nm, 0.156, 12.40 mV, 87.84 % and 32.23 nm, 0.160, 10.47 mV, 90.49 % respectively. DSC studies revealed that DOM was in an amorphous state and triglycerides were in the β prime form in SLN and NLC. Shape and surface morphology was determined by TEM revealed fairly spherical shape of nanoparticles. In vitro release studies demonstrated that both the SLN and NLC formulations possessed a controlled release over a period of 24 hrs. SLN and NLC formulations were subjected to stability over a period of 40 days. There was no significant (P < 0.05 change

  1. Formulation, characterization, and in vivo evaluation of celecoxib-PVP solid dispersion nanoparticles using supercritical antisolvent process.

    Science.gov (United States)

    Ha, Eun-Sol; Choo, Gwang-Ho; Baek, In-Hwan; Kim, Min-Soo

    2014-12-04

    The aim of this study was to develop celecoxib-polyvinylpyrrolidone (PVP) solid dispersion nanoparticles with and without surfactant using the supercritical antisolvent (SAS) process. The effect of different surfactants such as gelucire 44/14, poloxamer 188, poloxamer 407, Ryoto sugar ester L1695, and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) on nanoparticle formation and dissolution as well as oral absorption of celecoxib-PVP K30 solid dispersion nanoparticles was investigated. Spherical celecoxib solid dispersion nanoparticles less than 300 nm in size were successfully developed using the SAS process. Analysis by differential scanning calorimetry and powder X-ray diffraction showed that celecoxib existed in the amorphous form within the solid dispersion nanoparticles fabricated using the SAS process. The celecoxib-PVP-TPGS solid dispersion nanoparticles significantly enhanced in vitro dissolution and oral absorption of celecoxib relative to that of the unprocessed form. The area under the concentration-time curve (AUC0→24 h) and peak plasma concentration (Cmax) increased 4.6 and 5.7 times, respectively, with the celecoxib-PVP-TPGS formulation. In addition, in vitro dissolution efficiency was well correlated with in vivo pharmacokinetic parameters. The present study demonstrated that formulation of celecoxib-PVP-TPGS solid dispersion nanoparticles using the SAS process is a highly effective strategy for enhancing the bioavailability of poorly water-soluble celecoxib.

  2. Formulation, Characterization, and in Vivo Evaluation of Celecoxib-PVP Solid Dispersion Nanoparticles Using Supercritical Antisolvent Process

    Directory of Open Access Journals (Sweden)

    Eun-Sol Ha

    2014-12-01

    Full Text Available The aim of this study was to develop celecoxib-polyvinylpyrrolidone (PVP solid dispersion nanoparticles with and without surfactant using the supercritical antisolvent (SAS process. The effect of different surfactants such as gelucire 44/14, poloxamer 188, poloxamer 407, Ryoto sugar ester L1695, and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS on nanoparticle formation and dissolution as well as oral absorption of celecoxib-PVP K30 solid dispersion nanoparticles was investigated. Spherical celecoxib solid dispersion nanoparticles less than 300 nm in size were successfully developed using the SAS process. Analysis by differential scanning calorimetry and powder X-ray diffraction showed that celecoxib existed in the amorphous form within the solid dispersion nanoparticles fabricated using the SAS process. The celecoxib-PVP-TPGS solid dispersion nanoparticles significantly enhanced in vitro dissolution and oral absorption of celecoxib relative to that of the unprocessed form. The area under the concentration-time curve (AUC0→24 h and peak plasma concentration (Cmax increased 4.6 and 5.7 times, respectively, with the celecoxib-PVP-TPGS formulation. In addition, in vitro dissolution efficiency was well correlated with in vivo pharmacokinetic parameters. The present study demonstrated that formulation of celecoxib-PVP-TPGS solid dispersion nanoparticles using the SAS process is a highly effective strategy for enhancing the bioavailability of poorly water-soluble celecoxib.

  3. Chitosan nanoparticles for siRNA delivery: optimization of processing/formulation parameters.

    Science.gov (United States)

    Esmaeilzadeh Gharehdaghi, Elina; Amani, Amir; Khoshayand, Mohammad Reza; Banan, Mehdi; Esmaeilzadeh Gharehdaghi, Elika; Amini, Mohammad Ali; Faramarzi, Mohammad Ali

    2014-12-01

    Chitosan nanoparticles were prepared using ultrasonication methodology at specific amplitudes and times of sonication. Subsequently, small interfering RNA (siRNA) was added to the solution at predetermined values of nitrogen to phosphorous ratio (N/P), and stirring time. Employing response surfaces generated from a statistical model, the effect of sonication time and amplitude, stirring time, and N/P ratio was studied on the particle size, polydispersity, and loading efficiency of prepared siRNA/chitosan nanoparticles. It was found that to obtain the smallest size, amplitude and time of sonication as well as stirring time should be kept at ∼45%, 165 seconds, and 50 minutes, respectively. Minimum polydispersity values were also obtained at similar values of sonication time/amplitude and stirring time in addition to N/P values of ∼28. Also, the maximum proportion of siRNA loading was observed at approximate values of 300 seconds, 80% and 280 for sonication time, amplitude, and N/P ratio, respectively. The optimum conditions (i.e., to prepare a sample with minimum values of particle size and polydispersity index and maximum values of loading efficiency) were determined as 60.6, 30.0 (seconds), 28.0, and 12.5 (minutes) for amplitude, time of sonication, N/P, and stirring time, respectively. In this scrutiny, the predicted values of optimum formulation were 456 nm size, 89.6% loading efficiency, and 0.4 polydispersity index. PMID:25272198

  4. Chitosan nanoparticles for siRNA delivery: optimization of processing/formulation parameters.

    Science.gov (United States)

    Esmaeilzadeh Gharehdaghi, Elina; Amani, Amir; Khoshayand, Mohammad Reza; Banan, Mehdi; Esmaeilzadeh Gharehdaghi, Elika; Amini, Mohammad Ali; Faramarzi, Mohammad Ali

    2014-12-01

    Chitosan nanoparticles were prepared using ultrasonication methodology at specific amplitudes and times of sonication. Subsequently, small interfering RNA (siRNA) was added to the solution at predetermined values of nitrogen to phosphorous ratio (N/P), and stirring time. Employing response surfaces generated from a statistical model, the effect of sonication time and amplitude, stirring time, and N/P ratio was studied on the particle size, polydispersity, and loading efficiency of prepared siRNA/chitosan nanoparticles. It was found that to obtain the smallest size, amplitude and time of sonication as well as stirring time should be kept at ∼45%, 165 seconds, and 50 minutes, respectively. Minimum polydispersity values were also obtained at similar values of sonication time/amplitude and stirring time in addition to N/P values of ∼28. Also, the maximum proportion of siRNA loading was observed at approximate values of 300 seconds, 80% and 280 for sonication time, amplitude, and N/P ratio, respectively. The optimum conditions (i.e., to prepare a sample with minimum values of particle size and polydispersity index and maximum values of loading efficiency) were determined as 60.6, 30.0 (seconds), 28.0, and 12.5 (minutes) for amplitude, time of sonication, N/P, and stirring time, respectively. In this scrutiny, the predicted values of optimum formulation were 456 nm size, 89.6% loading efficiency, and 0.4 polydispersity index.

  5. Formulation and Physicochemical Characterization of Lycopene-Loaded Solid Lipid Nanoparticles

    Science.gov (United States)

    Nazemiyeh, Elham; Eskandani, Morteza; Sheikhloie, Hossein; Nazemiyeh, Hossein

    2016-01-01

    Purpose: Lycopene belongs to the carotenoids that shows good pharmacological properties including antioxidant, anti-inflammatory and anticancer. However, as a result of very low aqueous solubility, it has a limited systemic absorption, following oral administration. Methods: Here, we prepared a stable lycopene-loaded solid lipid nanoparticles using Precirol® ATO5, Compritol 888 ATO and myristic acid by hot homogenization method with some modification. The size and morphological characteristics of nanoparticles were evaluated using Scanning Electron Microscopy (SEM). Moreover, zeta potential and dispersity index (DI) were measured using zeta sizer. In addition, encapsulation efficiency (EE%), drug loading (DL) and cumulative drug release were quantified. Results: The results showed that the size and DI of particles was generally smaller in the case of SLNs prepared with precirol when compared to SLNs prepared with compritol. Scanning electron microscopy (SEM) and particle size analyses showed spherical SLNs (125 ± 3.89 nm), monodispersed distribution, and zeta potential of −10.06 ± 0.08 mV. High EE (98.4 ± 0.5 %) and DL (44.8 ± 0.46 mg/g) were achieved in the case of nanoparticles prepared by precirol. The stability study of the lycopene-SLNs in aqueous medium (4 °C) was showed that after 2 months there is no significant differences seen in size and DI compared with the fresh formulation. Conclusion: Conclusively, in this investigation we prepared a stable lycopene-SLNs with good physicochemical characteristic which candidate it for the future in vivo trials in nutraceutical industries. PMID:27478786

  6. Preclinical evaluation of injectable sirolimus formulated with polymeric nanoparticle for cancer therapy

    Directory of Open Access Journals (Sweden)

    Woo HN

    2012-04-01

    Full Text Available Ha Na Woo1*, Hye Kyung Chung2*, Eun Jin Ju1, Joohee Jung1,3, Hye-Won Kang4, Sa-Won Lee4, Min-Hyo Seo4, Jin Seong Lee5, Jung Shin Lee1,6, Heon Joo Park7, Si Yeol Song1,8, Seong-Yun Jeong1, Eun Kyung Choi1,2,81Institute for Innovative Cancer Research, 2Center for Development and Commercialization of Anti-cancer Therapeutics, Asan Medical Center, Seoul, 3College of Pharmacy, Duksung Women's University, Seoul, 4Department of Parenteral Delivery Program, Samyang Pharmaceuticals R&D, Daejeon, 5Department of Radiology and Research Institute of Radiology, 6Department of Internal Medicine, Asan Medical Center, Seoul, 7Department of Microbiology, College of Medicine, Inha University, Inchon, 8Department of Radiation Oncology, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea*These authors contributed equally to this studyAbstract: Nanoparticles are useful delivery vehicles for promising drug candidates that face obstacles for clinical applicability. Sirolimus, an inhibitor of mammalian target of rapamycin has gained attention for targeted anticancer therapy, but its clinical application has been limited by its poor solubility. This study was designed to enhance the feasibility of sirolimus for human cancer treatment. Polymeric nanoparticle (PNP–sirolimus was developed as an injectable formulation and has been characterized by transmission electron microscopy and dynamic light scattering. Pharmacokinetic analysis revealed that PNP–sirolimus has prolonged circulation in the blood. In addition, PNP–sirolimus preserved the in vitro killing effect of free sirolimus against cancer cells, and intravenous administration displayed its potent in vivo anticancer efficacy in xenograft tumor mice. In addition, PNP–sirolimus enhanced the radiotherapeutic efficacy of sirolimus both in vitro and in vivo. Clinical application of PNP–sirolimus is a promising strategy for human cancer treatment.Keywords: sirolimus, polymeric nanoparticle

  7. Determination of Biotin in Pharmaceutical Formulations by Potassium Permanganate-luminol-CdTe Nanoparticles Chemiluminescence System

    Institute of Scientific and Technical Information of China (English)

    TRAORE Zoumana Sékou; SU Xing-guang

    2012-01-01

    A sensitive flow-injection chemiluminescence method was developed for the determination of biotin in the pharmaceutical formulations.The affinity between avidin and biotin was used to adsorb biotin on the polystyrene,with subsequent quantification of biotin based on its ability to enhance the chemiluminescence(CL) signal generated by the redox reaction of potassium permanganate-luminol-CdTe nanoparticles CL system.The investigations prove that apart from 3-aminophthalate,the CdTe quantum dots(QDs) play both catalytic and emitter roles.Under optimum conditions,the linear range for the determination of biotin was 0.01-25 ng/mL with a detection limit of 7.3×10-3ng/mL(S/N=3).The relative standard deviation of 5 ng/L biotin was 2.06%(n=7).The proposed method was used to determine the biotin concentration in the pharmaceutical formulations and the recovery was between 96.4% and 104%.The proposed method is simple,convenient,rapid and sensitive.

  8. New Perspective in the Formulation and Characterization of Didodecyldimethylammonium Bromide (DMAB Stabilized Poly(Lactic-co-Glycolic Acid (PLGA Nanoparticles.

    Directory of Open Access Journals (Sweden)

    Rebecca Gossmann

    Full Text Available Over the last few decades the establishment of nanoparticles as suitable drug carriers with the transport of drugs across biological barriers such as the gastrointestinal barrier moved into the focus of many research groups. Besides drug transport such carrier systems are well suited for the protection of drugs against enzymatic and chemical degradation. The preparation of biocompatible and biodegradable nanoparticles based on poly(lactic-co-glycolic acid (PLGA is intensively described in literature, while especially nanoparticles with cationic properties show a promising increased cellular uptake. This is due to the electrostatic interaction between the cationic surface and the negatively charged lipid membrane of the cells. Even though several studies achieved the successful preparation of nanoparticles stabilized with the cationic surfactants such as didodecyldimethylammonium bromide (DMAB, in most cases insufficient attention was paid to a precise analytical characterization of the nanoparticle system. The aim of the present work was to overcome this deficit by presenting a new perspective in the formulation and characterization of DMAB-stabilized PLGA nanoparticles. Therefore these nanoparticles were carefully examined with regard to particle diameter, zeta potential, the effect of variation in stabilizer concentration, residual DMAB content, and electrolyte stability. Without any steric stabilization, the DMAB-modified nanoparticles were sensitive to typical electrolyte concentrations of biological environments due to compression of the electrical double layer in conjunction with a decrease in zeta potential. To handle this problem, the present study proposed two modifications to enable electrolyte stability. Both polyvinyl alcohol (PVA and polyethylene glycol (PEG modified DMAB-PLGA-nanoparticles were stable during electrolyte addition. Furthermore, in contrast to unmodified DMAB-PLGA-nanoparticles and free DMAB, such modifications led to

  9. A novel in situ hydrophobic ion paring (HIP) formulation strategy for clinical product selection of a nanoparticle drug delivery system.

    Science.gov (United States)

    Song, Young Ho; Shin, Eyoung; Wang, Hong; Nolan, Jim; Low, Susan; Parsons, Donald; Zale, Stephen; Ashton, Susan; Ashford, Marianne; Ali, Mir; Thrasher, Daniel; Boylan, Nicholas; Troiano, Greg

    2016-05-10

    The present studies were aimed at formulating AZD2811-loaded polylactic acid-polyethylene glycol (PLA-PEG) nanoparticles with adjustable release rates without altering the chemical structures of the polymer or active pharmaceutical ingredient (API). This was accomplished through the use of a hydrophobic ion pairing approach. A series of AZD2811-containing nanoparticles with a variety of hydrophobic counterions including oleic acid, 1-hydroxy-2-naphthoic acid, cholic acid, deoxycholic acid, dioctylsulfosuccinic acid, and pamoic acid is described. The hydrophobicity of AZD2811 was increased through formation of ion pairs with these hydrophobic counterions, producing nanoparticles with exceptionally high drug loading-up to five fold higher encapsulation efficiency and drug loading compared to nanoparticles made without hydrophobic ion pairs. Furthermore, the rate at which the drug was released from the nanoparticles could be controlled by employing counterions with various hydrophobicities and structures, resulting in release half-lives ranging from about 2 to 120h using the same polymer, nanoparticle size, and nanoemulsion process. Process recipe variables affecting drug load and release rate were identified, including pH and molarity of quench buffer. Ion pair formation between AZD2811 and pamoic acid as a model counterion was investigated using solubility enhancement as well as nuclear magnetic resonance spectroscopy to demonstrate solution-state interactions. Further evidence for an ion pairing mechanism of controlled release was provided through the measurement of API and counterion release profiles using high-performance liquid chromatography, which had stoichiometric relationships. Finally, Raman spectra of an AZD2811-pamoate salt compared well with those of the formulated nanoparticles, while single components (AZD2811, pamoic acid) alone did not. A library of AZD2811 batches was created for analytical and preclinical characterization. Dramatically improved

  10. Formulation, characterization, and expression of a recombinant MOMP Chlamydia trachomatis DNA vaccine encapsulated in chitosan nanoparticles

    Directory of Open Access Journals (Sweden)

    Cambridge CD

    2013-05-01

    Full Text Available Chino D Cambridge, Shree R Singh, Alain B Waffo, Stacie J Fairley, Vida A DennisCenter for NanoBiotechnology Research (CNBR, Alabama State University, Montgomery, AL, USAAbstract: Chlamydia trachomatis is a bacterial sexually transmitted infection affecting millions of people worldwide. Previous vaccination attempts have employed the recombinant major outer membrane protein (MOMP of C. trachomatis nonetheless, with limited success, perhaps, due to stability, degradation, and delivery issues. In this study we cloned C. trachomatis recombinant MOMP DNA (DMOMP and encapsulated it in chitosan nanoparticles (DMCNP using the complex coacervation technique. Physiochemical characterizations of DMCNP included transmission and scanning electron microcopy, Fourier transform infrared and ultraviolet-visible spectroscopy, and zeta potential. Encapsulated DMOMP was 167–250 nm, with a uniform spherical shape and homogenous morphology, and an encapsulation efficiency > 90%. A slow release pattern of encapsulated DMOMP, especially in acidic solution, was observed over 7 days. The zeta potential of DMCNP was ~8.80 mV, which indicated that it was highly stable. Toxicity studies of DMCNP (25–400 µg/mL to Cos-7 cells using the MTT assay revealed minimal toxicity over 24–72 hours with >90% viable cells. Ultra-violet visible (UV-vis spectra indicated encapsulated DMOMP protection by chitosan, whereas agarose gel electrophoresis verified its protection from enzymatic degradation. Expression of MOMP protein in DMCNP-transfected Cos-7 cells was demonstrated via Western blotting and immunofluorescence microscopy. Significantly, intramuscular injection of BALB/c mice with DMCNP confirmed the delivery of encapsulated DMOMP, and expression of the MOMP gene transcript in thigh muscles and spleens. Our data show that encapsulation of DMOMP in biodegradable chitosan nanoparticles imparts stability and protection from enzymatic digestion, and enhances delivery and

  11. Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion

    Science.gov (United States)

    Harsha, Sree N; Aldhubiab, Bander E; Nair, Anroop B; Alhaider, Ibrahim Abdulrahman; Attimarad, Mahesh; Venugopala, Katharigatta N; Srinivasan, Saminathan; Gangadhar, Nagesh; Asif, Afzal Haq

    2015-01-01

    Diabetes is considered one of the main threats to global public health in this era. It is increasing rapidly in every part of the world; the prevalence of the disease will grow to the point where 366 million people will be affected by 2030. The prevalence of diabetes mellitus (DM) in the Saudi population is high, and the majority of patients suffer from type 2 DM. Marketed oral antidiabetic drugs have indicated poor tolerability during chronic treatments, and this contributes to the moderately large proportion of type 2 DM patients that remain inadequately managed. Vildagliptin nanospheres were prepared with aminated gelatin using a spray-drying method; narrow particle-size distribution was seen at 445 nm. The angle of repose was found to be θ <33.5°. The nanospheres appeared to be spherical with a smooth surface. The drug content and percentage yield of the nanospheres were found to be 76.2%±4.6% and 83%±2%, respectively. The nanosphere-swell profile was found to be 165%±7%. The pure drug was 100% dissolved in 30 minutes, and the nanosphere formulation took 12 hours to dissolve (97.5%±2%), and followed a Korsmeyer–Peppas kinetic model with an R2 of 0.9838. The wash-off test of nanospheres found that they exhibited an excellent mucoadhesive property at 86.7% for 8 hours. The stability-study data showed no changes in the physicochemical properties of the nanospheres, and suggested that the nanospheres be stored below room temperature. The amount of vildagliptin retained was 1.6% within 3 hours, and in comparison with the gelatin vildagliptin nanoparticles formulation, the percentage that was retained was much higher (98.2% in 12 hours). PMID:25670882

  12. Formulation of Functionalized PLGA-PEG Nanoparticles for In Vivo Targeted Drug Delivery

    Science.gov (United States)

    Cheng, Jianjun; Teply, Benjamin A.; Sherifi, Ines; Sung, Josephine; Luther, Gaurav; Gu, Frank X.; Levy-Nissenbaum, Etgar; Radovic-Moreno, Aleksandar F.; Langer, Robert; Farokhzad, Omid C.

    2009-01-01

    Nanoparticle (NP) size has been shown to significantly effect the biodistribution of targeted and non-targeted NPs in an organ specific manner. Herein we have developed NPs from carboxy-terminated poly (d,l-lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-b-PEG-COOH) polymer and studied the effects of altering the following formulation parameters on the size of NPs, including: 1) polymer concentration, 2) drug loading, 3) water miscibility of solvent, and 4) the ratio of water to solvent. We found that NP mean volumetric size correlates linearly with polymer concentration for NPs between 70 and 250 nm in diameter (linear coefficient = 0.99 for NPs formulated with solvents studied). NPs with desirable size, drug loading, and polydispersity were conjugated to the A10 RNA aptamer (Apt) that binds to the Prostate Specific Membrane Antigen (PSMA), and NP and NP-Apt biodistribution was evaluated in a LNCaP (PSMA+) xenograft mouse model of PCa. The surface functionalization of NPs with the A10 PSMA aptamer significantly enhanced delivery of NPs to tumors vs. equivalent NPs lacking the A10 PSMA aptamer (a 3.77-fold increase at 24 hrs; NP-Apt 0.83% ± 0.21% vs. NP 0.22% ± 0.07% of injected dose per gram of tissue; mean ± s.d., n = 4, p = 0.002). The ability to control NP size together with targeted delivery may result in favorable biodistribution and development of clinically relevant targeted therapies. PMID:17055572

  13. Influence of paints formulations on nanoparticles release during their life cycle

    International Nuclear Information System (INIS)

    Pristine nanoparticles (NPs) may present a hazard to humans and the environment, and hence it is important to know to what extent NPs can be freely released from commercialized products in which they are added. The purpose of this study was to identify the parameters of the paint formulation containing SiO2 NPs of 19-nm diameter that could have an impact on the release induced by aging and abrasion. In order to simulate outdoor aging during the life cycle of the product, painted panels were exposed to accelerated weathering experiments in accordance with the norm EN ISO 16474-3:2013. The surface modification of these paints was characterized by scanning electron microscope coupled with energy dispersive spectrometry (SEM–EDS). These analyses showed that the acrylic copolymer binder has undergone a more significant chemical degradation compared with the styrene-acrylic copolymer. To simulate a mechanical aging, abrasion tests were conducted using a Taber Abraser, simulating critical scenarios of the abrasion standard. The particle size distributions and particle concentrations of the abraded particles were measured using an electric low-pressure impactor. After accelerated aging and abrasion tests, we observed a link between the paint degradations occurring with the release of pristine NPs and the embedded pristine NPs. Surface degradation of acrylic copolymer paints was more significant than that of the styrene-acrylic copolymer paints, and this induced a release of NPs 2.7 times higher. Other parameters like TiO2 addition as pigments induced a strong stability of paint against light and water, decreasing the total number of NPs released from paints from 30,000 to 1200 particles/cm3. These results revealed that formulations can be tuned to decrease the number of free NPs released and get a “safe-by-design” product

  14. Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion.

    Science.gov (United States)

    Harsha, Sree N; Aldhubiab, Bander E; Nair, Anroop B; Alhaider, Ibrahim Abdulrahman; Attimarad, Mahesh; Venugopala, Katharigatta N; Srinivasan, Saminathan; Gangadhar, Nagesh; Asif, Afzal Haq

    2015-01-01

    Diabetes is considered one of the main threats to global public health in this era. It is increasing rapidly in every part of the world; the prevalence of the disease will grow to the point where 366 million people will be affected by 2030. The prevalence of diabetes mellitus (DM) in the Saudi population is high, and the majority of patients suffer from type 2 DM. Marketed oral antidiabetic drugs have indicated poor tolerability during chronic treatments, and this contributes to the moderately large proportion of type 2 DM patients that remain inadequately managed. Vildagliptin nanospheres were prepared with aminated gelatin using a spray-drying method; narrow particle-size distribution was seen at 445 nm. The angle of repose was found to be θ <33.5°. The nanospheres appeared to be spherical with a smooth surface. The drug content and percentage yield of the nanospheres were found to be 76.2%±4.6% and 83%±2%, respectively. The nanosphere-swell profile was found to be 165%±7%. The pure drug was 100% dissolved in 30 minutes, and the nanosphere formulation took 12 hours to dissolve (97.5%±2%), and followed a Korsmeyer-Peppas kinetic model with an R (2) of 0.9838. The wash-off test of nanospheres found that they exhibited an excellent mucoadhesive property at 86.7% for 8 hours. The stability-study data showed no changes in the physicochemical properties of the nanospheres, and suggested that the nanospheres be stored below room temperature. The amount of vildagliptin retained was 1.6% within 3 hours, and in comparison with the gelatin vildagliptin nanoparticles formulation, the percentage that was retained was much higher (98.2% in 12 hours). PMID:25670882

  15. Influence of paints formulations on nanoparticles release during their life cycle

    Energy Technology Data Exchange (ETDEWEB)

    Fiorentino, Brice, E-mail: brice.fiorentino@cea.fr; Golanski, Luana; Guiot, Arnaud; Damlencourt, Jean-François; Boutry, Delphine [Commissariat à l’énergie atomique et aux énergies alternatives (France)

    2015-03-15

    Pristine nanoparticles (NPs) may present a hazard to humans and the environment, and hence it is important to know to what extent NPs can be freely released from commercialized products in which they are added. The purpose of this study was to identify the parameters of the paint formulation containing SiO{sub 2} NPs of 19-nm diameter that could have an impact on the release induced by aging and abrasion. In order to simulate outdoor aging during the life cycle of the product, painted panels were exposed to accelerated weathering experiments in accordance with the norm EN ISO 16474-3:2013. The surface modification of these paints was characterized by scanning electron microscope coupled with energy dispersive spectrometry (SEM–EDS). These analyses showed that the acrylic copolymer binder has undergone a more significant chemical degradation compared with the styrene-acrylic copolymer. To simulate a mechanical aging, abrasion tests were conducted using a Taber Abraser, simulating critical scenarios of the abrasion standard. The particle size distributions and particle concentrations of the abraded particles were measured using an electric low-pressure impactor. After accelerated aging and abrasion tests, we observed a link between the paint degradations occurring with the release of pristine NPs and the embedded pristine NPs. Surface degradation of acrylic copolymer paints was more significant than that of the styrene-acrylic copolymer paints, and this induced a release of NPs 2.7 times higher. Other parameters like TiO{sub 2} addition as pigments induced a strong stability of paint against light and water, decreasing the total number of NPs released from paints from 30,000 to 1200 particles/cm{sup 3}. These results revealed that formulations can be tuned to decrease the number of free NPs released and get a “safe-by-design” product.

  16. Application of Solid-State NMR Relaxometry for Characterization and Formulation Optimization of Grinding-Induced Drug Nanoparticle.

    Science.gov (United States)

    Ueda, Keisuke; Higashi, Kenjirou; Moribe, Kunikazu

    2016-03-01

    The formation mechanism of drug nanoparticles was investigated using solid-state nuclear magnetic resonance (NMR) techniques for the efficient discovery of an optimized nanoparticle formulation. The cogrinding of nifedipine (NIF) with polymers, including hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP), and sodium dodecyl sulfate (SDS) was performed to prepare the NIF nanoparticle formulations. Then, solid-state NMR relaxometry was used for the nanometer-order characterization of NIF in the polymer matrix. Solid-state NMR measurements revealed that the crystal size of NIF was reduced to several tens of nanometers with amorphization of NIF by cogrinding with HPMC and SDS for 100 min. Similarly, the size of the NIF crystal was reduced to less than 90 nm in the 40 min ground mixture of NIF/PVP/SDS. Furthermore, 100 min grinding of NIF/PVP/SDS induced amorphization of almost all the NIF crystals followed by nanosizing. The hydrogen bond between NIF and PVP led to the efficient amorphization of NIF in the NIF/PVP/SDS system compared with NIF/HPMC/SDS system. The efficient nanosizing of the NIF crystal in the solid state, revealed by the solid-state NMR relaxation time measurements, enabled the formation of large amounts of NIF nanoparticles in water followed by the polymer dissolution. In contrast, excess amorphization of the NIF crystals failed to efficiently prepare the NIF nanoparticles. The solid-state characterization of the crystalline NIF revealed good correlation with the NIF nanoparticles formation during aqueous dispersion. Furthermore, the solid-state NMR measurements including relaxometry successfully elucidated the nanometer-order dispersion state of NIF in polymer matrix, leading to the discovery of optimized conditions for the preparation of suitable drug nanoparticles.

  17. Docetaxel-loaded polylactic acid-co-glycolic acid nanoparticles: formulation, physicochemical characterization and cytotoxicity studies.

    Science.gov (United States)

    Pradhan, Roshan; Poudel, Bijay Kumar; Ramasamy, Thiruganesh; Choi, Han-Gon; Yong, Chul Soon; Kim, Jong Oh

    2013-08-01

    In the present study, we developed novel docetaxel (DTX)-loaded polylactic acid-co-glycolic acid (PLGA) nanoparticles (NPs) using the combination of sodium lauryl sulfate (SLS) and poloxamer 407, the anionic and non-ionic surfactants respectively for stabilization. The NPs were prepared by emulsification/solvent evaporation method. The combination of these surfactants at weight ratio of 1:0.5 was able to produce uniformly distributed small sized NPs and demonstrated the better stability of NP dispersion with high encapsulation efficiency (85.9 +/- 0.6%). The drug/polymer ratio and phase ratio were 2:10 and 1:10, respectively. The optimized formulation of DTX-loaded PLGA NPs had a particle size and polydispersity index of 104.2 +/- 1.5 nm and 0.152 +/- 0.006, respectively, which was further supported by TEM image. In vitro release study was carried out with dialysis membrane and showed 32% drug release in 192 h. When in vitro release data were fitted to Korsmeyer-Peppas model, the n value was 0.481, which suggested the drug was released by anomalous or non-Fickian diffusion. In addition, DTX-loaded PLGA NPs in 72 h, displayed approximately 75% cell viability reduction at 10 microg/ml DTX concentration, in MCF-7 cell lines, indicating sustained release from NPs. Therefore, our results demonstrated that incorporation of DTX into PLGA NPs could provide a novel effective nanocarrier for the treatment of cancer.

  18. Brain delivery of camptothecin by means of solid lipid nanoparticles: Formulation design, in vitro and in vivo studies

    DEFF Research Database (Denmark)

    Martins, S.; Tho, I.; Reimold, I.;

    2012-01-01

    For the purpose of brain delivery upon intravenous injection, formulations of camptothecin-loaded solid lipid nanoparticles (SLN), prepared by hot high pressure homogenisation, were designed. Incorporation of camptothecin in the hydrophobic and acidic environment of SLN matrix was chosen to stabi......For the purpose of brain delivery upon intravenous injection, formulations of camptothecin-loaded solid lipid nanoparticles (SLN), prepared by hot high pressure homogenisation, were designed. Incorporation of camptothecin in the hydrophobic and acidic environment of SLN matrix was chosen...... affinity of the SLN to the porcine brain capillary endothelial cells (BCEC) was shown in comparison to macrophages. MTT studies in BCEC revealed a moderate decrease in the cell viability of camptothecin, when incorporated in SLN compared to free camptothecin in solution. In vivo studies in rats showed...

  19. Solid Lipid Nanoparticle-Based Calix[n]arenes and Calix-Resorcinarenes as Building Blocks: Synthesis, Formulation and Characterization

    OpenAIRE

    Coleman, Anthony W.; Imed Montasser; Patrick Shahgaldian; Florent Perret

    2013-01-01

    Solid lipid nanoparticles (SLNs) have attracted increasing attention during recent years. This paper presents an overview about the use of calix[n]arenes and calix-resorcinarenes in the formulation of SLNs. Because of their specific inclusion capability both in the intraparticle spaces and in the host cavities as well as their capacity for functionalization, these colloidal nanostructures represent excellent tools for the encapsulation of different active pharmaceutical ingredients (APIs) in ...

  20. Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion

    Directory of Open Access Journals (Sweden)

    Harsha SN

    2015-01-01

    temperature. The amount of vildagliptin retained was 1.6% within 3 hours, and in comparison with the gelatin vildagliptin nanoparticles formulation, the percentage that was retained was much higher (98.2% in 12 hours. Keywords: nanospheres, vildagliptin, Büchi Nano Spray Dryer, diabetes

  1. Formulation optimization and in vitro skin penetration of spironolactone loaded solid lipid nanoparticles.

    Science.gov (United States)

    Kelidari, H R; Saeedi, M; Akbari, J; Morteza-Semnani, K; Gill, P; Valizadeh, H; Nokhodchi, A

    2015-04-01

    The aim of the current investigation was to prepare and evaluate the potential use of solid lipid nanoparticles for the dermal delivery of spironolactone (SP). The spironolactone loaded SLN (SP-SLN) was prepared by emulsion-solvent evaporation method followed by ultrasonication. The properties of obtained SLNs were characterized by photon correlation spectroscopy (PCS), scanning tunneling microscopy (STM) and differential scanning calorimetry. FT-IR was also used to investigate any interaction between SP and excipients in the molecular level during the preparation of SLNs. The performance of the formulations was investigated in terms of drug release, skin permeation and also the retention of drug by the skin. The SP-SLNs presented spherical shape with the mean diameter, zeta potential and entrapment efficiency of 88.9 nm, -23.9 mV and 59.86%, respectively. DSC study showed that SP alone encapsulated in SLNs was in the amorphous form. FT-IR analysis revealed that there were hydrogen bond interactions between the SP alone and SLN components. The dissolution results revealed that the drug release from SP-SLNs was at least 4.9 times faster than original SP within the first 30 min. The cumulative amount of SP penetrated through rat skin from SP-SLNs was almost twofold that of the SP alone in 24h after the administration. In vitro permeation studies indicated that SP-SLN may be a promising vector for use in the topical treatment. It can be concluded that SLNs provide good skin permeation for SP and may be a promising carrier for topical delivery of spironolactone offering the biphasic release pattern that might be interesting for topical application resulting in an effective treatment for skin disorders such as acne. PMID:25797482

  2. Synthesis, characterization, and in vivo efficacy of shell cross-linked nanoparticle formulations carrying silver antimicrobials as aerosolized therapeutics.

    Science.gov (United States)

    Shah, Parth N; Lin, Lily Yun; Smolen, Justin A; Tagaev, Jasur A; Gunsten, Sean P; Han, Daniel S; Heo, Gyu Seong; Li, Yali; Zhang, Fuwu; Zhang, Shiyi; Wright, Brian D; Panzner, Matthew J; Youngs, Wiley J; Brody, Steven L; Wooley, Karen L; Cannon, Carolyn L

    2013-06-25

    The use of nebulizable, nanoparticle-based antimicrobial delivery systems can improve efficacy and reduce toxicity for treatment of multi-drug-resistant bacteria in the chronically infected lungs of cystic fibrosis patients. Nanoparticle vehicles are particularly useful for applying broad-spectrum silver-based antimicrobials, for instance, to improve the residence time of small-molecule silver carbene complexes (SCCs) within the lung. Therefore, we have synthesized multifunctional, shell cross-linked knedel-like polymeric nanoparticles (SCK NPs) and capitalized on the ability to independently load the shell and core with silver-based antimicrobial agents. We formulated three silver-loaded variants of SCK NPs: shell-loaded with silver cations, core-loaded with SCC10, and combined loading of shell silver cations and core SCC10. All three formulations provided a sustained delivery of silver over the course of at least 2-4 days. The two SCK NP formulations with SCC10 loaded in the core each exhibited excellent antimicrobial activity and efficacy in vivo in a mouse model of Pseudomonas aeruginosa pneumonia. SCK NPs with shell silver cation-load only, while efficacious in vitro, failed to demonstrate efficacy in vivo. However, a single dose of core SCC10-loaded SCK NPs (0.74 ± 0.16 mg Ag) provided a 28% survival advantage over sham treatment, and administration of two doses (0.88 mg Ag) improved survival to 60%. In contrast, a total of 14.5 mg of Ag(+) delivered over 5 doses at 12 h intervals was necessary to achieve a 60% survival advantage with a free-drug (SCC1) formulation. Thus, SCK NPs show promise for clinical impact by greatly reducing antimicrobial dosage and dosing frequency, which could minimize toxicity and improve patient adherence. PMID:23718195

  3. Early development drug formulation on a chip: Fabrication of nanoparticles using a microfluidic spray dryer

    OpenAIRE

    Shum, HC; Thiele, J; Windbergs, M; Abate, AR; Trebbin, M.; Förster, S.; Weitz, DA

    2011-01-01

    Early development drug formulation is exacerbated by increasingly poor bioavailability of potential candidates. Prevention of attrition due to formulation problems necessitates physicochemical analysis and formulation studies at a very early stage during development, where the availability of a new substance is limited to small quantities, thus impeding extensive experiments. Miniaturization of common formulation processes is a strategy to overcome those limitations. We present a versatile te...

  4. Encapsulation of Alpha-1 antitrypsin in PLGA nanoparticles: In Vitro characterization as an effective aerosol formulation in pulmonary diseases

    Directory of Open Access Journals (Sweden)

    Pirooznia Nazanin

    2012-05-01

    Full Text Available Abstract Background Alpha 1- antitrypsin (α1AT belongs to the superfamily of serpins and inhibits different proteases. α1AT protects the lung from cellular inflammatory enzymes. In the absence of α1AT, the degradation of lung tissue results to pulmonary complications. The pulmonary route is a potent noninvasive route for systemic and local delivery. The aerosolized α1AT not only affects locally its main site of action but also avoids remaining in circulation for a long period of time in peripheral blood. Poly (D, L lactide-co glycolide (PLGA is a biodegradable and biocompatible polymer approved for sustained controlled release of peptides and proteins. The aim of this work was to prepare a wide range of particle size as a carrier of protein-loaded nanoparticles to deposit in different parts of the respiratory system especially in the deep lung. Various lactide to glycolide ratio of the copolymer was used to obtain different release profile of the drug which covers extended and rapid drug release in one formulation. Results Nonaqueous and double emulsion techniques were applied for the synthesis of nanoparticles. Nanoparticles were characterized in terms of surface morphology, size distribution, powder X-ray diffraction (XRD, encapsulation efficiency, in vitro drug release, FTIR spectroscopy and differential scanning calorimetry (DSC. To evaluate the nanoparticles cytotoxicity, cell cytotoxicity test was carried out on the Cor L105 human epithelial lung cancer cell line. Nanoparticles were spherical with an average size in the range of 100 nm to 1μ. The encapsulation efficiency was found to be higher when the double emulsion technique was applied. XRD and DSC results indicated that α1AT encapsulated in the nanoparticles existed in an amorphous or disordered-crystalline status in the polymer matrix. The lactic acid to glycolic acid ratio affects the release profile of α1AT. Hence, PLGA with a 50:50 ratios exhibited the ability to release

  5. Application of quality by design approach to optimize process and formulation parameters of rizatriptan loaded chitosan nanoparticles

    Directory of Open Access Journals (Sweden)

    Ajinath Eknath Shirsat

    2015-01-01

    Full Text Available The purpose of present study was to optimize rizatriptan (RZT chitosan (CS nanoparticles using ionic gelation method by application of quality by design (QbD approach. Based on risk assessment, effect of three variables, that is CS %, tripolyphosphate % and stirring speed were studied on critical quality attributes (CQAs; particle size and entrapment efficiency. Central composite design (CCD was implemented for design of experimentation with 20 runs. RZT CS nanoparticles were characterized for particle size, polydispersity index, entrapment efficiency, in-vitro release study, differential scanning calorimetric, X-ray diffraction, scanning electron microscopy (SEM. Based on QbD approach, design space (DS was optimized with a combination of selected variables with entrapment efficiency > 50% w/w and a particle size between 400 and 600 nm. Validation of model was performed with 3 representative formulations from DS for which standard error of − 0.70-3.29 was observed between experimental and predicted values. In-vitro drug release followed initial burst release 20.26 ± 2.34% in 3-4 h with sustained drug release of 98.43 ± 2.45% in 60 h. Lower magnitude of standard error for CQAs confirms the validation of selected CCD model for optimization of RZT CS nanoparticles. In-vitro drug release followed dual mechanism via, diffusion and polymer erosion. RZT CS nanoparticles were prepared successfully using QbD approach with the understanding of the high risk process and formulation parameters involved and optimized DS with a multifactorial combination of critical parameters to obtain predetermined RZT loaded CS nanoparticle specifications.

  6. Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics.

    Science.gov (United States)

    Elzoghby, Ahmed O; Helmy, Maged W; Samy, Wael M; Elgindy, Nazik A

    2013-01-01

    A novel particulate delivery matrix based on ionically crosslinked casein (CAS) nanoparticles was developed for controlled release of the poorly soluble anticancer drug flutamide (FLT). Nanoparticles were fabricated via oil-in-water emulsification then stabilized by ionic crosslinking of the positively charged CAS molecules below their isoelectric point, with the polyanionic crosslinker sodium tripolyphosphate. With the optimal preparation conditions, the drug loading and incorporation efficiency achieved were 8.73% and 64.55%, respectively. The nanoparticles exhibited a spherical shape with a size below 100 nm and a positive zeta potential (+7.54 to +17.3 mV). FLT was molecularly dispersed inside the nanoparticle protein matrix, as revealed by thermal analysis. The biodegradability of CAS nanoparticles in trypsin solution could be easily modulated by varying the sodium tripolyphosphate crosslinking density. A sustained release of FLT from CAS nanoparticles for up to 4 days was observed, depending on the crosslinking density. After intravenous administration of FLT-CAS nanoparticles into rats, CAS nanoparticles exhibited a longer circulation time and a markedly delayed blood clearance of FLT, with the half-life of FLT extended from 0.88 hours to 14.64 hours, compared with drug cosolvent. The results offer a promising method for tailoring biodegradable, drug-loaded CAS nanoparticles as controlled, long-circulating drug delivery systems of hydrophobic anticancer drugs in aqueous vehicles.

  7. Optimization of controlled release nanoparticle formulation of verapamil hydrochloride using artificial neural networks with genetic algorithm and response surface methodology.

    Science.gov (United States)

    Li, Yongqiang; Abbaspour, Mohammadreza R; Grootendorst, Paul V; Rauth, Andrew M; Wu, Xiao Yu

    2015-08-01

    This study was performed to optimize the formulation of polymer-lipid hybrid nanoparticles (PLN) for the delivery of an ionic water-soluble drug, verapamil hydrochloride (VRP) and to investigate the roles of formulation factors. Modeling and optimization were conducted based on a spherical central composite design. Three formulation factors, i.e., weight ratio of drug to lipid (X1), and concentrations of Tween 80 (X2) and Pluronic F68 (X3), were chosen as independent variables. Drug loading efficiency (Y1) and mean particle size (Y2) of PLN were selected as dependent variables. The predictive performance of artificial neural networks (ANN) and the response surface methodology (RSM) were compared. As ANN was found to exhibit better recognition and generalization capability over RSM, multi-objective optimization of PLN was then conducted based upon the validated ANN models and continuous genetic algorithms (GA). The optimal PLN possess a high drug loading efficiency (92.4%, w/w) and a small mean particle size (∼100nm). The predicted response variables matched well with the observed results. The three formulation factors exhibited different effects on the properties of PLN. ANN in coordination with continuous GA represent an effective and efficient approach to optimize the PLN formulation of VRP with desired properties. PMID:25986587

  8. Effect of isotonic solutions and peptide adsorption on zeta potential of porous silicon nanoparticle drug delivery formulations.

    Science.gov (United States)

    Kaasalainen, Martti; Mäkilä, Ermei; Riikonen, Joakim; Kovalainen, Miia; Järvinen, Kristiina; Herzig, Karl-Heinz; Lehto, Vesa-Pekka; Salonen, Jarno

    2012-07-15

    Recently, highly promising results considering the use of porous silicon (PSi) nanoparticles as a controlled and targeted drug delivery system have been published. Drugs are typically loaded into PSi nanoparticles by electrostatic interactions, and the drug-loaded nanoparticles are then administered parenterally in isotonic solutions. Zeta potential has an important role in drug adsorption and overall physical stability of nanosuspensions. In the present study, we used zeta potential measurements to study the impact of the formulation components to the nanosuspension stability. The impact of medium was studied by measuring isoelectric points (IEP) and zeta potentials in isotonic media. The role of drug adsorption was demonstrated with gastrointestinal peptides GLP-1(7-37) and PYY (3-36) and the selection of isotonic additive was demonstrated with peptide-loaded PSi nanoparticles. The results show the notable effect of isotonic solutions and peptide adsorption on zeta potential of PSi nanosuspensions. As a rule of thumb, the sugars (sucrose, dextrose and mannitol) seem to be good media for negatively charged peptide-loaded particles and weak acids (citric- and lactic acid) for positively charged particles. Nevertheless, perhaps the most important rule can be given for isotonic salt solutions which all are very poor media when the stability of nanosuspension is considered.

  9. Solid Lipid Nanoparticle-Based Calix[n]arenes and Calix-Resorcinarenes as Building Blocks: Synthesis, Formulation and Characterization

    Directory of Open Access Journals (Sweden)

    Anthony W. Coleman

    2013-11-01

    Full Text Available Solid lipid nanoparticles (SLNs have attracted increasing attention during recent years. This paper presents an overview about the use of calix[n]arenes and calix-resorcinarenes in the formulation of SLNs. Because of their specific inclusion capability both in the intraparticle spaces and in the host cavities as well as their capacity for functionalization, these colloidal nanostructures represent excellent tools for the encapsulation of different active pharmaceutical ingredients (APIs in the area of drug targeting, cosmetic additives, contrast agents, etc. Various synthetic routes to the supramolecular structures will be given. These various routes lead to the formulation of the corresponding SLNs. Characterization, properties, toxicological considerations as well as numerous corresponding experimental studies and analytical methods will be also exposed and discussed.

  10. Improved Poly (D,L-lactide) nanoparticles-based formulation for hair follicle targeting

    OpenAIRE

    Fernandes, Bruno Pacheco; Silva, R.; Ribeiro, Artur J.; Matamá, Maria Teresa; Gomes, A. C.; Paulo, Artur Cavaco

    2015-01-01

    Objective Hair follicles are widely recognized as the preferential target and site of accumulation for nanoparticles after topical application. This feature is of particular importance for hair cosmetics, having the potential to refine the treatment of several hair follicle-related disorders. The aim of this work was to improve the preparation of Poly (D,L-lactide) (PLA) nanoparticles for in vivo follicular target and drug delivery. Methods Envisaging a future industrial scale-up of ...

  11. Nanoparticles Containing High Loads of Paclitaxel-Silicate Prodrugs: Formulation, Drug Release, and Anticancer Efficacy.

    Science.gov (United States)

    Han, Jing; Michel, Andrew R; Lee, Han Seung; Kalscheuer, Stephen; Wohl, Adam; Hoye, Thomas R; McCormick, Alon V; Panyam, Jayanth; Macosko, Christopher W

    2015-12-01

    We have investigated particle size, interior structure, drug release kinetics, and anticancer efficacy of PEG-b-PLGA-based nanoparticles loaded with a series of paclitaxel (PTX)-silicate prodrugs [PTX-Si(OR)3]. Silicate derivatization enabled us to adjust the hydrophobicity and hydrolytic lability of the prodrugs by the choice of the alkyl group (R) in the silicate derivatives. The greater hydrophobicity of these prodrugs allows for the preparation of nanoparticles that are stable in aqueous dispersion even when loaded with up to ca. 75 wt % of the prodrug. The hydrolytic lability of silicates allows for facile conversion of prodrugs back to the parent drug, PTX. A suite of eight PTX-silicate prodrugs was investigated; nanoparticles were made by flash nanoprecipitation (FNP) using a confined impingement jet mixer with a dilution step (CIJ-D). The resulting nanoparticles were 80-150 nm in size with a loading level of 47-74 wt % (wt %) of a PTX-silicate, which corresponds to 36-59 effective wt % of free PTX. Cryogenic transmission electron microscopy images show that particles are typically spherical with a core-shell structure. Prodrug/drug release profiles were measured. Release tended to be slower for prodrugs having greater hydrophobicity and slower hydrolysis rate. Nanoparticles loaded with PTX-silicate prodrugs that hydrolyze most rapidly showed in vitro cytotoxicity similar to that of the parent PTX. Nanoparticles loaded with more labile silicates also tended to show greater in vivo efficacy.

  12. Comparative evaluation of antibacterial activity of caffeic acid phenethyl ester and PLGA nanoparticle formulation by different methods

    Science.gov (United States)

    Arasoglu, Tülin; Derman, Serap; Mansuroglu, Banu

    2016-01-01

    The aim of the present study was to evaluate the antimicrobial activity of nanoparticle and free formulations of the CAPE compound using different methods and comparing the results in the literature for the first time. In parallel with this purpose, encapsulation of CAPE with the PLGA nanoparticle system (CAPE-PLGA-NPs) and characterization of nanoparticles were carried out. Afterwards, antimicrobial activity of free CAPE and CAPE-PLGA-NPs was determined using agar well diffusion, disk diffusion, broth microdilution and reduction percentage methods. P. aeroginosa, E. coli, S. aureus and methicillin-resistant S. aureus (MRSA) were chosen as model bacteria since they have different cell wall structures. CAPE-PLGA-NPs within the range of 214.0 ± 8.80 nm particle size and with an encapsulation efficiency of 91.59 ± 4.97% were prepared using the oil-in-water (o-w) single-emulsion solvent evaporation method. The microbiological results indicated that free CAPE did not have any antimicrobial activity in any of the applied methods whereas CAPE-PLGA-NPs had significant antimicrobial activity in both broth dilution and reduction percentage methods. CAPE-PLGA-NPs showed moderate antimicrobial activity against S. aureus and MRSA strains particularly in hourly measurements at 30.63 and 61.25 μg ml-1 concentrations (both p 0.05). In the reduction percentage method, in which the highest results of antimicrobial activity were obtained, it was observed that the antimicrobial effect on S. aureus was more long-standing (3 days) and higher in reduction percentage (over 90%). The appearance of antibacterial activity of CAPE-PLGA-NPs may be related to higher penetration into cells due to low solubility of free CAPE in the aqueous medium. Additionally, the biocompatible and biodegradable PLGA nanoparticles could be an alternative to solvents such as ethanol, methanol or DMSO. Consequently, obtained results show that the method of selection is extremely important and will influence the

  13. A novel spray-dried nanoparticles-in-microparticles system for formulating scopolamine hydrobromide into orally disintegrating tablets

    Directory of Open Access Journals (Sweden)

    Li FQ

    2011-04-01

    Full Text Available Feng-Qian Li1, Cheng Yan2, Juan Bi1, Wei-Lin Lv3, Rui-Rui Ji3, Xu Chen1, Jia-Can Su3, Jin-Hong Hu31Department of Pharmaceutics, Shanghai Eighth People’s Hospital, Shanghai, People’s Republic of China; 2Department of Pharmacy, Bethune International Peace Hospital, Shijiazhuang, People’s Republic of China; 3Changhai Hospital, Second Military Medical University, Shanghai, People’s Republic of ChinaAbstract: Scopolamine hydrobromide (SH-loaded microparticles were prepared from a colloidal fluid containing ionotropic-gelated chitosan nanoparticles using a spray-drying method. The spray-dried microparticles were then formulated into orally disintegrating tablets (ODTs using a wet granulation tablet formation process. A drug entrapment efficiency of about 90% (w/w and loading capacity of 20% (w/w were achieved for the microparticles, which ranged from 2 µm to 8 µm in diameter. Results of disintegration tests showed that the formulated ODTs could be completely dissolved within 45 seconds. Drug dissolution profiles suggested that SH is released more slowly from tablets made using the microencapsulation process compared with tablets containing SH that is free or in the form of nanoparticles. The time it took for 90% of the drug to be released increased significantly from 3 minutes for conventional ODTs to 90 minutes for ODTs with crosslinked microparticles. Compared with ODTs made with noncrosslinked microparticles, it was thus possible to achieve an even lower drug release rate using tablets with appropriate chitosan crosslinking. Results obtained indicate that the development of new ODTs designed with crosslinked microparticles might be a rational way to overcome the unwanted taste of conventional ODTs and the side effects related to SH’s intrinsic characteristics.Keywords: scopolamine hydrobromide, chitosan, nanoparticles-in-microparticles system, spray-drying, orally disintegrating tablets

  14. CHEMICAL MODIFICATION OF CHITOSAN AND FORMULATION OF ITS NANOPARTICLES FOR PROTEIN DRUG DELIVERY SYSTEM

    OpenAIRE

    Swastika Karwani; Rabindra Nanda; Jyoti Nirmal

    2013-01-01

    The most common route of administration of proteins has been parenterals using invasive ways of administration but this route has many side effects like lack of patient compliance, cost, high drug levels etc. The development of an oral dosage form that improves the absorption of protein drugs is the most desirable formulation but one of the greatest challenges in the pharmaceutical field. The major barriers in developing oral formulations for peptides and proteins include poor intrinsic perme...

  15. Molecular Mechanism of Enhanced Anticancer Effect of Nanoparticle Formulated LY2835219 via p16-CDK4/6-pRb Pathway in Colorectal Carcinoma Cell Line

    Directory of Open Access Journals (Sweden)

    Xu Tang

    2016-01-01

    Full Text Available LY2835219 is a dual inhibitor to CDK4 and CDK6. This study was to prepare LY2835219-loaded chitosan nanoparticles (CNP/LY and LY2835219-loaded hyaluronic acid-conjugated chitosan nanoparticles (HACNP/LY and revealed their anticancer effect and influence on p16-CDK4/6-pRb pathway against colon cell line. The nanoparticle sizes of CNP/LY and HACNP/LY were approximately 195±39.6 nm and 217±31.1 nm, respectively. The zeta potentials of CNP/LY and HACNP/LY were 37.3±1.5 mV and 30.3±2.2 mV, respectively. And the preparation process showed considerable drug encapsulation efficiency and loading efficiency. LY2835219, CNP/LY, and HACNP/LY inhibited HT29 cell proliferation with 0.68, 0.54, and 0.30 μM of IC50, respectively. G1 phase was arrested by LY2835219 and its formulations. Furthermore, inhibition of CDK4/6 by LY2835219 formulations induced CDK4, CDK6, cyclin D1, and pRb decrease and p16 increase at both protein and mRNA levels. Overall, nanoparticle formulated LY2835219 could enhance the cytotoxicity and cell cycle arrest, and HACNP/LY strengthened the trend furtherly compared to CNP/LY. It is the first time to demonstrate the anticancer effect and mechanism against HT29 by LY2835219 and its nanoparticles. The drug and its nanoparticle formulations delay the cell growth and arrest cell cycle through p16-CDK4/6-pRb pathway, while the nanoparticle formulated LY2835219 could strengthen the process.

  16. Highly Stable Tetra-Phenolato Titanium(IV Agent Formulated into Nanoparticles Demonstrates Anti-Tumoral Activity and Selectivity

    Directory of Open Access Journals (Sweden)

    Sigalit Meker

    2015-10-01

    Full Text Available Titanium(IV complexes exhibit high potential as anti-tumor agents, particularly due to their low intrinsic toxicity and cytotoxicity toward cisplatin resistant cells. Nevertheless, Ti(IV complexes generally undergo rapid hydrolysis that previously hampered their utilization as anticancer drugs. We recently overcame this difficulty by developing a highly stable Ti(IV complex that is based on tetra-phenolato, hexadentate ligand, formulated into organic nanoparticles. Herein we investigated the activity of this complex in vitro and in vivo. Although inactive when tested directly due to poor solubility, when formulated, this complex displayed (a high cytotoxicity toward cisplatin resistant human ovarian cells, A2780-cp, with resistance factor of 1.1; (b additive behavior in combination with cisplatin toward ovarian and colon cancer cells; (c selectivity toward cancer cells as implied by its mild activity toward non-cancerous, fibroblast lung cells, MRC-5; (d high stability and durability as manifested by the ability to maintain cytotoxicity, even following one week of incubation in 100% aquatic medium solution; and (e in vivo efficacy toward solid tumors of human colon cancer cells, HT-29, in nude mice without any clinical signs of toxicity. These features support the formulated phenolato Ti(IV complex being an effective and selective anti-tumoral agent.

  17. Novel formulation and evaluation of a Q10-loaded solid lipid nanoparticle cream: in vitro and in vivo studies

    Directory of Open Access Journals (Sweden)

    Farboud ES

    2011-03-01

    Full Text Available Effat Sadat Farboud, Saman Ahmad Nasrollahi, Zahra TabbakhiDepartment of Pharmaceutics, School of Pharmacy, Tehran University of Medical Sciences, Tehran, IranAbstract: Solid lipid nanoparticles (SLNs of coenzyme Q10 (CoQ10 were formulated by a high-pressure homogenization method. The best formulation of SLN dispersion consisted of 13% lipid (cetyl palmitate or stearic acid, 8% surfactant (Tween 80 or Tego Care 450, and water. Stability tests, particle size analysis, differential scanning calorimetry, transmission electron microscopy, and release study were conducted to find the best formulation. A simple cream of CoQ10 and a cream containing CoQ10-loaded SLNs were prepared and compared on volunteers aged 20–30 years. SLNs with particle size between 50 nm and100 nm exhibited the most suitable stability. In vitro release profiles of CoQ10 from simple cream, SLN alone, and CoQ10-loaded SLN cream showed prolonged release for SLNs compared with the simple cream, whereas there was no significant difference between SLN alone and SLN in cream. In vitro release studies also demonstrated that CoQ10-loaded SLN and SLN cream possessed a biphasic release pattern in comparison with simple cream. In vivo skin hydration and elasticity studies on 25 volunteers suggested good dermal penetration and useful activity of Q10 on skin as a hydratant and antiwrinkle cream.Keywords: coenzyme Q10, SLN, release study 

  18. Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies

    OpenAIRE

    Venkateswarlu Vobalaboina; Ravichandiran Velayutham; Anbu Jayaraman; Bhaskar Kesavan; Rao Yamsani

    2009-01-01

    Abstract The aim of the study is to prepare aqueous dispersions of lipid nanoparticles – flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses wer...

  19. Formulation and characterization of solid lipid nanoparticles loaded Neem oil for topical treatment of acne

    Directory of Open Access Journals (Sweden)

    V. Vijayan

    2013-01-01

    Conclusion: The result concluded that Neem oil loaded solid lipid nanoparticles with more lecithin content in their colloid exhibit sustained effect which satisfactorily produced the antibacterial action on Acne microbes. Therefore Neem oil loaded SLN was used successfully for prolonged treatment of Acne.

  20. Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design.

    Science.gov (United States)

    ElShaer, Amr; Mustafa, Shelan; Kasar, Mohamad; Thapa, Sapana; Ghatora, Baljit; Alany, Raid G

    2016-01-01

    Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including pharmaceutical dosage forms. Soft contact lenses are promising delivery devices that can sustain the drug release and prolong residence time by acting as a geometric barrier to drug diffusion to tear fluid. This study investigates experimental parameters such as composition of polymer mixtures, stabilizer and the amount of active pharmaceutical ingredient on the preparation of a polymeric drug delivery system for the topical ocular administration of Prednisolone. To achieve this goal, prednisolone-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by single emulsion solvent evaporation method. Prednisolone was quantified using a validated high performance liquid chromatography (HPLC) method. Nanoparticle size was mostly affected by the amount of co-polymer (PLGA) used whereas drug load was mostly affected by amount of prednisolone (API) used. Longer homogenization time along with higher amount of API yielded the smallest size nanoparticles. The nanoparticles prepared had an average particle size of 347.1 ± 11.9 nm with a polydispersity index of 0.081. The nanoparticles were then incorporated in the contact lens mixture before preparing them. Clear and transparent contact lenses were successfully prepared. When the nanoparticle (NP)-loaded contact lenses were compared with control contact lenses (unloaded NP contact lenses), a decrease in hydration by 2% (31.2% ± 1.25% hydration for the 0.2 g loaded NP contact lenses) and light transmission by 8% (unloaded NP contact lenses 94.5% NP 0.2 g incorporated contact lenses 86.23%). The wettability of the contact lenses remained within the desired value (<90 °C) even upon incorporation of the NP. NP alone and

  1. Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design

    Directory of Open Access Journals (Sweden)

    Amr ElShaer

    2016-04-01

    Full Text Available Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including pharmaceutical dosage forms. Soft contact lenses are promising delivery devices that can sustain the drug release and prolong residence time by acting as a geometric barrier to drug diffusion to tear fluid. This study investigates experimental parameters such as composition of polymer mixtures, stabilizer and the amount of active pharmaceutical ingredient on the preparation of a polymeric drug delivery system for the topical ocular administration of Prednisolone. To achieve this goal, prednisolone-loaded poly (lactic-co-glycolic acid (PLGA nanoparticles were prepared by single emulsion solvent evaporation method. Prednisolone was quantified using a validated high performance liquid chromatography (HPLC method. Nanoparticle size was mostly affected by the amount of co-polymer (PLGA used whereas drug load was mostly affected by amount of prednisolone (API used. Longer homogenization time along with higher amount of API yielded the smallest size nanoparticles. The nanoparticles prepared had an average particle size of 347.1 ± 11.9 nm with a polydispersity index of 0.081. The nanoparticles were then incorporated in the contact lens mixture before preparing them. Clear and transparent contact lenses were successfully prepared. When the nanoparticle (NP-loaded contact lenses were compared with control contact lenses (unloaded NP contact lenses, a decrease in hydration by 2% (31.2% ± 1.25% hydration for the 0.2 g loaded NP contact lenses and light transmission by 8% (unloaded NP contact lenses 94.5% NP 0.2 g incorporated contact lenses 86.23%. The wettability of the contact lenses remained within the desired value (<90 °C even upon incorporation of the NP. NP

  2. Nanoparticle-Laden Contact Lens for Controlled Ocular Delivery of Prednisolone: Formulation Optimization Using Statistical Experimental Design

    Science.gov (United States)

    ElShaer, Amr; Mustafa, Shelan; Kasar, Mohamad; Thapa, Sapana; Ghatora, Baljit; Alany, Raid G.

    2016-01-01

    Human eye is one of the most accessible organs in the body, nonetheless, its physiology and associated precorneal factors such as nasolacrimal drainage, blinking, tear film, tear turnover, and induced lacrimation has significantly decreased the residence time of any foreign substances including pharmaceutical dosage forms. Soft contact lenses are promising delivery devices that can sustain the drug release and prolong residence time by acting as a geometric barrier to drug diffusion to tear fluid. This study investigates experimental parameters such as composition of polymer mixtures, stabilizer and the amount of active pharmaceutical ingredient on the preparation of a polymeric drug delivery system for the topical ocular administration of Prednisolone. To achieve this goal, prednisolone-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles were prepared by single emulsion solvent evaporation method. Prednisolone was quantified using a validated high performance liquid chromatography (HPLC) method. Nanoparticle size was mostly affected by the amount of co-polymer (PLGA) used whereas drug load was mostly affected by amount of prednisolone (API) used. Longer homogenization time along with higher amount of API yielded the smallest size nanoparticles. The nanoparticles prepared had an average particle size of 347.1 ± 11.9 nm with a polydispersity index of 0.081. The nanoparticles were then incorporated in the contact lens mixture before preparing them. Clear and transparent contact lenses were successfully prepared. When the nanoparticle (NP)-loaded contact lenses were compared with control contact lenses (unloaded NP contact lenses), a decrease in hydration by 2% (31.2% ± 1.25% hydration for the 0.2 g loaded NP contact lenses) and light transmission by 8% (unloaded NP contact lenses 94.5% NP 0.2 g incorporated contact lenses 86.23%). The wettability of the contact lenses remained within the desired value (<90 °C) even upon incorporation of the NP. NP alone and

  3. Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

    Directory of Open Access Journals (Sweden)

    El-Habashy SE

    2016-05-01

    Full Text Available Salma E El-Habashy, Ahmed N Allam, Amal H El-Kamel Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt Abstract: Nanoparticles (NPs have long gained significant interest for their use in various drug formulations in order to increase bioavailability, prolong drug release, and decrease side effects of highly toxic drugs. The objective of this investigation was to evaluate the potential of ethyl cellulose-based NPs (EC-NPs to modulate the release and reduce ulcerogenicity of piroxicam (PX after oral administration. PX-loaded EC-NPs were prepared by solvent evaporation technique using different stabilizers at three concentration levels. Morphological examination of selected formulas confirmed the formation of spherical NPs with slightly porous surface. Formulation containing poloxamer-stabilized EC-NPs (P188/0.2, having a particle size of 240.26±29.24 nm, polydispersity index of 0.562±0.030, entrapment efficiency of 85.29%±1.57%, and modulated release of PX (88% after 12 hours, was selected as the optimum formulation. Differential scanning calorimetry demonstrated the presence of PX in an amorphous form in the NPs. Fourier-transform infrared spectroscopy revealed the possible formation of hydrogen bond and the absence of chemical interaction. In vivo study, evaluation of pharmacokinetic parameters, evaluation of gastric irritation potential, and histological examination were conducted after administration of the selected formulation. Time to reach maximum plasma concentration, tmax, of poloxamer-stabilized EC-NPs was significantly higher than that of Feldene® 20 mg capsules (P≤0.001. Encapsulation of the acidic, gastric offender PX into NPs managed to significantly suppress gastric ulceration potential in rats (P≤0.05 as compared to that of PX suspension. A reduction of 66% in mean ulcer index was observed. In conclusion, poloxamer-stabilized EC-NPs (P188/0.2 had a significant potential of

  4. Green and ecofriendly synthesis of silver nanoparticles: Characterization, biocompatibility studies and gel formulation for treatment of infections in burns.

    Science.gov (United States)

    Jadhav, Kiran; Dhamecha, Dinesh; Bhattacharya, Debdutta; Patil, Mrityunjaya

    2016-02-01

    The current study summarizes a unique green process for the synthesis of silver nanoparticles (AgNPs) by simple treatment of silver nitrate with aqueous extract of Ammania baccifera. Phytosynthesized AgNPs were characterized by various advanced analytical methods and studied for its use against infections associated with burns. Formation of AgNPs was observed by visual color change from colorless to dark brown and confirmed by UV-visible characteristic peak at 436 nm. Zeta potential, particle size and polydispersity index of nano-silver were found to be -33.1 ± 1.12, 112.6 ± 6.8 nm and 0.3 ± 0.06 respectively. XRD spectra revealed crystalline nature of AgNPs whereas TEM confirmed the presence of mixed morphology of AgNPs. The overall approach designated in the present research investigation for the synthesis of AgNPs is based on all 12 principles of green chemistry, in which no man-made chemical other than the silver nitrate was used. Synthesized nano-silver colloidal dispersion was initially tested for minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against a panel of organisms involved in infections associated with burns (Pseudomonas aeruginosa (PA), Staphylococcus aureus (SA) and methicillin resistant S. aureus (MRSA)). MIC and MBC were found to be in range of 0.992 to 7.93 and 7.93 to 31.75 μg/mL respectively. MBC was used for formulation of AgNP gel and tested for its efficacy using agar well diffusion method against PA, SA and MRSA. Comparative bactericidal efficacy of formulated gel (0.03% w/w) and marked formulation Silverex™ ionic (silver nitrate gel 0.2% w/w) showed equal zone of inhibition against all pathogenic bacteria. Formulated AgNP gel consisting of 95% lesser concentration of silver compared to marketed formulation was found to be equally effective against all organisms. Hence, the formulated AgNP gel could serve as a better alternative with least toxicity towards the treatment presently available for

  5. Precious metal carborane polymer nanoparticles: characterisation of micellar formulations and anticancer activity.

    Science.gov (United States)

    Barry, Nicolas P E; Pitto-Barry, Anaïs; Romero-Canelón, Isolda; Tran, Johanna; Soldevila-Barreda, Joan J; Hands-Portman, Ian; Smith, Corinne J; Kirby, Nigel; Dove, Andrew P; O'Reilly, Rachel K; Sadler, Peter J

    2014-01-01

    We report the encapsulation of highly hydrophobic 16-electron organometallic ruthenium and osmium carborane complexes [Ru/Os(p-cymene)(1,2-dicarba-closo-dodecarborane-1,2-dithiolate)] ( and ) in Pluronic® triblock copolymer P123 core-shell micelles. The spherical nanoparticles and , dispersed in water, were characterized by dynamic light scattering (DLS), cryogenic transmission electron microscopy (cryo-TEM), and synchrotron small-angle X-ray scattering (SAXS; diameter ca. 15 and 19 nm, respectively). Complexes and were highly active towards A2780 human ovarian cancer cells (IC(50) 0.17 and 2.50 μM, respectively) and the encapsulated complexes, as and nanoparticles, were less potent (IC(50) 6.69 μM and 117.5 μM, respectively), but more selective towards cancer cells compared to normal cells.

  6. Formulation and characterization of solid lipid nanoparticles loaded Neem oil for topical treatment of acne

    Institute of Scientific and Technical Information of China (English)

    V. Vijayan; Shaik Aafreen; S. Sakthivel; K. Ravindra Reddy

    2013-01-01

    Objective:To investigate the treatment of acne and pimples as well as improves skin elasticity by solid lipid nanoparticles(SLNs) loadedNeem oil.Method:Neem oil as a natural agent was incorporated intoSLNs prepared by double emulsification method using different concentration of lecithin andTween80.The characteristics ofSLNs with different concentration of lipid were investigated.Result:The average particlesize ofNeem oil loadedSLNs decreased with increasing concentration of surfactant.SLNs of(221.6±2.0) nm with aPolydispersity index of (0.948±0.040) were obtained at higher concentration of lipid and surfactant.High entrapment efficiency of82.10% revealed the ability of solid lipid nanoparticles to incorporate a high quantity ofNeem oil.Furthermore the stability ofSLNs indicated with negligible drug leakage after3 weeks.Conclusion:The result concluded thatNeem oil loaded solid lipid nanoparticles with more lecithin content in their colloid exhibit sustained effect which satisfactorily produced the antibacterial action onAcne microbes.ThereforeNeem oil loadedSLN was used successfully for prolonged treatment ofAcne.

  7. Sucrose ester stabilized solid lipid nanoparticles and nanostructured lipid carriers: I. Effect of formulation variables on the physicochemical properties, drug release and stability of clotrimazole-loaded nanoparticles

    Science.gov (United States)

    Das, Surajit; Kiong Ng, Wai; Tan, Reginald B. H.

    2014-03-01

    The objective of this study was to develop and evaluate solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) utilizing sucrose ester as a stabilizer/emulsifier for the controlled release of drug/active. Both SLNs and NLCs were prepared using different sugar esters to screen out the most suitable stabilizer. Clotrimazole was used as a model active/drug. The effect of different formulation variables on the particle size, polydispersity index and drug encapsulation efficiency of SLNs and NLCs was evaluated and compared. SLNs and NLCs were physicochemically characterized and compared using Cryo-SEM, DSC and XRD. Furthermore, a drug release study of SLNs and NLCs was conducted. Finally, physicochemical stability (size, PI, ZP, EE) of the SLNs and NLCs was checked at 25 ± 2 °C and at 2-8 °C. Among the sucrose esters, D-1216 was found to be most suitable for both SLNs and NLCs. Formulation variables exhibited a significant impact on size, PI and EE of the nanoparticles. SLNs with ˜120 nm size, ˜0.23 PI, ˜I26I mV ZP, ˜87% EE and NLCs with ˜160 nm size, 0.15 PI, ˜I26I mV ZP, ˜88% EE were produced. Cryo-SEM revealed spherical particles with a smooth surface but did not exhibit any difference in surface morphology between SLNs and NLCs. DSC and XRD results demonstrated the disappearance of clotrimazole peak(s) in drug-loaded SLNs and NLCs. Faster drug release was observed from SLNs than NLCs. NLCs were found to be more stable than SLNs in terms of size, PI, EE and drug release. The results indicated that both SLNs and NLCs stabilized with sucrose ester D-1216 can be used as controlled release carriers although NLCs have an edge over SLNs.

  8. Formulation and characterization of hydrophilic drug diclofenac sodium-loaded solid lipid nanoparticles based on phospholipid complexes technology.

    Science.gov (United States)

    Liu, Dongfei; Chen, Li; Jiang, Sunmin; Zhu, Shuning; Qian, Yong; Wang, Fengzhen; Li, Rui; Xu, Qunwei

    2014-03-01

    To successfully prepare the diclofenac sodium (DS)-loaded solid lipid nanoparticles (SLNs), phospholipid complexes (PCs) technology was applied here to improve the liposolubility of DS. Solid lipid nanoparticles (SLNs) loaded with phospholipid complexes (PCs) were prepared by the modified emulsion/solvent evaporation method. DS could be solubilized effectively in the organic solvents with the existence of phospholipid and apparent partition coefficient of DS in PCs increased significantly. X-ray diffraction analysis suggested that DS in PCs was either molecularly dispersed or in an amorphous form. However, no significant difference was observed between the Fourier transform infrared spectroscopy (FT-IR) spectra of physical mixture and that of PCs. Particles with small sizes, narrow polydispersity indexes and high entrapment efficiencies could be obtained with the addition of PCs. Furthermore, according to the transmission electron microscopy, a core-shell structure was likely to be formed. The presence of PCs caused the change of zeta potential and retarded the drug release of SLNs, which indicated that phospholipid formed multilayers around the solid lipid core of SLNs. Both FT-IR and differential scanning calorimetry analysis also illustrated that some weak interactions between DS and lipid materials might take place during the preparation of SLNs. In conclusion, the model hydrophilic drug-DS can be formulated into the SLNs with the help of PCs. PMID:24236407

  9. Formulation, characteristics and antiatherogenic bioactivities of CD36-targeted epigallocatechin gallate (EGCG)-loaded nanoparticles.

    Science.gov (United States)

    Zhang, Jia; Nie, Shufang; Martinez-Zaguilan, Raul; Sennoune, Souad R; Wang, Shu

    2016-04-01

    Intimal macrophages are determinant cells for atherosclerotic lesion formation by releasing inflammatory factors and taking up oxidized low-density lipoprotein (oxLDL) via scavenger receptors, primarily the CD36 receptor. (-)-Epigallocatechin-3-gallate (EGCG) has a potential to decrease cholesterol accumulation and inflammatory responses in macrophages. We made EGCG-loaded nanoparticles (Enano) using phosphatidylcholine, kolliphor HS15, alpha-tocopherol acetate and EGCG. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine (KOdiA-PC), a CD36-targeted ligand found on oxLDL, was incorporated on the surface of Enano to make ligand-Enano (L-Enano). The objectives of this study are to deliver EGCG to macrophages via CD36-targeted L-Enano and to determine its antiatherogenic bioactivities. The optimized nanoparticles obtained in our study were spherical and around 108 nm in diameter, and had about 10% of EGCG loading capacity and 96% of EGCG encapsulation efficiency. Compared to Enano, CD36-targeted L-Enano had significantly higher binding affinity to and uptake by macrophages at the same pattern as oxLDL. CD36-targeted L-Enano dramatically improved EGCG stability, increased macrophage EGCG content, delivered EGCG to macrophage cytosol and avoided lysosomes. L-Enano significantly decreased macrophage mRNA levels and protein secretion of monocyte chemoattractant protein 1, but did not significantly change macrophage cholesterol content. The innovative CD36-targeted nanoparticles may facilitate targeted delivery of diagnostic, preventive and therapeutic compounds to intimal macrophages for the diagnosis, prevention and treatment of atherosclerosis with enhanced efficacy and decreased side effects. PMID:27012617

  10. Development of a novel nanoparticle formulation of thymoquinone with a cold wet-milling system and its pharmacokinetic analysis.

    Science.gov (United States)

    Nihei, Takuya; Suzuki, Hiroki; Aoki, Asako; Yuminoki, Kayo; Hashimoto, Naofumi; Sato, Hideyuki; Seto, Yoshiki; Onoue, Satomi

    2016-09-10

    The present study aimed to develop a nanoparticle (NP) formulation of thymoquinone (TQ), a potent anti-oxidant chemical, with use of a cold wet-milling (CWM) system to improve its dissolution behavior and pharmacokinetic properties. The NP formulation of TQ (TQ/CWM) was prepared by CWM system, and its physicochemical properties were characterized in terms of particle size distribution, morphology, crystallinity, and dissolution. The photochemical properties of TQ were also examined upon UV/VIS absorption, reactive oxygen species (ROS) generation, and photostability. Pharmacokinetic studies were carried out in rats. Application of the CWM system to TQ led to successful development of nano-sized TQ. The mean diameter of TQ in TQ/CWM was calculated to be 143nm, and TQ particles in TQ/CWM were found to be amorphous. There was a marked improvement in dissolution rate compared with TQ. TQ showed significant generation of singlet oxygen and superoxide upon exposure to simulated sunlight, suggesting its high photoreactivity, and solid samples such as TQ and TQ/CWM exhibited higher photostability than TQ solution. In comparison with TQ, enhanced TQ exposure was observed with a ca. 6-fold increase of oral bioavailability, and the Tmax was shown to be a quarter. From these findings, the NP approach employing the CWM system might be a promising dosage option for improving the nutraceutical values of TQ. PMID:27451272

  11. Gold Nanoparticle Sensor for the Visual Detection of Pork Adulteration in Meatball Formulation

    OpenAIRE

    Ali, M. E.; Hashim, U.; MUSTAFA, S.; Che Man, Y. B.; Kh. N. Islam

    2012-01-01

    We visually identify pork adulteration in beef and chicken meatball preparations using 20 nm gold nanoparticles (GNPs) as colorimetric sensors. Meatball is a popular food in certain Asian and European countries. Verification of pork adulteration in meatball is necessary to meet the Halal and Kosher food standards. Twenty nm GNPs change color from pinkish-red to gray-purple, and their absorption peak at 525 nm is red-shifted by 30–50 nm in 3 mM phosphate buffer saline (PBS). Adsorption of sing...

  12. Formulation of solid lipid nanoparticles (SLN): the value of different alkyl polyglucoside surfactants.

    Science.gov (United States)

    Keck, Cornelia M; Kovačević, Andjelka; Müller, Rainer H; Savić, Snežana; Vuleta, Gordana; Milić, Jela

    2014-10-20

    Alkyl polyglycosides (APGs) represent a group of nonionic tensides with excellent skin compatibility. Thus they seem to be excellent stabilizers for lipid nanoparticles for dermal application. To investigate this, different APGs were selected to evaluate their influence on the formation and characteristics of solid lipid nanoparticles (SLN). Contact angle analysis of the aqueous solutions/dispersions of the APGs on cetyl palmitate films revealed good wettability for all APG surfactants. Cetyl palmitate based SLN were prepared by hot high pressure homogenization and subjected to particle size, charge and inner structure analysis. 1% of each APG was sufficient to obtain SLN with a mean size between 150 nm and 175 nm and a narrow size distribution. The zeta potential in water was ∼ -50 mV; the values in the original medium were distinctly lower, but still sufficient high to provide good physical stability. Physical stability at different temperatures (5°C, 25°C and 40°C) was confirmed by a constant particle size over an observation period of 90 days in all dispersions. In comparison to SLN stabilized with classical surfactants, e.g., Polysorbate, APG stabilized SLN possess a smaller size, improved physical stability and contain less surfactant. Therefore, the use of APGs for the stabilization of lipid nanoparticles is superior in comparison to classical stabilizers. Further, the results indicate that the length of the alkyl chain of the APG influences the diminution efficacy, the final particle size and the crystallinity of the particles. APGs with short alkyl chain led to a faster reduction in size during high pressure homogenization, to a smaller particle size of the SLN and to a lower recrystallization index, i.e., to a lower crystallinity of the SLN. The crystallinity of the SLN increased with an increase in the alkyl chain length of APGs. Therefore, by using the tested APGs differing in the alkyl chain length, not only small sized and physically stable but

  13. Gold Nanoparticle Sensor for the Visual Detection of Pork Adulteration in Meatball Formulation

    Directory of Open Access Journals (Sweden)

    M. E. Ali

    2012-01-01

    Full Text Available We visually identify pork adulteration in beef and chicken meatball preparations using 20 nm gold nanoparticles (GNPs as colorimetric sensors. Meatball is a popular food in certain Asian and European countries. Verification of pork adulteration in meatball is necessary to meet the Halal and Kosher food standards. Twenty nm GNPs change color from pinkish-red to gray-purple, and their absorption peak at 525 nm is red-shifted by 30–50 nm in 3 mM phosphate buffer saline (PBS. Adsorption of single-stranded DNA protects the particles against salt-induced aggregation. Mixing and annealing of a 25-nucleotide (nt single-stranded (ss DNA probe with denatured DNA of different meatballs differentiated well between perfectly matched and mismatch hybridization at a critical annealing temperature. The probes become available in nonpork DNA containing vials due to mismatches and interact with GNPs to protect them from salt-induced aggregation. Whereas, all the pork containing vials, either in pure and mixed forms, consumed the probes totally by perfect hybridization and turned into grey, indicating aggregation. This is clearly reflected by a well-defined red-shift of the absorption peak and significantly increased absorbance in 550–800 nm regimes. This label-free low-cost assay should find applications in food analysis, genetic screening, and homology studies.

  14. A novel nanoparticle formulation overcomes multiple types of membrane efflux pumps in human breast cancer cells.

    Science.gov (United States)

    Prasad, Preethy; Cheng, Ji; Shuhendler, Adam; Rauth, Andrew M; Wu, Xiao Yu

    2012-04-01

    Multidrug resistance (MDR) in cancer cells can involve overexpression of different types of membrane drug efflux pumps and other drug resistance mechanisms. Hence, inhibition of one resistance mechanism may not be therapeutically effective. Previously we demonstrated a new polymer lipid hybrid nanoparticle (PLN) system was able to circumvent drug resistance of P-glycoprotein (P-gp) overexpressing breast cancer cells. The objectives of the present study were 2-fold: (1) to evaluate the ability of the PLN system to overcome two other membrane efflux pumps-multidrug resistance protein 1 (MRP1+) and breast cancer resistance protein (BCRP+) overexpressed on human breast cancer cell lines MCF7 VP (MRP1+) and MCF7 MX (BCRP+); and (2) to evaluate possible synergistic effects of doxorubicin (Dox)-mitomycin C (MMC) in these cell lines. These objectives were accomplished by measuring in vitro cellular uptake, intracellular trafficking, and cytotoxicity (using a clonogenic assay and median effect analysis), of Dox, MMC, or Dox-MMC co-loaded PLN. Treatment of MDR cells with PLN encapsulating single anticancer agents significantly enhanced cell kill compared to free Dox or MMC solutions. Dox-MMC co-loaded PLN were 20-30-folds more effective in killing MDR cells than free drugs. Co-encapsulated Dox-MMC was more effective in killing MDR cells than single agent-encapsulated PLN. Microscopic images showed perinuclear localization of fluorescently labelled PLN in all cell lines. These results are consistent with our previous results for P-gp overexpressing breast cancer cells suggesting the PLN system can overcome multiple types of membrane efflux pumps increasing the cytotoxicity of Dox-MMC at significantly lower doses than free drugs. PMID:25786718

  15. Formulation Optimization of Rosuvastatin Calcium-Loaded Solid Lipid Nanoparticles by 32 Full-Factorial Design

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    Kruti A. Dhoranwala

    2015-12-01

    Full Text Available The present investigation was aimed at developing Rosuvastatin Calcium loaded solid lipid nanoparticles (SLNs. The SLNs were prepared using high pressure homogenization technique. Glyceryl monostearate (GMS and Poloxamer 188 were employed as lipid carrier and surfactant respectively. A two factor, three level (32 full factorial design was applied to study the effect of independent variables i.e. amount of GMS (X1 and amount of Poloxamer 188 (X2 on dependent variables i.e. Particle size (Y1 and % entrapment efficiency (Y2. Particles size, % entrapment efficiency (%EE, zeta potential, drug content, in vitro drug release and particles morphology were evaluated for SLNs. Contour plots and response surface plots showed visual representation of relationship between the experimental responses (dependent variables and the set of input (independent variables. The adequacy of the regression model was verified by a check point analysis. The optimized batch (B10 contained 2.2 gm of GMS and 1% of Poloxamer 188. Batch B 10 exhibited mean particle size of 529.6 nm ± 6.36 nm; polydispersity index (PDI of 0.306 ± 0.042; zeta potential of -31.88 mV ± (-2.50 mV and %EE of 48.90% ± 1.72%. The drug release experiments exhibited an initial rapid release followed by sustained release extended upto 36 h. Differential scanning calorimetry (DSC studies showed that there was no chemical interaction between drug (Rosuvastatin Calcium and lipid (GMS whereas scanning electron microscopy (SEM studies indicated that Rosuvastatin Calcium loaded SLNs are spherical, discrete and homogenous. Accelerated stability studies showed that there was no significant change occurring in the responses after storage for a total period of 3 months.

  16. Design and syntheses of MMP inhibitors and photosensitive lipid nanoparticle formulations for drug delivery

    Science.gov (United States)

    Subramaniam, Rajesh

    Drug administration without any compromise to the quality of life and lifespan is the ideal goal for disease management. The molecular mechanisms of several pathologies have shown that site-specific delivery of target-specific drugs seems to be a promising avenue to achieve this goal. This thesis describes the initial steps that we have taken toward that goal. Matrix metalloproteinases (MMPs) are a family of about 23 isozymes in humans that were actively targeted for treating a multitude of pathologies. Clinical studies carried out on cancer patients have revealed the complexity of the working of this enzyme family and necessitated the development of isozyme-specific MMP inhibitors. Our studies toward the development of isozyme-specific inhibitors have resulted in the development of several inhibitors that seem to be selective toward some MMP isozymes. Our understanding on the molecular mechanism that confers this selectivity is documented in this thesis. Another aspect of discussion in the thesis is the development of photosensitive liposomes for drug delivery that could be triggered to release the drug by irradiation with light of appropriate wavelength. Development of such delivery vehicles, in principle, would confer external spatiotemporal control on drug delivery. This could potentially lead to better disease management by minimizing side effects and enhancing patient compatibility. The thesis discusses our attempts toward the development of photosensitive liposomes. These liposomes incorporated a photosensitive lipid (PSL) that would be cleaved upon irradiation with UV light, causing liposomal destabilization and release of the enclosed drug. The discussion includes: (i) the syntheses of the PSLs, (ii) formulation of the photosensitive liposomes that contained a model drug, (iii) light-mediated release of the drug and (iv) the mechanism of photocleavage of the PSL that leads to content release from liposomes. The thesis concludes with suggestions toward the

  17. Design of Curcumin Loaded PLGA Nanoparticles Formulation with Enhanced Cellular Uptake, and Increased Bioactivity in vitro and Superior Bioavailability in vivo

    OpenAIRE

    Anand, Preeta; Nair, Harish B.; Sung, Bokyung; Kunnumakkara, Ajaikumar B.; Yadav, Vivek R.; Tekmal, Rajeshwar R.; Aggarwal, Bharat B.

    2009-01-01

    Curcumin, a yellow pigment present in the spice turmeric (Curcuma longa), has been linked with antioxidant, anti-inflammatory, anti-proliferative, anticancer, antidiabetic, antirheumatic, and antiviral effects, but its optimum potential is limited by its lack of solubility in aqueous solvents and poor oral bioavailability. We employed a polymer-based nanoparticle approach to improve bioavailability. Curcumin was encapsulated with 97.5% efficiency in biodegradable nanoparticulate formulation b...

  18. New formulation of an old drug in hypertension treatment: the sustained release of captopril from cyclodextrin nanoparticles

    Directory of Open Access Journals (Sweden)

    de Azevedo MB

    2011-05-01

    observed upon CAP administration. The nanoparticles obtained by the kneading method (CAP/α-CD:KM showed a potent and long-lasting inhibitory activity (~22 hours on the angiotensin I pressor effect. The results suggest that the inclusion complex of CAP and α-CD can function as a novel antihypertensive formulation that may improve therapeutic use of CAP by reducing its oral dose administration to once per day, thus providing better quality of life for almost 25% of the world's population who suffer from hypertension.Keywords: captopril, cyclodextrin nanoparticles, sustained release

  19. Enhanced tumor delivery and antitumor response of doxorubicin-loaded albumin nanoparticles formulated based on a Schiff base.

    Science.gov (United States)

    Li, Fang; Zheng, Chunli; Xin, Junbo; Chen, Fangcheng; Ling, Hua; Sun, Linlin; Webster, Thomas J; Ming, Xin; Liu, Jianping

    2016-01-01

    A novel method was developed here to prepare albumin-based nanoparticles (NPs) for improving the therapeutic and safety profiles of chemotherapeutic agents. This approach involved crosslinking bovine serum albumin (BSA) using a Schiff base-containing vanillin, into NPs and loading doxorubicin (DOX) into the NPs by incubation. The resultant NPs (DOX-BSA-V-NPs) displayed a particle size of 100.5±1.3 nm with a zeta potential of -23.05±1.45 mV and also showed high drug-loading efficiency and excellent stability with respect to storage and temperature. The encapsulation of DOX into the BSA-V-NPs was confirmed by dynamic scanning calorimetry and Raman spectroscopy. DOX-BSA-V-NPs exhibited a significantly faster DOX release at pH 6.5 than pH 7.4, as well as in a solution with a higher glutathione concentration. In vitro studies showed that the cellular uptake of DOX-BSA-V-NPs was time-dependent, concentration-dependent, and faster than free DOX, while the cytotoxicity of DOX-BSA-V-NPs (IC50 value of 3.693 μg/mL) was superior to free DOX (IC50 value of 4.007 μg/mL). More importantly, DOX-BSA-V-NPs showed a longer mean survival time of 24.83 days, a higher tumor inhibition rate of 56.66%, and a decreased distribution in the heart than other DOX formulations in animal studies using a tumor xenograft model. Thus, the vanillin-based albumin NPs were shown here to be a promising carrier for tumor-targeted delivery of chemotherapeutic agents and, thus, should be further studied. PMID:27574421

  20. Enhanced tumor delivery and antitumor response of doxorubicin-loaded albumin nanoparticles formulated based on a Schiff base

    Science.gov (United States)

    Li, Fang; Zheng, Chunli; Xin, Junbo; Chen, Fangcheng; Ling, Hua; Sun, Linlin; Webster, Thomas J; Ming, Xin; Liu, Jianping

    2016-01-01

    A novel method was developed here to prepare albumin-based nanoparticles (NPs) for improving the therapeutic and safety profiles of chemotherapeutic agents. This approach involved crosslinking bovine serum albumin (BSA) using a Schiff base-containing vanillin, into NPs and loading doxorubicin (DOX) into the NPs by incubation. The resultant NPs (DOX-BSA-V-NPs) displayed a particle size of 100.5±1.3 nm with a zeta potential of −23.05±1.45 mV and also showed high drug-loading efficiency and excellent stability with respect to storage and temperature. The encapsulation of DOX into the BSA-V-NPs was confirmed by dynamic scanning calorimetry and Raman spectroscopy. DOX-BSA-V-NPs exhibited a significantly faster DOX release at pH 6.5 than pH 7.4, as well as in a solution with a higher glutathione concentration. In vitro studies showed that the cellular uptake of DOX-BSA-V-NPs was time-dependent, concentration-dependent, and faster than free DOX, while the cytotoxicity of DOX-BSA-V-NPs (IC50 value of 3.693 μg/mL) was superior to free DOX (IC50 value of 4.007 μg/mL). More importantly, DOX-BSA-V-NPs showed a longer mean survival time of 24.83 days, a higher tumor inhibition rate of 56.66%, and a decreased distribution in the heart than other DOX formulations in animal studies using a tumor xenograft model. Thus, the vanillin-based albumin NPs were shown here to be a promising carrier for tumor-targeted delivery of chemotherapeutic agents and, thus, should be further studied. PMID:27574421

  1. Synthesis and Characterization of Silicate Ester Prodrugs and Poly(ethylene glycol)-b-poly(lactic-co-glycolic acid) Block Copolymers for Formulation into Prodrug-Loaded Nanoparticles

    Science.gov (United States)

    Wohl, Adam Richard

    Fine control of the physical and chemical properties of customized materials is a field that is rapidly advancing. This is especially critical in pursuits to develop and optimize novel nanoparticle drug delivery. Specifically, I aim to apply chemistry concepts to test the hypothesis "Silicate ester prodrugs of paclitaxel, customized to have the proper hydrophobicity and hydrolytic lability, can be formulated with well-defined, biocompatible, amphiphilic block copolymers into nanoparticles that are effective drugs." Chapter 1 briefly describes the context and motivation of the scientific pursuits described in this thesis. In Chapter 2, a family of model silicate esters is synthesized, the hydrolysis rate of each compound is benchmarked, and trends are established based upon the steric bulk and leaving group ability of the silicate substituents. These trends are then applied to the synthesis of labile silicate ester prodrugs in Chapter 3. The bulk of this chapter focuses on the synthesis, hydrolysis, and cytotoxicity of prodrugs based on paclitaxel, a widely used chemotherapeutic agent. In Chapter 4, a new methodology for the synthesis of narrowly dispersed, "random" poly(lactic-co-glycolic acid) polymers by a constant infusion of the glycolide monomer is detailed. Using poly(ethylene glycol) as a macroinitiator, amphiphilic block copolymers were synthesized. Co-formulating a paclitaxel silicate and an amphiphilic block copolymer via flash nanoprecipitation led to highly prodrug-loaded, kinetically trapped nanoparticles. Studies to determine the structure, morphology, behavior, and efficacy of these nanoparticles are described in Chapter 5. Efforts to develop a general strategy for the selective end-functionalization of the polyether block of these amphiphilic block copolymers are discussed in Chapter 6. Examples of this strategy include functionalization of the polyether with an azide or a maleimide. Finally, Chapter 7 provides an outlook for future development of

  2. Formulation and in vitro evaluation of polymeric enteric nanoparticles as dermal carriers with pH-dependent targeting potential.

    Science.gov (United States)

    Sahle, Fitsum Feleke; Balzus, Benjamin; Gerecke, Christian; Kleuser, Burkhard; Bodmeier, Roland

    2016-09-20

    pH-sensitive nanoparticles which release in a controlled fashion on the skin or dissolve in the hair follicle could significantly improve treatment effectiveness and make transfollicular drug delivery a success. Dexamethasone-loaded Eudragit® L 100 nanoparticles were prepared by nanoprecipitation from an organic drug-polymer solution. Their toxicity potential was assessed using isolated human fibroblasts. pH-dependent swelling and erosion kinetics of the nanoparticles were investigated by dynamic light scattering and viscosity measurements and its effect on drug release was assessed in vitro with Franz diffusion cells. Stable, 100-550nm-sized dexamethasone-loaded Eudragit® L 100 nanoparticles with drug loading capacity and entrapment efficiency as high as 8.3% and 85%, respectively, were obtained by using polyvinyl alcohol as a stabilizer and ethanol as organic solvent. The nanoparticles showed little or no toxicity on isolated normal human fibroblasts. Dexamethasone existed in the nanoparticles as solid solution or in amorphous form. The nanoparticles underwent extensive swelling and slow drug release in media with a low buffer capacity (as low as 10mM) and a higher pH or at a pH close to the dissolution pH of the polymer (pH6) and a higher buffer capacity. In 40mM buffer and above pH6.8, the nanoparticles eroded fast or dissolved completely and thus released the drug rapidly. pH-sensitive nanoparticles which potentially release in a controlled manner on the stratum corneum but dissolve in the hair follicle could be prepared.

  3. Formulation and in vitro evaluation of polymeric enteric nanoparticles as dermal carriers with pH-dependent targeting potential.

    Science.gov (United States)

    Sahle, Fitsum Feleke; Balzus, Benjamin; Gerecke, Christian; Kleuser, Burkhard; Bodmeier, Roland

    2016-09-20

    pH-sensitive nanoparticles which release in a controlled fashion on the skin or dissolve in the hair follicle could significantly improve treatment effectiveness and make transfollicular drug delivery a success. Dexamethasone-loaded Eudragit® L 100 nanoparticles were prepared by nanoprecipitation from an organic drug-polymer solution. Their toxicity potential was assessed using isolated human fibroblasts. pH-dependent swelling and erosion kinetics of the nanoparticles were investigated by dynamic light scattering and viscosity measurements and its effect on drug release was assessed in vitro with Franz diffusion cells. Stable, 100-550nm-sized dexamethasone-loaded Eudragit® L 100 nanoparticles with drug loading capacity and entrapment efficiency as high as 8.3% and 85%, respectively, were obtained by using polyvinyl alcohol as a stabilizer and ethanol as organic solvent. The nanoparticles showed little or no toxicity on isolated normal human fibroblasts. Dexamethasone existed in the nanoparticles as solid solution or in amorphous form. The nanoparticles underwent extensive swelling and slow drug release in media with a low buffer capacity (as low as 10mM) and a higher pH or at a pH close to the dissolution pH of the polymer (pH6) and a higher buffer capacity. In 40mM buffer and above pH6.8, the nanoparticles eroded fast or dissolved completely and thus released the drug rapidly. pH-sensitive nanoparticles which potentially release in a controlled manner on the stratum corneum but dissolve in the hair follicle could be prepared. PMID:27393341

  4. A Tetravalent Sub-unit Dengue Vaccine Formulated with Ionizable Cationic Lipid Nanoparticle induces Significant Immune Responses in Rodents and Non-Human Primates

    Science.gov (United States)

    Swaminathan, Gokul; Thoryk, Elizabeth A.; Cox, Kara S.; Smith, Jeffrey S.; Wolf, Jayanthi J.; Gindy, Marian E.; Casimiro, Danilo R.; Bett, Andrew J.

    2016-01-01

    Dengue virus has emerged as an important arboviral infection worldwide. As a complex pathogen, with four distinct serotypes, the development of a successful Dengue virus vaccine has proven to be challenging. Here, we describe a novel Dengue vaccine candidate that contains truncated, recombinant, Dengue virus envelope protein from all four Dengue virus serotypes (DEN-80E) formulated with ionizable cationic lipid nanoparticles (LNPs). Immunization studies in mice, Guinea pigs, and in Rhesus macaques, revealed that LNPs induced high titers of Dengue virus neutralizing antibodies, with or without co-administration or encapsulation of a Toll-Like Receptor 9 agonist. Importantly, LNPs were also able to boost DEN-80E specific CD4+ and CD8+ T cell responses. Cytokine and chemokine profiling revealed that LNPs induced strong chemokine responses without significant induction of inflammatory cytokines. In addition to being highly efficacious, the vaccine formulation proved to be well-tolerated, demonstrating no elevation in any of the safety parameters evaluated. Notably, reduction in cationic lipid content of the nanoparticle dramatically reduced the LNP’s ability to boost DEN-80E specific immune responses, highlighting the crucial role for the charge of the LNP. Overall, our novel studies, across multiple species, reveal a promising tetravalent Dengue virus sub-unit vaccine candidate. PMID:27703172

  5. pH-responsive artemisinin derivatives and lipid nanoparticle formulations inhibit growth of breast cancer cells in vitro and induce down-regulation of HER family members.

    Directory of Open Access Journals (Sweden)

    Yitong J Zhang

    Full Text Available Artemisinin (ART dimers show potent anti-proliferative activities against breast cancer cells. To facilitate their clinical development, novel pH-responsive artemisinin dimers were synthesized for liposomal nanoparticle formulations. A new ART dimer was designed to become increasingly water-soluble as pH declines. The new artemisinin dimer piperazine derivatives (ADPs remained tightly associated with liposomal nanoparticles (NPs at neutral pH but were efficiently released at acidic pH's that are known to exist within solid tumors and organelles such as endosomes and lysosomes. ADPs incorporated into nanoparticles down regulated the anti-apoptotic protein, survivin, and cyclin D1 when incubated at low concentrations with breast cancer cell lines. We demonstrate for the first time, for any ART derivative, that ADP NPs can down regulate the oncogenic protein HER2, and its counterpart, HER3 in a HER2+ cell line. We also show that the wild type epidermal growth factor receptor (EGFR or HER1 declines in a triple negative breast cancer (TNBC cell line in response to ADP NPs. The declines in these proteins are achieved at concentrations of NP109 at or below 1 µM. Furthermore, the new artemisinin derivatives showed improved cell-proliferation inhibition effects compared to known dimer derivatives.

  6. Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and bioavailability

    Science.gov (United States)

    Guo, Shujie; Pham, Kevin; Li, Diana; Penzak, Scott R; Dong, Xiaowei

    2016-01-01

    Purpose The purpose of this study was to develop a novel lipid-based nanotechnology to formulate poorly water-soluble drugs in oral solid granules to improve stability, palatability, and bioavailability. Materials and methods In one method, we prepared ritonavir (RTV) nanoparticles (NPs) by a microemulsion-precursor method and then converted the RTV NPs to solid granules by wet granulation to produce RTV NP-containing granules. In the other innovative method, we did not use water in the formulation preparation, and discovered novel in situ self-assembly nanoparticles (ISNPs). We prepared RTV ISNP granules that did not initially contain NPs, but spontaneously produced RTV ISNPs when the granules were introduced to water with gentle agitation. We fully characterized these RTV nanoformulations. We also used rats to test the bioavailability of RTV ISNP granules. Finally, an Astree electronic tongue was used to assess the taste of the RTV ISNP granules. Results RTV NP-containing granules only had about 1% drug loading of RTV in the solid granules. In contrast, RTV ISNP granules achieved over 16% drug loading and were stable at room temperature over 24 weeks. RTV ISNPs had particle size between 160 nm and 300 nm with narrow size distribution. RTV ISNPs were stable in simulated gastric fluid for 2 hours and in simulated intestinal fluid for another 6 hours. The data from the electronic tongue showed that the RTV ISNP granules were similar in taste to blank ISNP granules, but were much different from RTV solution. RTV ISNP granules increased RTV bioavailability over 2.5-fold compared to RTV solution. Conclusion We successfully discovered and developed novel ISNPs to manufacture RTV ISNP granules that were reconstitutable, stable, and palatable, and improved RTV bioavailability. The novel ISNP nanotechnology is a platform to manufacture oral solid dosage forms for poorly water-soluble drugs, especially for pediatric formulation development. PMID:27103803

  7. Novel in situ self-assembly nanoparticles for formulating a poorly water-soluble drug in oral solid granules, improving stability, palatability, and bioavailability

    Directory of Open Access Journals (Sweden)

    Guo S

    2016-04-01

    Full Text Available Shujie Guo,1 Kevin Pham,2 Diana Li,2 Scott R Penzak,3 Xiaowei Dong2 1State Key Laboratory of Medical Genomics, Shanghai Key Laboratory of Hypertension, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, People’s Republic of China; 2Department of Pharmaceutical Sciences, 3Department of Pharmacotherapy, University of North Texas Health Science Center, Fort Worth, TX, USA Purpose: The purpose of this study was to develop a novel lipid-based nanotechnology to formulate poorly water-soluble drugs in oral solid granules to improve stability, palatability, and bioavailability. Materials and methods: In one method, we prepared ritonavir (RTV nanoparticles (NPs by a microemulsion-precursor method and then converted the RTV NPs to solid granules by wet granulation to produce RTV NP-containing granules. In the other innovative method, we did not use water in the formulation preparation, and discovered novel in situ self-assembly nanoparticles (ISNPs. We prepared RTV ISNP granules that did not initially contain NPs, but spontaneously produced RTV ISNPs when the granules were introduced to water with gentle agitation. We fully characterized these RTV nanoformulations. We also used rats to test the bioavailability of RTV ISNP granules. Finally, an Astree electronic tongue was used to assess the taste of the RTV ISNP granules. Results: RTV NP-containing granules only had about 1% drug loading of RTV in the solid granules. In contrast, RTV ISNP granules achieved over 16% drug loading and were stable at room temperature over 24 weeks. RTV ISNPs had particle size between 160 nm and 300 nm with narrow size distribution. RTV ISNPs were stable in simulated gastric fluid for 2 hours and in simulated intestinal fluid for another 6 hours. The data from the electronic tongue showed that the RTV ISNP granules were similar in taste to blank ISNP granules, but were much different from RTV solution. RTV ISNP granules increased RTV bioavailability

  8. Chitosan-tripolyphosphate nanoparticles: Optimization of formulation parameters for improving process yield at a novel pH using artificial neural networks.

    Science.gov (United States)

    Hashad, Rania A; Ishak, Rania A H; Fahmy, Sherif; Mansour, Samar; Geneidi, Ahmed S

    2016-05-01

    At a novel pH value of the polymeric solution (6.2), variable chitosan (Cs) and sodium tripolyphosphate (TPP) concentrations and mass ratios were optimized to improve the process yield without undesirable particle flocculation. Prepared formulations were characterized in terms of particle size (PS), zeta potential (ZP) and percentage yield (% yield). Artificial neural networks (ANN) were built up and used to identify the parameters that control nanoparticle (NP) size and yield, in addition to being tested for their ability to predict these two experimental outputs. Using these networks, it was found that TPP concentration has the greatest effect on PS and% yield. The most optimum formulation was characterized by a notable process yield reaching 91.5%, a mean hydrodynamic PS 227 nm, ZP+24.13 mv and spherical compact morphology. Successful Cs-TPP interaction in NP formation was confirmed by both Fourier transform-infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). This study demonstrated the ability of ANN to predict not only PS of the formed particles but also NP% yield. This may have a great impact on Cs-TPP NPs preparation and can be used to customize the required target formulations. PMID:26783636

  9. Drugs Approved for Pancreatic Cancer

    Science.gov (United States)

    ... Ask about Your Treatment Research Drugs Approved for Pancreatic Cancer This page lists cancer drugs approved by the ... that are not listed here. Drugs Approved for Pancreatic Cancer Abraxane (Paclitaxel Albumin-stabilized Nanoparticle Formulation) Afinitor (Everolimus) ...

  10. A to Z List of Cancer Drugs

    Science.gov (United States)

    ... Y Z Get email updates from NCI on cancer health information, news, and other topics Get email updates from NCI A Abiraterone Acetate Abitrexate (Methotrexate) Abraxane (Paclitaxel Albumin-stabilized Nanoparticle Formulation) ABVD ABVE ...

  11. Panthenol-stabilized cerium dioxide nanoparticles for cosmeceutic formulations against ROS-induced and UV-induced damage.

    Science.gov (United States)

    Zholobak, N M; Shcherbakov, A B; Bogorad-Kobelska, A S; Ivanova, O S; Baranchikov, A Ye; Spivak, N Ya; Ivanov, V K

    2014-01-01

    A method of panthenol-stabilized cerium dioxide nanoparticles synthesis was developed and their effect on the survival rate of human epidermoid cancer cells HEp-2 and diploid epithelial swine testicular cell line (ST-cells) under oxidative stress conditions induced by hydrogen peroxide introduction and UV irradiation was studied. The results obtained indicate that the use of panthenol as a stabilizer supposedly provides a substantial increase in the efficiency of protection. The degree of protection is determined by panthenol-to-ceria molar ratio. The combination of panthenol and nano-ceria protects biological objects under study from reactive oxygen species (ROS) and UV-irradiation more effectively than individual panthenol or ceria. The protective action of panthenol-stabilized cerium dioxide nanoparticles depends strongly on their composition and the means of their application. PMID:24300997

  12. Formulation and in vitro characterization of poly(dl-lactide-co-glycolide)/Eudragit RLPO or RS30D nanoparticles as an oral carrier of levofloxacin hemihydrate.

    Science.gov (United States)

    Hasan, Azza A; Sabry, Shereen A; Abdallah, Marwa H; El-Damasy, Dalia A

    2016-09-01

    The main objective of this study was to design positively charged Levofloxacin Hemihydrate (Levo-h)-loaded nanoparticles with improved entrapment efficiency and antibacterial activity. PLGA alone or in combinations with Eudragit® RLPO or RS30D with or without positively charged inducing agent; 1,2-dioleoyl-3-trimethylammonium-propane, chloride salt (DOTAP); were used for preparation of nanoparticles. Blending between PLGA and Eudragit® RLPO or RS30D with inclusion of DOTAP caused a marked increase in entrapment efficiency and switched zeta potential from negative to positive. Nanoparticle formulations; NR3 (Levo-h:PLGA:Eudragit® RLPO; 1:1:1 w/w with DOTAP) and NS3 (Levo-h:PLGA:Eudragit® RS30D; 1:1:1 w/w with DOTAP) that possess high positive zeta potential (59.3 ± 7.5 and 55.1 ± 8.2 mV, respectively) and Efficient Levo-h entrapment (89.54 ± 1.5 and 77.65 ± 1.8%, respectively) were selected for further examinations; in vitro release, physical stability and microbiological study. NR3 and NS3 showed significant sustained release of Levo-h. NR3 and NS3 exhibited good stability after storage at room temperature. Microbiological assay showed strengthened antibacterial activity of NR3 against both types of gram-negative bacteria (E. coli, Ps. aeruginosa) and of NS3 against Ps. aeruginosa compared to free Levo-h solution. NR3 and NS3 appear to be promising oral delivery system for Levo-h. PMID:25915180

  13. In vitro evaluation of Aurora kinase inhibitor—VX680—in formulation of PLA-TPGS nanoparticles

    Science.gov (United States)

    Thuy Duong Le, Thi; Thu Ha, Phuong; Hai Yen Tran, Thi; Nguyen, Dac Tu; Nguyen, Hoai Nam; Khanh Bui, Van; Nhung Hoang, My

    2016-06-01

    Polymeric nanoparticles prepared from poly(lactide)-tocopheryl polyethylene glycol succinate (PLA-TPGS) were used as potential drug carries with many advantages to overcome the disadvantages of insoluble anticancer drugs and enhance blood circulation time and tissues. VX680 is an Aurora kinase inhibitor and is also the foremost Aurora kinase inhibitor to be studied in clinical trials. In this study, we aimed to investigate whether VX680-loaded PLA-TPGS nanoparticles (VX680-NPs) are able to effectively increase the toxicity of chemotherapy. Accordingly, we first synthesized VX680-loaded nanoparticles and NP characterizations of morphology, mean size, zeta potential, and encapsulation efficiency were spherical shape, 63 nm, ‑30 mV and 76%, respectively. Then, we investigated the effects on HeLa cells. The cell cytotoxicity was evaluated by the xCELLigence real-time cell analyzer allowing measurement of changes in electrical impedance on the surface of the E-plate. Analysis of nucleus morphology and level of histone H3 phosphorylation was observed by confocal fluorescence scanning microscopy. Cell cycle distribution and apoptosis were analyzed by flow cytometry. Our results showed that VX680-NPs reduced cell viability with IC50 value lower 3.4 times compared to free VX680. Cell proliferation was inhibited by VX680-NPs accompanied by other effects such as high abnormal changes of nucleus, a decrease of phospho-histone H3 at Ser10 level, an increase of polyploid cells and resulted in higher apoptotic cells. These results demonstrated that VX680-NPs had more cytotoxicity than as treated with VX680 alone. Thus, VX680-NPs may be considered as promising drug delivery system for cancer treatment.

  14. 冬凌草甲素纳米制剂的研究和应用%Research and Application in Nanoparticle Formulation of Oridonin

    Institute of Scientific and Technical Information of China (English)

    陈美婉; 陈锐娥; 李颖博; 谭雯; 王一涛

    2011-01-01

    Oridonin, named isodonal and rubescensin A, can be achieved by alcohol extraction,extraction, chromatography and crystallization from the herba of Rabdosia rubescens. Oridonin is able to kill and inhibit different types of cancer cells, such as leukemia, breast cancer, melanoma and so on. Therefore, it's widely used as anti-humor, antibacterial, anti-inflammatory and antinociceptive agent nowadays. However, due to its poor water-soluble and extremely bitter taste, the clinical application of oridonin is limited. Nanoparticle formulation, a new kind of drug delivery system, could improve its water-soluble and bioavailability effectively.Nanoparticles, liposomes, microemulsion, polymer micelles and nanosuspensions of oridonin have been developed during these years. This paper mainly reviews the latest research and application in nanoparticle formulation of oridonin. It will provide foundation for further research and development of new formulation for oridonin.%冬凌草甲素(oridonin),别名冬凌草素、延命草宁,是唇形科香茶菜属植物碎米亚桠Rabdosia rubescens的全草,由醉提、萃取、层析、结晶等工序完成.冬凌草甲素对白血病、乳腺癌、黑色素瘤等多种肿瘤,具有显著的抑制或杀伤作用,主要用于抗肿瘤,抗菌,清热解毒,消炎止痛和健胃活血等方面的治疗.但因其微溶于水,且味道极苦,很大程度上限制了其在临床上的应用.纳米制剂作为一种新型的药物传递系统,近年来已有学者开展了冬凌草甲素纳米制剂的研究探索,其中包括冬凌草甲素的β-环糊精包合物、纳米粒、脂质体、微乳聚合物胶束和纳米混悬剂等.研究发现,纳米制剂能够有效地改善冬凌草素水溶性,提高其生物利用度,具有开发价值和广阔的应用前景.该文对当前冬凌草甲素纳米制剂的研究和应用状况进行了综述,为冬凌草甲素新制剂的研究开发提供依据.

  15. Synthesis and tribological studies of nanoparticle additives for pyrolysis bio-oil formulated as a diesel fuel

    International Nuclear Information System (INIS)

    The tribological behaviour of pyrolysis bio-oil with a synthesized nano-Lanthanum oxide (La2O3) additive was evaluated using a point contact four ball tribometer under different frictional conditions. Results were compared against a micro (μ)-La2O3 additive and an un-additised bio-oil as a control. The results show that nano-La2O3 impregnated bio-oil had better tribological properties than the control groups. Under the operating loads, the optimum nanoparticle concentration within the bio-oil was investigated. At these levels, the combined action of adsorbed bio-oil films on the worn surfaces and the bearing effects of the nano-La2O3 minimized friction and wear. The tribo-mechanisms were ascribed to adhesive wear as a result of lubrication starvation under high loads, and abrasive wear at high rotational speeds as a result of combined deformation and aggregation of the nano-La2O3 particles. - Highlights: • The tribological properties of pyrolysis bio-oil with (μ & n) La2O3 were assessed. • Nano-La2O3 was synthesized with diameters of approximately 20–1000 nm. • Bio-oil w. 1% nano-La2O3 was the optimum additive & concentration for tribological properties. • 1% nano-La2O3 reduced corrosive wear with stable lubrication film for test conditions. • Wear mechanisms were predominately adhesive for higher loads and abrasive for higher speeds

  16. Nanoparticle formulation enhanced protective immunity provoked by PYGPI8p-transamidase related protein (PyTAM) DNA vaccine in Plasmodium yoelii malaria model.

    Science.gov (United States)

    Cherif, Mahamoud Sama; Shuaibu, Mohammed Nasir; Kodama, Yukinobu; Kurosaki, Tomoaki; Helegbe, Gideon Kofi; Kikuchi, Mihoko; Ichinose, Akitoyo; Yanagi, Tetsuo; Sasaki, Hitoshi; Yui, Katsuyuki; Tien, Nguyen Huy; Karbwang, Juntra; Hirayama, Kenji

    2014-04-01

    We have previously reported the new formulation of polyethylimine (PEI) with gamma polyglutamic acid (γ-PGA) nanoparticle (NP) to have provided Plasmodium yoelii merozoite surface protein-1 (PyMSP-1) plasmid DNA vaccine with enhanced protective cellular and humoral immunity in the lethal mouse malaria model. PyGPI8p-transamidase-related protein (PyTAM) was selected as a possible candidate vaccine antigen by using DNA vaccination screening from 29 GPI anchor and signal sequence motif positive genes picked up using web-based bioinformatics tools; though the observed protection was not complete. Here, we observed augmented protective effect of PyTAM DNA vaccine by using PEI and γ-PGA complex as delivery system. NP-coated PyTAM plasmid DNA immunized mice showed a significant survival rate from lethal P. yoelii challenge infection compared with naked PyTAM plasmid or with NP-coated empty plasmid DNA group. Antigen-specific IgG1 and IgG2b subclass antibody levels, proportion of CD4 and CD8T cells producing IFN-γ in the splenocytes and IL-4, IFN-γ, IL-12 and TNF-α levels in the sera and in the supernatants from ex vivo splenocytes culture were all enhanced by the NP-coated PyTAM DNA vaccine. These data indicates that NP augments PyTAM protective immune response, and this enhancement was associated with increased DC activation and concomitant IL-12 production.

  17. Development of shampoo, soap and ointment formulated by green synthesised silver nanoparticles functionalised with antimicrobial plants oils in veterinary dermatology: treatment and prevention strategies.

    Science.gov (United States)

    Bansod, Sunita Dashrath; Bawaskar, Manisha Subrashrao; Gade, Aniket Krishnarao; Rai, Mahendra Kumar

    2015-08-01

    Many scientists have focused their research on the role of nanotechnology for the control of human pathogens, but there are also many topical pathogens present in animals, which infect animals and transfer to humans. Topical therapy is extremely important for the management of dermatological condition in animals. Therefore, the present study aims to evaluate the efficacy of biogenic silver nanoparticles (AgNPs) in combination with herbal oils against animal skin infections which may be responsible for causing infections in human beings. Here, the authors synthesised and characterised the AgNPs from Azadirachta indica. The oils were extracted from medicinal plants including Cymbopogon citratus, Cymbopogon martini, Eucalyptus globules, A. indica and Ocimum sanctum and the antifungal and antibacterial activity of plant oils along with AgNPs were evaluated. An excision wound model was used for the study of wound healing activity in rabbits. AgNPs functionalised oil has demonstrated remarkable antimicrobial activity against pathogens present on the skin of animals. The nano-functionalised antimicrobial oils were used in the formulation of shampoo, soap and ointment for veterinary dermatology. Antimicrobial products of plant origin with AgNPs are valuable, safe and have a specific role in controlling diseases. The authors believe that this approach will be a good alternative therapy to solve the continuous antibiotic resistance developed by many bacterial pathogens and will be utilised in various animal contacting areas in medicine. PMID:26224344

  18. Development of shampoo, soap and ointment formulated by green synthesised silver nanoparticles functionalised with antimicrobial plants oils in veterinary dermatology: treatment and prevention strategies.

    Science.gov (United States)

    Bansod, Sunita Dashrath; Bawaskar, Manisha Subrashrao; Gade, Aniket Krishnarao; Rai, Mahendra Kumar

    2015-08-01

    Many scientists have focused their research on the role of nanotechnology for the control of human pathogens, but there are also many topical pathogens present in animals, which infect animals and transfer to humans. Topical therapy is extremely important for the management of dermatological condition in animals. Therefore, the present study aims to evaluate the efficacy of biogenic silver nanoparticles (AgNPs) in combination with herbal oils against animal skin infections which may be responsible for causing infections in human beings. Here, the authors synthesised and characterised the AgNPs from Azadirachta indica. The oils were extracted from medicinal plants including Cymbopogon citratus, Cymbopogon martini, Eucalyptus globules, A. indica and Ocimum sanctum and the antifungal and antibacterial activity of plant oils along with AgNPs were evaluated. An excision wound model was used for the study of wound healing activity in rabbits. AgNPs functionalised oil has demonstrated remarkable antimicrobial activity against pathogens present on the skin of animals. The nano-functionalised antimicrobial oils were used in the formulation of shampoo, soap and ointment for veterinary dermatology. Antimicrobial products of plant origin with AgNPs are valuable, safe and have a specific role in controlling diseases. The authors believe that this approach will be a good alternative therapy to solve the continuous antibiotic resistance developed by many bacterial pathogens and will be utilised in various animal contacting areas in medicine.

  19. Pharmacokinetics, tissue distribution, and metabolites of a polyvinylpyrrolidone-coated norcantharidin chitosan nanoparticle formulation in rats and mice, using LC-MS/MS

    Directory of Open Access Journals (Sweden)

    Ding XY

    2012-04-01

    Full Text Available Xin-Yuan Ding1, Cheng-Jiao Hong2, Yang Liu1, Zong-Lin Gu1, Kong-Lang Xing1, Ai-Jun Zhu1, Wei-Liang Chen1, Lin-Seng Shi1, Xue-Nong Zhang1, Qiang Zhang31Department of Pharmaceutics, College of Pharmaceutical science, Soochow University, Suzhou, 2Jiang Su Provincial Key Laboratory of Radiation Medicine and Protection, Suzhou, 3Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing, People’s Republic of ChinaAbstract: A novel formulation containing polyvinylpyrrolidone (PVP K30-coated norcantharidin (NCTD chitosan nanoparticles (PVP–NCTD–NPs was prepared by ionic gelation between chitosan and sodium tripolyphosphate. The average particle size of the PVP–NCTD–NPs produced was 140.03 ± 6.23 nm; entrapment efficiency was 56.33% ± 1.41%; and drug-loading efficiency was 8.38% ± 0.56%. The surface morphology of NCTD nanoparticles (NPs coated with PVP K30 was characterized using various analytical techniques, including X-ray diffraction and atomic force microscopy. NCTD and its metabolites were analyzed using a sensitive and specific liquid chromatography-tandem mass spectrometry method with samples from mice and rats. The results indicated the importance of the PVP coating in controlling the shape and improving the entrapment efficiency of the NPs. Pharmacokinetic profiles of the NCTD group and PVP–NCTD–NP group, after oral and intravenous administration in rats, revealed that relative bioavailabilities were 173.3% and 325.5%, respectively. The elimination half-life increased, and there was an obvious decrease in clearance. The tissue distribution of NCTD in mice after the intravenous administration of both formulations was investigated. The drug was not quantifiable at 6 hours in all tissues except for the liver and kidneys. The distribution of the drug in the liver and bile was notably improved in the PVP–NCTD–NP group. The metabolites and excretion properties of NCTD were investigated by analyzing

  20. Nano composite system based on coumarin derivative–titanium dioxide nanoparticles and ionic liquid: Determination of levodopa and carbidopa in human serum and pharmaceutical formulations

    Energy Technology Data Exchange (ETDEWEB)

    Mazloum-Ardakani, Mohammad, E-mail: mazloum@yazd.ac.ir; Khoshroo, Alireza

    2013-10-10

    Graphical abstract: -- Highlights: •Nanostructured electrochemical sensor based on TiO{sub 2} and ionic liquid was used for the determination of levodopa in the presence of carbidopa. •Selectivity, reproducibility and low detection limit make the nanostructured modified electrode very useful for accurate determination of levodopa. •This sensor was applied in determination of levodopa and carbidopa in pharmaceutical formulations, blood serum and urine. -- Abstract: The combination of coumarin derivative (7-(1,3-dithiolan-2-yl)-9,10-dihydroxy-6H-benzofuro[3,2-c]chromen-6-on), (DC)–titanium dioxide nanoparticles (TiO{sub 2}) and ionic liquid (IL) yields nanostructured electrochemical sensor, formed a novel kind of structurally uniform and electrocatalytic activity material. This new ionic liquid–TiO{sub 2} nanoparticles modified carbon paste electrode (IL–CTP) due to its enhanced conductivity presented very large current response from electroactive substrates. The modified electrode was characterized by different methods including a scanning electron microscope (SEM), electrochemical impedance spectroscopy (EIS) and voltammetry. A pair of well-defined quasi reversible redox peaks of coumarin derivative was obtained at the modified carbon paste electrode (DC/IL–CTP) by direct electron transfer between the coumarin derivative and the CP electrode. Dramatically enhanced electrocatalytic activity was exemplified at the DC/IL–CTP electrode, as an electrochemical sensor to study the electro oxidation of levodopa (LD) and carbidopa (CD). Based on differential pulse voltammetry (DPV), the oxidation of LD and CD exhibited the dynamic range between 0.10– 900.0 μM and 20.0–900.0 μM respectively, and the detection limit (3σ) for LD and CD were 41 nM and 0.38 μM, respectively. DPV was used for simultaneous determination of LD and CD at the DC/IL–CTP electrode, and quantitation of LD and CD in some real samples (such as tablets of Parkin-C Fort and Madopar

  1. nanoparticles

    Science.gov (United States)

    Andreu-Cabedo, Patricia; Mondragon, Rosa; Hernandez, Leonor; Martinez-Cuenca, Raul; Cabedo, Luis; Julia, J. Enrique

    2014-10-01

    Thermal energy storage (TES) is extremely important in concentrated solar power (CSP) plants since it represents the main difference and advantage of CSP plants with respect to other renewable energy sources such as wind, photovoltaic, etc. CSP represents a low-carbon emission renewable source of energy, and TES allows CSP plants to have energy availability and dispatchability using available industrial technologies. Molten salts are used in CSP plants as a TES material because of their high operational temperature and stability of up to 500°C. Their main drawbacks are their relative poor thermal properties and energy storage density. A simple cost-effective way to improve thermal properties of fluids is to dope them with nanoparticles, thus obtaining the so-called salt-based nanofluids. In this work, solar salt used in CSP plants (60% NaNO3 + 40% KNO3) was doped with silica nanoparticles at different solid mass concentrations (from 0.5% to 2%). Specific heat was measured by means of differential scanning calorimetry (DSC). A maximum increase of 25.03% was found at an optimal concentration of 1 wt.% of nanoparticles. The size distribution of nanoparticle clusters present in the salt at each concentration was evaluated by means of scanning electron microscopy (SEM) and image processing, as well as by means of dynamic light scattering (DLS). The cluster size and the specific surface available depended on the solid content, and a relationship between the specific heat increment and the available particle surface area was obtained. It was proved that the mechanism involved in the specific heat increment is based on a surface phenomenon. Stability of samples was tested for several thermal cycles and thermogravimetric analysis at high temperature was carried out, the samples being stable.

  2. A novel bottom-up process to produce thymopentin nanoparticles and their formulation optimization%胸腺五肽纳米粒的制备及其处方优化

    Institute of Scientific and Technical Information of China (English)

    单紫筠; 谭银合; 杨志文; 余思琴; 陈宝; 吴传斌

    2012-01-01

    目的 建立制备胸腺五肽纳米粒的方法并对其处方进行优化,为制备符合要求的压力定量吸入气雾剂奠定基础.方法 将胸腺五肽、卵磷脂、乳糖溶于叔丁醇-水的混合溶剂中,冷冻干燥,将冻干产物用异丙醇混悬,离心除去多余的卵磷脂以得到纯药物纳米粒.采用星点设计-效应面法对其中水、卵磷脂、胸腺五肽的用量进行优化,因胸腺五肽的含量受此处方影响不显著,所以只选取纳米粒的粒径、粒径分布为结果考察指标.结果 最优处方:水∶叔丁醇、卵磷脂∶叔丁醇、胸腺五肽∶水的比例分别为0.5(mL∶mL) 、213.5(mg∶mL) 、17.0(mg∶mL),即水的用量1.5 mL、卵磷脂的用量640.57 mg、胸腺五肽的用量25.57 mg、叔丁醇的用量3.0 mL.按此处方制备的纳米粒粒径在150 nm左右,多分散系数为0.1以下,含量均能保持在98%以上.结论 采用该方法制备胸腺五肽纳米粒,质量佳,重现性好,方法简便,具有良好的应用前景.%Objective A noveJ bottom-up process was developed to produce nanoparticles containing thymopentin and the formulation was optimized to produce desirable nanoparticles for development of pressed metered dose inhaler ( pMDI) of thymopentin( TP-5 ). Methods A solution of TP-5 , lecithin and lactose in tert-butyl alcohol( TBA )/ water co-solvent system was freeze-dried to generate nanoparticles and residual lecithin was washed off in lyophilizate through eentrifugation. Formulation parameters such as lecithin content in organic phase,water content in TB A/water co-solvent, and TP-5 content in water were optimized with the central composite design-response surface methodology. As the retained content of TP-5 in nanoparticles did not significantly vary with the above formulation parameters, only particle size and size distribution of TP-5 nanoparticles was taken as response parameters. Results The ratios of water to TBA, lecithin to TBA and TP-5 to water in the

  3. Novel Formulations for Antimicrobial Peptides

    Directory of Open Access Journals (Sweden)

    Ana Maria Carmona-Ribeiro

    2014-10-01

    Full Text Available Peptides in general hold much promise as a major ingredient in novel supramolecular assemblies. They may become essential in vaccine design, antimicrobial chemotherapy, cancer immunotherapy, food preservation, organs transplants, design of novel materials for dentistry, formulations against diabetes and other important strategical applications. This review discusses how novel formulations may improve the therapeutic index of antimicrobial peptides by protecting their activity and improving their bioavailability. The diversity of novel formulations using lipids, liposomes, nanoparticles, polymers, micelles, etc., within the limits of nanotechnology may also provide novel applications going beyond antimicrobial chemotherapy.

  4. In vivo evaluation of a conjugated poly(lactide-ethylene glycol nanoparticle depot formulation for prolonged insulin delivery in the diabetic rabbit model

    Directory of Open Access Journals (Sweden)

    Tomar L

    2013-02-01

    Full Text Available Lomas Tomar,1,2 Charu Tyagi,1,3 Manoj Kumar,2 Pradeep Kumar,1 Harpal Singh,2 Yahya E Choonara,1 Viness Pillay11University of the Witwatersrand, Faculty of Health Sciences, Department of Pharmacy and Pharmacology, Johannesburg, Gauteng, South Africa; 2Centre for Biomedical Engineering, Indian Institute of Technology, Delhi, India; 3VSPG College, Chaudhary Charan Singh University, Meerut, IndiaAbstract: Poly(ethylene glycol (PEG and polylactic acid (PLA-based copolymeric nanoparticles were synthesized and investigated as a carrier for prolonged delivery of insulin via the parenteral route. Insulin loading was simultaneously achieved with particle synthesis using a double emulsion solvent evaporation technique, and the effect of varied PEG chain lengths on particle size and insulin loading efficiency was determined. The synthesized copolymer and nanoparticles were analyzed by standard polymer characterization techniques of gel permeation chromatography, dynamic light scattering, nuclear magnetic resonance, and transmission electron microscopy. In vitro insulin release studies performed under simulated conditions provided a near zero-order release pattern up to 10 days. In vivo animal studies were undertaken with varied insulin loads of nanoparticles administered subcutaneously to fed diabetic rabbits and, of all doses administered, nanoparticles containing 50 IU of insulin load per kg body weight controlled the blood glucose level within the physiologically normal range of 90–140 mg/dL, and had a prolonged effect for more than 7 days. Histopathological evaluation of tissue samples from the site of injection showed no signs of inflammation or aggregation, and established the nontoxic nature of the prepared copolymeric nanoparticles. Further, the reaction profiles for PLA-COOH and NH2-PEGDA-NH2 were elucidated using molecular mechanics energy relationships in vacuum and in a solvated system by exploring the spatial disposition of various

  5. Lymphatic Biodistribution of Polylactide Nanoparticles

    OpenAIRE

    Chaney, Eric J.; Tang, Li; Tong, Rong; Cheng, Jianjun; Boppart, Stephen A.

    2010-01-01

    Tumor metastases occur through both the cardiovascular and lymphatic circulations. However, the majority of nanoparticle biodistribution studies have been focused on the cardiovascular circulation. In this study, we report the formulation of Cy5-labeled polylactide (Cy5-PLA) nanoparticles with controlled size and surface features and the subsequent evaluation of their lymphatic biodistribution. Cy5-PLA nanoparticles were formulated through Cy5/(BDI)ZnN(TMS)2-mediated [(BDI) = 2-((2,6-diisopro...

  6. Preclinical Evaluation of Genexol-PM, a Nanoparticle Formulation of Paclitaxel, as a Novel Radiosensitizer for the Treatment of Non-Small Cell Lung Cancer

    Energy Technology Data Exchange (ETDEWEB)

    Werner, Michael E.; Cummings, Natalie D.; Sethi, Manish; Wang, Edina C.; Sukumar, Rohit [Laboratory of Nano- and Translational Medicine, Department of Radiation Oncology, Lineberger Comprehensive Cancer Center, University of North Carolina-Chapel Hill, Chapel Hill, North Carolina (United States); Carolina Center for Cancer Nanotechnology Excellence, University of North Carolina-Chapel Hill, Chapel Hill, North Carolina (United States); Moore, Dominic T. [Division of Biostatistics and Data Management, Lineberger Comprehensive Cancer Center, University of North Carolina-Chapel Hill, Chapel Hill, North Carolina (United States); Wang, Andrew Z., E-mail: zawang@med.unc.edu [Laboratory of Nano- and Translational Medicine, Department of Radiation Oncology, Lineberger Comprehensive Cancer Center, University of North Carolina-Chapel Hill, Chapel Hill, North Carolina (United States); Carolina Center for Cancer Nanotechnology Excellence, University of North Carolina-Chapel Hill, Chapel Hill, North Carolina (United States)

    2013-07-01

    Purpose: A key research objective in radiation oncology is to identify agents that can improve chemoradiation therapy. Nanoparticle (NP) chemotherapeutics possess several properties, such as preferential accumulation in tumors, that are uniquely suited for chemoradiation therapy. To facilitate the clinical translation of NP chemotherapeutics in chemoradiation therapy, we conducted preclinical evaluation of Genexol-PM, the only clinically approved NP chemotherapeutic with a controlled drug release profile, as a radiosensitizer using non-small cell lung cancer (NSCLC) as a model disease. Methods and Materials: The physical characteristics and drug release profile of Genexol-PM were characterized. Genexol-PM's efficacy as a radiosensitizer was evaluated in vitro using NSCLC cell lines and in vivo using mouse xenograft models of NSCLC. Paclitaxel dose to normal lung and liver after Genexol-PM administration were quantified and compared with that after Taxol administration. Results: Genexol-PM has a size of 23.91 ± 0.41 nm and surface charge of −8.1 ± 3.1 mV. It releases paclitaxel in a controlled release profile. In vitro evaluation of Genexol-PM as a radiosensitizer showed it is an effective radiosensitizer and is more effective than Taxol, its small molecule counterpart, at the half maximal inhibitory concentration. In vivo study of Genexol-PM as a radiosensitizer demonstrated that it is more effective as a radiosensitizer than Taxol. We also found that Genexol-PM leads to lower paclitaxel exposure to normal lung tissue than Taxol at 6 hours postadministration. Conclusions: We have demonstrated that Genexol-PM is more effective than Taxol as a radiosensitizer in the preclinical setting and holds high potential for clinical translation. Our data support the clinical evaluation of Genexol-PM in chemoradiation therapy for NSCLC.

  7. Formulation and Optimization of Polymeric Nanoparticles for Intranasal Delivery of Lorazepam Using Box-Behnken Design: In Vitro and In Vivo Evaluation

    Directory of Open Access Journals (Sweden)

    Deepak Sharma

    2014-01-01

    Full Text Available The aim of the present study was to optimize lorazepam loaded PLGA nanoparticles (Lzp-PLGA-NPs by investigating the effect of process variables on the response using Box-Behnken design. Effect of four independent factors, that is, polymer, surfactant, drug, and aqueous/organic ratio, was studied on two dependent responses, that is, z-average and % drug entrapment. Lzp-PLGA-NPs were successfully developed by nanoprecipitation method using PLGA as polymer, poloxamer as surfactant and acetone as organic phase. NPs were characterized for particle size, zeta potential, % drug entrapment, drug release behavior, TEM, and cell viability. Lzp-PLGA-NPs were characterized for drug polymer interaction using FTIR. The developed NPs showed nearly spherical shape with z-average 167–318 d·nm, PDI below 0.441, and −18.4 mV zeta potential with maximum % drug entrapment of 90.1%. In vitro drug release behavior followed Korsmeyer-Peppas model and showed initial burst release of 21.7±1.3% with prolonged drug release of 69.5±0.8% from optimized NPs up to 24 h. In vitro drug release data was found in agreement with ex vivo permeation data through sheep nasal mucosa. In vitro cell viability study on Vero cell line confirmed the safety of optimized NPs. Optimized Lzp-PLGA-NPs were radiolabelled with Technitium-99m for scintigraphy imaging and biodistribution studies in Sprague-Dawley rats to establish nose-to-brain pathway.

  8. Box-Behnken响应面法优化吲哚美辛固体脂质纳米粒处方%Formulation Optimization of Indomethacin-loading Solid Lipid Nanoparticles by Box-Behnken Response Surface Methodology

    Institute of Scientific and Technical Information of China (English)

    陈凯; 李收; 金凯; 赵晶; 郝吉福

    2016-01-01

    目的:优化吲哚美辛固体脂质纳米粒处方。方法:以吲哚美辛为模型药物、山嵛酸甘油酯为油相、泊洛沙姆188和聚乙二醇-12-羟基硬脂酸酯为乳化剂,以浊度、包封率、载药量为指标,采用Box-Behnken响应面法优化处方中油相用量、乳化剂-油相比例、药物-油相比例。采用扫描电镜、差示扫描热分析(DSC)表征固体脂质纳米粒的理化性质。结果:最优处方的油相用量为0.91%,乳化剂-油相比例为1∶1,药物-油相比例为1∶5;所制吲哚美辛固体脂质纳米粒的浊度为1025~1030 NTU,包封率为98.94%~99.08%,载药量为2.43%~2.46%,粒径为181.5~182.3 nm,多分散性指数(PDI)为0.340~0.341(n=3);DSC结果显示吲哚美辛不是以结晶状态存在于固体脂质纳米粒中。结论:成功筛选出最优处方,制得吲哚美辛固体脂质纳米粒。%OBJECTIVE:To optimize the formulation of indomethacin-loading solid lipid nanoparticle(SLN). METHODS:Us-ing indomethacin as model drug,glyceryl behenate as oil phase,poloxamer 188 and polyethylene glycol-12-hydroxystearic acid as emulsifier,with turbidity,entrapment efficiency and drug loading amount as index,Box-Behnken response surface methodology was used to optimize the amount of oil phase,emulsifier-oil phase ratio,drug-oil phase ratio. The physicochemical properties of SLNs were characterized by SEM and DSC. RESULTS:The optimal formulation was as follows as oil phase of 0.91%,emulsifier-oil ratio of 1∶1,drug-oil phase ratio of 1∶5. The turbidity,entrapment efficiency and drug loading amount of prepared nanoparticle were 1 025-1 030 NTU,98.94%-99.08%,2.43%-2.46%,respectively;particle size and polydispersity index(PDI)were 181.5-182.3 nm and 0.340-0.341(n=3). The results of DSC showed that indomethacin was not present in crystalline state dispersed into SLNs. CONCLUSIONS:The optimal formulation is screened successfully

  9. Formulation of Anti-miR-21 and 4-Hydroxytamoxifen Co-loaded Biodegradable Polymer Nanoparticles and Their Antiproliferative Effect on Breast Cancer Cells.

    Science.gov (United States)

    Devulapally, Rammohan; Sekar, Thillai V; Paulmurugan, Ramasamy

    2015-06-01

    Breast cancer is the second leading cause of cancer-related death in women. The majority of breast tumors are estrogen receptor-positive (ER+) and hormone-dependent. Neoadjuvant anti-estrogen therapy has been widely employed to reduce tumor mass prior to surgery. Tamoxifen is a broadly used anti-estrogen for early and advanced ER+ breast cancers in women and the most common hormone treatment for male breast cancer. 4-Hydroxytamoxifen (4-OHT) is an active metabolite of tamoxifen that functions as an estrogen receptor antagonist and displays higher affinity for estrogen receptors than that of tamoxifen and its other metabolites. MicroRNA-21 (miR-21) is a small noncoding RNA of 23 nucleotides that regulates several apoptotic and tumor suppressor genes and contributes to chemoresistance in numerous cancers, including breast cancer. The present study investigated the therapeutic potential of 4-OHT and anti-miR-21 coadministration in an attempt to combat tamoxifen resistance, a common problem often encountered in anti-estrogen therapy. A biodegradable poly(d,l-lactide-co-glycolide)-block-poly(ethylene glycol) (PLGA-b-PEG-COOH) copolymer was utilized as a carrier to codeliver 4-OHT and anti-miR-21 to ER+ breast cancer cells. 4-OHT and anti-miR-21 co-loaded PLGA-b-PEG nanoparticles (NPs) were developed using emulsion-diffusion evaporation (EDE) and water-in-oil-in-water (w/o/w) double emulsion methods. The EDE method was found to be best method for 4-OHT loading, and the w/o/w method proved to be more effective for coloading NPs with anti-miR-21 and 4-OHT. The optimal NPs, which were prepared using the double emulsion method, were evaluated for their antiproliferative and apoptotic effects against MCF7, ZR-75-1, and BT-474 human breast cancer cells as well as against 4T1 mouse mammary carcinoma cells. We demonstrated that PLGA-b-PEG NP encapsulation significantly extended 4-OHT's stability and biological activity compared to that of free 4-OHT. MTT assays indicated that

  10. Preparation of nanoscale pulmonary drug delivery formulations by spray drying

    DEFF Research Database (Denmark)

    Bohr, Adam; Ruge, Christian A; Beck-Broichsitter, Moritz

    2014-01-01

    of the lungs. The colloidal nature of nanoparticles provides important advantages to the formulation of drugs, which are normally difficult to administer due to poor stability or uptake, partly because nanoparticles protect the drug from the physiological milieu, facilitate transport across biological barriers......Advances in preparation technologies for nanomedicines have provided novel formulations for pulmonary drug delivery. Application of drugs via the lungs can be considered as one of the most attractive implementations of nanoparticles for therapeutic use due to the unique anatomy and physiology...... and can offer controlled drug release. There are numerous methods for producing therapeutic nanoparticles, each with their own advantages and suitable application. Liquid atomization techniques such as spray drying can produce nanoparticle formulations in a dry powder form suitable for pulmonary...

  11. Crystallization Formulation Lab

    Data.gov (United States)

    Federal Laboratory Consortium — The Crystallization Formulation Lab fills a critical need in the process development and optimization of current and new explosives and energetic formulations. The...

  12. Nano-formulations of drugs: Recent developments, impact and challenges.

    Science.gov (United States)

    Jeevanandam, Jaison; Chan, Yen San; Danquah, Michael K

    2016-01-01

    Nano-formulations of medicinal drugs have attracted the interest of many researchers for drug delivery applications. These nano-formulations enhance the properties of conventional drugs and are specific to the targeted delivery site. Dendrimers, polymeric nanoparticles, liposomes, nano-emulsions and micelles are some of the nano-formulations that are gaining prominence in pharmaceutical industry for enhanced drug formulation. Wide varieties of synthesis methods are available for the preparation of nano-formulations to deliver drugs in biological system. The choice of synthesis methods depend on the size and shape of particulate formulation, biochemical properties of drug, and the targeted site. This article discusses recent developments in nano-formulation and the progressive impact on pharmaceutical research and industries. Additionally, process challenges relating to consistent generation of nano-formulations for drug delivery are discussed.

  13. IT Supporting Strategy Formulation

    NARCIS (Netherlands)

    Achterbergh, J.M.I.M.

    2005-01-01

    This overview approaches information and communication technology (ICT) for competitive intelligence from the perspective of strategy formulation. It provides an ICT architecture for supporting the knowledge processes producing relevant knowledge for strategy formulation. To determine what this arch

  14. IT Supporting Strategy Formulation

    OpenAIRE

    Achterbergh, J.M.I.M.

    2005-01-01

    This overview approaches information and communication technology (ICT) for competitive intelligence from the perspective of strategy formulation. It provides an ICT architecture for supporting the knowledge processes producing relevant knowledge for strategy formulation. To determine what this architecture looks like, we first examine the process of strategy formulation and determine the knowledge required in the process of strategy formulation. To this purpose, we use Beer’s viable system m...

  15. Formulation of Nematodes.

    Science.gov (United States)

    Peters, Arne

    2016-01-01

    The enduring stages of entomopathogenic nematodes of the genera Steinernema and Heterorhabditis are infective juveniles, which require a high humidity and sufficient ventilation for survival. Formulations must account for these requirements. Nematodes may be formulated inside the insects in which they reproduced or they need to be cleaned and mixed with a suitable binder to maintain humidity but allowing for gas exchange. Another method for formulation is the encapsulation in beads of Ca-alginate. Generic procedures for these formulation techniques are described. PMID:27565496

  16. Supercooled smectic nanoparticles

    DEFF Research Database (Denmark)

    Kuntsche, Judith; Koch, Michel H J; Fahr, Alfred;

    2009-01-01

    Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters......, laser diffraction combined with polarizing intensity differential scattering, DSC and SAXS. The morphology of selected formulations was studied by freeze-fracture electron microscopy. All smectic nanoparticles with a mixed cholesterol ester matrix were stable against recrystallization when stored...... at room temperature. Nanoparticles with a pure CN and mixed CM/CN matrix with a high fraction of CN (60% of the whole lipid matrix) could even be stored at 4 degrees C for at least 18 months without any recrystallization. As smectic nanoparticles are studied especially with regard to parenteral...

  17. Formulations in first encounters

    NARCIS (Netherlands)

    A. Hak (Tony); F. de Boer (Fijgje)

    1994-01-01

    markdownabstractThe paper describes and compares the use and function of the formulation--decision pair in three types of diagnostic interviewing. The investigatory type of interviewing, which typically occurs in the medical interview, is characterized by the absence of formulations. In the explora

  18. Audits of radiopharmaceutical formulations

    International Nuclear Information System (INIS)

    A procedure for auditing radiopharmaceutical formulations is described. To meet FDA guidelines regarding the quality of radiopharmaceuticals, institutional radioactive drug research committees perform audits when such drugs are formulated away from an institutional pharmacy. All principal investigators who formulate drugs outside institutional pharmacies must pass these audits before they can obtain a radiopharmaceutical investigation permit. The audit team meets with the individual who performs the formulation at the site of drug preparation to verify that drug formulations meet identity, strength, quality, and purity standards; are uniform and reproducible; and are sterile and pyrogen free. This team must contain an expert knowledgeable in the preparation of radioactive drugs; a radiopharmacist is the most qualified person for this role. Problems that have been identified by audits include lack of sterility and apyrogenicity testing, formulations that are open to the laboratory environment, failure to use pharmaceutical-grade chemicals, inadequate quality control methods or records, inadequate training of the person preparing the drug, and improper unit dose preparation. Investigational radiopharmaceutical formulations, including nonradiolabeled drugs, must be audited before they are administered to humans. A properly trained pharmacist should be a member of the audit team

  19. Audits of radiopharmaceutical formulations.

    Science.gov (United States)

    Castronovo, F P

    1992-03-01

    A procedure for auditing radiopharmaceutical formulations is described. To meet FDA guidelines regarding the quality of radiopharmaceuticals, institutional radioactive drug research committees perform audits when such drugs are formulated away from an institutional pharmacy. All principal investigators who formulate drugs outside institutional pharmacies must pass these audits before they can obtain a radiopharmaceutical investigation permit. The audit team meets with the individual who performs the formulation at the site of drug preparation to verify that drug formulations meet identity, strength, quality, and purity standards; are uniform and reproducible; and are sterile and pyrogen free. This team must contain an expert knowledgeable in the preparation of radioactive drugs; a radiopharmacist is the most qualified person for this role. Problems that have been identified by audits include lack of sterility and apyrogenicity testing, formulations that are open to the laboratory environment, failure to use pharmaceutical-grade chemicals, inadequate quality control methods or records, inadequate training of the person preparing the drug, and improper unit dose preparation. Investigational radiopharmaceutical formulations, including nonradiolabeled drugs, must be audited before they are administered to humans. A properly trained pharmacist should be a member of the audit team. PMID:1598931

  20. Applications of novel drug delivery system for herbal formulations.

    Science.gov (United States)

    Ajazuddin; Saraf, S

    2010-10-01

    Over the past several years, great advances have been made on development of novel drug delivery systems (NDDS) for plant actives and extracts. The variety of novel herbal formulations like polymeric nanoparticles, nanocapsules, liposomes, phytosomes, nanoemulsions, microsphere, transferosomes, and ethosomes has been reported using bioactive and plant extracts. The novel formulations are reported to have remarkable advantages over conventional formulations of plant actives and extracts which include enhancement of solubility, bioavailability, protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improved tissue macrophages distribution, sustained delivery, and protection from physical and chemical degradation. The present review highlights the current status of the development of novel herbal formulations and summarizes their method of preparation, type of active ingredients, size, entrapment efficiency, route of administration, biological activity and applications of novel formulations. PMID:20471457

  1. Assessment of strategy formulation

    DEFF Research Database (Denmark)

    Acur, Nuran; Englyst, Linda

    2006-01-01

    Purpose – Today, industrial firms need to cope with competitive challenges related to innovation, dynamic responses, knowledge sharing, etc. by means of effective and dynamic strategy formulation. In light of these challenges, the purpose of the paper is to present and evaluate an assessment tool...... for strategy formulation processes that ensures high quality in process and outcome. Design/methodology/approach – A literature review was conducted to identify success criteria for strategy formulation processes. Then, a simple questionnaire and assessment tool was developed and used to test the validity...... of the success criteria through face-to-face interviews with 46 managers, workshops involving 40 managers, and two in-depth case studies. The success criteria have been slightly modified due to the empirical results, to yield the assessment tool. Findings – The resulting assessment tool integrates three generic...

  2. Formulation of Automotive Lubricants

    Science.gov (United States)

    Atkinson, D.; Brown, A. J.; Jilbert, D.; Lamb, G.

    The formulation of lubricants for current light- and heavy-duty vehicles (passenger cars and trucks) and also motorcycles/small engines is described in terms of engine types and meeting European, US and Japanese emission control requirements. Trends in the formulation of lubricants are discussed and the importance of high and low 'SAPS' for future developments emphasised. Specification and evaluation of lubricant performance for light-vehicle gasoline and diesel, and also heavy-duty diesel engines are described. Emphasis is given to diesel engine cleanliness by soot and deposit control and the effect of emission controls on lubricant formulation. The lubricant requirements for motorcycle and small engines, primarily two-stroke cycle, and their specifications are described.

  3. Parenteral formulation of zopiclone

    Directory of Open Access Journals (Sweden)

    Swamy P

    2008-01-01

    Full Text Available The present study was undertaken with an intention to develop a stable and effective parenteral formulation, containing the drug zopiclone. Since zopiclone is a water insoluble drug, various methods such as co-solvency, pH control and hydrotrophy have been tried in order to enhance its solubility. When all these methods could not give adequate solubility enhancement of the drug, a hydrochloride salt was prepared, and it was found to be thermostable. Various batches of zopiclone hydrochloride injection formulation were prepared in order to assess the influence of light, atmospheric oxygen and antioxidant on the stability of the drug and the formulations were also subjected to accelerated stability testing in order to predict approximate shelf-life of the product.

  4. Responsive foams for nanoparticle delivery.

    Science.gov (United States)

    Tang, Christina; Xiao, Edward; Sinko, Patrick J; Szekely, Zoltan; Prud'homme, Robert K

    2015-09-01

    We have developed responsive foam systems for nanoparticle delivery. The foams are easy to make, stable at room temperature, and can be engineered to break in response to temperature or moisture. Temperature-responsive foams are based on the phase transition of long chain alcohols and could be produced using medical grade nitrous oxide as a propellant. These temperature-sensitive foams could be used for polyacrylic acid (PAA)-based nanoparticle delivery. We also discuss moisture-responsive foams made with soap pump dispensers. Polyethylene glycol (PEG)-based nanoparticles or PMMA latex nanoparticles were loaded into Tween 20 foams and the particle size was not affected by the foam formulation or foam break. Using biocompatible detergents, we anticipate this will be a versatile and simple approach to producing foams for nanoparticle delivery with many potential pharmaceutical and personal care applications. PMID:26091943

  5. Nanoparticles for the Treatment of Wounds.

    Science.gov (United States)

    Oyarzun-Ampuero, Felipe; Vidal, Alejandra; Concha, Miguel; Morales, Javier; Orellana, Sandra; Moreno-Villoslada, Ignacio

    2015-01-01

    The treatment of skin wounds represents an important research area due to the important physiological and aesthetic role of this tissue. During the last years, nanoparticles have emerged as important platforms to treat skin wounds. Silver, gold, and copper nanoparticles, as well as titanium and zinc oxide nanoparticles, have shown potential therapeutic effects on wound healing. Due to their specific characteristics, nanoparticles such as nanocapsules, polymersomes, solid lipid nanoparticles, and polymeric nanocomplexes are ideal vehicles to improve the effect of drugs (antibiotics, growth factors, etc.) aimed at wound healing. On the other hand, if active excipients are added during the formulation, such as hyaluronate or chitosan, the nanomedicine could significantly improve its potential. In addition, the inclusion of nanoparticles in different pharmaceutical materials may enhance the beneficial effects of the formulations, and allow achieving a better dose control. This paper aims at reviewing significant findings in the area of nanoparticles and wound treatment. Among the reviewed topics, we underline formulations comprising inorganic, polymeric, surfactant self-assembled, and lipid nanosystems. Among the drugs included in the nanoformulations, the paper refers to antibiotics, natural extracts, proteins, and growth factors, among others. Finally, the paper also addresses nanoparticles embedded in secondary vehicles (fibers, dressings, hydrogels, etc.) that could improve their application and/or upgrade the release profile of the active. PMID:26323420

  6. Cytotoxicity and ion release of alloy nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Hahn, Anne [Laser Zentrum Hannover e.V (Germany); Fuhlrott, Jutta; Loos, Anneke [Hannover Medical School, Biovertraeglichkeitslabor BioMedimplant (Germany); Barcikowski, Stephan, E-mail: stephan.barcikowski@uni-due.de [Laser Zentrum Hannover e.V (Germany)

    2012-01-15

    It is well-known that nanoparticles could cause toxic effects in cells. Alloy nanoparticles with yet unknown health risk may be released from cardiovascular implants made of Nickel-Titanium or Cobalt-Chromium due to abrasion or production failure. We show the bio-response of human primary endothelial and smooth muscle cells exposed to different concentrations of metal and alloy nanoparticles. Nanoparticles having primary particle sizes in the range of 5-250 nm were generated using laser ablation in three different solutions avoiding artificial chemical additives, and giving access to formulations containing nanoparticles only stabilized by biological ligands. Endothelial cells are found to be more sensitive to nanoparticle exposure than smooth muscle cells. Cobalt and Nickel nanoparticles caused the highest cytotoxicity. In contrast, Titanium, Nickel-Iron, and Nickel-Titanium nanoparticles had almost no influence on cells below a nanoparticle concentration of 10 {mu}M. Nanoparticles in cysteine dissolved almost completely, whereas less ions are released when nanoparticles were stabilized in water or citrate solution. Nanoparticles stabilized by cysteine caused less inhibitory effects on cells suggesting cysteine to form metal complexes with bioactive ions in media.

  7. Formulation and Stability Aspects of Nanosized Solid Drug Delivery Systems.

    Science.gov (United States)

    Szabo, Peter; Zelko, Romana

    2015-01-01

    Nano drug delivery systems are considered as useful means to remedy the problems of drugs of poor solubility, permeability and bioavailability, which became one of the most troublesome questions of the pharmaceutical industry. Different types of nanosized drug delivery systems have been developed and investigated for oral administration, providing auspicious solutions for drug development. In this paper nanosized drug delivery systems intended for oral administration are discussed based on the chemical nature of the carrier of drug molecules. Lipid nanoparticles comprising solid lipid nanoparticles, improved nanostructured lipid carriers and nanostructured silica- lipid hybrid particles have become popular in the formulation of lipophilic drugs of poor oral bioavailability. Polymeric nanoparticles including nanospheres and nanocapsules and polymeric fibrous systems have also emerged as potential drug delivery systems owing to their unique structure. The feasibility of surface functionalization of mesoporous materials and gold nanoparticles enables high level of control over particle characteristics making inorganic nanoparticles an exceptional formulation approach. The authors paid particular attention to the functionality-related stability of the reviewed delivery systems.

  8. Liposomal formulations for inhalation.

    Science.gov (United States)

    Cipolla, David; Gonda, Igor; Chan, Hak-Kim

    2013-08-01

    No marketed inhaled products currently use sustained release formulations such as liposomes to enhance drug disposition in the lung, but that may soon change. This review focuses on the interaction between liposomal formulations and the inhalation technology used to deliver them as aerosols. There have been a number of dated reviews evaluating nebulization of liposomes. While the information they shared is still accurate, this paper incorporates data from more recent publications to review the factors that affect aerosol performance. Recent reviews have comprehensively covered the development of dry powder liposomes for aerosolization and only the key aspects of those technologies will be summarized. There are now at least two inhaled liposomal products in late-stage clinical development: ARIKACE(®) (Insmed, NJ, USA), a liposomal amikacin, and Pulmaquin™ (Aradigm Corp., CA, USA), a liposomal ciprofloxacin, both of which treat a variety of patient populations with lung infections. This review also highlights the safety of inhaled liposomes and summarizes the clinical experience with liposomal formulations for pulmonary application. PMID:23919478

  9. Olaparib tablet formulation

    DEFF Research Database (Denmark)

    Plummer, Ruth; Swaisland, Helen; Leunen, Karin;

    2015-01-01

    BACKGROUND: The oral PARP inhibitor olaparib has shown efficacy in patients with BRCA-mutated cancer. This Phase I, open-label, three-part study (Parts A-C) in patients with advanced solid tumours evaluated the effect of food on the pharmacokinetics (PK) of olaparib when administered in tablet...... formulation. METHODS: PK data were obtained in Part A using a two-treatment period crossover design; single-dose olaparib 300 mg (two 150 mg tablets) was administered in two prandial states: fasted and fed. In Part B, patients received olaparib tablets (300 mg bid) for 5 days under fasting conditions; in Part...

  10. Systematic Equation Formulation

    DEFF Research Database (Denmark)

    Lindberg, Erik

    2007-01-01

    A tutorial giving a very simple introduction to the set-up of the equations used as a model for an electrical/electronic circuit. The aim is to find a method which is as simple and general as possible with respect to implementation in a computer program. The “Modified Nodal Approach”, MNA, and th......, and the “Controlled Source Approach”, CSA, for systematic equation formulation are investigated. It is suggested that the kernel of the P Spice program based on MNA is reprogrammed....

  11. Comparative evaluation of in vitro parameters of tamoxifen citrate loaded poly(lactide-co-glycolide), poly(epsilon-caprolactone) and chitosan nanoparticles.

    Science.gov (United States)

    Cirpanli, Y; Yerlikaya, F; Ozturk, K; Erdogar, N; Launay, M; Gegu, C; Leturgez, T; Bilensoy, E; Calis, S; Capan, Y

    2010-12-01

    Tamoxifen (TAM), the clinical choice for the antiestrogen treatment of advanced or metastatic breast cancer, was formulated in nanoparticulate carrier systems in the form of poly(lactide-co-glycolide) (PLGA), poly-epsilon-caprolactone (PCL) and chitosan (CS) nanoparticles. The PLGA and PCL nanoparticles were prepared by a nanoprecipitation technique whereas the CS nanoparticles were prepared by the ionic gelation method. Mean particle sizes were under 260 nm for PLGA and PCL nanoparticles and around 400 nm for CS nanoparticles. Polydispersity indices were less than 0.4 for all formulations. Zeta potential values were positive for TAM loaded nanoparticles because of the positive charge of the drug. Drug loading values were significantly higher for PCL nanoparticles when compared to PLGA and CS nanoparticles. All nanoparticle formulations exhibited controlled release properties. These results indicate that TAM loaded PLGA, PCL and CS nanoparticles may provide promising carrier systems for tumor targeting. PMID:21284254

  12. Plutonium Immobilization Project Baseline Formulation

    Energy Technology Data Exchange (ETDEWEB)

    Ebbinghaus, B.

    1999-02-01

    A key milestone for the Immobilization Project (AOP Milestone 3.2a) in Fiscal Year 1998 (FY98) is the definition of the baseline composition or formulation for the plutonium ceramic form. The baseline formulation for the plutonium ceramic product must be finalized before the repository- and plant-related process specifications can be determined. The baseline formulation that is currently specified is given in Table 1.1. In addition to the baseline formulation specification, this report provides specifications for two alternative formulations, related compositional specifications (e.g., precursor compositions and mixing recipes), and other preliminary form and process specifications that are linked to the baseline formulation. The preliminary specifications, when finalized, are not expected to vary tremendously from the preliminary values given.

  13. Development of novel solid-phase protein formulations

    Science.gov (United States)

    Montalvo Ortiz, Brenda Liz

    profiles and activity during in vitro release. These findings demonstrate that protein particle size is a crucial parameter for protein encapsulation in PLGA devices. Consequently, we developed a simple and effective method to obtain very small protein particles to further improve protein stability in PLGA microspheres. Protein nanoparticles of approximately 200 rim size were obtained by co-lyophilization of HRP with methyl-beta-cyclodextrin (MbetaCD), followed by suspension in ethyl acetate and sonication. We proved that protein integrity was maintained after the nanoparticle formulation. Finally, we encapsulated these protein nanospheres in PLGA microspheres by the s/o/w encapsulation method. The results showed that protein activity was improved when the HRP nanoparticle formulation was encapsulated in PLGA microspheres. In addition, we obtained a reduced initial protein release when the protein was encapsulated as nanoparticles and a linear release profile for more than 30 days. Furthermore, protein activity was maintained for prolonged times during release when compared to the lyophilized HRP formulation. Such improvements were attributed to the decrease in protein particle size. In general, these studies made a contribution in the protein-solid state formulation area. We demonstrate that protein dehydration could be done by a simple method and that particle size could be controlled to obtain the desired protein particle size. Moreover, with the nanoparticle formulation we obtained superior protein stability during encapsulation and release from PLGA microspheres. These new approaches will further increase the use of sustained delivery systems in clinical applications.

  14. Compatibility assessment of thermoplastic formulations

    OpenAIRE

    D. McAteer; Weaver, M.; Blair, L H; Flood, N; Gaulter, S E

    2016-01-01

    Prior to the large-scale preparation of any new chemical formulation an assessment of the potential reactivity between the components must be carried out. This practice, which is common to many fields including pharmaceutical science, is particularly essential in the case of energetic formulations whose chemical incompatibility may result in an unexpected and potentially explosive decomposition. The common method used to investigate incompatibility is to heat 1:1 (w/w) formulations and eva...

  15. Explosive Formulation Code Naming SOP

    Energy Technology Data Exchange (ETDEWEB)

    Martz, H. E. [Lawrence Livermore National Lab. (LLNL), Livermore, CA (United States)

    2014-09-19

    The purpose of this SOP is to provide a procedure for giving individual HME formulations code names. A code name for an individual HME formulation consists of an explosive family code, given by the classified guide, followed by a dash, -, and a number. If the formulation requires preparation such as packing or aging, these add additional groups of symbols to the X-ray specimen name.

  16. Baseline LAW Glass Formulation Testing

    Energy Technology Data Exchange (ETDEWEB)

    Kruger, Albert A. [USDOE Office of River Protection, Richland, WA (United States); Mooers, Cavin [The Catholic University of America, Washington, DC (United States). Vitreous State Lab.; Bazemore, Gina [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Pegg, Ian L. [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Hight, Kenneth [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Lai, Shan Tao [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Buechele, Andrew [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Rielley, Elizabeth [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Gan, Hao [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Muller, Isabelle S. [The Catholic University of America, Washington, DC (United States). Vitreous State Lab; Cecil, Richard [The Catholic University of America, Washington, DC (United States). Vitreous State Lab

    2013-06-13

    The major objective of the baseline glass formulation work was to develop and select glass formulations that are compliant with contractual and processing requirements for each of the LAW waste streams. Other objectives of the work included preparation and characterization of glasses with respect to the properties of interest, optimization of sulfate loading in the glasses, evaluation of ability to achieve waste loading limits, testing to demonstrate compatibility of glass melts with melter materials of construction, development of glass formulations to support ILAW qualification activities, and identification of glass formulation issues with respect to contract specifications and processing requirements.

  17. Formulation and Evaluation of Coprocessed Excipient for Mouth Dissolving Formulation

    Directory of Open Access Journals (Sweden)

    Gandhi PP and Mundada AS

    2016-03-01

    Full Text Available In the present study an attempt has been made to evaluate Ocimum bascilium mucilage coprocessed with Mannitol as a novel super disintegrant. Coprocessed excipients were prepared by solvent evaporation method and evaluated in the formulation of mouth dissolving tablets of Terbutaline sulphate. Formulated mouth dissolving tablets were characterised for physicochemical parameters like hardness, friability, weight variation, disintegration time, drug content and in vitro drug release behaviour. The outcomes of physicochemical evaluation of formulations showed that all developed formulations had desirable features. The coprocessed mucilage (Mannitol: Mucilage exhibited disintegration within 8 sec at the concentration of 1 gm: 65 mg as compared to the coprocessed Mannitol: SSG which disintegrated within 11 sec at the concentration of 1 gm: 85 mg. The developed excipient showed improvement in parent excipient functionalities and proving coprocessed mucilage of Ocimum bascilium to be an excellent novel superdisintegrant in mouth dissolving formulation and thus it can be exploited commercially.

  18. Saltstone Clean Cap Formulation

    Energy Technology Data Exchange (ETDEWEB)

    Langton, C

    2005-04-22

    The current operation strategy for using Saltstone Vault 4 to receive 0.2 Ci/gallon salt solution waste involves pouring a clean grout layer over the radioactive grout prior to initiating pour into another cell. This will minimize the radiating surface area and reduce the dose rate at the vault and surrounding area. The Clean Cap will be used to shield about four feet of Saltstone poured into a Z-Area vault cell prior to moving to another cell. The minimum thickness of the Clean Cap layer will be determined by the cesium concentration and resulting dose levels and it is expected to be about one foot thick based on current calculations for 0.1 Ci Saltstone that is produced in the Saltstone process by stabilization of 0.2 Ci salt solution. This report documents experiments performed to identify a formulation for the Clean Cap. Thermal transient calculations, adiabatic temperature rise measurements, pour height, time between pour calculations and shielding calculations were beyond the scope and time limitations of this study. However, data required for shielding calculations (composition and specific gravity) are provided for shielding calculations. The approach used to design a Clean Cap formulation was to produce a slurry from the reference premix (10/45/45 weight percent cement/slag/fly ash) and domestic water that resembled as closely as possible the properties of the Saltstone slurry. In addition, options were investigated that may offer advantages such as less bleed water and less heat generation. The options with less bleed water required addition of dispersants. The options with lower heat contained more fly ash and less slag. A mix containing 10/45/45 weight percent cement/slag/fly ash with a water to premix ratio of 0.60 is recommended for the Clean Cap. Although this mix may generate more than 3 volume percent standing water (bleed water), it has rheological, mixing and flow properties that are similar to previously processed Saltstone. The recommended

  19. Design and formulation of nano-sized spray dried efavirenz-part I: influence of formulation parameters

    Energy Technology Data Exchange (ETDEWEB)

    Katata, Lebogang, E-mail: lebzakate@yahoo.com; Tshweu, Lesego; Naidoo, Saloshnee; Kalombo, Lonji; Swai, Hulda [Materials Science and Manufacturing, Centre of Polymers and Composites, Council for Scientific and Industrial Research (South Africa)

    2012-11-15

    Efavirenz (EFV) is one of the first-line antiretroviral drugs recommended by the World Health Organisation for treating HIV. It is a hydrophobic drug that suffers from low aqueous solubility (4 {mu}g/mL), which leads to a limited oral absorption and low bioavailability. In order to improve its oral bioavailability, nano-sized polymeric delivery systems are suggested. Spray dried polycaprolactone-efavirenz (PCL-EFV) nanoparticles were prepared by the double emulsion method. The Taguchi method, a statistical design with an L{sub 8} orthogonal array, was implemented to optimise the formulation parameters of PCL-EFV nanoparticles. The types of sugar (lactose or trehalose), surfactant concentration and solvent (dichloromethane and ethyl acetate) were chosen as significant parameters affecting the particle size and polydispersity index (PDI). Small nanoparticles with an average particle size of less than 254 {+-} 0.95 nm in the case of ethyl acetate as organic solvent were obtained as compared to more than 360 {+-} 19.96 nm for dichloromethane. In this study, the type of solvent and sugar were the most influencing parameters of the particle size and PDI. Taguchi method proved to be a quick, valuable tool in optimising the particle size and PDI of PCL-EFV nanoparticles. The optimised experimental values for the nanoparticle size and PDI were 217 {+-} 2.48 nm and 0.093 {+-} 0.02.

  20. Design and formulation of nano-sized spray dried efavirenz-part I: influence of formulation parameters

    International Nuclear Information System (INIS)

    Efavirenz (EFV) is one of the first-line antiretroviral drugs recommended by the World Health Organisation for treating HIV. It is a hydrophobic drug that suffers from low aqueous solubility (4 μg/mL), which leads to a limited oral absorption and low bioavailability. In order to improve its oral bioavailability, nano-sized polymeric delivery systems are suggested. Spray dried polycaprolactone-efavirenz (PCL-EFV) nanoparticles were prepared by the double emulsion method. The Taguchi method, a statistical design with an L8 orthogonal array, was implemented to optimise the formulation parameters of PCL-EFV nanoparticles. The types of sugar (lactose or trehalose), surfactant concentration and solvent (dichloromethane and ethyl acetate) were chosen as significant parameters affecting the particle size and polydispersity index (PDI). Small nanoparticles with an average particle size of less than 254 ± 0.95 nm in the case of ethyl acetate as organic solvent were obtained as compared to more than 360 ± 19.96 nm for dichloromethane. In this study, the type of solvent and sugar were the most influencing parameters of the particle size and PDI. Taguchi method proved to be a quick, valuable tool in optimising the particle size and PDI of PCL-EFV nanoparticles. The optimised experimental values for the nanoparticle size and PDI were 217 ± 2.48 nm and 0.093 ± 0.02.

  1. In vitro skin permeation of artemisone and its nano-vesicular formulations

    OpenAIRE

    Dwivedi, Anupma; Mazumder, Anisha; Fox, Lizelle T.; Brümmer, Alicia; Gerber, Minja; du Preez, Jan L.; Haynes, Richard K.; Du Plessis, Jeanetta

    2016-01-01

    The artemisinin derivative artemisone has antitumor activity. In particular when encapsulated in solid lipid nanoparticles (SLNs) and niosomes, it is active against human melanoma A-375 cells, although such formulations have a negligible effect on human keratinocyte cells. The aim here was to determine whether these formulations could enhance the topical delivery and skin permeation of artemisone as a prelude to evaluating use of artemisone and related compounds for melanoma treat...

  2. Eudragit nanoparticles containing genistein: formulation, development, and bioavailability assessment

    OpenAIRE

    Tang J; Xu N; Ji H; Liu H.; Wang Z.; Wu L

    2011-01-01

    Jingling Tang2, Na Xu1,2, Hongyu Ji1, Hongmei Liu1, Zhiyong Wang1, Linhua Wu1,2 1Department of Pharmacy, the Second Affiliated Hospital of Harbin Medical University, Key Laboratory of College in Heilongjiang Province; 2Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, China Background: Genistein, one of the major isoflavones, has received great attention as a phytoestrogen and potential cancer chemoprevention agent. However, the dissolution and bioavailabili...

  3. Formulation and Particle Size Reduction Improve Bioavailability of Poorly Water-Soluble Compounds with Antimalarial Activity

    Directory of Open Access Journals (Sweden)

    Hongxing Wang

    2013-01-01

    Full Text Available Decoquinate (DQ is highly effective at killing malaria parasites in vitro; however, it is extremely insoluble in water. In this study, solid dispersion method was used for DQ formulation which created a suitable physical form of DQ in aqueous phase for particle manipulation. Among many polymers and surfactants tested, polyvinylpyrrolidone 10, a polymer, and L-α-phosphatidylcholine or polysorbate, two surfactants, were chosen as DQ formulation components. The formulation particles were reduced to a mean size between 200 to 400 nm, which was stable in aqueous medium for at least three weeks. Pharmacokinetic (PK studies showed that compared to DQ microparticle suspension, a nanoparticle formulation orally dosed to mice showed a 14.47-fold increase in area under the curve (AUC of DQ plasma concentration and a 4.53-fold increase in AUC of DQ liver distribution. WR 299666, a poorly water-soluble compound with antimalarial activity, was also tested and successfully made into nanoparticle formulation without undergoing solid dispersion procedure. We concluded that nanoparticles generated by using appropriate formulation components and sufficient particle size reduction significantly increased the bioavailability of DQ and could potentially turn this antimalarial agent to a therapeutic drug.

  4. Formulation and particle size reduction improve bioavailability of poorly water-soluble compounds with antimalarial activity.

    Science.gov (United States)

    Wang, Hongxing; Li, Qigui; Reyes, Sean; Zhang, Jing; Xie, Lisa; Melendez, Victor; Hickman, Mark; Kozar, Michael P

    2013-01-01

    Decoquinate (DQ) is highly effective at killing malaria parasites in vitro; however, it is extremely insoluble in water. In this study, solid dispersion method was used for DQ formulation which created a suitable physical form of DQ in aqueous phase for particle manipulation. Among many polymers and surfactants tested, polyvinylpyrrolidone 10, a polymer, and L- α -phosphatidylcholine or polysorbate, two surfactants, were chosen as DQ formulation components. The formulation particles were reduced to a mean size between 200 to 400 nm, which was stable in aqueous medium for at least three weeks. Pharmacokinetic (PK) studies showed that compared to DQ microparticle suspension, a nanoparticle formulation orally dosed to mice showed a 14.47-fold increase in area under the curve (AUC) of DQ plasma concentration and a 4.53-fold increase in AUC of DQ liver distribution. WR 299666, a poorly water-soluble compound with antimalarial activity, was also tested and successfully made into nanoparticle formulation without undergoing solid dispersion procedure. We concluded that nanoparticles generated by using appropriate formulation components and sufficient particle size reduction significantly increased the bioavailability of DQ and could potentially turn this antimalarial agent to a therapeutic drug.

  5. Bicontinuous cubic liquid crystalline nanoparticles for oral delivery of Doxorubicin

    DEFF Research Database (Denmark)

    Swarnakar, Nitin K; Thanki, Kaushik; Jain, Sanyog

    2014-01-01

    PURPOSE: The present study explores the potential of bicontinous cubic liquid crystalline nanoparticles (LCNPs) for improving therapeutic potential of doxorubicin. METHODS: Phytantriol based Dox-LCNPs were prepared using hydrotrope method, optimized for various formulation components, process...... variables and lyophilized. Structural elucidation of the reconstituted formulation was performed using HR-TEM and SAXS analysis. The developed formulation was subjected to exhaustive cell culture experiments for delivery potential (Caco-2 cells) and efficacy (MCF-7 cells). Finally, in vivo pharmacokinetics...

  6. Computer Optimization of Biodegradable Nanoparticles Fabricated by Dispersion Polymerization.

    Science.gov (United States)

    Akala, Emmanuel O; Adesina, Simeon; Ogunwuyi, Oluwaseun

    2016-01-01

    Quality by design (QbD) in the pharmaceutical industry involves designing and developing drug formulations and manufacturing processes which ensure predefined drug product specifications. QbD helps to understand how process and formulation variables affect product characteristics and subsequent optimization of these variables vis-à-vis final specifications. Statistical design of experiments (DoE) identifies important parameters in a pharmaceutical dosage form design followed by optimizing the parameters with respect to certain specifications. DoE establishes in mathematical form the relationships between critical process parameters together with critical material attributes and critical quality attributes. We focused on the fabrication of biodegradable nanoparticles by dispersion polymerization. Aided by a statistical software, d-optimal mixture design was used to vary the components (crosslinker, initiator, stabilizer, and macromonomers) to obtain twenty nanoparticle formulations (PLLA-based nanoparticles) and thirty formulations (poly-ɛ-caprolactone-based nanoparticles). Scheffe polynomial models were generated to predict particle size (nm), zeta potential, and yield (%) as functions of the composition of the formulations. Simultaneous optimizations were carried out on the response variables. Solutions were returned from simultaneous optimization of the response variables for component combinations to (1) minimize nanoparticle size; (2) maximize the surface negative zeta potential; and (3) maximize percent yield to make the nanoparticle fabrication an economic proposition. PMID:26703678

  7. Computer Optimization of Biodegradable Nanoparticles Fabricated by Dispersion Polymerization

    Directory of Open Access Journals (Sweden)

    Emmanuel O. Akala

    2015-12-01

    Full Text Available Quality by design (QbD in the pharmaceutical industry involves designing and developing drug formulations and manufacturing processes which ensure predefined drug product specifications. QbD helps to understand how process and formulation variables affect product characteristics and subsequent optimization of these variables vis-à-vis final specifications. Statistical design of experiments (DoE identifies important parameters in a pharmaceutical dosage form design followed by optimizing the parameters with respect to certain specifications. DoE establishes in mathematical form the relationships between critical process parameters together with critical material attributes and critical quality attributes. We focused on the fabrication of biodegradable nanoparticles by dispersion polymerization. Aided by a statistical software, d-optimal mixture design was used to vary the components (crosslinker, initiator, stabilizer, and macromonomers to obtain twenty nanoparticle formulations (PLLA-based nanoparticles and thirty formulations (poly-ɛ-caprolactone-based nanoparticles. Scheffe polynomial models were generated to predict particle size (nm, zeta potential, and yield (% as functions of the composition of the formulations. Simultaneous optimizations were carried out on the response variables. Solutions were returned from simultaneous optimization of the response variables for component combinations to (1 minimize nanoparticle size; (2 maximize the surface negative zeta potential; and (3 maximize percent yield to make the nanoparticle fabrication an economic proposition.

  8. Intermetallic nanoparticles

    Science.gov (United States)

    Singh, Dileep; Yusufoglu, Yusuf; Timofeeva, Elena; Routbort, Jules

    2015-07-14

    A process for preparing intermetallic nanoparticles of two or more metals is provided. In particular, the process includes the steps: a) dispersing nanoparticles of a first metal in a solvent to prepare a first metal solution, b) forming a reaction mixture with the first metal solution and a reducing agent, c) heating the reaction mixture to a reaction temperature; and d) adding a second metal solution containing a salt of a second metal to the reaction mixture. During this process, intermetallic nanoparticles, which contain a compound with the first and second metals are formed. The intermetallic nanoparticles with uniform size and a narrow size distribution is also provided. An electrochemical device such as a battery with the intermetallic nanoparticles is also provided.

  9. Preparation and Characterization of Nateglinide Loaded Hydrophobic Biocompatible Polymer Nanoparticles

    Science.gov (United States)

    Naik, Jitendra; Lokhande, Amolkumar; Mishra, Satyendra; Kulkarni, Ravindra

    2016-09-01

    The aim of the present study was to develop sustained release Nateglinide loaded Ethylcellulose nanoparticles and characterize the properties of recovered nanoparticles. The sustained release nanoparticles were prepared by oil in water single emulsion solvent evaporation method. The developed nanoparticles were characterised for their particle size, morphology, encapsulation efficiency, drug polymer compatibility and in vitro drug release. The drug polymer compatibility was investigated by XRPD. Imaging of particles was performed by field emission scanning electron microscopy. The highest particle size and encapsulation efficiency of recovered nanoparticles were 248.37 nm and 91.16 % respectively. The recovered nanoparticles are spherical in nature and uniform in size. Developed nanoparticles have low crystallinity than the pure Nateglinide. The highest drug-polymer ratio formulation showed drug release 61.1 ± 1.76 % up to 24 h.

  10. Relativistic formulation of quark model

    International Nuclear Information System (INIS)

    A relativistic model, which describes spin-orbital excitations of quark-antiquark bound system, is proposed. A formulation of the model provides the meson classification established in frame of the nonrelativistic quark model. 3 refs

  11. Formulation Optimization of Arecoline Patches

    Directory of Open Access Journals (Sweden)

    Pao-Chu Wu

    2014-01-01

    Full Text Available The response surface methodology (RSM including polynomial equations has been used to design an optimal patch formulation with appropriate adhesion and flux. The patch formulations were composed of different polymers, including Eudragit RS 100 (ERS, Eudragit RL 100 (ERL and polyvinylpyrrolidone K30 (PVP, plasticizers (PEG 400, and drug. In addition, using terpenes as enhancers could increase the flux of the drug. Menthol showed the highest enhancement effect on the flux of arecoline.

  12. Niosomal Formulation Of Orlistat: Formulation And In-Vitro Evaluation

    Directory of Open Access Journals (Sweden)

    SAMYUKTHA RANI. B

    2011-06-01

    Full Text Available The purpose of the research was to prepare Orlistat niosomes from proniosome to improve its poor and variable oral bioavailability. The non-ionic surfactant vesicles are prepared by the reverse phase evaporation technique (slurry method. The slurry of - Cyclodextrin and Span 60 was dried to form a free flowing powder in rotary flash evaporator which could be rehydrated by addition of buffer (0.5% NaCl with 3% SLS at pH 6.0. The lipid mixture consisted of cholesterol, Span 60 and - Cyclodextrin carrier in molar ratios of (0.1:0.9:1 to 0.9:0.1:1 respectively. The niosomal formulations were evaluated for particle size, entrapment efficiency, in-vitro drug release, release kinetics, Interactions and compatibility (FT-IR, surface morphology (SEM, stability studies, conductivity and sedimentation rate, pH density, viscosity. The formulation OT9 which showed higher entrapment efficiency of 44.09% and invitro releases of 94.59% at the end of 12hrs was found to be best among all the 9 formulations. Release was best fitted with Hixson kinetics and it shows that the drug release may follow diffusion mechanism. FT-IR data revealed that, compatible and there were no interactions between the drug and excipients added in the formulation. SEM images of niosomes with various magnifications revealed the mean size of the niosomes were 100 nm with smooth surface. Niosome formulation has showed appropriate stability for 90 days by storing the formulation at room temperature. Thus the niosomal formulations could be a promising delivery system for Orlistat with improved oral bioavailability, stability and for sustained drug release.

  13. Toxicity of novel nanosized formulations used in medicine.

    Science.gov (United States)

    El-Ansary, Afaf; Al-Daihan, Sooad; Bacha, Abir Ben; Kotb, Malak

    2013-01-01

    Nanotechnology involves the creation and manipulation of materials at nanoscale levels (1-100 nm) to create products that exhibit novel properties. While this motivation has driven nanoscience and technology in physics and engineering, it is not the main reason that nanoparticles are useful for systemic applications in the human body. The application of nanotechnology to medicine, known as nanomedicine, concerns the use of precisely engineered materials at this length scale to develop novel therapeutic and diagnostic modalities. A number of nanotherapeutic formulations are already approved for medical use and more are in the approval pipeline currently. This chapter is intended to provide an overview of the toxicity of these therapeutic nanoparticles and to summarize the current state of the field. We begin with background on the sources of exposure to nanoparticles, followed by reviewing different forms of nanosized therapeutic tools as quantum dots, nanoshells, nanocapsules, echogenic bubble, and "nanoshuttles." Moreover, cytotoxic effects of nanoparticles on cell membrane, mitochondrial function, prooxidant/antioxidant status, enzyme leakage, DNA, and other biochemical endpoints were elucidated. We highlight the need for caution during the use and disposal of such manufactured nanomaterials to prevent unintended environmental impacts. Moreover, different strategies which could be used to minimize or eliminate nanotoxicity were also discussed in detail. Understanding of how to tune size and surface properties to provide safety will permit the creation of new, more effective nanomedicines for systemic use. PMID:23740113

  14. Applications of lipid based formulation technologies in the delivery of biotechnology-based therapeutics.

    Science.gov (United States)

    du Plessis, Lissinda H; Marais, Etienne B; Mohammed, Faruq; Kotzé, Awie F

    2014-01-01

    In the last decades several new biotechnologically-based therapeutics have been developed due to progress in genetic engineering. A growing challenge facing pharmaceutical scientists is formulating these compounds into oral dosage forms with adequate bioavailability. An increasingly popular approach to formulate biotechnology-based therapeutics is the use of lipid based formulation technologies. This review highlights the importance of lipid based drug delivery systems in the formulation of oral biotechnology based therapeutics including peptides, proteins, DNA, siRNA and vaccines. The different production procedures used to achieve high encapsulation efficiencies of the bioactives are discussed, as well as the factors influencing the choice of excipient. Lipid based colloidal drug delivery systems including liposomes and solid lipid nanoparticles are reviewed with a focus on recent advances and updates. We further describe microemulsions and self-emulsifying drug delivery systems and recent findings on bioactive delivery. We conclude the review with a few examples on novel lipid based formulation technologies. PMID:25091118

  15. Recent advances in topical formulation carriers of antifungal agents.

    Science.gov (United States)

    Bseiso, Eman Ahmed; Nasr, Maha; Sammour, Omaima; Abd El Gawad, Nabaweya A

    2015-01-01

    Fungal infections are amongst the most commonly encountered diseases affecting the skin. Treatment approaches include both topical and oral antifungal agents. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments and gels. Several carrier systems loaded with antifungal drugs have demonstrated promising results in the treatment of skin fungal infections. Examples of these newer carriers include micelles, lipidic systems such as solid lipid nanoparticles and nanostructured lipid carriers, microemulsions and vesicular systems such as liposomes, niosomes, transfersomes, ethosomes, and penetration enhancer vesicles. PMID:26261140

  16. Nanobioprobe for the Determination of Pork Adulteration in Burger Formulations

    OpenAIRE

    Ali, M. E.; MUSTAFA, S.; Hashim, U.; Che Man, Y. B.; K L Foo

    2012-01-01

    We report the development of a swine-specific hybrid nanobioprobe through a covalent integration of a fluorophore-labeled 27-nucleotide AluI-fragment of swine cytochrome b gene to a 3 nm gold nanoparticle for the determination of pork adulteration in processed meat products. We tested the probe to estimate adulterated pork in ready-to-eat pork-spiked beef burgers. The probe quantitatively detected 1–100% spiked pork in burger formulations with ≥90% accuracy. A plot of observed fluorescence ag...

  17. Recent advances in topical formulation carriers of antifungal agents

    Directory of Open Access Journals (Sweden)

    Eman Ahmed Bseiso

    2015-01-01

    Full Text Available Fungal infections are amongst the most commonly encountered diseases affecting the skin. Treatment approaches include both topical and oral antifungal agents. The topical route is generally preferred due to the possible side effects of oral medication. Advances in the field of formulation may soon render outdated conventional products such as creams, ointments and gels. Several carrier systems loaded with antifungal drugs have demonstrated promising results in the treatment of skin fungal infections. Examples of these newer carriers include micelles, lipidic systems such as solid lipid nanoparticles and nanostructured lipid carriers, microemulsions and vesicular systems such as liposomes, niosomes, transfersomes, ethosomes, and penetration enhancer vesicles.

  18. Social Groupwork. A Model for Goal Formulation.

    Science.gov (United States)

    Tompkins, Rosamond P.; Gallo, Frank T.

    1978-01-01

    A conceptual model for goal formulation in social groupwork, discussion of existing models and their limitations, and an attempt to formulate an encompassing groupwork model that facilitates goal formulation. (Author/PD)

  19. Four formulations of noncommutative quantum mechanics

    CERN Document Server

    Gouba, Laure

    2016-01-01

    Four formulations of noncommutative quantum mechanics are reviewed. These are the canonical, path-integral, Weyl-Wigner and systematic formulations. The four formulations are charaterized by a deformed Heisenberg algebra but differ in mathematical and conceptual overview.

  20. A variational formulation of electrodynamics

    CERN Document Server

    De Nicola, Antonio

    2007-01-01

    We present a variational formulation of electrodynamics using de Rham even and odd differential forms. Our formulation relies on a variational principle more complete than the Hamilton principle and thus leads to field equations with external sources and permits the derivation of the constitutive relations. We interpret a domain in space-time as an odd de Rham 4-current. This permits a treatment of different types of boundary problems in an unified way. In particular we obtain a smooth transition to the infinitesimal version by using a current with a one point support.

  1. Hyperbolic Formulation of General Relativity

    CERN Document Server

    Abrahams, A M; Choquet-Bruhat, Y; York, J W; Abrahams, Andrew; Anderson, Arlen; Choquet-Bruhat, Yvonne; York, James W.

    1998-01-01

    Two geometrical well-posed hyperbolic formulations of general relativity are described. One admits any time-slicing which preserves a generalized harmonic condition. The other admits arbitrary time-slicings. Both systems have only the physical characteristic speeds of zero and the speed of light.

  2. Case Formulation in TADS CBT

    Science.gov (United States)

    Rogers, Gregory M.; Reinecke, Mark A.; Curry, John F.

    2005-01-01

    For the Treatment for Adolescents With Depression Study (TADS), a cognitive-behavioral therapy (CBT) manual was developed with the aim of balancing standardization and flexibility. In this article, we describe the manual's case formulation procedures, which served as one major mechanism of flexibility in TADS CBT. We first describe the essential…

  3. Curcumin nanodisks: formulation and characterization

    OpenAIRE

    Ghosh, Mistuni; Singh, Amareshwar T.K.; Xu, Wenwei; Sulchek, Todd; Gordon, Leo I.; Ryan, Robert O.

    2010-01-01

    Nanodisks (ND) are nanoscale, disk-shaped phospholipid bilayers whose edge is stabilized by apolipoproteins. In the present study, ND were formulated with the bioactive polyphenol, curcumin, at a 6:1 phospholipid:curcumin molar ratio. Atomic force microscopy revealed that curcumin-ND are particles with diameters

  4. Hamiltonian formulation of bond graphs

    NARCIS (Netherlands)

    Golo, Goran; Schaft, van der Arjan; Breedveld, Peter C.; Maschke, Bernhard M.; Johansson, R.; Rantzer, A.

    2003-01-01

    This paper deals with the mathematical formulation of bond graphs. It is proven that the power continuous part of bond graphs, the junction structure, can be associated with a Dirac structure and that the equations describing a bond graph model correspond to a port Hamiltonian system. The conditions

  5. Nanoparticles in dermatology.

    Science.gov (United States)

    Papakostas, Dimitrios; Rancan, Fiorenza; Sterry, Wolfram; Blume-Peytavi, Ulrike; Vogt, Annika

    2011-10-01

    Recent advances in the field of nanotechnology have allowed the manufacturing of elaborated nanometer-sized particles for various biomedical applications. A broad spectrum of particles, extending from various lipid nanostructures such as liposomes and solid lipid nanoparticles, to metal, nanocrystalline and polymer particles have already been tested as drug delivery systems in different animal models with remarkable results, promising an extensive commercialization in the coming years. Controlled drug release to skin and skin appendages, targeting of hair follicle-specific cell populations, transcutaneous vaccination and transdermal gene therapy are only a few of these new applications. Carrier systems of the new generation take advantage of improved skin penetration properties, depot effect with sustained drug release and of surface functionalization (e.g., the binding to specific ligands) allowing specific cellular and subcellular targeting. Drug delivery to skin by means of microparticles and nanocarriers could revolutionize the treatment of several skin disorders. However, the toxicological and environmental safety of micro- and nanoparticles has to be evaluated using specific toxicological studies prior to a wider implementation of the new technology. This review aims to give an overview of the most investigated applications of transcutaneously applied particle-based formulations in the fields of cosmetics and dermatology. PMID:21837474

  6. Biopolymeric nanoparticles

    Directory of Open Access Journals (Sweden)

    Sushmitha Sundar, Joydip Kundu and Subhas C Kundu

    2010-01-01

    Full Text Available This review on nanoparticles highlights the various biopolymers (proteins and polysaccharides which have recently revolutionized the world of biocompatible and degradable natural biological materials. The methods of their fabrication, including emulsification, desolvation, coacervation and electrospray drying are described. The characterization of different parameters for a given nanoparticle, such as particle size, surface charge, morphology, stability, structure, cellular uptake, cytotoxicity, drug loading and drug release, is outlined together with the relevant measurement techniques. Applications in the fields of medicine and biotechnology are discussed along with a promising future scope.

  7. Nanoparticles in relation to peptide and protein aggregation

    Directory of Open Access Journals (Sweden)

    Zaman M

    2014-02-01

    Full Text Available Masihuz Zaman, Ejaz Ahmad, Atiyatul Qadeer, Gulam Rabbani, Rizwan Hasan Khan Interdisciplinary Biotechnology Unit, Aligarh Muslim University, Aligarh, India Abstract: Over the past two decades, there has been considerable research interest in the use of nanoparticles in the study of protein and peptide aggregation, and of amyloid-related diseases. The influence of nanoparticles on amyloid formation yields great interest due to its small size and high surface area-to-volume ratio. Targeting nucleation kinetics by nanoparticles is one of the most searched for ways to control or induce this phenomenon. The observed effect of nanoparticles on the nucleation phase is determined by particle composition, as well as the amount and nature of the particle's surface. Various thermodynamic parameters influence the interaction of proteins and nanoparticles in the solution, and regulate the protein assembly into fibrils, as well as the disaggregation of preformed fibrils. Metals, organic particles, inorganic particles, amino acids, peptides, proteins, and so on are more suitable candidates for nanoparticle formulation. In the present review, we attempt to explore the effects of nanoparticles on protein and peptide fibrillation processes from both perspectives (ie, as inducers and inhibitors on nucleation kinetics and in the disaggregation of preformed fibrils. Their formulation and characterization by different techniques have been also addressed, along with their toxicological effects, both in vivo and in vitro. Keywords: amyloid formation, inducer, inhibitor, nanoparticle, nucleation, toxicity

  8. Langevin formulation of quantum dynamics

    International Nuclear Information System (INIS)

    We first show that nonrelativistic quantum mechanics formulated at imaginary-(h/2 π) can formally be viewed as the Fokker-Planck description of a frictionless brownian motion, which occurs (in general) in an absorbing medium. We next offer a new formulation of quantum mechanics, which is basically the Langevin treatment of this brownian motion. Explicitly, we derive a noise-average representation for the transition probability W(X'',t''|X',t'), in terms of the solutions to a Langevin equation with a Gaussian white-noise. Upon analytic continuation back to real-(h/2 π),W(X'',t''|X',t') becomes the propagator of the original Schroedinger equation. Our approach allows for a straightforward application to quantum dynamical problems of the mathematical techniques of classical stochastic processes. Moreover, computer simulations of quantum mechanical systems can be carried out by using numerical programs based on the Langevin dynamics. (author). 19 refs, 1 tab

  9. Statistical mechanics formulation of radiobiology

    CERN Document Server

    Sotolongo-Grau, O; Santos-Miranda, J A; Antoranz, J C; Sotolongo-Costa, Oscar

    2009-01-01

    The expression of survival factors for radiation damaged cells is empirical and based on probabilistic assumptions. We obtain it either from the maximum entropy principle for the classical Boltzmann-Gibbs entropy and/or from the Tsallis entropy. Empiric models are found to be particular cases of the obtained expression. The survival factor exhibits a phase transition behaviour. This formulation supports different tissues grouped as universality classes.

  10. Nanoparticles laden in situ gel for sustained ocular drug delivery

    Directory of Open Access Journals (Sweden)

    Himanshu Gupta

    2013-01-01

    Full Text Available Proper availability of drug on to corneal surface is a challenging task. However, due to ocular physiological barriers, conventional eye drops display poor ocular bioavailability of drugs (< 1%. To improve precorneal residence time and ocular penetration, earlier our group developed and evaluated in situ gel and nanoparticles for ocular delivery. In interest to evaluate the combined effect of in situ gel and nanoparticles on ocular retention, we combined them. We are the first to term this combination as "nanoparticle laden in situ gel", that is, poly lactic co glycolic acid nanoparticle incorporated in chitosan in situ gel for sparfloxacin ophthalmic delivery. The formulation was tested for various physicochemical properties. It showed gelation pH near pH 7.2. The observation of acquired gamma camera images showed good retention over the entire precorneal area for sparfloxacin nanoparticle laden in situ gel (SNG as compared to marketed formulation. SNG formulation cleared at a very slow rate and remained at corneal surface for longer duration as no radioactivity was observed in systemic circulation. The developed formulation was found to be better in combination and can go up to the clinical evaluation and application.

  11. Novel delivery system for natural products: Nano-curcumin formulations

    Directory of Open Access Journals (Sweden)

    Hamid Reza Rahimi

    2016-06-01

    Full Text Available Objective: Curcumin is extracted from Curcuma longa and regulates the intracellular signal pathways which control the growth of cancerous cell, inflammation, invasion and apoptosis. Curcumin molecules have special intrinsic features that can target the intracellular enzymes, genome (DNA and messengers (RNA. A wide range of studies have been conducted on the physicochemical traits and pharmacological effects of curcumin on different diseases like cardiovascular diseases, diabetes, cancer, rheumatoid arthritis, Alzheimer’s, inflammatory bowel disease (IBD, and even it has wound healing. Oral bioavailability of curcumin is rather poor, which would certainly put some boundaries in the employment of this drug. Materials and Methods: Bibliographical searches were performed using MEDLINE/ScienceDirect/OVID up to February 2015 using the following keywords (all fields: (“Curcumin” OR “Curcuma longa” AND [(nanoparticles OR (Nanomicelles OR (micro emulsions OR (liposome OR (phospholipid. Results: Consequently, for any developments of curcumin in the future, analogues of curcumin that have better bioavailability or substitute formulations are needed crucially. Conclusion: These studies indicated that nanotechnology can formulate curcumin effectively, and this nano-formulated curcumin with a potent ability against various cancer cells, were represented to have better efficacy and bioavailability under in vivo conditions.

  12. Novel delivery system for natural products: Nano-curcumin formulations

    Science.gov (United States)

    Rahimi, Hamid Reza; Nedaeinia, Reza; Sepehri Shamloo, Alireza; Nikdoust, Shima; Kazemi Oskuee, Reza

    2016-01-01

    Objective: Curcumin is extracted from Curcuma longa and regulates the intracellular signal pathways which control the growth of cancerous cell, inflammation, invasion and apoptosis. Curcumin molecules have special intrinsic features that can target the intracellular enzymes, genome (DNA) and messengers (RNA). A wide range of studies have been conducted on the physicochemical traits and pharmacological effects of curcumin on different diseases like cardiovascular diseases, diabetes, cancer, rheumatoid arthritis, Alzheimer’s, inflammatory bowel disease (IBD), and even it has wound healing. Oral bioavailability of curcumin is rather poor, which would certainly put some boundaries in the employment of this drug. Materials and Methods: Bibliographical searches were performed using MEDLINE/ScienceDirect/OVID up to February 2015 using the following keywords (all fields): (“Curcumin” OR “Curcuma longa”) AND [(nanoparticles) OR (Nanomicelles) OR (micro emulsions) OR (liposome) OR (phospholipid). Results: Consequently, for any developments of curcumin in the future, analogues of curcumin that have better bioavailability or substitute formulations are needed crucially. Conclusion: These studies indicated that nanotechnology can formulate curcumin effectively, and this nano-formulated curcumin with a potent ability against various cancer cells, were represented to have better efficacy and bioavailability under in vivo conditions.

  13. Novel delivery system for natural products: Nano-curcumin formulations

    Science.gov (United States)

    Rahimi, Hamid Reza; Nedaeinia, Reza; Sepehri Shamloo, Alireza; Nikdoust, Shima; Kazemi Oskuee, Reza

    2016-01-01

    Objective: Curcumin is extracted from Curcuma longa and regulates the intracellular signal pathways which control the growth of cancerous cell, inflammation, invasion and apoptosis. Curcumin molecules have special intrinsic features that can target the intracellular enzymes, genome (DNA) and messengers (RNA). A wide range of studies have been conducted on the physicochemical traits and pharmacological effects of curcumin on different diseases like cardiovascular diseases, diabetes, cancer, rheumatoid arthritis, Alzheimer’s, inflammatory bowel disease (IBD), and even it has wound healing. Oral bioavailability of curcumin is rather poor, which would certainly put some boundaries in the employment of this drug. Materials and Methods: Bibliographical searches were performed using MEDLINE/ScienceDirect/OVID up to February 2015 using the following keywords (all fields): (“Curcumin” OR “Curcuma longa”) AND [(nanoparticles) OR (Nanomicelles) OR (micro emulsions) OR (liposome) OR (phospholipid). Results: Consequently, for any developments of curcumin in the future, analogues of curcumin that have better bioavailability or substitute formulations are needed crucially. Conclusion: These studies indicated that nanotechnology can formulate curcumin effectively, and this nano-formulated curcumin with a potent ability against various cancer cells, were represented to have better efficacy and bioavailability under in vivo conditions. PMID:27516979

  14. Cellular uptake and concentrations of tamoxifen upon administration in poly(ε-caprolactone) nanoparticles

    OpenAIRE

    Chawla, Jugminder S.; Amiji, Mansoor M.

    2003-01-01

    Purpose: In an attempt to increase the local concentration of tamoxifen in estrogen receptor positive breast cancer cells, we have prepared and characterized poly (ε-caprolactone) (PCL) nanoparticle formulation. Methods: PCL (mol wt 14,800 daltons) nanoparticles were prepared by the solvent displacement method in acetonewater system in the presence of Pluronic F-68. PCL nanoparticles, labeled with rhodamine 123, were incubated with MCF-7 estrogen receptor positive breast cancer cells to deter...

  15. Investigation of formulation variables affecting the properties of lamotrigine nanosuspension using fractional factorial design

    Directory of Open Access Journals (Sweden)

    B Mishra

    2010-03-01

    Full Text Available "n  "n   Background and the purpose of the study: Lamotrigine (LMG undergoes extensive hepatic metabolism upon oral administration and its absorption is affected in the presence of food. This study was aimed to develop nanosuspension of LMG and investigate its formulation characteristics using L9 orthogonal array. Methods: Nanosuspension was prepared using emulsification-solvent diffusion method. All the formulations were subjected to in-vitro evaluation and the statistically optimized one was used for stability, scanning electron microscopic and differential scanning calorimetric studies. Results: Nanoparticles were spherical with little surface adsorbed drug. Formulation characteristics in terms of size, zeta potential, polydispersity index (PDI, entrapment efficiency (EE, drug content and in vitro drug release were consistent and within their acceptable range. All the batches provided a burst release profile during first 1 hr, followed by a controlled release extending up to 24 hrs. The values of n in Peppas model ranged between 0.2-0.4 for all the formulations indicative of Fickian release mechanism. The formulation remained reasonably stable up to 3 months. No interaction was observed among the drug and polymers.  Major conclusion: Results of in vitro drug release studies suggested that nanosuspension might be used as a sustained delivery vehicle for LMG. Statistical analysis revealed that size of the nanoparticles was most strongly affected by stabilizer type while EE was influenced by the drug-to-polymer ratio.  

  16. Preparation and in vitro evaluation of hydrophilic fenretinide nanoparticles.

    Science.gov (United States)

    Ledet, Grace A; Graves, Richard A; Glotser, Elena Y; Mandal, Tarun K; Bostanian, Levon A

    2015-02-20

    Fenretinide is an effective anti-cancer drug with high in vitro cytotoxicity and low in vivo systemic toxicity. In clinical trials, fenretinide has shown poor therapeutic efficacy following oral administration - attributed to its low bioavailability and solubility. The long term goal of this project is to develop a formulation for the oral delivery of fenretinide. The purpose of this part of the study was to prepare and characterize hydrophilic nanoparticle formulations of fenretinide. Three different ratios of polyvinyl pyrrolidone (PVP) to fenretinide were used, namely, 3:1, 4:1, and 5:1. Both drug and polymer were dissolved in a mixture of methanol and dichloromethane (2:23 v/v). Rotary evaporation was used to remove the solvents, and, following reconstitution with water, a high pressure homogenizer was used to form nanoparticles. The particle size and polydispersity index were measured before and after lyophilization. The formulations were studied by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD). The effectiveness of the formulations was assessed by release studies and Caco-2 cell permeability assays. As the PVP content increased, the recovered particle size following lyophilization became more consistent with the pre-lyophilization particle size, especially for those formulations with less lactose. The DSC scans of the formulations did not show any fenretinide melting endotherms, indicating that the drug was either present in an amorphous form in the formulation or that a solid solution of the drug in PVP had formed. For the release studies, the highest drug release among the formulations was 249.2±35.5ng/mL for the formulation with 4:1 polymer-to-drug. When the permeability of the formulations was evaluated in a Caco-2 cell model, the mean normalized flux for each treatment group was significantly higher (plactose-to-formulation ratio emerged as the optimal choice for further evaluation as a

  17. Path Integral Formulation of Noncommutative Quantum Mechanics

    CERN Document Server

    Acatrinei, C S

    2001-01-01

    We propose a phase-space path integral formulation of noncommutative quantum mechanics, and prove its equivalence to the operatorial formulation. As an illustration, the partition function of a noncommutative two-dimensional harmonic oscillator is calculated.

  18. Perfume formulation: words and chats.

    Science.gov (United States)

    Ellena, Céline

    2008-06-01

    What does it mean to create fragrances with materials from chemistry and/or from nature? How are they used to display their characteristic differences, their own personality? Is it easier to create with synthetic raw materials or with essential oils? This review explains why a perfume formulation corresponds in fact to a conversation, an interplay between synthetic and natural perfumery materials. A synthetic raw material carries a single information, and usually is very linear. Its smell is uniform, clear, and faithful. Natural raw materials, on the contrary, provide a strong, complex and generous image. While a synthetic material can be seen as a single word, a natural one such as rose oil could be compared to chatting: cold, warm, sticky, heavy, transparent, pepper, green, metallic, smooth, watery, fruity... full of information. Yet, if a very small amount of the natural material is used, nothing happens, the fragrance will not change. However, if a large amount is used, the rose oil will swallow up everything else. The fragrance will smell of nothing else except rose! To formulate a perfume is not to create a culinary recipe, with only dosing the ingredients in well-balanced amounts. To formulate rather means to flexibly knit materials together with a lively stitch, meeting or repelling each other, building a pleasant form, which is neither fixed, nor solid, nor rigid. A fragrance has an overall structure, which ranges from a clear sound, made up of stable, unique, and linear items, to a background chat, comfortable and reassuring. But that does, of course, not mean that there is only one way of creating a fragrance! PMID:18618806

  19. Perfume formulation: words and chats.

    Science.gov (United States)

    Ellena, Céline

    2008-06-01

    What does it mean to create fragrances with materials from chemistry and/or from nature? How are they used to display their characteristic differences, their own personality? Is it easier to create with synthetic raw materials or with essential oils? This review explains why a perfume formulation corresponds in fact to a conversation, an interplay between synthetic and natural perfumery materials. A synthetic raw material carries a single information, and usually is very linear. Its smell is uniform, clear, and faithful. Natural raw materials, on the contrary, provide a strong, complex and generous image. While a synthetic material can be seen as a single word, a natural one such as rose oil could be compared to chatting: cold, warm, sticky, heavy, transparent, pepper, green, metallic, smooth, watery, fruity... full of information. Yet, if a very small amount of the natural material is used, nothing happens, the fragrance will not change. However, if a large amount is used, the rose oil will swallow up everything else. The fragrance will smell of nothing else except rose! To formulate a perfume is not to create a culinary recipe, with only dosing the ingredients in well-balanced amounts. To formulate rather means to flexibly knit materials together with a lively stitch, meeting or repelling each other, building a pleasant form, which is neither fixed, nor solid, nor rigid. A fragrance has an overall structure, which ranges from a clear sound, made up of stable, unique, and linear items, to a background chat, comfortable and reassuring. But that does, of course, not mean that there is only one way of creating a fragrance!

  20. Peptide-Loaded Solid Lipid Nanoparticles Prepared through Coacervation Technique

    Directory of Open Access Journals (Sweden)

    Marina Gallarate

    2011-01-01

    Full Text Available Stearic acid solid lipid nanoparticles were prepared according to a new technique, called coacervation. The main goal of this experimental work was the entrapment of peptide drugs into SLN, which is a difficult task, since their chemical characteristics (molecular weight, hydrophilicity, and stability hamper peptide-containing formulations. Insulin and leuprolide, chosen as model peptide drugs, were encapsulated within nanoparticles after hydrophobic ion pairing with anionic surfactants. Peptide integrity was maintained after encapsulation, and nanoparticles can act in vitro as a sustained release system for peptide.

  1. BRST formulation of 4-monopoles

    CERN Document Server

    Gianvittorio, R; Restuccia, A

    1996-01-01

    A supersymmetric gauge invariant action is constructed over any 4-dimensional Riemannian manifold describing Witten's theory of 4-monopoles. The topological supersymmetric algebra closes off-shell. The multiplets include the auxiliary fields and the Wess-Zumino fields in an unusual way, arising naturally from BRST gauge fixing. A new canonical approach over Riemann manifolds is followed, using a Morse function as an euclidean time and taking into account the BRST boundary conditions that come from the BFV formulation. This allows a construction of the effective action starting from gauge principles.

  2. A Geometric Formulation of Supersymmetry

    CERN Document Server

    Freedman, Daniel Z; Van Proeyen, Antoine

    2016-01-01

    The scalar fields of supersymmetric models are coordinates of a geometric space. We propose a formulation of supersymmetry that is covariant with respect to reparametrizations of this target space. Employing chiral multiplets as an example, we introduce modified supersymmetry variations and redefined auxiliary fields that transform covariantly under reparametrizations. The resulting action and transformation laws are manifestly covariant and highlight the geometric structure of the supersymmetric theory. The covariant methods are developed first for general theories (not necessarily supersymmetric) whose scalar fields are coordinates of a Riemannian target space.

  3. The rational design of topical formulations

    OpenAIRE

    Duszynska-Krupa, A. M.

    2015-01-01

    This thesis addresses the development of topical formulations designed to treat atopic dermatitis (AD) using nicotinamide (NA). A rational approach to the development of topical formulations based on the physical and chemical properties of the drug and vehicle components is studied. This approach is an alternative to the model of formulation development where the drug is added into an existing vehicle without optimisation of the formulation in terms of the active delivery to its site of actio...

  4. Toxicology of antimicrobial nanoparticles for prosthetic devices

    OpenAIRE

    Nuñez-Anita, Rosa Elvira; Acosta-Torres, Laura Susana; Vilar-Pineda, Jorge; Martínez-Espinosa, Juan Carlos; de la Fuente-Hernández, Javier; Castaño, Víctor Manuel

    2014-01-01

    Advances in nanotechnology are producing an accelerated proliferation of new nanomaterial composites that are likely to become an important source of engineered health-related products. Nanoparticles with antifungal effects are of great interest in the formulation of microbicidal materials. Fungi are found as innocuous commensals and colonize various habitats in and on humans, especially the skin and mucosa. As growth on surfaces is a natural part of the Candida spp. lifestyle, one can expect...

  5. Formulation, Preparation, and Characterization of Polyurethane Foams

    Science.gov (United States)

    Pinto, Moises L.

    2010-01-01

    Preparation of laboratory-scale polyurethane foams is described with formulations that are easy to implement in experiments for undergraduate students. Particular attention is given to formulation aspects that are based on the main chemical reactions occurring in polyurethane production. This allows students to develop alternative formulations to…

  6. Encapsulation and retention of chelated-copper inside hydrophobic nanoparticles

    DEFF Research Database (Denmark)

    Hervella, Pablo; Parra, Elisa; Needham, David

    2016-01-01

    MOTIVATION: In the field of imaging, (18)F-fluorodeoxyglucose (FDG) PET imaging allows evaluation of glucose metabolism and is the most widely used imaging agent clinically for metastatic cancer. While it can certainly detect the metastatic disease, in order to provide a more fully "individualized...... that our endogenous-inspired nanoparticle strategies for imaging and therapeutics are focused on encapsulating and retaining imaging ions such as copper inside novel hydrophobic nanoparticles. In this paper, we describe a new approach to label the core of hydrophobic nanoparticles composed of Glyceryl...... Trioleate (Triolein) with copper using the hydrophobic chelator Octaethyl porphyrin (OEP). RESEARCH PLAN AND METHODS: The research plan for this study was to (1) Formulate nanoparticles and control nanoparticle size using a modification of the solvent injection technique, named fast ethanol injection; (2...

  7. Food protein-based phytosterol nanoparticles: fabrication and characterization.

    Science.gov (United States)

    Cao, Wen-Jun; Ou, Shi-Yi; Lin, Wei-Feng; Tang, Chuan-He

    2016-09-14

    The development of food-grade (nano)particles as a delivery system for poorly water soluble bioactives has recently attracted increasing attention. This work is an attempt to fabricate food protein-based nanoparticles as delivery systems for improving the water dispersion and bioaccessibility of phytosterols (PS) by an emulsification-evaporation method. The fabricated PS nanoparticles were characterized in terms of particle size, encapsulation efficiency (EE%) and loading amount (LA), and ξ-potential. Among all the test proteins, including soy protein isolate (SPI), whey protein concentrate (WPC) and sodium caseinate (SC), SC was confirmed to be the most suitable protein for the PS nano-formulation. Besides the type of protein, the particle size, EE% and LA of PS in the nanoparticles varied with the applied protein concentration in the aqueous phase and organic volume fraction. The freeze-dried PS nanoparticles with SC exhibited good water re-dispersion behavior and low crystallinity of PS. The LA of PS in the nanoparticles decreased upon storage, especially at high temperatures (e.g., >25 °C). The PS in the fabricated nanoparticles exhibited much better bioaccessibility than free PS. The findings would be of relevance for the fabrication of food-grade colloidal phytosterols, with great potential to be applied in functional food formulations.

  8. Nanoparticle-based therapy for respiratory diseases

    Directory of Open Access Journals (Sweden)

    ADRIANA L. DA SILVA

    2013-03-01

    Full Text Available Nanotechnology is an emerging science with the potential to create new materials and strategies involving manipulation of matter at the nanometer scale (<100 nm. With size-dependent properties, nanoparticles have introduced a new paradigm in pharmacotherapy – the possibility of cell-targeted drug delivery with minimal systemic side effects and toxicity. The present review provides a summary of published findings, especially regarding to nanoparticle formulations for lung diseases. The available data have shown some benefits with nanoparticle-based therapy in the development of the disease and lung remodeling in respiratory diseases. However, there is a wide gap between the concepts of nanomedicine and the published experimental data and clinical reality. In addition, studies are still required to determine the potential of nanotherapy and the systemic toxicity of nanomaterials for future human use.

  9. Comparative evaluation of the impact on endothelial cells induced by different nanoparticle structures and functionalization.

    Science.gov (United States)

    Landgraf, Lisa; Müller, Ines; Ernst, Peter; Schäfer, Miriam; Rosman, Christina; Schick, Isabel; Köhler, Oskar; Oehring, Hartmut; Breus, Vladimir V; Basché, Thomas; Sönnichsen, Carsten; Tremel, Wolfgang; Hilger, Ingrid

    2015-01-01

    In the research field of nanoparticles, many studies demonstrated a high impact of the shape, size and surface charge, which is determined by the functionalization, of nanoparticles on cell viability and internalization into cells. This work focused on the comparison of three different nanoparticle types to give a better insight into general rules determining the biocompatibility of gold, Janus and semiconductor (quantum dot) nanoparticles. Endothelial cells were subject of this study, since blood is the first barrier after intravenous nanoparticle application. In particular, stronger effects on the viability of endothelial cells were found for nanoparticles with an elongated shape in comparison to spherical ones. Furthermore, a positively charged nanoparticle surface (NH2, CyA) leads to the strongest reduction in cell viability, whereas neutral and negatively charged nanoparticles are highly biocompatible to endothelial cells. These findings are attributed to a rapid internalization of the NH2-functionalized nanoparticles in combination with the damage of intracellular membranes. Interestingly, the endocytotic pathway seems to be a size-dependent process whereas nanoparticles with a size of 20 nm are internalized by caveolae-mediated endocytosis and nanoparticles with a size of 40 nm are taken up by clathrin-mediated internalization and macropinocytosis. Our results can be summarized to formulate five general rules, which are further specified in the text and which determine the biocompatibility of nanoparticles on endothelial cells. Our findings will help to design new nanoparticles with optimized properties concerning biocompatibility and uptake behavior with respect to the respective intended application. PMID:25821668

  10. Comparative evaluation of the impact on endothelial cells induced by different nanoparticle structures and functionalization

    Directory of Open Access Journals (Sweden)

    Lisa Landgraf

    2015-01-01

    Full Text Available In the research field of nanoparticles, many studies demonstrated a high impact of the shape, size and surface charge, which is determined by the functionalization, of nanoparticles on cell viability and internalization into cells. This work focused on the comparison of three different nanoparticle types to give a better insight into general rules determining the biocompatibility of gold, Janus and semiconductor (quantum dot nanoparticles. Endothelial cells were subject of this study, since blood is the first barrier after intravenous nanoparticle application. In particular, stronger effects on the viability of endothelial cells were found for nanoparticles with an elongated shape in comparison to spherical ones. Furthermore, a positively charged nanoparticle surface (NH2, CyA leads to the strongest reduction in cell viability, whereas neutral and negatively charged nanoparticles are highly biocompatible to endothelial cells. These findings are attributed to a rapid internalization of the NH2-functionalized nanoparticles in combination with the damage of intracellular membranes. Interestingly, the endocytotic pathway seems to be a size-dependent process whereas nanoparticles with a size of 20 nm are internalized by caveolae-mediated endocytosis and nanoparticles with a size of 40 nm are taken up by clathrin-mediated internalization and macropinocytosis. Our results can be summarized to formulate five general rules, which are further specified in the text and which determine the biocompatibility of nanoparticles on endothelial cells. Our findings will help to design new nanoparticles with optimized properties concerning biocompatibility and uptake behavior with respect to the respective intended application.

  11. In vivo toxicity of enoxaparin encapsulated in mucoadhesive nanoparticles: Topical application in a wound healing model

    Science.gov (United States)

    Huber, S. C.; Marcato, P. D.; Barbosa, R. M.; Duran, N.; Annichino-Bizzacchi, J. M.

    2013-04-01

    Wound healing comprises four distinct phases and involves many cell events and biologic markers. The use of nanoparticles for topical application has gaining attention due to its deeper penetration in the skin and the retention capacity of the drug in the site of application. In this study the effect and toxicity of mucoadhesive polymeric nanoparticles loaded with enoxaparin was evaluated in in vivo model of skin ulcer. Our results showed an interesting formulation based on mucoadhesive nanoparticles with enoxaparin that improved wound healing without cytotoxicity in vitro in all endpoint evaluated. Then, this semi-solid formulation is a promising option for skin ulcer treatment.

  12. PRODUCTION MIX PROBLEMS: FORMULATION AND SOLUTION STRATEGIES

    Directory of Open Access Journals (Sweden)

    Graeme Warren

    2012-01-01

    Full Text Available

    ENGLISH ABSTRACT: This paper examines the sub-optimality of generalized greedy heuristics for solut ion of a certain well-known production mix problem formulation . The drawbacks of not modelling routing in the mix problem formulation are discussed, and an alternati ve mix prob lem formulation (with assoc iated solution strategies is proposed .

    AFRIKAANSE OPSOMMING: Hierdie artikel verduidelik die sub-optirnaliteit van ' n algemene gulsige heuristiek vir 'n sekere bekende produkmengsel probleemformulering. Die nadele van weglating van produk roete inligting in die formulering is bespreek, en ' n alternatiewe formulering (met geassosieerde oplossingsstrategiee is voorgestel.

  13. Physiologically based pharmacokinetic modeling of PLGA nanoparticles with varied mPEG content

    Directory of Open Access Journals (Sweden)

    Avgoustakis K

    2012-03-01

    Full Text Available Mingguang Li1, Zoi Panagi2, Konstantinos Avgoustakis2, Joshua Reineke11Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI, USA; 2Pharmaceutical Technology Laboratory, Department of Pharmacy, University of Patras, Rion, Patras, GreeceAbstract: Biodistribution of nanoparticles is dependent on their physicochemical properties (such as size, surface charge, and surface hydrophilicity. Clear and systematic understanding of nanoparticle properties' effects on their in vivo performance is of fundamental significance in nanoparticle design, development and optimization for medical applications, and toxicity evaluation. In the present study, a physiologically based pharmacokinetic model was utilized to interpret the effects of nanoparticle properties on previously published biodistribution data. Biodistribution data for five poly(lactic-co-glycolic acid (PLGA nanoparticle formulations prepared with varied content of monomethoxypoly (ethyleneglycol (mPEG (PLGA, PLGA-mPEG256, PLGA-mPEG153, PLGA-mPEG51, PLGA-mPEG34 were collected in mice after intravenous injection. A physiologically based pharmacokinetic model was developed and evaluated to simulate the mass-time profiles of nanoparticle distribution in tissues. In anticipation that the biodistribution of new nanoparticle formulations could be predicted from the physiologically based pharmacokinetic model, multivariate regression analysis was performed to build the relationship between nanoparticle properties (size, zeta potential, and number of PEG molecules per unit surface area and biodistribution parameters. Based on these relationships, characterized physicochemical properties of PLGA-mPEG495 nanoparticles (a sixth formulation were used to calculate (predict biodistribution profiles. For all five initial formulations, the developed model adequately simulates the experimental data indicating that the model is suitable for

  14. Using a modified shepards method for optimization of a nanoparticulate cyclosporine a formulation prepared by a static mixer technique.

    Science.gov (United States)

    Douroumis, Dionysios; Scheler, Stefan; Fahr, Alfred

    2008-02-01

    An innovative methodology has been used for the formulation development of Cyclosporine A (CyA) nanoparticles. In the present study the static mixer technique, which is a novel method for producing nanoparticles, was employed. The formulation optimum was calculated by the modified Shepard's method (MSM), an advanced data analysis technique not adopted so far in pharmaceutical applications. Controlled precipitation was achieved injecting the organic CyA solution rapidly into an aqueous protective solution by means of a static mixer. Furthermore the computer based MSM was implemented for data analysis, visualization, and application development. For the optimization studies, the gelatin/lipoid S75 amounts and the organic/aqueous phase were selected as independent variables while the obtained particle size as a dependent variable. The optimum predicted formulation was characterized by cryo-TEM microscopy, particle size measurements, stability, and in vitro release. The produced nanoparticles contain drug in amorphous state and decreased amounts of stabilizing agents. The dissolution rate of the lyophilized powder was significantly enhanced in the first 2 h. MSM was proved capable to interpret in detail and to predict with high accuracy the optimum formulation. The mixer technique was proved capable to develop CyA nanoparticulate formulations. PMID:17853428

  15. Formulation and Optimization of Eudragit RS PO-Tenofovir Nanocarriers Using Box-Behnken Experimental Design

    Directory of Open Access Journals (Sweden)

    Kefilwe Matlhola

    2015-01-01

    Full Text Available The objective of present study was to develop an optimized polymeric nanoparticle system for the antiretroviral drug tenofovir. A modified nanoprecipitation method was used to prepare Eudragit RS PO nanoparticles of the drug. The effect of amount of polymer, surfactant concentration, and sonication time on particle size, particle distribution, encapsulation efficiency (EE, and zeta potential were assessed and optimized utilizing a three-factor, three-level Box-Behnken Design (BBD of experiment. Fifteen formulations of nanoparticles were prepared as per BBD and evaluated for particle size, polydispersity index (PDI, EE, and zeta potential. The results showed that the measured mean particle sizes were in the range of 233 to 499 nm, PDI ranged from 0.094 to 0.153, average zeta potential ranged from −19.9 to −45.8 mV, and EE ranged between 98 and 99%. The optimized formulation was characterized for in vitro drug release and structural characterization. The mean particle size of this formulation was 233 nm with a PDI of 0.0107. It had a high EE of 98% and average zeta potential of −35 mV, an indication of particle stability. The FTIR showed some noncovalent interactions between the drug and polymer but a sustained release was observed in vitro for up to 80 hours.

  16. Lipid Self-Assemblies and Nanostructured Emulsions for Cosmetic Formulations

    Directory of Open Access Journals (Sweden)

    Chandrashekhar V. Kulkarni

    2016-10-01

    Full Text Available A majority of cosmetic products that we encounter on daily basis contain lipid constituents in solubilized or insolubilized forms. Due to their amphiphilic nature, the lipid molecules spontaneously self-assemble into a remarkable range of nanostructures when mixed with water. This review illustrates the formation and finely tunable properties of self-assembled lipid nanostructures and their hierarchically organized derivatives, as well as their relevance to the development of cosmetic formulations. These lipid systems can be modulated into various physical forms suitable for topical administration including fluids, gels, creams, pastes and dehydrated films. Moreover, they are capable of encapsulating hydrophilic, hydrophobic as well as amphiphilic active ingredients owing to their special morphological characters. Nano-hybrid materials with more elegant properties can be designed by combining nanostructured lipid systems with other nanomaterials including a hydrogelator, silica nanoparticles, clays and carbon nanomaterials. The smart materials reviewed here may well be the future of innovative cosmetic applications.

  17. On Hamiltonian formulation of cosmologies

    Indian Academy of Sciences (India)

    K D Krori; S Dutta

    2000-03-01

    Novello et al [1,2] have shown that it is possible to find a pair of canonically conjugate variables (written in terms of gauge-invariant variables) so as to obtain a Hamiltonian that describes the dynamics of a cosmological system. This opens up the way to the usual technique of quantization. Elbaz et al [4] have applied this method to the Hamiltonian formulation of FRW cosmological equations. This note presents a generalization of this approach to a variety of cosmologies. A general Schrödinger wave equation has been derived and exact solutions have been worked out for the stiff matter era for some cosmological models. It is argued that these solutions appear to hint at their possible relevance in the early phase of cosmological evolution.

  18. Hamiltonian formulation of teleparallel gravity

    CERN Document Server

    Ferraro, Rafael

    2016-01-01

    The Hamiltonian formulation of the teleparallel equivalent of general relativity (TEGR) is developed from an ordinary second-order Lagrangian, which is written as a quadratic form of the coefficients of anholonomy of the orthonormal frames (vielbeins). We analyze the structure of eigenvalues of the multi-index matrix entering the (linear) relation between canonical velocities and momenta to obtain the set of primary constraints. The canonical Hamiltonian is then built with the Moore-Penrose pseudo-inverse of that matrix. The set of constraints, including the subsequent secondary constraints, completes a first class algebra. This means that all of them generate gauge transformations. The gauge freedoms are basically the diffeomorphisms, and the (local) Lorentz transformations of the vielbein. In particular, the ADM algebra of general relativity is recovered as a sub-algebra.

  19. Dynamic light scattering and atomic force microscopy techniques for size determination of polyurethane nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Giehl Zanetti-Ramos, Betina [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas (Brazil)], E-mail: betinagzramos@pq.cnpq.br; Beddin Fritzen-Garcia, Mauricia [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas (Brazil); Schweitzer de Oliveira, Cristian; Avelino Pasa, Andre [Laboratorio de Filmes Finos e Superficie, Departamento de Fisica (Brazil); Soldi, Valdir [Grupo de Estudos em Materiais Polimericos, Departamento de Quimica, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); Borsali, Redouane [Centre de Recherche sur les Macromolecules Vegetales CERMAV/CNRS, 38041 - Grenoble (France); Creczynski-Pasa, Tania Beatriz [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas (Brazil)

    2009-03-01

    Nanoparticles have applications in various industrial fields principally in drug delivery. Nowadays, there are several processes for manufacturing colloidal polymeric systems and methods of preparation as well as of characterization. In this work, Dynamic Light Scattering and Atomic Force Microscopy techniques were used to characterize polyurethane nanoparticles. The nanoparticles were prepared by miniemulsion technique. The lipophilic monomers, isophorone diisocyanate (IPDI) and natural triol, were emulsified in water containing surfactant. In some formulations the poly(ethylene glycol) was used as co-monomer to obtain the hydrophilic and pegylated nanoparticles. Polyurethane nanoparticles observed by atomic force microscopy (AFM) were spherical with diameter around 209 nm for nanoparticles prepared without PEG. From AFM imaging two populations of nanoparticles were observed in the formulation prepared with PEG (218 and 127 nm) while dynamic light scattering (DLS) measurements showed a monodisperse size distribution around 250 nm of diameters for both formulations. The polydispersity index of the formulations and the experimental procedures could influence the particle size determination with these techniques.

  20. Photoelectron emission from plasmonic nanoparticles: Comparison between surface and volume photoelectric effects

    CERN Document Server

    Uskov, Alexander V; Ikhsanov, Renat Sh; Babicheva, Viktoriia E; Zhukovsky, Sergei V; Lavrinenko, Andrey V; OReilly, Eoin P; Xu, Hongxing

    2013-01-01

    We study emission of photoelectrons from plasmonic nanoparticles into surrounding matrix. We consider two mechanisms of the photoelectric effect from nanoparticles - surface and volume ones, and use models of these two effects which allow us to obtain analytical results for the photoelectron emission rates from nanoparticle. Calculations have been done for the step potential at surface of spherical nanoparticle, and the simple model for the hot electron cooling have been used. We highlight the effect of the discontinuity of the dielectric permittivity at the nanoparticle boundary in the surface mechanism, which leads to substantial (by 5 times) increase of photoelectron emission rate from nanoparticle compared to the case when such discontinuity is absent. For plasmonic nanoparticle, a comparison of two mechanisms of the photoeffect was done for the first time and showed that surface photoeffect, at least, does not concede the volume one, which agrees with results for the flat metal surface first formulated b...

  1. New Generation of Silver Nanoparticles against Extended Spectrum Beta Lactamase Producing Organisms

    Directory of Open Access Journals (Sweden)

    Bindu D

    2015-08-01

    Full Text Available Silver nanoparticles are nanoparticles of silver which are in the range of 1 and 100 nm in size. Silver nanoparticles are used in antimicrobial agents, textile industries, water treatment, sunscreen lotions etc. Biological synthesis of silver nanoparticles using microorganisms has received profound interest because of their potential to synthesize nanoparticles of various size, shape and morphology. In this study, a simple biological and low cost approach for preparation of stable silver nanoparticles by reduction of silver nitrate solution with a bioreduction method using Pseudomonas aeruginosa has been reported. Silver nanoparticles were found to have antibacterial activity against extended spectrum beta lactamase producing organisms like Escherichia coli and Klebsiella pneumoniae. These nontoxic materials which can be prepared in a simple and cost effective manner may be suitable for the formulation of new types of bactericidal materials. Hence it has wide application in medical field.

  2. Preparation,formulation optimization and preliminary pharmacodynamic experi-ment of insulin-loaded N-trimethyl chitosan nanoparticles%季铵化壳聚糖胰岛素纳米粒的制备、处方优化及其初步药效学实验

    Institute of Scientific and Technical Information of China (English)

    苑旺; 王美玲; 石岩; 崔黎丽

    2015-01-01

    目的:采用正交设计试验优化载胰岛素季铵化壳聚糖纳米粒的处方工艺,并初步考察其降糖效果。方法用离子交联法制备载胰岛素的季铵化壳聚糖纳米粒,用正交试验确定其最佳处方工艺。用透射电子显微镜观察纳米粒的表面形态;用粒径/Zeta电位仪测定纳米粒的粒径和Zeta电位;用高效液相色谱(HPLC)法测定纳米粒的包封率、载药量及体外释放情况。对糖尿病大鼠皮下注射给药,对其药效学进行初步考察。结果制得的纳米粒呈球形,分布均匀;平均粒径(63.26±1.88) nm ;Zeta电位(33.1±0.3) mV ;包封率(37.92±2.11)%;载药量(5.42±0.3)%;24 h累计释放率63.83%。皮下注射给药8h,糖尿病大鼠血糖较单纯注射胰岛素组下降平缓,且药效持久。结论优化后的载胰岛素的季铵化壳聚糖纳米粒形态较好、粒径较小,为研究胰岛素的新型给药途径奠定了基础。%Objective To prepare and optimize insulin-loaded N-trimethyl chitosan nanoparticles via orthogonal design , and preliminarily study the effects on blood glucose level .Methods The insulin-loaded N-trimethyl chitosan nanoparticles (INS-NPs) were prepared by ionic gelation ,and the optimal proportion was obtained with orthogonal design .The nanoparticles were characterized by transmission electron microscopy and zeta/sizer nano analyzer .The entrapment efficiency of insulin-load-ed nanoparticles and the in vitro releasing characteristics were studied by HPLC .A preliminary pharmacodynamic study of the insulin-loaded nanoparticles was also carried out .Results The INS-NPs exhibited narrow distribution .The mean diameter of INS-NPs was (63 .26 ± 1 .88)nm ,while the entrapment efficiency was (37 .92 ± 2 .11)% .After 8 hours of subcutaneous injec-tion of the INS-NPs ,the blood glucose level in diabetic rats decreased to normal level and kept stable .Conclusion The

  3. On fictitious domain formulations for Maxwell's equations

    DEFF Research Database (Denmark)

    Dahmen, W.; Jensen, Torben Klint; Urban, K.

    2003-01-01

    We consider fictitious domain-Lagrange multiplier formulations for variational problems in the space H(curl: Omega) derived from Maxwell's equations. Boundary conditions and the divergence constraint are imposed weakly by using Lagrange multipliers. Both the time dependent and time harmonic...... formulations of the Maxwell's equations are considered. and we derive well-posed formulations for both cases. The variational problem that arises can be discretized by functions that do not satisfy an a-priori divergence constraint....

  4. Formulation of disperse systems science and technology

    CERN Document Server

    Tadros, Tharwat F

    2014-01-01

    This book presents comprehensively the science and technology behind the formulation of disperse systems like emulsions, suspensions, foams and others. Starting with a general introduction, the book covers a broad range of topics like the role of different classes of surfactants, stability of disperse systems, formulation of different dispersions, evaluation of formulations and many more. Many examples are included, too. Written by the experienced author and editor Tharwart Tadros, this book is indispensable for every scientist working in the field.

  5. Pediatric drug development: formulation considerations.

    Science.gov (United States)

    Ali, Areeg Anwer; Charoo, Naseem Ahmad; Abdallah, Daud Baraka

    2014-10-01

    Absence of safe, effective and appropriate treatment is one of the main causes of high mortality and morbidity rates among the pediatric group. This review provides an overview of pharmacokinetic differences between pediatric and adult population and their implications in pharmaceutical development. Different pediatric dosage forms, their merits and demerits are discussed. Food and Drug Administration Act of 1997 and the Best Pharmaceuticals for Children Act 2002 added 6 months patent extension and exclusivity incentives to pharmaceutical companies for evaluation of medicinal products in children. Prescription Drug User Fee Act and Food and Drug Administration Amendments Act of 2007 made it mandatory for pharmaceutical companies to perform pediatric clinical studies on new drug products. Drug development program should include additional clinical bridge studies to evaluate differences in pharmacokinetics and pharmacodynamics of drugs in adult and child populations. Additionally, pharmaceutical development should consider ease of administration, palatability, appropriate excipients, stability and therapeutic equivalency of pediatric dosage forms. Pediatric population is diverse with individual preferences and demand for custom made dosage formulations. Practically it is not feasible to have different pharmaceutical dosage forms for each group. Hence, an appropriate dosage form that can be administered across pediatric population is warranted. PMID:24483293

  6. MOND and its bimetric formulation

    CERN Document Server

    Milgrom, Mordehai

    2013-01-01

    I first give a succinct account of the MOND paradigm--emphasizing the centrality of scale invariance in the nonrelativistic, deep-MOND limit--and describing rudiments of its phenomenology. I then present my credo, and some generalities, concerning existing MOND theories. Then I concentrate on one relativistic formulation of MOND in the form of a bimetric theory (BIMOND). I describe its various limits: the weak field, with application to gravitational waves, the nonrelativistic limit, and their further deep-MOND (low acceleration) limits, which are scale invariant. Other aspects of BIMOND that have been explored are aspects of cosmology, matter fluctuations in cosmology, and matter-twin-matter interactions. BIMOND remains largely unexplored, despite its promise in several regards: It tends to GR for a0 goes to 0 (a0 is the MOND constant); it has a simple nonrelativistic limit; it describes gravitational lensing correctly; and, it has a generic appearance of a cosmological-constant term that is of order a0^2/c^...

  7. Postmodern string theory stochastic formulation

    CERN Document Server

    Aurilia, A

    1994-01-01

    In this paper we study the dynamics of a statistical ensemble of strings, building on a recently proposed gauge theory of the string geodesic field. We show that this stochastic approach is equivalent to the Carath\\'eodory formulation of the Nambu-Goto action, supplemented by an averaging procedure over the family of classical string world-sheets which are solutions of the equation of motion. In this new framework, the string geodesic field is reinterpreted as the Gibbs current density associated with the string statistical ensemble. Next, we show that the classical field equations derived from the string gauge action, can be obtained as the semi-classical limit of the string functional wave equation. For closed strings, the wave equation itself is completely analogous to the Wheeler-DeWitt equation used in quantum cosmology. Thus, in the string case, the wave function has support on the space of all possible spatial loop configurations. Finally, we show that the string distribution induces a multi-phase, or ...

  8. Hamiltonian formulation of reduced magnetohydrodynamics

    International Nuclear Information System (INIS)

    Reduced magnetohydrodynamics (RMHD) has become a principal tool for understanding nonlinear processes, including disruptions, in tokamak plasmas. Although analytical studies of RMHD turbulence have been useful, the model's impressive ability to simulate tokamak fluid behavior has been revealed primarily by numerical solution. The present work describes a new analytical approach, not restricted to turbulent regimes, based on Hamiltonian field theory. It is shown that the nonlinear (ideal) RMHD system, in both its high-beta and low-beta versions, can be expressed in Hanmiltonian form. Thus a Poisson bracket, [ , ], is constructed such that each RMHD field quantitity, xi/sub i/, evolves according to xi/sub i/ = [xi/sub i/,H], where H is the total field energy. The new formulation makes RMHD accessible to the methodology of Hamiltonian mechanics; it has lead, in particular, to the recognition of new RMHD invariants and even exact, nonlinear RMHD solutions. A canonical version of the Poisson bracket, which requires the introduction of additional fields, leads to a nonlinear variational principle for time-dependent RMHD

  9. In vivo gene delivery with L-tyrosine polyphosphate nanoparticles.

    Science.gov (United States)

    Ditto, Andrew J; Reho, John J; Shah, Kush N; Smolen, Justin A; Holda, James H; Ramirez, Rolando J; Yun, Yang H

    2013-05-01

    The concept of gene therapy is promising; however, the perceived risks and side effects associated with this technology have severely dampened the researchers' enthusiasm. Thus, the development of a nonviral gene vector without immunological effects and with high transfection efficiency is necessary. Currently, most nonviral vectors have failed to achieve the in vivo transfection efficiencies of viral vectors due to their toxicity, rapid clearance, and/or inappropriate release rates. Although our previous studies have successfully demonstrated the controlled-release of plasmid DNA (pDNA) polyplexes encapsulated into nanoparticles formulated with l-tyrosine polyphosphate (LTP-pDNA nanoparticles), the in vivo transfection capabilities and immunogenicity of this delivery system have yet to be examined. Thus, we evaluate LTP-pDNA nanoparticles in an in vivo setting via injection into rodent uterine tissue. Our results demonstrate through X-gal staining and immunohistochemistry of uterine tissue that transfection has successfully occurred after a nine-day incubation. In contrast, the results for the control nanoparticles show results similar to those of shams. Furthermore, reverse transcriptase polymerase chain reaction (RT-PCR) from the injected tissues confirms the transfection in vivo. To examine the immunogenicity, the l-tyrosine polyphosphate (LTP) nanoparticles have been evaluated in a mouse model. No significant differences in the activation of the innate immune system are observed. These data provide the first report for the potential use of controlled-release nanoparticles formulated from an amino acid based polymer as an in vivo nonviral vector for gene therapy.

  10. FORMULATION OF CLINDAMYCIN NANO-EMULSION

    Directory of Open Access Journals (Sweden)

    K. Jiyauddin *, A. Fadli , J. C. Wei , A. Jawad , A. D. Samer , M. Kaleemullah, S. Budiasih, S. Rasha , M. R. Rasny , Y. K. Sung , A. H. Junainah , H. Todo and Y. Eddy

    2015-05-01

    Full Text Available Nano-emulsions consist of fine oil-in-water or water-in-oil dispersions, having droplets covering the size range of 10 - 600 nm. The aim of this study is to formulate nano-emulsion of Clindamycin by using Emulsion Phase Inversion method and olive oil as the oil phase. Pseudo ternary phase diagram was first developed by using distilled water, olive oil and mixture of surfactants (Tween®80 and Span®20 at a ratio of 1:1. Then, appearance test and microscopic examination were done for all the pre-formulation. Three potential pre-formulation were then selected and incorporated with the Clindamycin Phosphate and Methyl Paraben. The mean droplet size and stability studies were done for these three formulations. Clindamycin Nano-emulsions were not obtained using the Emulsion Phase Inversion (EPI method in this study, whereby the mean droplet sizes were in micro-range. However, out of all the three formulations which undergone extensive studies which include the heating-cooling cycle, whereby the formulation F8 and F17 were found to be physically stable. Significant differences were identified on the pH value and viscosity measurement for all the three formulations which undergone the heating-cooling cycle; except for the pH in F17. Furthermore, the formulation F8 had the smallest droplet size of 0.92 µm. Future research on this topic is needed to reduce the droplet size of the formulation.

  11. Necessity of rethinking oral pediatric formulations

    DEFF Research Database (Denmark)

    Bar-Shalom, Daniel

    2014-01-01

    This commentary reviews the difficulties in formulating oral products for children. The significance of the fragmentation of the pediatric population in terms of development and ability to ingest different dosage formulations is examined. It is postulated that a flexible formulation, acceptable...... by all patient groups, is needed, and an automated compounding concept is proposed. The finishing of the formulation is done at the dispensing pharmacy using an automated process. The individual components (pudding-like carrier, microencapsulated drug, and the dispensing robot and its software...

  12. A novel paclitaxel-loaded poly(epsilon-caprolactone)/Poloxamer 188 blend nanoparticle overcoming multidrug resistance for cancer treatment.

    Science.gov (United States)

    Zhang, Yangqing; Tang, Lina; Sun, Leilei; Bao, Junbo; Song, Cunxian; Huang, Laiqiang; Liu, Kexin; Tian, Yan; Tian, Ge; Li, Zhen; Sun, Hongfan; Mei, Lin

    2010-06-01

    Multidrug resistance (MDR) of tumor cells is a major obstacle to the success of cancer chemotherapy. Poloxamers have been used in cancer therapy to overcome MDR. The objective of this research is to test the feasibility of paclitaxel-loaded poly(epsilon-caprolactone)/Poloxamer 188 (PCL/Poloxamer 188) nanoparticles to overcome MDR in a paclitaxel-resistant human breast cancer cell line. Paclitaxel-loaded nanoparticles were prepared by a water-acetone solvent displacement method using commercial PCL and self-synthesized PCL/Poloxamer 188 compound, respectively. PCL/Poloxamer 188 nanoparticles were found to be of spherical shape and tended to have a rough and porous surface. The nanoparticles had an average size of around 220nm, with a narrow size distribution. The in vitro drug release profile of both nanoparticle formulations showed a clear biphasic release pattern. There was an increased level of uptake of PCL/Poloxamer 188 nanoparticles (PPNP) in the paclitaxel-resistant human breast cancer cell line MCF-7/TAX, in comparison with PCL nanoparticles. The cytotoxicity of PCL nanoparticles was higher than commercial Taxol in the MCF-7/TAX cell culture, but the differences were not significant. However, the PCL/Poloxamer 188 nanoparticles achieved a significantly higher level of cytotoxicity than both of PCL nanoparticle formulation and Taxol(R), indicating that paclitaxel-loaded PCL/Poloxamer 188 nanoparticles could overcome MDR in human breast cancer cells and therefore could have considerable therapeutic potential for breast cancer. PMID:19969111

  13. Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study

    Science.gov (United States)

    Bohrey, Sarvesh; Chourasiya, Vibha; Pandey, Archna

    2016-03-01

    Nanoparticles formulated from biodegradable polymers like poly(lactic-co-glycolic acid) (PLGA) are being extensively investigated as drug delivery systems due to their two important properties such as biocompatibility and controlled drug release characteristics. The aim of this work to formulated diazepam loaded PLGA nanoparticles by using emulsion solvent evaporation technique. Polyvinyl alcohol (PVA) is used as stabilizing agent. Diazepam is a benzodiazepine derivative drug, and widely used as an anticonvulsant in the treatment of various types of epilepsy, insomnia and anxiety. This work investigates the effects of some preparation variables on the size and shape of nanoparticles prepared by emulsion solvent evaporation method. These nanoparticles were characterized by photon correlation spectroscopy (PCS), transmission electron microscopy (TEM). Zeta potential study was also performed to understand the surface charge of nanoparticles. The drug release from drug loaded nanoparticles was studied by dialysis bag method and the in vitro drug release data was also studied by various kinetic models. The results show that sonication time, polymer content, surfactant concentration, ratio of organic to aqueous phase volume, and the amount of drug have an important effect on the size of nanoparticles. Hopefully we produced spherical shape Diazepam loaded PLGA nanoparticles with a size range under 250 nm with zeta potential -23.3 mV. The in vitro drug release analysis shows sustained release of drug from nanoparticles and follow Korsmeyer-Peppas model.

  14. The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability

    Directory of Open Access Journals (Sweden)

    Ma YR

    2012-02-01

    Full Text Available Yiran Ma, Xinyi Zhao, Jian Li, Qi ShenSchool of Pharmacy, Shanghai Jiao Tong University, Shanghai, ChinaAbstract: The aim of this research was to increase the oral bioavailability of daidzein by the formulations of poly(lactic-co-glycolic acid (PLGA nanoparticles loaded with daidzein. Amongst the various traditional and novel techniques of preparing daidzein-loaded PLGA nanoparticles, daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were selected. The average drug entrapment efficiency, particle size, and zeta potential of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were 81.9% ± 5%, 309.2 ± 14.0 nm, -32.14 ± 2.53 mV and 83.2% ± 7.2%, 323.2 ± 4.8 nm, -18.73 ± 1.68 mV, respectively. The morphological characterization of nanoparticles was observed with scanning electron microscopy by stereological method and the physicochemical state of nanoparticles was valued by differential scanning calorimetry. The in vitro drug-release profile of both nanoparticle formulations fitted the Weibull dynamic equation. Pharmacokinetic studies demonstrated that after oral administration of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles to rats at a dose of 10 mg/kg, relative bioavailability was enhanced about 5.57- and 8.85-fold, respectively, compared to daidzein suspension as control. These results describe an effective strategy for oral delivery of daidzein-loaded PLGA nanoparticles and might provide a fresh approach to enhancing the bioavailability of drugs with poor lipophilic and poor hydrophilic properties.Keywords: daidzein, phospholipid complexes, cyclodextrin inclusion complexes, PLGA, nanoparticles

  15. Chemicals-Based Formulation Design: Virtual Experimentations

    DEFF Research Database (Denmark)

    Conte, Elisa; Gani, Rafiqul

    2011-01-01

    This paper presents a systematic procedure for virtual experimentations related to the design of liquid formulated products. All the experiments that need to be performed when designing a liquid formulated product (lotion), such as ingredients selection and testing, solubility tests, property...... measurements, can now be performed through the virtual Product-Process Design laboratory [[1], [2] and [3

  16. Digluconate and Isopropyl Alcohol Biocide Formulation

    Directory of Open Access Journals (Sweden)

    Barbara Conway

    2012-10-01

    Full Text Available Effective surface disinfection is a fundamental infection control strategy within healthcare. This study assessed the antimicrobial efficacy of novel biocide formulations comprising 5% and 2% eucalyptus oil (EO combined with 2% chlorhexidine digluconate (CHG and 70% isopropyl alcohol (IPA contained within a wipe. The efficacy of this novel antimicrobial formulation to remove and eliminate methicillin-resistant Staphylococcus aureus (MRSA, Escherichia coli and Candida albicans from steel surfaces was investigated. Adpression studies of pre-contaminated wipes were also utilised to assess their potential to induce cross-contamination between hard surfaces. Furthermore, the bactericidal nature of the EO-formulation was established in addition to time-kill. The EO-containing formulations demonstrated bactericidal antimicrobial efficacy against all microorganisms and did not induce surface cross-contamination. There was no significant difference (p < 0.05 between the 5% and 2% EO formulations in their ability to remove microorganisms from steel surfaces, however both significantly (p < 0.05 removed more than the control formulations. Microbial biofilms were eliminated within 10 min (p < 0.05 when exposed to the EO formulations. Our novel EO-formulation demonstrated rapid antimicrobial efficacy for potential disinfection and elimination of microbial biofilms from hard surfaces and may therefore be a useful adjunct to current infection control strategies currently employed within healthcare facilities.

  17. A New Resistance Formulation for Carbon Nanotubes

    Directory of Open Access Journals (Sweden)

    Ji-Huan He

    2008-01-01

    Full Text Available A new resistance formulation for carbon nanotubes is suggested using fractal approach. The new formulation is also valid for other nonmetal conductors including nerve fibers, conductive polymers, and molecular wires. Our theoretical prediction agrees well with experimental observation.

  18. Bioavailability of sustained-release theophylline formulations.

    Science.gov (United States)

    Bonora Regazzi, M; Rondanelli, R; Vidale, E; Cristiani, D

    1983-05-01

    Sustained-release formulations of theophylline as well as of other drugs are designed to effect a delayed but constant release of the active principle in the gastrointestinal tract, thus ensuring more prolonged blood level curves. This study was made to assess the bioavailability of two sustained-release microencapsulated formulations and one sustained-release Diffucaps formulation, in comparison with an equivalent dose of theophylline solution. As regards bioavailability, none of the three formulations differed significantly from the reference formulation. The blood levels at steady state were estimated on the basis of data obtained after a single-dose study. All three sustained release formulations showed good results after prolonged administration in terms of peaks and troughs. The time duration at which the theophylline plasma levels remain higher than 75% of the maximum steady-state levels, following 12-h dosing interval, was evaluated: for the sustained-release microencapsulated formulations this time duration reaches 100% of the dosing interval. A multiple-dose administration of the sustained-release formulations used in this study should guarantee almost complete time coverage, with blood levels sharply exceeding the minimum threshold level of the theophylline therapeutic range.

  19. Similarity Measures for Boolean Search Request Formulations.

    Science.gov (United States)

    Radecki, Tadeusz

    1982-01-01

    Proposes a means for determining the similarity between search request formulations in online information retrieval systems, and discusses the use of similarity measures for clustering search formulations and document files in such systems. Experimental results using the proposed methods are presented in three tables. A reference list is provided.…

  20. Development and evaluation of paclitaxel nanoparticles using a quality-by-design approach.

    Science.gov (United States)

    Yerlikaya, Firat; Ozgen, Aysegul; Vural, Imran; Guven, Olgun; Karaagaoglu, Ergun; Khan, Mansoor A; Capan, Yilmaz

    2013-10-01

    The aims of this study were to develop and characterize paclitaxel nanoparticles, to identify and control critical sources of variability in the process, and to understand the impact of formulation and process parameters on the critical quality attributes (CQAs) using a quality-by-design (QbD) approach. For this, a risk assessment study was performed with various formulation and process parameters to determine their impact on CQAs of nanoparticles, which were determined to be average particle size, zeta potential, and encapsulation efficiency. Potential risk factors were identified using an Ishikawa diagram and screened by Plackett-Burman design and finally nanoparticles were optimized using Box-Behnken design. The optimized formulation was further characterized by Fourier transform infrared spectroscopy, X-ray diffractometry, differential scanning calorimetry, scanning electron microscopy, atomic force microscopy, and gas chromatography. It was observed that paclitaxel transformed from crystalline state to amorphous state while totally encapsulating into the nanoparticles. The nanoparticles were spherical, smooth, and homogenous with no dichloromethane residue. In vitro cytotoxicity test showed that the developed nanoparticles are more efficient than free paclitaxel in terms of antitumor activity (more than 25%). In conclusion, this study demonstrated that understanding formulation and process parameters with the philosophy of QbD is useful for the optimization of complex drug delivery systems.

  1. Polymeric Nanoparticles, Nanospheres and Nanocapsules, for Cutaneous Applications

    Directory of Open Access Journals (Sweden)

    Adriana R. Pohlmann

    2007-01-01

    Full Text Available This review presents an overview about pharmaceutical and cosmetic topical products containing polymeric nanoparticles (nanospheres and nanocapsules, reporting the main preparation and characterization methods and the studies of penetration and transport of substances through the skin. The penetration and transport extent of those systems through the skin depends on the ingredients chemical composition, on the encapsulation mechanism influencing the drug release, on the size of nanoparticles and on the viscosity of the formulations. The polymeric nanoparticles are able to modify the activity of drugs, delay and control the drug release, and increase the drug adhesivity or its time of permanence in the skin. Briefly, the nanoparticles can be useful as reservoirs of lipophilic drugs to deliver them in the stratum corneum becoming an important strategy to control their permeation into the skin.

  2. Inherent formulation issues of kinase inhibitors.

    Science.gov (United States)

    Herbrink, M; Schellens, J H M; Beijnen, J H; Nuijen, B

    2016-10-10

    The small molecular Kinase Inhibitor (smKI) drug class is very promising and rapidly expanding. All of these drugs are administered orally. The clear relationship between structure and function has led to drugs with a general low intrinsic solubility. The majority of the commercial pharmaceutical formulations of the smKIs are physical mixtures that are limited by the low drug solubility of a salt form. This class of drugs is therefore characterized by an impaired and variable bioavailability rendering them costly and their therapies suboptimal. New formulations are sparingly being reported in literature and patents. The presented data suggests that continued research into formulation design can help to develop more efficient and cost-effective smKI formulation. Moreover, it may also be of help in the future design of the formulations of new smKIs.

  3. Thiolated chitosan nanoparticles for enhancing oral absorption of docetaxel: preparation, in vitro and ex vivo evaluation

    Science.gov (United States)

    Saremi, Shahrooz; Atyabi, Fatemeh; Akhlaghi, Seyedeh Parinaz; Ostad, Seyed Nasser; Dinarvand, Rassoul

    2011-01-01

    The aim of this study was to prepare and evaluate mucoadhesive core-shell nanoparticles based on copolymerization of thiolated chitosan coated on poly methyl methacrylate cores as a carrier for oral delivery of docetaxel. Docetaxel-loaded nanoparticles with various concentrations were prepared via a radical emulsion polymerization method using cerium ammonium nitrate as an initiator. The physicochemical properties of the obtained nanoparticles were characterized by: dynamic light-scattering analysis for their mean size, size distribution, and zeta potential; scanning electron microscopy and transmission electron microscopy for surface morphology; and differential scanning calorimetry analysis for confirmation of molecular dispersity of docetaxel in the nanoparticles. Nanoparticles were spherical with mean diameter below 200 nm, polydispersity of below 0.15, and positive zeta potential values. The entrapment efficiency of the nanoparticles was approximately 90%. In vitro release studies showed a sustained release characteristic for 10 days after a burst release at the beginning. Ex vivo studies showed a significant increase in the transportation of docetaxel from intestinal membrane of rat when formulated as nanoparticles. Cellular uptake of nanoparticles was investigated using fluoresceinamine-loaded nanoparticles. Docetaxel nanoparticles showed a high cytotoxicity effect in the Caco-2 and MCF-7 cell lines after 72 hours. It can be concluded that by combining the advantages of both thiolated polymers and colloidal particles, these nanoparticles can be proposed as a drug carrier system for mucosal delivery of hydrophobic drugs. PMID:21289989

  4. Applications of medical nanoparticles

    Institute of Scientific and Technical Information of China (English)

    LIU Yuan-gang; WANG Shi-bin; WENG Lian-jin

    2001-01-01

    @@ INTRODUCTION Nanoparticles, for their subcellular size, have been a important carrier in somefields. These fields include pharmacology, food, cosmetic, etc. Here, we focus onpresent applications of nanoparticles in drug carrier and gene carrier.

  5. Nanotechnology in oncology: Characterization and in vitro release kinetics of cisplatin-loaded albumin nanoparticles: Implications in anticancer drug delivery

    Directory of Open Access Journals (Sweden)

    Saikat Das

    2011-01-01

    Results and Conclusions: Using the coacervation method, nanoparticles of less than 70 nm diameter were produced. Drug encapsulation measured by ultraviolet spectroscopy varied from 30% to 80% for different ratios of cisplatin and protein. In vitro release kinetics shows that the nanoparticle-based formulation has biphasic release kinetics and is capable of sustained release compared with the free drug (80% release in 45 h. The study proves the feasibility of the albumin-based cisplatin nanoparticle formulation as a sustained release vehicle of cisplatin.

  6. Curcumin-loaded polymeric nanoparticles for enhanced anti-colorectal cancer applications.

    Science.gov (United States)

    Udompornmongkol, Panisa; Chiang, Been-Huang

    2015-11-01

    The purpose of the present study was to fabricate polymeric nanoparticles as drug carriers for encapsulated curcumin with enhanced anti-colorectal cancer applications. Nanoparticles were formulated from chitosan and gum arabic, natural polysaccharides, via an emulsification solvent diffusion method. The formation of curcumin nanoparticles was confirmed by Fourier transform infrared spectroscopy and differential scanning calorimeter. The results show that curcumin was entrapped in carriers with +48 mV, 136 nm size, and high encapsulation efficiency (95%). Based on an in vitro release study, we inferred that curcumin nanoparticles could tolerate hydrolysis due to gastric juice or small intestinal enzymes, and therefore, it should reach the colon largely intact. In addition, curcumin nanoparticles had higher anti-colorectal cancer properties than free curcumin due to greater cellular uptake. Therefore, we concluded that curcumin was successfully encapsulated in chitosan-gum arabic nanoparticles with superior anti-colorectal cancer activity.

  7. Atomic force microscopy imaging of polyurethane nanoparticles onto different solid substrates

    Energy Technology Data Exchange (ETDEWEB)

    Beddin Fritzen-Garcia, Mauricia [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); POLIMAT, Departamento de Quimica, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil)], E-mail: maurifritzen@hotmail.com; Giehl Zanetti-Ramos, Betina [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); Schweitzer de Oliveira, Cristian [Laboratorio de Filmes Finos e Superficies, Departamento de Fisica, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); Soldi, Valdir [POLIMAT, Departamento de Quimica, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); Avelino Pasa, Andre [Laboratorio de Filmes Finos e Superficies, Departamento de Fisica, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil); Creczynski-Pasa, Tania Beatriz [Laboratorio de Bioenergetica e Bioquimica de Macromoleculas, Departamento de Ciencias Farmaceuticas, Universidade Federal de Santa Catarina, 88040-900, Florianopolis, SC (Brazil)

    2009-03-01

    Atomic force microscopy (AFM) is a technique suited for characterizing nanoparticles on solid surfaces because it offers the capability of 3D visualization and quantitative information about the topography of the samples. In the present work, contact-mode AFM has been applied to imaging polyurethane nanoparticles formulated from a natural triol and isophorone diisocyanate (IPDI) in the presence of poly(ethylene glycol) (PEG). The colloidal polymeric system was deposited on mica, hydrophilic and hydrophobic silicon solid substrates to evaluate the size and shape of the nanoparticles. Our data showed that the nanoparticles were better distributed on mica and hydrophilic silicon. From the analysis of line-scan profiles we obtained different values for the ratio between the diameter and the height of the nanoparticles, indicating that the shape of the particles depends on the interaction between the nanoparticles and the substrate.

  8. Preparation and characterization of PEG-Mentha oil nanoparticles for housefly control.

    Science.gov (United States)

    Kumar, Peeyush; Mishra, Sapna; Malik, Anushree; Satya, Santosh

    2014-04-01

    Nanoparticles of Mentha × piperita essential oil were prepared by melt-dispersion method. The nanoparticles prepared at varying oil doses (5-10%, w/v) showed an encapsulation efficiency of 78.2-83.4%, while the oil load was observed to range between 3.64 and 7.46%. The average particle size of the nanoparticles varied between 226 and 331 nm, while polydispersity index showed variation between 0.547 and 1.000. DSC analysis indicated endothermic reaction during formation of nanoparticles, while a 2-term exponential kinetic model was followed during oil release. Nanoparticles showed considerable mortality against housefly larvae in lab (100%) as well as simulated field condition after first week (93%) and 6th week (57%) of application. This was the first study utilizing controlled release property of nanoparticles to formulate a cost effective product for breeding site application against housefly.

  9. Synthesis of berberine loaded polymeric nanoparticles by central composite design

    Science.gov (United States)

    Mehra, Meenakshi; Sheorain, Jyoti; Kumari, Santosh

    2016-04-01

    Berberine is an isoquinoline alkaloid which is extracted from bark and roots of Berberis vulgaris plant. It has been used in ayurvedic medicine as it possess antimicrobial, antidiabetic, anticancer, antioxidant properties etc. But poor solubility of berberine leads to poor stability and bioavailability in medical formulations decreasing its efficacy. Hence nanoformulations of berberine can help in removing the limiting factors of alkaloid enhancing its utilization in pharmaceutical industry. Sodium alginate polymer was used to encapsulate berberine within nanoparticles by emulsion solvent evaporation method using tween 80 as a surfactant. Two factors and three level in central composite design was used to study the formulation. The optimized formulation (1% v/v of Tween 80 and 0.01% w/v of sodium alginate) of polymeric nanoparticles was taken for further evaluations. The size of synthesized nanoparticles was found to be 71.18 nm by particle size analysis (PSA). The berberine loaded polymeric nanoparticles showed better antibacterial activity compared to aqueous solution of berberine by well diffusion assay.

  10. Formulation of heat absorbing glasses

    Directory of Open Access Journals (Sweden)

    Álvarez-Casariego, Pedro

    1996-06-01

    Full Text Available In the thermal exchanges between buildings and environment, glazing is an element of major importance, for it largely influences the so-called Solar Heat Gain and Thermal Losses. These parameters can be modified by applying different type of coatings onto glass surface or by adding colorant compounds during glass melting. The latter is a cheaper way to control the Solar Heat Gain. The knowledge of the laws governing the interaction between colorant compounds and solar radiation, allows us to define glass formulations achieving specific aesthetic requirements and solar energy absorption. In this paper two examples of application of the modelling of glass colorants spectral absorptance are presented. First is addressed to obtaining a glass with high luminous transmittance and low solar energy transmittance, and the other one to obtaining a glass with neutral colour appearance and minimized solar energy transmittance. Calculation formulas are defined together with photometric properties so-obtained. These type of glasses are particularly suitable to be used as building and automotive glazing, for they retain the mechanical characteristics and possibilities of transformation of standard glass.

    En los intercambios de energía entre un edificio y el medio exterior, el vidrio es el elemento de mayor importancia, por su influencia en la Ganancia de Calor Solar y en las Pérdidas Térmicas. Estos parámetros pueden ser modificados mediante el depósito de capas sobre el vidrio o mediante la adición de compuestos absorbentes de la radiación solar. Esta última vía es la más económica para controlar la Ganancia de Calor Solar. El conocimiento de las leyes que gobiernan la interacción de los diversos colorantes con la radiación solar, permite definir formulaciones de vidrios con características especificas de tipo estético y de absorción energética. En este trabajo se presentan dos ejemplos de aplicación de esta modelización de las

  11. Design and development of hydrogel nanoparticles for mercaptopurine

    Directory of Open Access Journals (Sweden)

    V Senthil

    2010-01-01

    Full Text Available Hydrogel nanoparticles have gained attention in recent years as they demonstrate the features and characters of hydrogels and nanoparticles at the same time. In the present study chitosan and carrageenan have been used, as hydrogel nanoparticles of mercaptopurine are developed using natural, biodegradable, and biocompatible polymers like chitosan and carrageenan. As these polymers are hydrophilic in nature, the particles will have a long life span in systemic circulation. Hydrogel nanoparticles with mercaptopurine is form an antileukemia drug by the counter polymer gelation method. Fourier-Transform Infrared (FT-IR studies have shown a compatibility of polymers with the drug. The diameter of hydrogel nanoparticles was about 370 - 800 nm with a positive zeta potential of 26 - 30 mV. The hydrogel nanoparticles were almost spherical in shape, as revealed by scanning electron microscopy (SEM. Drug loading varied from 9 to 17%. Mercaptopurine released from the nanoparticles at the end of the twenty-fourth hour was about 69.48 - 76.52% at pH 7.4. The drug release from the formulation was following zero order kinetics, which was evident from the release kinetic studies and the mechanism of drug release was anomalous diffusion, which indicated that the drug release was controlled by more than one process.

  12. Decontamination formulations for disinfection and sterilization

    Science.gov (United States)

    Tucker, Mark D.; Engler, Daniel E.

    2007-09-18

    Aqueous decontamination formulations that neutralize biological pathogens for disinfection and sterilization applications. Examples of suitable applications include disinfection of food processing equipment, disinfection of areas containing livestock, mold remediation, sterilization of medical instruments and direct disinfection of food surfaces, such as beef carcasses. The formulations include at least one reactive compound, bleaching activator, inorganic base, and water. The formulations can be packaged as a two-part kit system, and can have a pH value in the range of 7-8.

  13. A covariant formulation of classical spinning particle

    CERN Document Server

    Cho, J H; Kim, J K; Jin-Ho Cho; Seungjoon Hyun; Jae-Kwan Kim

    1994-01-01

    Covariantly we reformulate the description of a spinning particle in terms of the which entails all possible constraints explicitly; all constraints can be obtained just from the Lagrangian. Furthermore, in this covariant reformulation, the Lorentz element is to be considered to evolve the momentum or spin component from an arbitrary fixed frame and not just from the particle rest frame. In distinction with the usual formulation, our system is directly comparable with the pseudo-classical formulation. We get a peculiar symmetry which resembles the supersymmetry of the pseudo-classical formulation.

  14. Geometric Formulation of Gauge Theory of Gravity

    Institute of Scientific and Technical Information of China (English)

    WUNing; ZHANGDa-Hua; RUANTu-Nan

    2003-01-01

    DitTerential geometric formulation of quantum gauge theory of gravity is studied in this paper. The quantum gauge theory of gravity is formulated completely in the framework of traditional quantum field theory. In order to study the relationship between quantum gauge theory of gravity and traditional quantum gravity which is formulated in curved space, it is important to set up the geometry picture of quantum gauge theory of gravity. The correspondence between quantum gauge theory of gravity and differential geometry is discussed and the geometry picture of quantum gauge theory of gravity is studied.

  15. Geometric Formulation of Gauge Theory of Gravity

    Institute of Scientific and Technical Information of China (English)

    WU Ning; ZHANG Da-Hua; RUAN Tu-Nan

    2003-01-01

    Differential geometric formulation of quantum gauge theory of gravity is studied in this paper. The quantumgauge theory of gravity is formulated completely in the framework of traditional quantum field theory. In order to studythe relationship between quantum gauge theory of gravity and traditional quantum gravity which is formulated in curvedspace, it is important to set up the geometry picture of quantum gauge theory of gravity. The correspondence betweenquantum gauge theory of gravity and differential geometry is discussed and the geometry picture of quantum gaugetheory of gravity is studied.

  16. A New Formulation of Quantum Mechanics

    CERN Document Server

    Arbab, Arbab I

    2010-01-01

    A new formulation of quantum mechanics based on differential commutator brackets is developed. We have found a wave equation representing the fermionic particle. In this formalism, the continuity equation mixes the Klein-Gordon and Schrodinger probability density while keeping the Klein -Gordon and Schrodinger current un altered. We have found time and space transformations under which Dirac's equation is invariant. The invariance of Maxwell's equations under these transformations shows that the electric and magnetic fields of a moving charged particle are perpendicular to the particle's velocity. This formulation agrees with the quaternionic formulation developed recently by Arbab.

  17. Galactose decorated PLGA nanoparticles for hepatic delivery of acyclovir.

    Science.gov (United States)

    Gupta, Swati; Agarwal, Abhinav; Gupta, Nishant Kumar; Saraogi, Gauravkant; Agrawal, Himanshu; Agrawal, G P

    2013-12-01

    The present study explores prospective of surface tailored nanoparticles for targeted delivery of acyclovir along with the interception of minimal side effects. Acyclovir loaded plain and galactosylated poly lectic co glycolic acid (PLGA) nanoparticles were efficiently prepared and characterized by Fourier transform infrared spectroscopy, scanning electron microscopy (SEM), size, polydispersity index, zeta potential, and entrapment efficiency. The formulations were evaluated for in vitro drug release and hemolysis. Further, biodistribution study and fluorescent microscopic studies were carried out to determine the targeting potential of formulations. SEM revealed smooth morphology and spherical shape of the nanoparticles. In vitro, the galactosylated nanoparticles were found to be least hemolytic and exhibited a sustained release pattern. In vivo studies exhibited an augmented bioavailability, increased residence time and enhanced delivery of acyclovir to the liver upon galactosylation. It may therefore be concluded that galactose conjugated PLGA nanoparticles can be used suitably as vehicles for delivery of bioactives specifically to the hepatic tissues and may be thus exploited in the effective management of various liver disorders.

  18. Nitric oxide-releasing porous silicon nanoparticles

    Science.gov (United States)

    Kafshgari, Morteza Hasanzadeh; Cavallaro, Alex; Delalat, Bahman; Harding, Frances J.; McInnes, Steven JP; Mäkilä, Ermei; Salonen, Jarno; Vasilev, Krasimir; Voelcker, Nicolas H.

    2014-07-01

    In this study, the ability of porous silicon nanoparticles (PSi NPs) to entrap and deliver nitric oxide (NO) as an effective antibacterial agent is tested against different Gram-positive and Gram-negative bacteria. NO was entrapped inside PSi NPs functionalized by means of the thermal hydrocarbonization (THC) process. Subsequent reduction of nitrite in the presence of d-glucose led to the production of large NO payloads without reducing the biocompatibility of the PSi NPs with mammalian cells. The resulting PSi NPs demonstrated sustained release of NO and showed remarkable antibacterial efficiency and anti-biofilm-forming properties. These results will set the stage to develop antimicrobial nanoparticle formulations for applications in chronic wound treatment.

  19. Preparation and Standardization of Polyherbomineral Formulation

    Directory of Open Access Journals (Sweden)

    Gupta Reena

    2014-06-01

    Full Text Available Standardization of herbal formulation is essential in order to assess the quality of drugs. The present paper reports preparation and standardization of a herbomineral formulation which contains Zingiber officinalis (rhizome, Piper longum (fruit, Piper nigrum (fruit, Emblica officinalis (fruit,seed, Terminalia chebula (mature fruit, Terminalia belerica (pericarp of ripe fruit, Piper retrofractum (stem, Coriander sativum (fruit, Cuminum cyminum (fruit, Mercury, sulphur, loh bhasam, abharak bhasam. This Ayurvedic formulation is used to treat cold and cough. Here we discussed and focused about Morphology, Microscopy, Total ash, Acid insoluble ash, Water soluble and Alcohol soluble extractive value, bulk density, tapped density, Carr’s index, Hausner ratio, phytochemical tests, and Thin layer chromatography (TLC etc. These parameters are required for authentication of any herbal drug and its Herbo-mineral formulation.

  20. Formulating and Solving Problems in Computational Chemistry.

    Science.gov (United States)

    Norris, A. C.

    1980-01-01

    Considered are the main elements of computational chemistry problems and how these elements can be used to formulate the problems mathematically. Techniques that are useful in devising an appropriate solution are also considered. (Author/TG)

  1. Lagrangian formulation of noncommutative fluid models

    Energy Technology Data Exchange (ETDEWEB)

    Marcial, M.V., E-mail: mateusmarcial@fisica.ufjf.b [Departamento de Fisica, ICE, Universidade Federal de Juiz de Fora, 36036-330, Juiz de Fora, MG (Brazil); Mendes, A.C.R., E-mail: albert@fisica.ufjf.b [Departamento de Fisica, ICE, Universidade Federal de Juiz de Fora, 36036-330, Juiz de Fora, MG (Brazil); Neves, C., E-mail: clifford@fat.uerj.b [Departamento de Matematica e Computacao, Universidade do Estado do Rio de Janeiro Rodovia Presidente Dutra, km 298, 27537-000, Resende, Rio de Janeiro (Brazil); Oliveira, W., E-mail: wilson@fisica.ufjf.b [Departamento de Fisica, ICE, Universidade Federal de Juiz de Fora, 36036-330, Juiz de Fora, MG (Brazil); Takakura, F.I., E-mail: takakura@fisica.ufjf.b [Departamento de Fisica, ICE, Universidade Federal de Juiz de Fora, 36036-330, Juiz de Fora, MG (Brazil)

    2010-08-02

    In this work we study Lagrangian formulations for the noncommutative versions of the irrotational and rotational fluid models. These formulations will be obtained by using the Faddeev-Jackiw symplectic formalism. In this context, interesting results will be revealed, for example, a chiral behavior into both fluid models comes up. In fact, distinct and non-dynamically equivalent Lagrangian descriptions of the noncommutative versions of the fluid models can be proposed.

  2. Compatibility of DLC coatings with formulated oils

    OpenAIRE

    Sedlaček, Marko; PODGORNIK, Bojan; Vižintin, Jože

    2015-01-01

    In the present study, the tribological performance and compatibility of hydrogenated amorphous carbon coating (a-C:H) and metal-doped diamond-like carbon (DLC) coating (Me-C:H) with formulated oils under the boundary lubrication regime was investigated. The investigation employed ball-on-flat contact geometry in reciprocating sliding motion and six formulated oils (manual gearbox oil, automatic gearbox oil, hydraulic oil, compressor oil, andnormal and high performance motor oil), with pure po...

  3. Dual algebraic formulation of differential GPS

    Science.gov (United States)

    Lannes, A.; Dur, S.

    2003-05-01

    A new approach to differential GPS is presented. The corresponding theoretical framework calls on elementary concepts of algebraic graph theory. The notion of double difference, which is related to that of closure in the sense of Kirchhoff, is revisited in this context. The Moore-Penrose pseudo-inverse of the closure operator plays a key role in the corresponding dual formulation. This approach, which is very attractive from a conceptual point of view, sheds a new light on the Teunissen formulation.

  4. The Boltzmann equation in the difference formulation

    Energy Technology Data Exchange (ETDEWEB)

    Szoke, Abraham [Lawrence Livermore National Lab. (LLNL), Livermore, CA (United States); Brooks III, Eugene D. [Lawrence Livermore National Lab. (LLNL), Livermore, CA (United States)

    2015-05-06

    First we recall the assumptions that are needed for the validity of the Boltzmann equation and for the validity of the compressible Euler equations. We then present the difference formulation of these equations and make a connection with the time-honored Chapman - Enskog expansion. We discuss the hydrodynamic limit and calculate the thermal conductivity of a monatomic gas, using a simplified approximation for the collision term. Our formulation is more consistent and simpler than the traditional derivation.

  5. USE OF LIPOSOMES AND NANOPARTICLES FOR BRAIN DRUG TARGETING

    Directory of Open Access Journals (Sweden)

    Goutam Pal

    2012-08-01

    Full Text Available The Blood Brain Barrier (BBB poses a obstacle for a drugs, including antineoplastic agent, antibiotics, neuropeptides, CNS active agents, to be delivered to the brain for therapeutic reasons. The use of formulation dependent strategy such as the use of heterogenous pharmaceutical systems for its effective targeting to the brain is being explored recently. Liposomes and Nanoparticles are good possibilities to achieve the goal. Chemically modified liposomes and nanoparticles are tried in recent times to act as brain targeting aids, and this article tries to explain the possibilities and problems behind such an endeavor.KEY WORDS:

  6. Optimized optical "tractor beam" for core-shell nanoparticles.

    Science.gov (United States)

    Wang, Neng; Lu, Wanli; Ng, Jack; Lin, Zhifang

    2014-04-15

    It is known that core-shell subwavelength nanoparticles consisting of a dielectric shell and a metallic core can simultaneously support electric and magnetic dipolar resonances, which enhance forward scattering and suppress backward scattering. This creates favorable conditions for optical tractor beam applications. Using the generalized Lorenz-Mie theory and Maxwell stress tensor formulation, we demonstrate how optical pulling forces can be induced and optimized by first-order Bessel beams with appropriate polarization. The transverse stability of the core-shell nanoparticle under ambient damping is also verified by linear stability analysis and dynamical simulation. PMID:24979003

  7. A generalized anisotropic deformation formulation for geomaterials

    Science.gov (United States)

    Lei, Z.; Rougier, Esteban; Knight, E. E.; Munjiza, A.; Viswanathan, H.

    2016-04-01

    In this paper, the combined finite-discrete element method (FDEM) has been applied to analyze the deformation of anisotropic geomaterials. In the most general case geomaterials are both non-homogeneous and non-isotropic. With the aim of addressing anisotropic material problems, improved 2D FDEM formulations have been developed. These formulations feature the unified hypo-hyper elastic approach combined with a multiplicative decomposition-based selective integration for volumetric and shear deformation modes. This approach is significantly different from the co-rotational formulations typically encountered in finite element codes. Unlike the co-rotational formulation, the multiplicative decomposition-based formulation naturally decomposes deformation into translation, rotation, plastic stretches, elastic stretches, volumetric stretches, shear stretches, etc. This approach can be implemented for a whole family of finite elements from solids to shells and membranes. This novel 2D FDEM based material formulation was designed in such a way that the anisotropic properties of the solid can be specified in a cell by cell basis, therefore enabling the user to seed these anisotropic properties following any type of spatial variation, for example, following a curvilinear path. In addition, due to the selective integration, there are no problems with volumetric or shear locking with any type of finite element employed.

  8. De-alloyed platinum nanoparticles

    Science.gov (United States)

    Strasser, Peter; Koh, Shirlaine; Mani, Prasanna; Ratndeep, Srivastava

    2011-08-09

    A method of producing de-alloyed nanoparticles. In an embodiment, the method comprises admixing metal precursors, freeze-drying, annealing, and de-alloying the nanoparticles in situ. Further, in an embodiment de-alloyed nanoparticle formed by the method, wherein the nanoparticle further comprises a core-shell arrangement. The nanoparticle is suitable for electrocatalytic processes and devices.

  9. Surface coating mediates the toxicity of polymeric nanoparticles towards human-like macrophages.

    Science.gov (United States)

    Grabowski, Nadège; Hillaireau, Hervé; Vergnaud, Juliette; Tsapis, Nicolas; Pallardy, Marc; Kerdine-Römer, Saadia; Fattal, Elias

    2015-03-30

    The purpose of this study was to investigate the toxicity of a series of poly(lactide-co-glycolic) (PLGA) nanoparticles on human-like THP-1 macrophages. Positively-, negatively-charged and neutral nanoparticles (200 nm) were prepared using chitosan (CS), poloxamer 188 (PF68) and poly(vinyl alcohol) (PVA) as stabilizer. Stabilizer-free PLGA nanoparticles were obtained as well. When used at therapeutically relevant concentrations (up to 0.1 mg/mL in vitro), all tested nanoparticles showed no or scarce signs of toxicity, as assessed by cell mitochondrial activity, induction of apoptosis and necrosis, production of intracellular reactive oxygen species (ROS) and secretion of pro-inflammatory cytokines. At high concentrations (above 1mg/mL), cytotoxicity was found to be induced by the presence of stabilizers, whatever the toxicological pattern of the stabilizer itself. While stabilizer-free PLGA nanoparticles exerted no cytotoxicity, the slightly cytotoxic CS polymer conferred PLGA nanoparticles significant cytotoxicity when used as nanoparticle stabilizer; more surprisingly, the otherwise innocuous PVA and PF68 polymers also conferred a significant cytotoxicity to PLGA nanoparticles. These results unveiled the critical toxicological contribution played by stabilizers used for the formulation of PLGA nanoparticles when used at high concentrations, which may have implications for local toxicities of PLGA-based nanomedicine, and provided additional insight in cytotoxic effects of internalized nanoparticles.

  10. Improved solubilization of curcumin with a microemulsification formulation

    Directory of Open Access Journals (Sweden)

    ROMICĂ CREŢU

    Full Text Available Due to the large number of bioactive substances, with low and very low solubility in water, new and improved investigation methods were developed. Researches in this area have shown that lipid systems in lipophilic substances formulation increase their bioavailability and prevent or reduce the toxicological risk because most of the components involved in the formulation are of natural origin, with a structure compatible with biological membranes components. Among the lipid systems used in the leaching, transport and release of lipophilic substances there are: liposomes, solid lipid nanoparticles, double and single emulsions, autoemulsionante and auto-microemulsionante lipid systems. The last are the subject of the present research and meet specialists in concern for the harmonization of cost-benefit-risk in order to improve population health. Curcumin [(1E, 6E-1,7-bis(4-hydroxy-3-methoxyphenyl-1,6-heptadiene-3,5-dione] is a yellow pigment derived from the rhizome of the plant Curcuma Longa with phenol groups and conjugated double bounds which is unstable at light and basic pH, degrading within 30 minutes. The aim of this study is curcumin solubilization used as alimentary dye in automicroemulsionante systems. Dye/oil/surfactant/cosurfactant mixing ratio was made, based on quaternary phase diagrams. Mesofazice structures were revealed by conductivity and viscosimetric analysis. A curcumin solubilization system in aqueous medium was obtained. On the other hand, this paper studies the colour evolution of these automicroemulsionante systems comparing with hexane dye solution. The use of the chromatic attributes L*, a* and b* and L*, C* and hab, suggested by the Commission Internationale de l’Eclairage (CIE (i.e., the CIELAB system, obtained from direct transmitance measurements, which made it possible to follow the evolution of colour.

  11. Preparation and Characterization of Starch Nanoparticles for Controlled Release of Curcumin

    OpenAIRE

    Chin, Suk Fun; Mohd Yazid, Siti Nur Akmar; Pang, Suh Cem

    2014-01-01

    Curcumin was loaded onto starch nanoparticles by using in situ nanoprecipitation method and water-in-oil microemulsion system. Curcumin loaded starch nanoparticles exhibited enhanced solubility in aqueous solution as compared to free curcumin. Effects of formulation parameters such as types of reaction medium, types of surfactant, surfactant concentrations, oil/ethanol ratios, loading time, and initial curcumin concentration were found to affect the particle size and loading efficiency (LF) o...

  12. Polymeric Curcumin Nanoparticle Pharmacokinetics and Metabolism in Bile Duct Cannulated Rats

    OpenAIRE

    Zou, Peng; Helson, Lawrence; Maitra, Anirban; Stern, Stephan T; McNeil, Scott E.

    2013-01-01

    The objective of this study was to compare the pharmacokinetics and metabolism of polymeric nanoparticle encapsulated (nanocurcumin), and solvent solubilized curcumin formulations in Sprague Dawley (SD) rats. Nanocurcumin is currently under development for cancer therapy. Since free, unencapsulated curcumin is rapidly metabolized and excreted in rats, upon i.v. administration of nanocurcumin only nanoparticle encapsulated curcumin can be detected in plasma samples. Hence, the second objective...

  13. Co-encapsulation of lyoprotectants improves the stability of protein-loaded PLGA nanoparticles upon lyophilization

    DEFF Research Database (Denmark)

    Fonte, Pedro; Araújo, Francisca; Seabra, Vítor;

    2015-01-01

    The purpose of this work was to evaluate the influence of the co-encapsulation of lyoprotectants with insulin into PLGA nanoparticles, on the stability of the protein and nanoparticles upon lyophilization. Different lyoprotectants were used, namely trehalose, glucose, sucrose, fructose and sorbitol...... confirmed by circular dichroism spectroscopy. Surprisingly, the simultaneous co-encapsulation and addition of lyoprotectants was detrimental to protein stabilization. The insulin in vitro release studies demonstrated that formulations with co-encapsulated trehalose, glucose, sucrose, fructose and sorbitol...

  14. Preparation and characterization of Tamoxifen citrate loaded nanoparticles for breast cancer therapy

    OpenAIRE

    Maji R; Dey NS; Satapathy BS; Mukherjee B.; Mondal S

    2014-01-01

    Ruma Maji, Niladri Shekhar Dey, Bhabani Sankar Satapathy, Biswajit Mukherjee, Subhasish MondalDepartment of Pharmaceutical Technology, Jadavpur University, Kolkata (Calcutta), IndiaBackground: Four formulations of Tamoxifen citrate loaded polylactide-co-glycolide (PLGA) based nanoparticles (TNPs) were developed and characterized. Their internalization by Michigan Cancer Foundation-7 (MCF-7) breast cancer cells was also investigated.Methods: Nanoparticles were prepared by a multiple e...

  15. Synthesis of zinc oxide nanoparticles elaborated by microemulsion method

    Energy Technology Data Exchange (ETDEWEB)

    Yildirim, Ozlem Altintas [Department of Metallurgical and Materials Engineering, Middle East Technical University, 06531 Ankara (Turkey); Durucan, Caner, E-mail: cdurucan@metu.edu.t [Department of Metallurgical and Materials Engineering, Middle East Technical University, 06531 Ankara (Turkey)

    2010-09-17

    Graphical abstract: . Display Omitted Research highlights: {yields} Spherical and rod-like ZnO nanostructures obtained in reverse microemulsion. {yields} Morphological variations for microemulsion products with surfactant amount. {yields} Formation mechanism for ZnO nanosructres in a reverse emulsion system. {yields} Optical properties of the ZnO nanoparticles. - Abstract: Zinc oxide (ZnO) nanoparticles were synthesized by a reverse microemulsion system formed from sodium bis(2-ethylhexyl)sulfosuccinate (Aerosol OT, or AOT):glycerol:n-heptane. The zinc precursor was zinc acetate dihydrate. The formation of ZnO nanoparticles was achieved by calcination of premature zinc glycerolate microemulsion product in air at 300, 400 and 500 {sup o}C. The crystal structure and the morphology of the ZnO nanoparticles were characterized by X-ray diffraction (XRD) and scanning electron microscopy (SEM). Thermal analysis was employed to reveal structural and chemical changes during calcination. Both surfactant concentrations - AOT - in the initial microemulsion formulation and the calcination temperature influenced the morphology and size of the ZnO nanoparticles. Low surfactant concentrations (5:5:90, AOT:glycerol:n-heptane, wt.%) resulted in formation of spherical ZnO nanoparticles. The average particle size increased from 15 {+-} 1 to 24 {+-} 1 nm with calcination temperature, but spherical morphology remained unchanged after all calcination treatments. The microemulsion system containing higher surfactant amount (30:5:65, AOT:glycerol:n-heptane, wt.%) resulted in rod-like ZnO nanostructures after calcination at 300 and 400 {sup o}C, with a diameter of 22 {+-} 3 and 28 {+-} 1 nm; and with a length of 66 {+-} 3 and 72 {+-} 1 nm, respectively. Further increase in the calcination temperature to 500 {sup o}C initiated rod-to-sphere shape transformation for the ZnO nanoparticles produced using this particular microemulsion formulation. For all ZnO microemulsion products, the

  16. DESIGN AND EVALUATION OF POLYLACTIC-CO-GLYCOLIC ACID NANOPARTICLES CONTAINING SIMVASTATIN

    Directory of Open Access Journals (Sweden)

    Anilkumar J. Shinde

    2011-06-01

    Full Text Available The objective of the present work was to formulate nanoparticles for simvastatin drug. Simvastatin is a lipid lowering agent, and BCS class-II drug having low solubility and high permeability. Since simvastatin undergoes extensive first pass extraction in the liver, the availability of the drug to the general circulation is low (< 5%. Nanoparticles were prepared by precipitation-solvent deposition method using 3² full factorial design. From the preliminary trials, the constraints for independent variables X1 (amount of PLGA and X2 (amount of Pleuronic F-68 have been fixed. The prepared formulations were further evaluated for drug content, in vitro drug release pattern, short term stability and drug excipient interactions. The application of factorial design gave a statistically systematic approach for the formulation and optimization of nanoparticles with desired particle size and high entrapment efficiency. Drug: polymer ratio and concentration of stabilizer were found to influence the particle size and entrapment efficiency of simvastatin loaded PLGA nanoparticles. In vitro drug release study of selected factorial formulations (PS1, PS4, PS7 showed, 84.56%, 89.65 %, and 73.46 % release respectively in 24 hrs. The release was found to follow first order release kinetics with fickian diffusion mechanism for all batches. These results indicate that simvastatin loaded PLGA nanoparticles could be effective in sustaining drug release for a prolonged period.

  17. Characterization of pDNA-TMC Nanoparticle Interaction and Stability.

    Science.gov (United States)

    Poecheim, Johanna; Patrulea, Viorica; Reichert, Christian; Borchard, Gerrit

    2016-01-01

    Formulation of nanoparticulate DNA vaccines requires the assessment of stability and integrity of the components implicated. Stability of cationic nanoparticles made of N-trimethyl chitosan and chondroitin sulfate (TMC nanoparticles) was investigated in aqueous solution and after freeze-drying by characterization of their size, polydispersity index (PDI), and zeta potential. Furthermore, the structural integrity of plasmid DNA (pDNA) on adsorption to the nanoparticle surface was investigated. Agarose gel electrophoresis showed DNA retention when applied with the nanocarrier, suggesting that pDNA adsorption on nanoparticles took place. In circular dichroism (CD) spectra, ellipticity of pDNA decreased at 280 nm and increased at 245 nm, and the maximum wavelength shifted from 275 nm to 285 nm when nanoparticles were present. Once released from the particles, the secondary structure of the plasmid was retained in its native form. pDNA release from pDNA-TMC nanoparticles was indicated by a rise in zeta potential from initially -32 mV (pDNA adsorbed to particles) to 14 mV during one hour, and to 36 mV after 24 hours. Unloaded TMC nanoparticles remained stable in suspension for 24 hours, maintaining diameters of around 200 nm, and zeta potential values of approximately 38 mV. Freeze-drying with sucrose could ensure storage for 30 days, with minimal increase in size (291 nm) and charge (62 mV). In conclusion, TMC nanoparticles may potentially be freeze-dried in the presence of sucrose to be stored for prolonged periods of time. Furthermore, pDNA was successfully adsorbed to the cationic nanoparticles and remained intact after being released. PMID:26638979

  18. TURVA-2012: Formulation of radionuclide release scenarios

    International Nuclear Information System (INIS)

    TURVA-2012 is Posiva's safety case in support of the Preliminary Safety Analysis Report (PSAR) and application for a construction licence for a repository for disposal of spent nuclear fuel at the Olkiluoto site in south-western Finland. This paper gives a summary of the scenarios and the methodology followed in formulating them as described in TURVA-2012: Formulation of Radionuclide Release Scenarios (Posiva, 2013). The scenarios are further analysed in TURVA-2012: Assessment of Radionuclide Release Scenarios for the Repository System and TURVA-2012: Biosphere Assessment (Posiva, 2012a, 2012b). The formulation of scenarios takes into account the safety functions of the main barriers of the repository system and the uncertainties in the features, events, and processes (FEP) that may affect the entire disposal system (i.e. repository system plus the surface environment) from the emplacement of the first canister until the far future. In the report TURVA-2012: Performance Assessment (2012d), the performance of the engineered and natural barriers has been assessed against the loads expected during the evolution of the repository system and the site. Uncertainties have been identified and these are taken into account in the formulation of radionuclide release scenarios. The uncertainties in the FEP and evolution of the surface environment are taken into account in formulating the surface environment scenarios used ultimately in estimating radiation exposure. Formulating radionuclide release scenarios for the repository system links the reports Performance Assessment and Assessment of Radionuclide Release Scenarios for the Repository System. The formulation of radionuclide release scenarios for the surface environment brings together biosphere description and the surface environment FEP and is the link to the assessment of the surface environment scenarios summarised in TURVA-2012: Biosphere Assessment. (authors)

  19. Design and physicochemical characterization of poly(amidoamine) nanoparticles and the toxicological evaluation in human endothelial cells: applications to peptide delivery to the brain

    NARCIS (Netherlands)

    Coue, G.M.J.P.C.; Freese, C.; Unger, R.E.; Kirkpatrick, C.J.; Pickl, K.E.; Sinner, F.M.; Engbersen, J.F.J.

    2013-01-01

    In this study, we investigated nanoparticles formulated by self-assembly of a biodegradable poly(amidoamine) (PAA) and a fluorescently labeled peptide, in their capacity to internalize in endothelial cells and deliver the peptide, with possible applications for brain drug delivery. The nanoparticles

  20. Enhanced magnetic resonance contrast of iron oxide nanoparticles embedded in a porous silicon nanoparticle host

    Science.gov (United States)

    Kinsella, Joseph; Ananda, Shalini; Andrew, Jennifer; Grondek, Joel; Chien, Miao-Ping; Scandeng, Miriam; Gianneschi, Nathan; Ruoslahti, Erkki; Sailor, Michael

    2013-02-01

    In this report, we prepared a porous Si nanoparticle with a pore morphology that facilitates the proximal loading and alignment of magnetite nanoparticles. We characterized the composite materials using superconducting quantum interference device magnetometry, dynamic light scattering, transmission electron microscopy, and MRI. The in vitro cytotoxicity of the composite materials was tested using cell viability assays on human liver cancer cells and rat hepatocytes. An in vivo analysis using a hepatocellular carcinoma (HCC) Sprague Dawley rat model was used to determine the biodistribution properties of the material, while naïve Sprague Dawley rats were used to determine the pharmocokinetic properties of the nanomaterials. The composite material reported here demonstrates an injectable nanomaterial that exploits the dipolar coupling of superparamagnetic nanoparticles trapped within a secondary inorganic matrix to yield significantly enhanced MRI contrast. This preparation successfully avoids agglomeration issues that plague larger ferromagnetic systems. A Fe3O4:pSi composite formulation consisting of 25% by mass Fe3O4 yields an maximal T2* value of 556 mM Fe-1 s-1. No cellular (HepG2 or rat hepatocyte cells) or in vivo (rat) toxicity was observed with the formulation, which degrades and is eliminated after 4-8 h in vivo. The ability to tailor the magnetic properties of such materials may be useful for in vivo imaging, magnetic hyperthermia, or drug-delivery applications.

  1. Anti-platelet agents augment cisplatin nanoparticle cytotoxicity by enhancing tumor vasculature permeability and drug delivery

    International Nuclear Information System (INIS)

    Tumor vasculature is critically dependent on platelet mediated hemostasis and disruption of the same can augment delivery of nano-formulation based chemotherapeutic agents which depend on enhanced permeability and retention for tumor penetration. Here, we evaluated the role of Clopidogrel, a well-known inhibitor of platelet aggregation, in potentiating the tumor cytotoxicity of cisplatin nano-formulation in a murine breast cancer model. In vivo studies in murine syngeneic 4T1 breast cancer model showed a significant greater penetration of macromolecular fluorescent nanoparticles after clopidogrel pretreatment. Compared to self-assembling cisplatin nanoparticles (SACNs), combination therapy with clopidogrel and SACN was associated with a 4 fold greater delivery of cisplatin to tumor tissue and a greater reduction in tumor growth as well as higher survival rate. Clopidogrel enhances therapeutic efficiency of novel cisplatin based nano-formulations agents by increasing tumor drug delivery and can be used as a potential targeting agent for novel nano-formulation based chemotherapeutics. (paper)

  2. Anti-platelet agents augment cisplatin nanoparticle cytotoxicity by enhancing tumor vasculature permeability and drug delivery

    Science.gov (United States)

    Pandey, Ambarish; Sarangi, Sasmit; Chien, Kelly; Sengupta, Poulomi; Papa, Anne-Laure; Basu, Sudipta; Sengupta, Shiladitya

    2014-11-01

    Tumor vasculature is critically dependent on platelet mediated hemostasis and disruption of the same can augment delivery of nano-formulation based chemotherapeutic agents which depend on enhanced permeability and retention for tumor penetration. Here, we evaluated the role of Clopidogrel, a well-known inhibitor of platelet aggregation, in potentiating the tumor cytotoxicity of cisplatin nano-formulation in a murine breast cancer model. In vivo studies in murine syngeneic 4T1 breast cancer model showed a significant greater penetration of macromolecular fluorescent nanoparticles after clopidogrel pretreatment. Compared to self-assembling cisplatin nanoparticles (SACNs), combination therapy with clopidogrel and SACN was associated with a 4 fold greater delivery of cisplatin to tumor tissue and a greater reduction in tumor growth as well as higher survival rate. Clopidogrel enhances therapeutic efficiency of novel cisplatin based nano-formulations agents by increasing tumor drug delivery and can be used as a potential targeting agent for novel nano-formulation based chemotherapeutics.

  3. Formulation of chitosan-TPP-pDNA nanocapsules for gene therapy applications

    Science.gov (United States)

    Gaspar, V. M.; Sousa, F.; Queiroz, J. A.; Correia, I. J.

    2011-01-01

    The encapsulation of DNA inside nanoparticles meant for gene delivery applications is a challenging process where several parameters need to be modulated in order to design nanocapsules with specific tailored characteristics. The purpose of this study was to investigate and improve the formulation parameters of plasmid DNA (pDNA) loaded in chitosan nanocapsules using tripolyphosphate (TPP) as polyanionic crosslinker. Nanocapsule morphology and encapsulation efficiency were analyzed as a function of chitosan degree of deacetylation and chitosan-TPP ratio. The manipulation of these parameters influenced not only the particle size but also the encapsulation and release of pDNA. Consequently the transfection efficiency of the nanoparticulated systems was also enhanced with the optimization of the particle characteristics. Overall, the differently formulated nanoparticulated systems possess singular properties that can be employed according to the desired gene delivery application.

  4. Formulation of chitosan-TPP-pDNA nanocapsules for gene therapy applications

    International Nuclear Information System (INIS)

    The encapsulation of DNA inside nanoparticles meant for gene delivery applications is a challenging process where several parameters need to be modulated in order to design nanocapsules with specific tailored characteristics. The purpose of this study was to investigate and improve the formulation parameters of plasmid DNA (pDNA) loaded in chitosan nanocapsules using tripolyphosphate (TPP) as polyanionic crosslinker. Nanocapsule morphology and encapsulation efficiency were analyzed as a function of chitosan degree of deacetylation and chitosan-TPP ratio. The manipulation of these parameters influenced not only the particle size but also the encapsulation and release of pDNA. Consequently the transfection efficiency of the nanoparticulated systems was also enhanced with the optimization of the particle characteristics. Overall, the differently formulated nanoparticulated systems possess singular properties that can be employed according to the desired gene delivery application.

  5. Atorvastatin calcium loaded chitosan nanoparticles: in vitro evaluation and in vivo pharmacokinetic studies in rabbits

    Directory of Open Access Journals (Sweden)

    Abdul Baquee Ahmed

    2015-06-01

    Full Text Available In this study, we prepared atorvastatin calcium (AVST loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, in vitro release and surface morphology by scanning electron microscopy (SEM. In addition, the pharmacokinetics of AVST from the optimized formulation (FT5 was compared with marketed immediate release formulation (Atorva(r in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. In vitro release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC of the optimized formulation as compared to marketed formulation (Atorva(r. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.

  6. 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.

  7. FORMULATION AND EVALUATION OF AMISULPRIDE ORODISPERSIBLE TABLET

    Directory of Open Access Journals (Sweden)

    Dr. Hitesh P. Dalvadi

    2016-03-01

    Full Text Available Orodispersible dosage forms have lured the market for a certain section of the patient population which includes dysphagia, bed ridden, psychic, and geriatric patients. Moreover Orodispersible tablets shows increased bioavailability as compared to conventional dosage forms. Amisulpride is a psychotropic agent belonging to the chemical class of benzamide derivatives. At low doses, it enhances dopaminergic neurotransmission by preferentially blocking presynaptic dopamine D2/D3 auto receptors. The tablets were prepared by using direct compression method, and drug solubility is enhanced by solid dispersion. Formulation were prepared by using different superdisintegrant, combination of different superdisintegrant and effect of hydrophilic lubricant was studied and evaluated pre and post compression parameters. Tablets were evaluated for content uniformity, Disintegration time, wetting time, hardness, friability and In-vitro dissolution studies. More than 90% of drug was released from almost all the formulations within 10 min. Formulation C4 containing Sodium starch glycolate (4.5%, Crospovidone (2.5% and crosscarmellose sodium (3.5%, was having disintegration time 24 seconds, wetting time 18 seconds, hardness 3.4Kg/cm2 and in vitro drug release of 99.96% in pH 6.8. Based on this data C4 was found to be the best formulation. Further formulations were subjected to accelerated stability studies. Tablets showed no appreciable changes with respect to disintegration and dissolution profiles. Results of this study indicate among the superdisintegrants tried, combination of superdisintegrant gave the best result.

  8. Formulation and optimization of carbamazepine floating tablets

    Directory of Open Access Journals (Sweden)

    Patel D

    2007-01-01

    Full Text Available Floating tablets of carbamazepine were developed using melt granulation technique. Bees wax was used as a hydrophobic meltable material. Hydroxypropylmethylcellulose, sodium bicarbonate and ethyl cellulose were used as matrixing agent, gas-generating agent and floating enhancer, respectively. The tablets were evaluated for in vitro buoyancy and dissolution studies. A simplex lattice design was applied to investigate the combined effect of 3 formulation variables i.e. amount of hydroxypropyl methylcellulose ( X 1 , ethyl cellulose ( X 2 and sodium bicarbonate ( X 3 . The floating lag time (F lag , time required for 50% (t 50 and 80% drug dissolution (t 80 were taken as responses. Results of multiple regression analysis indicated that, low level of X 1 and X 2 , and high level of X 3 should be used to manufacture the tablet formulation with desired in vitro floating time and dissolution. Formulations developed using simplex lattice design were fitted to various kinetic models for drug release. Formulation S3 was selected as a promising formulation and was found stable at 40 o and 75% relative humidity for 3 months. Present study demonstrates the use of simplex lattice design in the development of floating tablets with minimum experimentation.

  9. Automatic query formulations in information retrieval.

    Science.gov (United States)

    Salton, G; Buckley, C; Fox, E A

    1983-07-01

    Modern information retrieval systems are designed to supply relevant information in response to requests received from the user population. In most retrieval environments the search requests consist of keywords, or index terms, interrelated by appropriate Boolean operators. Since it is difficult for untrained users to generate effective Boolean search requests, trained search intermediaries are normally used to translate original statements of user need into useful Boolean search formulations. Methods are introduced in this study which reduce the role of the search intermediaries by making it possible to generate Boolean search formulations completely automatically from natural language statements provided by the system patrons. Frequency considerations are used automatically to generate appropriate term combinations as well as Boolean connectives relating the terms. Methods are covered to produce automatic query formulations both in a standard Boolean logic system, as well as in an extended Boolean system in which the strict interpretation of the connectives is relaxed. Experimental results are supplied to evaluate the effectiveness of the automatic query formulation process, and methods are described for applying the automatic query formulation process in practice. PMID:10299297

  10. Gamma Ray Bursts Cook Book I: Formulation

    CERN Document Server

    Ziaeepour, Houri

    2008-01-01

    Since the suggestion of relativistic shocks as the origin of gamma-ray bursts (GRBs) in early 90's, the mathematical formulation of this process has stayed at phenomenological level. One of the reasons for the slow development of theoretical works in this domain has been the simple power-law behaviour of the afterglows hours or days after the prompt gamma-ray emission. Nowadays with the launch of the Swift satellite, gamma-ray bursts can be observed in multi-wavelength from a few tens of seconds after trigger onward. These observations have leaded to the discovery of features unexplainable by the simple formulation of the shocks and emission processes used up to now. But "devil is in details" and some of these features may be explained with a more detailed formulation of phenomena and without adhoc addition of new processes. Such a formulation is the goal of this work. We present a consistent formulation of the collision between two spherical relativistic shells. The model can be applied to both internal and ...

  11. Additive Technology for EU Ecolabel Formulations

    Institute of Scientific and Technical Information of China (English)

    Eric Nehls; Tassilo Habereder; Edward Ng

    2009-01-01

    Currently, Bio -lubricants are still regarded as niche products. Within the global lubricant market, however, the ar-ea of environmentally acceptable fluids represents one of the fast growing markets with an estimated annual growth of more than 6% per year. This growth is supported by various market drivers such as legal regulations, public subsidies and the im-plementation of national or international labeling schemes.With the implementation of the European Ecolabel for lubricants in 2005, a common standard specifying ecological and performance requirements for Bio - lubricants was defined. Applying for the EU Ecolabel requires a comprehensive assess-ment, not only of the final formulation, but also of the additives used. Additives are required to meet specifications for oxi-dation and thermal stability, as well as to impart metal protection (of both steel and yellow metals), thus improving corro-sion protection and wear performance of the formulation. Therefore, it is challenging in terms of formulation technology to develop the right formulation that meets the technical specifications as well as the stringent requirements of the EU - Ecola-bel.The paper describes how, by using ester base fluids and additives currently available in the market, lubricants can be developed to meet the technical and eco - toxicological requirements of the EU - Ecolabel, approaching the performance lev-els of lubricants formulated with traditional base fluids.

  12. Novel silicone elastomer formulations for DEAPs

    DEFF Research Database (Denmark)

    Skov, Anne Ladegaard; Vudayagiri, Sindhu; Benslimane, Mohamed

    2013-01-01

    We demonstrate that the force output and work density of polydimethylsiloxane (PDMS) based dielectric elastomer transducers can be significantly enhanced by the addition of high permittivity titanium dioxide nanoparticles which was also shown by Stoyanov et al[1] for pre-stretched elastomers and ...

  13. Nanoparticle agglomerates in magnetoliposomes

    International Nuclear Information System (INIS)

    Magnetoliposomes consist of vesicles composed of a phospholipid membrane encapsulating magnetic nanoparticles. These systems have several important applications, such as in MRI contrast agents, drug and gene carriers, and cancer treatment devices. For all of these applications, controlling the number of encapsulated magnetic nanoparticles is a key issue. In this work, we used a magneto-optical technique to obtain information about the efficiency of encapsulation, the number of nanoparticles encapsulated per liposome and also about the formation of the nanoparticle structures. The parameters studied included the effect of the duration of sonication, the presence of cholesterol in the liposome membrane, as well as time-related stability. For the liposomal vesicles prepared in this work, we found between 35 and 300 nanoparticles encapsulated per liposome, depending on the experimental conditions, consisting of small linear chains of nanoparticles, basically trimers and tetramers. The methodology developed might be useful for the investigation and improvement of the properties of several magnetic nanocarrier systems.

  14. Marshall Convergent Spray Formulation Improvement for High Temperatures

    Science.gov (United States)

    Scarpa, Jack; Patterson,Chat

    2011-01-01

    The Marshall Convergent Coating-1 (MCC-1) formulation was produced in the 1990s, and uses a standard bisphenol A epoxy resin system with a triamine accelerator. With the increasing heat rates forecast for the next generation of vehicles, higher-temperature sprayable coatings are needed. This work substitutes the low-temperature epoxy resins used in the MCC-1 coating with epoxy phenolic, epoxy novalac, or resorcinolinic resins (higher carbon content), which will produce a higher char yield upon exposure to high heat and increased glass transition temperature. High-temperature filler materials, such as granular cork and glass ecospheres, are also incorporated as part of the convergent spray process, but other sacrificial (ablative) materials are possible. In addition, the use of polyhedral oligomeric silsesquioxanes (POSS) nanoparticle hybrids will increase both reinforcement aspects and contribute to creating a tougher silacious char, which will reduce recession at higher heat rates. Use of expanding epoxy resin (lightweight MCC) systems are also useful in that they reduce system weight, have greater insulative properties, and a decrease in application times can be realized.

  15. Nanotechnology Formulations for Antibacterial Free Fatty Acids and Monoglycerides.

    Science.gov (United States)

    Jackman, Joshua A; Yoon, Bo Kyeong; Li, Danlin; Cho, Nam-Joon

    2016-03-03

    Free fatty acids and monoglycerides have long been known to possess broad-spectrum antibacterial activity that is based on lytic behavior against bacterial cell membranes. Considering the growing challenges of drug-resistant bacteria and the need for new classes of antibiotics, the wide prevalence, affordable cost, and broad spectrum of fatty acids and monoglycerides make them attractive agents to develop for healthcare and biotechnology applications. The aim of this review is to provide a brief introduction to the history of antimicrobial lipids and their current status and challenges, and to present a detailed discussion of ongoing research efforts to develop nanotechnology formulations of fatty acids and monoglycerides that enable superior in vitro and in vivo performance. Examples of nano-emulsions, liposomes, solid lipid nanoparticles, and controlled release hydrogels are presented in order to highlight the potential that lies ahead for fatty acids and monoglycerides as next-generation antibacterial solutions. Possible application routes and future directions in research and development are also discussed.

  16. Nanobioprobe for the Determination of Pork Adulteration in Burger Formulations

    International Nuclear Information System (INIS)

    We report the development of a swine-specific hybrid nanobioprobe through a covalent integration of a fluorophore-labeled 27-nucleotide AluI-fragment of swine cytochrome b gene to a 3 nm gold nanoparticle for the determination of pork adulteration in processed meat products. We tested the probe to estimate adulterated pork in ready-to-eat pork-spiked beef burgers. The probe quantitatively detected 1-100% spiked pork in burger formulations with ≥90% accuracy. A plot of observed fluorescence against the known concentration of AluI-digested pork DNA targets generated a concave curve, demonstrating a power relationship (y=2.956x0.509) with a regression coefficient (R2) of 0.986. No cross-species detection was found in a standard set of pork, beef, chicken, mutton, and chevon burgers. The method is suitable for the determination of very short-length nucleic acid targets which cannot be estimated by conventional and real-time PCR but are essential for the determination of micro RNA in bio diagnostics and degraded DNA in forensic testing and food analysis.

  17. Nanobioprobe for the Determination of Pork Adulteration in Burger Formulations

    Directory of Open Access Journals (Sweden)

    M. E. Ali

    2012-01-01

    Full Text Available We report the development of a swine-specific hybrid nanobioprobe through a covalent integration of a fluorophore-labeled 27-nucleotide AluI-fragment of swine cytochrome b gene to a 3 nm gold nanoparticle for the determination of pork adulteration in processed meat products. We tested the probe to estimate adulterated pork in ready-to-eat pork-spiked beef burgers. The probe quantitatively detected 1–100% spiked pork in burger formulations with ≥90% accuracy. A plot of observed fluorescence against the known concentration of AluI-digested pork DNA targets generated a concave curve, demonstrating a power relationship (y=2.956x0.509 with a regression coefficient (R2 of 0.986. No cross-species detection was found in a standard set of pork, beef, chicken, mutton, and chevon burgers. The method is suitable for the determination of very short-length nucleic acid targets which cannot be estimated by conventional and real-time PCR but are essential for the determination of microRNA in biodiagnostics and degraded DNA in forensic testing and food analysis.

  18. Nanotechnology Formulations for Antibacterial Free Fatty Acids and Monoglycerides

    Directory of Open Access Journals (Sweden)

    Joshua A. Jackman

    2016-03-01

    Full Text Available Free fatty acids and monoglycerides have long been known to possess broad-spectrum antibacterial activity that is based on lytic behavior against bacterial cell membranes. Considering the growing challenges of drug-resistant bacteria and the need for new classes of antibiotics, the wide prevalence, affordable cost, and broad spectrum of fatty acids and monoglycerides make them attractive agents to develop for healthcare and biotechnology applications. The aim of this review is to provide a brief introduction to the history of antimicrobial lipids and their current status and challenges, and to present a detailed discussion of ongoing research efforts to develop nanotechnology formulations of fatty acids and monoglycerides that enable superior in vitro and in vivo performance. Examples of nano-emulsions, liposomes, solid lipid nanoparticles, and controlled release hydrogels are presented in order to highlight the potential that lies ahead for fatty acids and monoglycerides as next-generation antibacterial solutions. Possible application routes and future directions in research and development are also discussed.

  19. Nanotechnology Formulations for Antibacterial Free Fatty Acids and Monoglycerides.

    Science.gov (United States)

    Jackman, Joshua A; Yoon, Bo Kyeong; Li, Danlin; Cho, Nam-Joon

    2016-01-01

    Free fatty acids and monoglycerides have long been known to possess broad-spectrum antibacterial activity that is based on lytic behavior against bacterial cell membranes. Considering the growing challenges of drug-resistant bacteria and the need for new classes of antibiotics, the wide prevalence, affordable cost, and broad spectrum of fatty acids and monoglycerides make them attractive agents to develop for healthcare and biotechnology applications. The aim of this review is to provide a brief introduction to the history of antimicrobial lipids and their current status and challenges, and to present a detailed discussion of ongoing research efforts to develop nanotechnology formulations of fatty acids and monoglycerides that enable superior in vitro and in vivo performance. Examples of nano-emulsions, liposomes, solid lipid nanoparticles, and controlled release hydrogels are presented in order to highlight the potential that lies ahead for fatty acids and monoglycerides as next-generation antibacterial solutions. Possible application routes and future directions in research and development are also discussed. PMID:26950108

  20. Glyburide nanosuspension: Influence of processing and formulation parameter on solubility and in vitro dissolution behavior

    Directory of Open Access Journals (Sweden)

    Vinod Mokale

    2013-01-01

    Full Text Available The aim of this study was to formulate and optimize Glyburide (GB nanosuspension which is poorly water-soluble antidiabetic drug with optimization of the dissolution property and bioavailability by reducing the particle at nano size. The nanosuspension is prepared by Top down technique, i.e. high pressure homogenization. The formulation factors which affects particle size including concentration of surfactant while processing parameters includes homogenization pressure and homogenization cycle. After particle size reduction, we observe that there are increases in the surface energy which requires adequate stabilization by surfactant. In this study, practically water insoluble GB was nanoground and surfactant was employed for their stabilizing effect. In-vitro dissolution study revealed that increase in release rate of GB from nanoparticles (NPS as compare to pure raw GB. Field Emission Scanning Electron Microscope (FE-SEM study showed the spherical morphology of NPS. Particles size distribution, zeta potential, and crystal form of the formulated nanosuspension were studied by using particle size analyzer and X-ray powder diffraction. The result showed that the drug dissolution rate in nanosuspension formulation is depending upon crystal form, solubility, preparation procedure, and stabilizer employed.

  1. Sterically stabilized polymeric nanoparticles with a combinatorial approach for multi drug resistant cancer: in vitro and in vivo investigations.

    Science.gov (United States)

    Zafar, Sobiya; Negi, Lalit Mohan; Verma, Anita Kamra; Kumar, Vijay; Tyagi, Aakriti; Singh, Pratibha; Iqbal, Zeenat; Talegaonkar, Sushama

    2014-12-30

    The present work describes the preparation of sterically stabilize polymeric nanoparticles of mitoxantrone dihydrochloride (MTO) along with an efflux transporter (Pgp/BCRP) inhibitor that enhance the circulation time of nanoparticles and simultaneously surmount the problem of multidrug resistance (MDR). Mitoxantrone dihydrochloride being hydrophilic in nature had very low entrapment efficiency (%E.E.), thus in order to further enhance the lipophilicity and the %E.E., it was complexed with sodium deoxycholate (SDC) and this MTO-SDC-complex was used to formulate nanoparticles with/without Pgp/BCRP inhibitor by nanoprecipitation technique and was characterized for various in vitro and in vivo attributes. In vitro cell line studies were conducted on MCF7, A2780(p) and A2780(adr) cells. Furthermore, the targeting potential of hyaluronic acid (HA) coated nanoparticles for CD44 receptors was investigated using the MCF7 cell line. A reduction in the IC50 value observed with the inhibitor loaded nanoparticles in different cell lines indicated the BCRP/Pgp inhibiting ability of the formulated nanoparticles. The reduced macrophage uptake and the increased residence time in blood demonstrated the long circulating behaviour of the nanoparticles. The enhanced cellular uptake of HA coated nanoparticles in MCF7 cells revealed their targeting potential. The HA coated nanoparticles along with efflux transporter inhibitor exhibits a great potential for targeted chemotherapy in CD44 overexpressing MDR breast cancer.

  2. Microbial mediated preparation, characterization and optimization of gold nanoparticles.

    Science.gov (United States)

    Barabadi, Hamed; Honary, Soheila; Ebrahimi, Pouneh; Mohammadi, Milad Ali; Alizadeh, Ahad; Naghibi, Farzaneh

    2014-01-01

    The need for eco-friendly and cost effective methods for nanoparticles synthesis is developing interest in biological approaches which are free from the use of toxic chemicals as byproducts. This study aimed to biosynthesize and optimize the size of gold nanoparticles which produced by biotechnological method using Penicillium crustosum isolated from soil. Initially, Penicillium crustosum was grown in fluid czapek dox broth on shaker at 28 °C and 200 rpm for ten days and then the supernatant was separated from the mycelia to convert AuCl₄ solution into gold nanoparticles. The synthesized nanoparticles in the optimum conditions were formed with fairly well-defined dimensions and good monodispersity. The characterizations were done by using different methods (UV-Visible Spectroscopy, Fluorescence, FT-IR, AFM (Atomic Force Microscopy) and DLS (Dynamic Light Scattering). The bioconversion was optimized by Box-Behnken experimental design. The results show that the effective factors in this process were concentration of AuCl₄, pH of medium and temperature of shaker incubator. The R(2) value was calculated to be 0.9999 indicating the accuracy and ability of the polynomial model. It can be concluded that the use of multivariate analysis facilitated to find out the optimum conditions for the biosynthesis of gold nanoparticles induced by Penicillium crustosum in a time and cost effective process. The current approach suggested that rapid synthesis of gold nanoparticles would be suitable for developing a biological process for mass scale production of formulations.

  3. Development and characterization of voriconazole loaded nanoparticles for parenteral delivery.

    Science.gov (United States)

    Füredi, Petra; Kovács, Kristóf; Ludányi, Krisztina; Antal, István; Klebovich, Imre

    2016-08-20

    Human serum albumin (HSA) has attracted the most attention in the last decades as a new nanocarrier system of active pharmaceutical ingredients (API) due to its biocompatibility and high binding capacity to hydrophobic drugs. Voriconazole (VCZ), an antifungal agent with low water solubility, was selected to produce albumin based nanoparticles using nanoparticle albumin-bound technology (nab™-technology). Aim of our study was to study the development process of VCZ-loaded nanoparticles for parenteral drug delivery, such as homogenizing pressure, homogenizing cycle number and drug loading capacity. The main characters of nanoparticles such as particle size distribution and polydispersity index (PDI) were determined by dynamic light scattering. Six homogenization cycles at 1800bar were ensured the acceptable PDI value (lower than 0.3) of the VCZ content nanoparticles. Optimized formulation process produced 81.2±1nm average particle size which meets the requirements of intravenous administration. Furthermore, the encapsulated concentration of VCZ was 69.7±4.2% and the water solubility was over 2 times greater than the API itself which were determined by the developed HPLC method. The in vivo release behavior can be predicted from our applied in vitro dissolution study. Almost 50% of VCZ was liberated from the nanoparticles in the first 60min. PMID:27291972

  4. Characterization of progesterone loaded biodegradable blend polymeric nanoparticles

    Directory of Open Access Journals (Sweden)

    Fernanda Vitória Leimann

    2015-11-01

    Full Text Available ABSTRACT: The encapsulation of progesterone in poly (hydroxybutirate-co-hydroxyvalerate (PHBV, poly (ε-caprolactone (PCL, poly (L-lactic acid (PLLA nanoparticles and PHBV/PCL and PHBV/PLLA blend nanoparticles was investigated in this research. Nanoparticles were produced by miniemulsion/solvent evaporation technique with lecithin as surfactant and were characterized regarding to z-average diameter (Dz and polydispersity (PDI, progesterone recovery yield and encapsulation efficiency. Possible interactions between progesterone and the polymer matrices were investigated by Fourier Transform Infrared Spectroscopy (FTIR. High recoveries (up to 102.43±1.80% for the PHBV/PLLA blend and encapsulation efficiencies (up to 99.53±0.04% for PCL were achieved and the nanoparticles presented narrow size distribution (0.12±0.03 for PLLA. PCL nanoparticles (217.5±2.12nm presented significant difference with the Dz from all the other formulations (P<0.05. The most evident interaction between progesterone and the nanoparticles polymeric matrix was found to PHBV/PCL due to the increase in the intensity of the band located in 1631 cm-1.

  5. Quantum Holonomy Theory, Lattice-Independent Formulation

    CERN Document Server

    Aastrup, Johannes

    2016-01-01

    Quantum holonomy theory is a candidate for a non-perturbative theory of quantum gravity coupled to fermions. The theory is based on the QHD-algebra, which essentially encodes how local degrees of freedom are moved on a three-dimensional manifold. In this paper we continue the development of the theory by providing a lattice-independent formulation. We first define a Dirac type operator over a configuration space of Ashtekar connections and use it to formulate a graded version of the QHD-algebra. Next we formulate necessary conditions for a state to exist on this algebra and use the GNS construction to build a kinematical Hilbert space. Finally we find that operators, that correspond to the Dirac and gravitational Hamiltonians in a semi-classical limit, are background independent.

  6. Formulations for children: problems and solutions

    Science.gov (United States)

    Batchelor, Hannah K; Marriott, John F

    2015-01-01

    Paediatric formulation design is complex as there is a need to understand the developmental physiological changes that occur during childhood and their impact on the absorption of drugs. Paediatric dose adjustments are usually based on achieving pharmacokinetic or pharmacodynamic profiles equivalent to those achieved in adult populations. However, differences in the way in which children handle adult products or the use of bespoke paediatric formulations can result in unexpected pharmacokinetic drug profiles with altered clinical efficacy. Differences in drug formulations need to be understood by healthcare professionals involved in the prescribing, administration or dispensing of drugs to children such that appropriate advice is given to ensure that therapeutic outcomes are achieved. This issue is not confined to oral medicines but is applicable for all routes of administration encountered in paediatric therapy. PMID:25855822

  7. Engaged Problem Formulation in IS Research

    DEFF Research Database (Denmark)

    Nielsen, Peter Axel; Persson, John Stouby

    2016-01-01

    problems requires a more substantial engagement with the different stakeholders, especially when their problems are ill structured and situated in complex organizational settings. On this basis, we present an engaged approach to formulating IS problems with, not for, IS practitioners. We have come......“Is this the problem?”: the question that haunts many information systems (IS) researchers when they pursue work relevant to both practice and research. Nevertheless, a deliberate answer to this question requires more than simply asking the involved IS practitioners. Deliberately formulating...... to understand engaged problem formulation as joint researching and as the defining of contemporary and complex problems by researchers and those practitioners who experience and know these problems. We used this approach in investigating IS management in Danish municipalities. In this paper, we present...

  8. Chemical-Based Formulation Design: Virtual Experimentation

    DEFF Research Database (Denmark)

    Conte, Elisa; Gani, Rafiqul

    This paper presents a software, the virtual Product-Process Design laboratory (virtual PPD-lab) and the virtual experimental scenarios for design/verification of consumer oriented liquid formulated products where the software can be used. For example, the software can be employed for the design o......, hair spray, sunscreen lotion, insect repellent lotion). The results of the virtual experimentations will be illustrated through the (initial) base case designs that were obtained and their verification through real experiments and/or available product data analysis......., the additives and/or their mixtures (formulations). Therefore, the experimental resources can focus on a few candidate product formulations to find the best product. The virtual PPD-lab allows various options for experimentations related to design and/or verification of the product. For example, the selection...

  9. "Sustained release formulation of Metoclopramide Hydrochloride "

    Directory of Open Access Journals (Sweden)

    Dabbagh MA

    2000-08-01

    Full Text Available In this research, several formulations containing, an anti emetic agent (Metoclopramide hydrochloride, a hydrophilic polymer (hydroxypropylmethylcellulose and a hydrophobic polymer (ethylcellulose 10 cP were prepared by direct compression. Different factors such as: the effect of different ratios of the polymers, particle size, pressure force and differences of release in acidic and distilled water as media were investigated. After developing the ideal formulation, the effect of changing the ratio of drug in core: coating on the formulation was investigated. Coating of tablets with ethylcellulose, changed the release mechanism of drug and shifted it to near zero order release. The results showed that except when matrices were coated with ethylcellulose, drug release was proportioned to the square root of time, which might be due to the change of release pattern from matrix to reservoir system.

  10. Nanoparticle-coated organic-inorganic microparticles: experimental design and gastrointestinal tolerance evaluation

    Directory of Open Access Journals (Sweden)

    Beck Ruy Carlos R.

    2006-01-01

    Full Text Available The influences of the spray-drying parameters and the type of nanoparticles (nanocapsules or nanospheres on the characteristics of nanoparticle-coated diclofenac-loaded microparticles were investigated by using a factorial design 3². Gastrointestinal tolerance following oral administration in rats was evaluated. Formulations were selected considering the best yields, the best encapsulation efficiencies and the lowest water contents, presenting surfaces completely coated by nanostructures and a decrease in the surface areas in relation to the uncoated core. In vitro drug release demonstrated the influence of the nanoparticle-coating on the dissolution profiles of diclofenac. Nanocapsule-coated microparticles presented a protective effect on the gastrointestinal mucosa.

  11. Nanoparticle-coated organic-inorganic microparticles: experimental design and gastrointestinal tolerance evaluation

    Directory of Open Access Journals (Sweden)

    Ruy Carlos R. Beck

    2006-10-01

    Full Text Available The influences of the spray-drying parameters and the type of nanoparticles (nanocapsules or nanospheres on the characteristics of nanoparticle-coated diclofenac-loaded microparticles were investigated by using a factorial design 3². Gastrointestinal tolerance following oral administration in rats was evaluated. Formulations were selected considering the best yields, the best encapsulation efficiencies and the lowest water contents, presenting surfaces completely coated by nanostructures and a decrease in the surface areas in relation to the uncoated core. In vitro drug release demonstrated the influence of the nanoparticle-coating on the dissolution profiles of diclofenac. Nanocapsule-coated microparticles presented a protective effect on the gastrointestinal mucosa.

  12. Thiolated chitosan-modified PLA-PCL-TPGS nanoparticles for oral chemotherapy of lung cancer

    Science.gov (United States)

    Jiang, Liqin; Li, Xuemin; Liu, Lingrong; Zhang, Qiqing

    2013-02-01

    Oral chemotherapy is a key step towards `chemotherapy at home', a dream of cancer patients, which will radically change the clinical practice of chemotherapy and greatly improve the quality of life of the patients. In this research, three types of nanoparticle formulation from commercial PCL and self-synthesized d-α-tocopheryl polyethylene glycol 1000 succinate (PLA-PCL-TPGS) random copolymer were prepared in this research for oral delivery of antitumor agents, including thiolated chitosan-modified PCL nanoparticles, unmodified PLA-PCL-TPGS nanoparticles, and thiolated chitosan-modified PLA-PCL-TPGS nanoparticles. Firstly, the PLA-PCL-TPGS random copolymer was synthesized and characterized. Thiolated chitosan greatly increases its mucoadhesiveness and permeation properties, thus increasing the chances of nanoparticle uptake by the gastrointestinal mucosa and improving drug absorption. The PLA-PCL-TPGS nanoparticles were found by FESEM that they are of spherical shape and around 200 nm in diameter. The surface charge of PLA-PCL-TPGS nanoparticles was reversed from anionic to cationic after thiolated chitosan modification. The thiolated chitosan-modified PLA-PCL-TPGS nanoparticles have significantly higher level of the cell uptake than that of thiolated chitosan-modified PLGA nanoparticles and unmodified PLA-PCL-TPGS nanoparticles. In vitro cell viability studies showed advantages of the thiolated chitosan-modified PLA-PCL-TPGS nanoparticles over Taxol® in terms of cytotoxicity against A549 cells. It seems that the mucoadhesive nanoparticles can increase paclitaxel transport by opening tight junctions and bypassing the efflux pump of P-glycoprotein. In conclusion, PLA-PCL-TPGS nanoparticles modified by thiolated chitosan could enhance the cellular uptake and cytotoxicity, which revealed a potential application for oral chemotherapy of lung cancer.

  13. In vitro, in vivo and pharmacokinetic assessment of amikacin sulphate laden polymeric nanoparticles meant for controlled ocular drug delivery

    Science.gov (United States)

    Sharma, Upendra Kumar; Verma, Amita; Prajapati, Sunil Kuamr; Pandey, Himanshu; Pandey, Avinash C.

    2015-02-01

    The rationale of current exploration was to formulate positively charged amikacin-loaded polymeric nanoparticles providing a controlled release attribute. Amikacin sulphate-loaded nanoparticles were prepared by w/o/w emulsification solvent evaporation approach succeeded by high-pressure homogenization. Two bioadhesive positively charged polymers, Eudragit® RS 100 and Eudragit® RL 100, were used in the blend, with variable ratios of drug and polymer. The formulations were assessed in terms of particle size and zeta potential. Thermal gravimetric analysis was brought out on the samples of drug, polymer and drug polymer complex. Drug loading and release attributes of the nanoparticles were scrutinized and antimicrobial activity in contrast to Staphylococcus aureus was appraised. Ocular irritation test, in vivo ocular retention study, in vivo release profile (permeation study) and in vivo antibacterial activity of polymeric nanosuspensions were executed. No rupture consequence but a lengthened drug release was contemplated from all formulations. Amikacin sulphate release from the polymeric nanoparticles reflected a better fit with Korsmeyer-Peppas model. In the course of the antibacterial activity of nanoparticles against S. aureus, formulation AE1 displays the most prominent inhibitory effect as compared with marketed formulation of amikacin sulphate.

  14. Optimization of size controlled poly (lactide-co-glycolic acid nanoparticles using quality by design concept

    Directory of Open Access Journals (Sweden)

    Padmanabha R. V. Reddy

    2015-01-01

    Full Text Available Quality by design (QbD is a risk management and science-based approach laid down by the ICH as well as other Regulatory agencies to enhance pharmaceutical development throughout a product′s lifecycle. Poly(lactide-co-glycolic acid (PLGA is the material of choice for development of depot particulate formulations due to its biodegradable nature and is also considered as the ′green′ eco-friendly material due its biocompatibility and non-toxic properties. Further, PLGA based formulations are approved by regulatory agencies and currently in clinical practice. The aim of the current investigation involves formulation, optimization and in vitro characterization of size controlled PLGA based nanoparticles by employing modified nanoprecipitation technique. An initial risk-assessment analysis was conducted with different formulation and process variables along with their impact on critical quality attributes of the formulation which were identified as particle size and percentage process yield. The Ishikawa diagram was employed to determine the potential risk factors and subsequently optimized by statistical experimental design concept. Box-Behnken design was utilized to optimize nanoparticles and further characterizing the optimized nanoparticulate formulation in vitro. From the present study, it can be concluded that PLGA based nanoparticles with controlled particle size and process yield can be obtained by inculcating the concept of QbD in the product development.

  15. A Novel Formulation of Baroclinic Rotational Equilibria

    CERN Document Server

    Yasutake, Nobutoshi

    2014-01-01

    We have developed a new formulation to obtain self-gravitating, axisymmetric configurations in permanent rotation. It is applicable not only to barotropic equations of state but also to baroclinic ones, for which angular momentum distributions are not cylindrical. The formulation is based on the Lagrangian variational principle. Some test calculations are presented, in which we have achieved an error of $O(10^{-4})$ in the Virial relation. We believe that this method could be a major break-through in stellar evolution theory, in which it is a common practice that rotation is included only approximately in one dimensional models.

  16. Parent formulation at the Lagrangian level

    CERN Document Server

    Grigoriev, Maxim

    2010-01-01

    The recently proposed first-order parent formalism at the level of equations of motion is specialized to the case of Lagrangian systems. It is shown that for diffeomorphism-invariant theories the parent formulation takes the form of an AKSZ-type sigma model. The proposed formulation can be also seen as a Lagrangian version of the BV-BRST extension of the Vasiliev unfolded approach. We also discuss its possible interpretation as a multidimensional generalization of the Hamiltonian BFV-BRST formalism. The general construction is illustrated by examples of mechanics, relativistic particle, Yang-Mills theory, and gravity.

  17. Quaternionic formulation of the exact parity model

    Energy Technology Data Exchange (ETDEWEB)

    Brumby, S.P.; Foot, R.; Volkas, R.R.

    1996-02-28

    The exact parity model (EPM) is a simple extension of the standard model which reinstates parity invariance as an unbroken symmetry of nature. The mirror matter sector of the model can interact with ordinary matter through gauge boson mixing, Higgs boson mixing and, if neutrinos are massive, through neutrino mixing. The last effect has experimental support through the observed solar and atmospheric neutrino anomalies. In the paper it is shown that the exact parity model can be formulated in a quaternionic framework. This suggests that the idea of mirror matter and exact parity may have profound implications for the mathematical formulation of quantum theory. 13 refs.

  18. Solid lipid nanoparticles with and without hydroxypropyl-β-cyclodextrin: a comparative study of nanoparticles designed for colonic drug delivery

    Science.gov (United States)

    Spada, Gianpiera; Gavini, Elisabetta; Cossu, Massimo; Rassu, Giovanna; Giunchedi, Paolo

    2012-03-01

    New solid lipid nanoparticles (SLN), composed of Compritol ATO888 (C) and hydroxypropyl-β-cyclodextrin (HP), were developed in order to study a new colon-specific formulation for diclofenac sodium (D) delivery. The prepared batches differ from each other by the molecular ratio between HP and D and by the composition of the matrix. Nanoparticles composed of an exclusively lipid matrix and nanoparticles with an oligomeric and lipid matrix were compared in order to establish the effect of both components on the drug delivery tests performed. The SLN preparation method was based on the oil/water hot homogenization process. Emulsions produced were cooled at room temperature and lyophilized in order to obtain dried nanoparticles; possible damage to nanoparticle shape and size was avoided by the addition of cryoprotectants to the aqueous dispersion of nanoparticles before exsiccation. An in vitro toxicity study was performed using CaCo2 cells to establish the safety of the prepared SLN. Data obtained showed that production method studied guarantees emulsions composed of nanosized drops which can be dried by lyophilization into SLN with a size range of 300-600 nm. In vitro and ex vivo tests demonstrated that dried SLN can be considered as colon delivery systems; however, the matrix composition as well as the presence of cryoprotectant on their surface influences the release and permeation rate of D. The in vitro toxicity studies indicated that the SLN are well tolerated.

  19. Characteristics of indium-tin-oxide (ITO) nanoparticle ink-coated layers recycled from ITO scraps

    Science.gov (United States)

    Cha, Seung-Jae; Hong, Sung-Jei; Lee, Jae Yong

    2015-09-01

    This study investigates the characteristics of an indium-tin-oxide (ITO) ink layer that includes nanoparticles synthesized from ITO target scraps. The particle size of the ITO nanoparticle was less than 15 nm, and the crystal structure was cubic with a (222) preferred orientation. Also, the composition ratio of In to Sn was 92.7 to 7.3 in weight. The ITO nanoparticles were well dispersed in the ink solvent to formulate a 20-wt% ITO nanoparticle ink. Furthermore, the ITO nanoparticle ink was coated onto a glass substrate, followed by heat-treatment at 600 °C. The layer showed good sheet resistances below 400 Ω/□ and optical transmittances higher than 88% at 550 nm. Thus, we can conclude that the characteristics of the layer make it highly applicable to a transparent conductive electrode.

  20. Full factorial design, physicochemical characterisation and biological assessment of cyclosporine A loaded cationic nanoparticles.

    Science.gov (United States)

    Hermans, Kris; Van den Plas, Dave; Everaert, Arnout; Weyenberg, Wim; Ludwig, Annick

    2012-09-01

    Cyclosporine A loaded poly(lactide-co-glycolide) nanoparticles coated with chitosan were prepared using the o/w emulsification solvent evaporation method. A 2(3) full factorial design was used to investigate the effect of 3 preparation parameters on the particle size, polydispersity index, zeta potential and drug release. In vitro experiments were performed in order to evaluate the cytotoxicity and anti-inflammatory activity of the developed nanoparticles. Particle sizes varied from 156 nm to 314 nm, and polydispersity index values of 0.07-0.56 were obtained depending on the different preparation parameters. All nanoparticles showed positive zeta potential values. Nanoparticles prepared with the highest concentration chitosan retained a positive zeta potential after dispersion in simulated lachrymal fluid, which supports the possibility of an electrostatic interaction between these particles and the negatively charged mucus layer at the eye. The in vitro release profile of cyclosporine A from the chitosan-coated nanoparticles was strongly dependent on the release medium used. None of the cationic nanoparticle formulations showed significant cytotoxicity compared to the negative control using human epithelial cells (HaCaT). Cyclosporine A encapsulated in the various nanoparticle formulations remained anti-inflammatory active as significant suppression of interleukine-2 secretion in concanavalin A stimulated Jurkat T cells was observed.

  1. Organically Modified Silica Nanoparticles Interaction with Macrophage Cells: Assessment of Cell Viability on the Basis of Physicochemical Properties.

    Science.gov (United States)

    Kumar, Dhiraj; Mutreja, Isha; Keshvan, Prashant C; Bhat, Madhusudan; Dinda, Amit K; Mitra, Susmita

    2015-11-01

    Silica nanoparticles have drawn a lot of attention for nanomedicine application, and this is attributed to their biocompatibility and ease of surface functionalization. However, successful utilization of these inorganic systems for biomedical application depends on their physicochemical properties. This study, therefore, discusses in vitro toxicity of organically modified silica nanoparticles on the basis of size, shape, and surface properties of silica nanoparticles. Spherical- and oval-shaped nanoparticles having hydroxyl and amine groups were synthesized in Tween 80 micelles using different organosilanes. Nanoparticles of similar size and morphology were considered for comparative assessment. "As-prepared" nanoparticles were characterized in terms of size, shape, and surface properties using ZetaSizer, transmission electron microscopy, and Fourier transform infrared to establish the above parameters. In vitro analysis in terms of nanoparticle-based toxicity was performed on J-774 (macrophage) cell line using propidium iodide-4',6-diamidino-2-phenylindol and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Fluorescent dye-entrapped nanoparticles were used to visualize the uptake of the nanoparticles by macrophage cells. Results from cell studies suggested low levels of toxicity for different nanoparticle formulations studied, therefore are suitable for nanocarrier application for poorly soluble molecules. On the contrary, the nanoparticles of similar size and shape, having amine groups and low net negative charge, do not exhibit any in vitro cytotoxicity.

  2. Target Nanoparticles for Therapy - SANS and DLS of Drug Carrier Liposomes and Polymer Nanoparticles

    Science.gov (United States)

    Nawroth, T.; Johnson, R.; Krebs, L.; Khoshakhlagh, P.; Langguth, P.; Hellmann, N.; Goerigk, G.; Boesecke, P.; Bravin, A.; Le Duc, G.; Szekely, N.; Schweins, R.

    2016-09-01

    T arget Nano-Pharmaceutics shall improve therapy and diagnosis of severe diseases, e.g. cancer, by individual targeting of drug-loaded nano-pharmaceuticals towards cancer cells, and drug uptake receptors in other diseases. Specific ligands, proteins or cofactors, which are recognized by the diseased cells or cells of food and drug uptake, are bound to the nanoparticle surface, and thus capable of directing the drug carriers. The strategy has two branches: a) for parenteral cancer medicine a ligand set (2-5 different, surface-linked) are selected according to the biopsy analysis of the patient tissue e.g. from tumor.; b) in the oral drug delivery part the drug transport is enforced by excipients/ detergents in combination with targeting materials for cellular receptors resulting in an induced drug uptake. Both targeting nanomaterials are characterized by a combination of SANS + DLS and SAXS or ASAXS in a feedback process during development by synthesis, nanoparticle assembly and formulation.

  3. Safety and efficacy of antioxidants-loaded nanoparticles for an anti-aging application.

    Science.gov (United States)

    Felippi, Cândice C; Oliveira, Dileusa; Ströher, Alessandra; Carvalho, Anderson R; Van Etten, Eliana A M Aquino; Bruschi, Márcia; Raffin, Renata P

    2012-04-01

    The aim of this work was to perform a pilot study on the safety and efficacy of nanoparticle formulation for cosmetic application. The encapsulated actives in the nanoparticles were a blend of coenzyme Q10, retinyl palmitate, tocopheryl acetate, grape seed oil and linseed oil. The nanoparticle suspension was characterized in terms of pH and particle size. For the safety assessment, alternative methods as cytotoxicity and HET CAM were used. The clinical skin compatibility tests were also performed. The efficacy was evaluated in healthy volunteers presenting different degrees of periorbital wrinkles. Skin hydration was performed by corneometry. The nanoparticles presented narrow size around 140 nm and pH close to neutral and were suitable to cutaneous application. The alternative tests demonstrated that the nanoparticles did not present potential to induce skin irritant effects, cytotoxicity or generate oxidative stress. The clinical assays confirmed the in vitro results, demonstrating the safety of the nanoparticles, which were not irritant, sensitizing and comedogenic. Furthermore, the exposure to UVA light did not cause photoxicity. Regarding the efficacy, nanoparticles presented significant reduction in wrinkle degree after 21 days of application compared to the control. The volunteers could differentiate the nanoparticles and the control product by means of subjective analyses. In conclusion, the nanoparticles containing antioxidant actives were safe for topical use and presented anti-aging activity in vivo and are suitable to be used as cosmetic ingredient.

  4. Transdermal delivery of propranolol hydrochloride through chitosan nanoparticles dispersed in mucoadhesive gel.

    Science.gov (United States)

    Al-Kassas, Raida; Wen, Jingyuan; Cheng, Angel En-Miao; Kim, Amy Moon-Jung; Liu, Stephanie Sze Mei; Yu, Joohee

    2016-11-20

    This study aimed at improving the systemic bioavailability of propranolol-HCl by the design of transdermal drug delivery system based on chitosan nanoparticles dispersed into gels. Chitosan nanoparticles were prepared by ionic gelation technique using tripolyphosphate (TPP) as a cross-linking agent. Characterization of the nanoparticles was focused on particle size, zeta potential, surface texture and morphology, and drug encapsulation efficiency. The prepared freeze dried chitosan nanoparticles were dispersed into gels made of poloxamer and carbopol and the rheological behaviour and the adhesiveness of the gels were investigated. The results showed that smallest propranolol loaded chitosan nanoparticles were achieved with 0.2% chitosan and 0.05% TPP. Nanoparticles were stable in suspension with a zeta potential (ZP) above ±30mV to prevent aggregation of the colloid. Zeta potential was found to increase with increasing chitosan concentration due to its cationic nature. At least 70% of entrapment efficiency and drug loading were achieved for all prepared nanoparticles. When chitosan nanoparticles dispersed into gel consisting of poloxamer and carbopol, the resultant formulation exhibited thixotropic behaviour with a prolonged drug release properties as shown by the permeation studies through pig ear skin. Our study demonstrated that the designed nanoparticles-gel transdermal delivery system has a potential to improve the systemic bioavailability and the therapeutic efficacy of propranolol-HCl. PMID:27561485

  5. Safety and efficacy of antioxidants-loaded nanoparticles for an anti-aging application.

    Science.gov (United States)

    Felippi, Cândice C; Oliveira, Dileusa; Ströher, Alessandra; Carvalho, Anderson R; Van Etten, Eliana A M Aquino; Bruschi, Márcia; Raffin, Renata P

    2012-04-01

    The aim of this work was to perform a pilot study on the safety and efficacy of nanoparticle formulation for cosmetic application. The encapsulated actives in the nanoparticles were a blend of coenzyme Q10, retinyl palmitate, tocopheryl acetate, grape seed oil and linseed oil. The nanoparticle suspension was characterized in terms of pH and particle size. For the safety assessment, alternative methods as cytotoxicity and HET CAM were used. The clinical skin compatibility tests were also performed. The efficacy was evaluated in healthy volunteers presenting different degrees of periorbital wrinkles. Skin hydration was performed by corneometry. The nanoparticles presented narrow size around 140 nm and pH close to neutral and were suitable to cutaneous application. The alternative tests demonstrated that the nanoparticles did not present potential to induce skin irritant effects, cytotoxicity or generate oxidative stress. The clinical assays confirmed the in vitro results, demonstrating the safety of the nanoparticles, which were not irritant, sensitizing and comedogenic. Furthermore, the exposure to UVA light did not cause photoxicity. Regarding the efficacy, nanoparticles presented significant reduction in wrinkle degree after 21 days of application compared to the control. The volunteers could differentiate the nanoparticles and the control product by means of subjective analyses. In conclusion, the nanoparticles containing antioxidant actives were safe for topical use and presented anti-aging activity in vivo and are suitable to be used as cosmetic ingredient. PMID:22515083

  6. Cellular trafficking and anticancer activity of Garcinia mangostana extract-encapsulated polymeric nanoparticles

    Science.gov (United States)

    Pan-In, Porntip; Wanichwecharungruang, Supason; Hanes, Justin; Kim, Anthony J

    2014-01-01

    Garcinia mangostana Linn extract (GME) is a natural product that has received considerable attention in cancer therapy, and has the potential to reduce side effects of chemotherapeutics and improve efficacy. We formulated GME-encapsulated ethyl cellulose (GME-EC) and a polymer blend of ethyl cellulose and methyl cellulose (GME-EC/MC) nanoparticles. We achieved high drug-loading and encapsulation efficiency using a solvent-displacement method with particle sizes around 250 nm. Cellular uptake and accumulation of GME was higher for GME-encapsulated nanoparticles compared to free GME. In vitro cytotoxicity analysis showed effective anticancer activity of GME-EC and GME-EC/MC nanoparticles in HeLa cells in a dose-dependent manner. GME-EC/MC nanoparticles showed approximately twofold-higher anticancer activity compared to GME-EC nanoparticles, likely due to their enhanced bioavailability. GME-encapsulated nanoparticles primarily entered HeLa cells by clathrin-mediated endocytosis and trafficked through the endolysosomal pathway. As far as we know, this is the first report on the cellular uptake and intracellular trafficking mechanism of drug-loaded cellulose-based nanoparticles. In summary, encapsulation of GME using cellulose-derivative nanoparticles – GME-EC and GME-EC/MC nanoparticles – successfully improved the bioavailability of GME in aqueous solution, enhanced cellular uptake, and displayed effective anticancer activity. PMID:25125977

  7. Synthesis of chitosan based nanoparticles and their in vitro evaluation against phytopathogenic fungi.

    Science.gov (United States)

    Saharan, Vinod; Mehrotra, Akanksha; Khatik, Rajesh; Rawal, Pokhar; Sharma, S S; Pal, Ajay

    2013-11-01

    The main aim of present study was to prepare chitosan, chitosan-saponin and Cu-chitosan nanoparticles to evaluate their in vitro antifungal activities. Various nanoparticles were prepared using ionic gelation method by interaction of chitosan, sodium tripolyphosphate, saponin and Cu ions. Their particle size, polydispersity index, zeta potential and structures were confirmed by DLS, FTIR, TEM and SEM. The antifungal properties of nanoparticles against phytopathogenic fungi namely Alternaria alternata, Macrophomina phaseolina and Rhizoctonia solani were investigated at various concentrations ranging from 0.001 to 0.1%. Among the various formulations of nanoparticles, Cu-chitosan nanoparticles were found most effective at 0.1% concentration and showed 89.5, 63.0 and 60.1% growth inhibition of A. alternata, M. phaseolina and R. solani, respectively in in vitro model. At the same concentration, Cu-chitosan nanoparticles also showed maximum of 87.4% inhibition rate of spore germination of A. alternata. Chitosan nanoparticles showed the maximum growth inhibitory effects (87.6%) on in vitro mycelial growth of M. phaseolina at 0.1% concentration. From our study it is evident that chitosan based nanoparticles particularly chitosan and Cu-chitosan nanoparticles have tremendous potential for further field screening towards crop protection.

  8. Study on Tat Mediated Magnetic Nanoparticles Having Composite Targeting Function

    Institute of Scientific and Technical Information of China (English)

    YAO Peng; HUANG Jie; ZHAO Ai-jie; KANG Chun-sheng; CHANG Jin; PU Pei-yu

    2005-01-01

    This paper describes a new formulation of magnetic nanoparticles coated by a novel polymer matrix-O-Carboxylmethylated Chitosan (O-CMC) as a drug/gene carrier. The O-CMC magnetic nanoparticles were derivatized with a peptide sequence from the HIV-tat protein and transferrin to improve the translocationai property and cellar uptake of the nanoparticles. To evaluate the O-MNPsTat-Tf as a drug carrier, Methotrexate (MTX) was incorporated as a model drug and MTX-Ioaded O-MNPs-Tat-Tf with an average diameter of 75 nm were prepared and characterized by TEM, AFM and VSM. The cytotoxicity of MTX-Ioaded OMNPs-Tat-Tf was investigated with C6 cells. The results showed that the MTXloaded O-MNPs-Tat-Tf retained significant antitumor toxicity.

  9. Molecular confinement of human amylin in lipidic nanoparticles.

    Science.gov (United States)

    Braga, Raquel Rennó; Almeida, Luciana; Guerreiro, Luiz Henrique; Tinoco, Priscilla; Miranda, Kildare R; Braga, Carolina A; Gadelha, Ana Paula; Garcia, Sheila; Lima, Luis Mauricio T R

    2016-09-01

    Amylin is a pancreatic hormone involved in the regulation of glucose metabolism and homeostasis. Restoration of the post-prandial and basal levels of human amylin in diabetic individuals is a key in controlling glycemia, controlling glucagon, reducing the insulin dose and increasing satiety, among other physiologic functions. Human amylin has a high propensity to aggregate. We have addressed this issue by designing a liposomal human amylin formulation. Nanoparticles of multilamellar liposomes comprising human amylin were obtained with 53% encapsulation efficiency. The in vitro kinetic release assay shows a biphasic profile. The stabilization of the lipidic nanoparticle against freeze-drying was achieved by using mannitol as a cryoprotectant, as evidenced by morphological characterization. The effectiveness of the human amylin entrapped in lipidic nanoparticles was tested by the measurement of its pharmacological effect in vivo after subcutaneous administration in mice. Collectively these results demonstrate the compatibility of human amylin with the lipidic interface as an effective pharmaceutical delivery system. PMID:26340033

  10. Label-free gold nanoparticles for the determination of neomycin

    Science.gov (United States)

    Apyari, Vladimir V.; Dmitrienko, Stanislava G.; Arkhipova, Viktoriya V.; Atnagulov, Aydar G.; Gorbunova, Mariya V.; Zolotov, Yury A.

    2013-11-01

    A new spectrophotometric method for the determination of neomycin has been developed. The method is based on aggregation of label-free gold nanoparticles leading to change in absorption spectra and color of the solution. Influence of different factors (the concentration of ethylenediaminetetraacetate (EDTA), pH, the concentrations of neomycin and the nanoparticles) on the aggregation and analytical performance of the method was investigated. EDTA plays an important role not only as a masking agent to eliminate interferences of metal cations but strongly affects the sensitivity of the nanoparticles relative to neomycin. The method allows to determine neomycin with detection limit of 28 ng mL-1. It was applied to analysis of eye- and ear-drops. The sample pretreatment is simply done by diluting the formulation with water.

  11. Collective plasmon modes in a compositionally asymmetric nanoparticle dimer

    Directory of Open Access Journals (Sweden)

    Fuyi Chen

    2011-09-01

    Full Text Available The plasmon coupling phenomenon of heterodimers composed of silver, gold and copper nanoparticles of 60 nm in size and spherical in shape were studied theoretically within the scattered field formulation framework. In-phase dipole coupled σ-modes were observed for the Ag-Au and Ag-Cu heterodimers, and an antiphase dipole coupled π-mode was observed for the Ag-Au heterodimer. These observations agree well with the plasmon hybridization theory. However, quadrupole coupled modes dominate the high energy wavelength range from 357-443 nm in the scattering cross section of the D=60 nm Ag-Au and Ag-Cu heterodimer. We demonstrate for the first time that collective plasmon modes in a compositionally asymmetric nanoparticle dimer have to be predicted from the dipole-dipole approximation of plasmon hybridization theory together with the interband transition effect of the constitutive metals and the retardation effect of the nanoparticle size.

  12. Lipid nanoparticles with accessible nickel as a vaccine delivery system for single and multiple his-tagged HIV antigens

    OpenAIRE

    Yan, Weili; Jain, Anekant; O’Carra, Ronan; Woodward, Jerold G.; LI, Wenxue; Li,Guanhan; Nath, Avindra; Russell J Mumper

    2009-01-01

    Lipid-based nanoparticles (NPs) with a small amount of surface-chelated nickel (Ni-NPs) were developed to easily formulate the human immunodeficiency virus (HIV) his-tagged Tat (his-Tat) protein, as well as to formulate and co-deliver two HIV antigens (his-p24 and his-Nef) on one particle. Female BALB/c mice were immunized by subcutaneous injection with his-Tat/Ni-NP formulation (1.5 μg his-Tat/mouse) and control formulations on day 0 and 14. The day 28 anti-Tat specific immunoglobulin G tite...

  13. Cell Membrane-Cloaked Nanoparticles for Targeted Therapeutics

    Science.gov (United States)

    Luk, Brian Tsengchi

    The advent of nanoparticle-based delivery systems has made a significant impact on clinical patient outcomes. In recent decades, myriad nanoparticle-based therapeutic agents have been developed for the treatment and management of ailments such as cancer, diabetes, pain, bacterial infections, and asthma, among many others. Nanotherapeutics offer many distinct advantages over conventional free drug formulations. For example, nanoparticles are able to accumulate at tumor sites by extravasation through leaky vasculature at tumor sites via the enhanced permeability and retention (EPR) effect; nanoparticles can also be tailored to have desirable characteristics, such as prolonged circulation in the blood stream, improved drug encapsulation, and sustained or triggered drug release. Currently, a growing number of nanoformulations with favorable pharmacological profiles and promising efficacy are being used in clinical trials for the treatment of various cancers. Building on the success of these encouraging clinical results, new engineering strategies have emerged that combine synthetic nanoparticles with natural biomaterials to create nature-inspired biomimetic delivery systems. The work presented in this dissertation focuses on the biointerfacing between synthetic and natural materials, namely in the manifestation of cell membrane-coated nanoparticles. By exploiting the natural functionalities of source cell membranes, cell membrane-cloaked nanoparticles have huge potential in the delivery of therapeutic agents for a variety of applications. The first portion of this thesis will focus on understanding the fundamentals underlying cell membrane coating on synthetic nanoparticles. First introduced in 2011, cell membrane-cloaked nanoparticles showed immediate promise in drug delivery applications, but further understanding was necessary to be able to harness the full potential of the membrane coating platform. The first section provides further insight into the interfacial

  14. Stability of Decontamination Foam Containing Silica Nanoparticles and Viscosifier

    Energy Technology Data Exchange (ETDEWEB)

    Yoon, In Ho; Jung, Chong Hun; Yoon, Suk Bon; Kim, Chorong; Jung, Jun Young; Park, Sang Yoon; Moon, Jei Kwon; Choi, Wang Kyu [Korea Atomic Energy Research Institute, Daejeon (Korea, Republic of)

    2013-10-15

    This formulation can significantly decrease the amounts of chemical reagents and secondary waste. The advantage of decontamination foam is its potentially wide application for metallic walls, overhead surfaces, and the elements of complex components and facilities. In addition, foam is a good material for in situ decontamination because it generates low final waste volumes owing to its volume expansion. The application of foam allows for remote decontamination processing using only an injection nozzle and the equipment to generate the decontamination foam, which reduces operator exposure to high radioactivity. The decontamination efficiency can be enhanced by improving the contact time between chemical reagents and a contaminated surface through the addition of surfactants and viscosifiers into the decontamination foam. The objective of this study is to investigate the effect of silica nanoparticles and a viscosifier on the foam stability and the dissolution behaviors of corroded specimens using a non-ionic surfactant. This study showed the effect of viscosifiers and nanoparticles on the foam stability when developing new formulations of decontamination foam. The addition of xanthan gum and the mixture of xanthan gum and silica nanoparticles (M-5) significantly increased the foam stability, compared to the surfactant solution alone. This result indicates that both the viscosifier and nanoparticles have a synergistic effect on the foam stability. As the contact time increased, the dissolution rate increased to become similar to the dissolution that contained decontamination liquid.

  15. Stability of Decontamination Foam Containing Silica Nanoparticles and Viscosifier

    International Nuclear Information System (INIS)

    This formulation can significantly decrease the amounts of chemical reagents and secondary waste. The advantage of decontamination foam is its potentially wide application for metallic walls, overhead surfaces, and the elements of complex components and facilities. In addition, foam is a good material for in situ decontamination because it generates low final waste volumes owing to its volume expansion. The application of foam allows for remote decontamination processing using only an injection nozzle and the equipment to generate the decontamination foam, which reduces operator exposure to high radioactivity. The decontamination efficiency can be enhanced by improving the contact time between chemical reagents and a contaminated surface through the addition of surfactants and viscosifiers into the decontamination foam. The objective of this study is to investigate the effect of silica nanoparticles and a viscosifier on the foam stability and the dissolution behaviors of corroded specimens using a non-ionic surfactant. This study showed the effect of viscosifiers and nanoparticles on the foam stability when developing new formulations of decontamination foam. The addition of xanthan gum and the mixture of xanthan gum and silica nanoparticles (M-5) significantly increased the foam stability, compared to the surfactant solution alone. This result indicates that both the viscosifier and nanoparticles have a synergistic effect on the foam stability. As the contact time increased, the dissolution rate increased to become similar to the dissolution that contained decontamination liquid

  16. Encapsulation of gold nanoparticles into self-assembling protein nanoparticles

    OpenAIRE

    Yang Yongkun; Burkhard Peter

    2012-01-01

    Abstract Background Gold nanoparticles are useful tools for biological applications due to their attractive physical and chemical properties. Their applications can be further expanded when they are functionalized with biological molecules. The biological molecules not only provide the interfaces for interactions between nanoparticles and biological environment, but also contribute their biological functions to the nanoparticles. Therefore, we used self-assembling protein nanoparticles (SAPNs...

  17. State-Space Formulation for Circuit Analysis

    Science.gov (United States)

    Martinez-Marin, T.

    2010-01-01

    This paper presents a new state-space approach for temporal analysis of electrical circuits. The method systematically obtains the state-space formulation of nondegenerate linear networks without using concepts of topology. It employs nodal/mesh systematic analysis to reduce the number of undesired variables. This approach helps students to…

  18. Discrete formulation of teleportation of continuous variables

    OpenAIRE

    van Enk, S. J.

    1999-01-01

    Teleportation of continuous variables can be described in two different ways, one in terms of Wigner functions, the other in terms of discrete basis states. The latter formulation provides the connection between the theory of teleportation of continuous degrees of freedom of a light field and the standard description of teleportation of discrete variables.

  19. Formulation of statistical mechanics for chaotic systems

    Indian Academy of Sciences (India)

    Vishnu M Bannur; Ramesh Babu Thayyullathil

    2009-02-01

    We formulate the statistical mechanics of chaotic system with few degrees of freedom and investigated the quartic oscillator system using microcanonical and canonical ensembles. Results of statistical mechanics are numerically verified by considering the dynamical evolution of quartic oscillator system with two degrees of freedom.

  20. Structural design using equilibrium programming formulations

    Science.gov (United States)

    Scotti, Stephen J.

    1995-06-01

    Solutions to increasingly larger structural optimization problems are desired. However, computational resources are strained to meet this need. New methods will be required to solve increasingly larger problems. The present approaches to solving large-scale problems involve approximations for the constraints of structural optimization problems and/or decomposition of the problem into multiple subproblems that can be solved in parallel. An area of game theory, equilibrium programming (also known as noncooperative game theory), can be used to unify these existing approaches from a theoretical point of view (considering the existence and optimality of solutions), and be used as a framework for the development of new methods for solving large-scale optimization problems. Equilibrium programming theory is described, and existing design techniques such as fully stressed design and constraint approximations are shown to fit within its framework. Two new structural design formulations are also derived. The first new formulation is another approximation technique which is a general updating scheme for the sensitivity derivatives of design constraints. The second new formulation uses a substructure-based decomposition of the structure for analysis and sensitivity calculations. Significant computational benefits of the new formulations compared with a conventional method are demonstrated.

  1. Implicit Hamiltonian formulation of bond graphs

    NARCIS (Netherlands)

    Golo, G.; Schaft, A.J. van der; Breedveld, P.C.; Maschke, B.M.

    2003-01-01

    This paper deals with mathematical formulation of bond graphs. It is proven that the power continuous part of bond graphs, the junction structure, can be associated with a Dirac structure and that equations describing a bond graph model correspond to an implicit port-controlled Hamiltonian system wi

  2. Game Theory Formulated on Hilbert Space

    OpenAIRE

    Cheon, Taksu

    2006-01-01

    We present a consistent formulation of quantum game theory that accommodates all possible strategies in Hilbert space. The physical content of the quantum strategy is revealed as a family of classical games representing altruistic game play supplemented by quantum interferences. Crucial role of the entanglement in quantum strategy is illustrated by an example of quantum game representing the Bell's experiment.

  3. The Effects of Dogmatism on Message Formulation.

    Science.gov (United States)

    Smith, Craig Allen

    This paper presents two research studies on the use of dogmatism as a predictor of verbal communication behavior. The studies examined the effects of dogmatism on the formulation of written and oral persuasive messages by comparing college students' scores on the Rokeach D and California F Scales with a content analysis of the written or oral…

  4. [Optimization of formulations for dietetic pastry products].

    Science.gov (United States)

    Villarroel, M; Uquiche, E; Brito, G; Cancino, M

    2000-03-01

    Optimized formulations of dietetic pastry products such as cake and sponge cake premixes were formulated using the surface response methodology. % Emulsifier agent and baking time were the selected independent variables for cake, as well as % emulsifier agent % chlorinated flour the variables selected for sponge cake. Three different level of each variable summing up thirteen experimental formulae of each product were assessed to optimize the variables that could have some influence in the sensory characteristics of these dietetic products. The total sensory quality was determined for both dietetic products using the composite scoring test and a panel of 18 trained judges. Looking at the contour graphic and considering economic aspects the best combination of variables for cake formulation was 2% emulsifier agent and 48 minutes for baking time, With respect to sponge cake, the best combination was 6% emulsifier agent and 48% chlorinated flour. Shelf life studies showed that both dietetic formulations remained stable during storage conditions of 75 days at 30 degrees C. During this period, significant differences in sensory characteristics were not found (p < 0.05). Data of peroxide values were kept under the critical value reported for detection of organoleptic rancidity. Reported values of hedonic test showed that these dietetics pastry products had good acceptability, and open up marketing opportunities for new products with potential health benefits to consumers. PMID:11048573

  5. Initial value formulation of Newtonian gravity

    CERN Document Server

    Natario, J

    2004-01-01

    We show that there exists a remarkable analogy between the initial value formulation of General Relativity and Newton's gravity theory, which can be recast as an evolution problem for a flat metric in R^3. We identify conditions for solutions of both evolution problems to coincide and present examples, including a Newtonian analogue of the warp drive.

  6. Long Slot Arrays - Part 1: Theoretical Formulation

    NARCIS (Netherlands)

    Neto, A.; Lee, J.J.

    2005-01-01

    This work deals with the properties of an array of long slots fed by periodically located feed elements spaced at Nyquist interval. The presentation is structured in two parts. This first part introduces the theoretical formulation of the problem and the input impedance properties of the array when

  7. An alternative formulation of classical electromagnetic duality

    CERN Document Server

    Li, K; Li, Kang; Naón, Carlos M.

    2001-01-01

    By introducing a doublet of electromagnetic four dimensional vector potentials, we set up a manifestly Lorentz covariant and SO(2) duality invariant classical field theory of electric and magnetic charges. In our formulation one does not need to introduce the concept of Dirac string.

  8. Obscurities in the Formulation of Legal Argumentation

    NARCIS (Netherlands)

    H.J. Plug

    2012-01-01

    The Dutch Supreme Court hears grievances against motivations of judicial decisions that are based on the ground that formulations in a motivation of a decision are obscure. It is, however, difficult to determine if such an appeal against the decision will be successful. From a pragma-dialectical per

  9. Screening of mucoadhesive vaginal gel formulations

    Directory of Open Access Journals (Sweden)

    Ana Ochoa Andrade

    2014-12-01

    Full Text Available Rational design of vaginal drug delivery formulations requires special attention to vehicle properties that optimize vaginal coating and retention. The aim of the present work was to perform a screening of mucoadhesive vaginal gels formulated with carbomer or carrageenan in binary combination with a second polymer (carbomer, guar or xanthan gum. The gels were characterised using in vitroadhesion, spreadability and leakage potential studies, as well as rheological measurements (stress and frequency sweep tests and the effect of dilution with simulated vaginal fluid (SVF on spreadability. Results were analysed using analysis of variance and multiple factor analysis. The combination of polymers enhanced adhesion of both primary gelling agents, carbomer and carrageenan. From the rheological point of view all formulations presented a similar behaviour, prevalently elastic and characterised by loss tangent values well below 1. No correlation between rheological and adhesion behaviour was found. Carbomer and carrageenan gels containing the highest percentage of xanthan gum displayed good in vitro mucoadhesion and spreadability, minimal leakage potential and high resistance to dilution. The positive results obtained with carrageenan-xanthan gum-based gels can encourage the use of natural biocompatible adjuvants in the composition of vaginal products, a formulation field that is currently under the synthetic domain.

  10. Potential Vorticity Formulation of Compressible Magnetohydrodynamics

    OpenAIRE

    Arter, Wayne

    2012-01-01

    Compressible ideal magnetohydrodynamics (MHD) is formulated in terms of the time evolution of potential vorticity and magnetic flux per unit mass using a compact Lie bracket notation. It is demonstrated that this simplifies analytic solution in at least one very important situation relevant to magnetic fusion experiments. Potentially important implications for analytic and numerical modelling of both laboratory and astrophysical plasmas are also discussed.

  11. Clinical pharmacology of novel anticancer drug formulations

    NARCIS (Netherlands)

    Stuurman, F.E.

    2013-01-01

    Studies outlined in this thesis describe the impact of drug formulations on pharmacology of anticancer drugs. It consists of four parts and starts with a review describing the mechanisms of low oral bioavailability of anti-cancer drugs and strategies for improvement of the bioavailability. The major

  12. Loop formulation of gauge theory and gravity

    NARCIS (Netherlands)

    Loll, R.

    1993-01-01

    This chapter contains a overview of the loop formulation of Yang-Mills theory and 3+1-dimensional gravity in the Ashtekar form. Since the configuration space of these theories are spaces of gauges potentials, their classical and quantum descriptions may be given in terms of gauges-invariant Wilson

  13. Structural design using equilibrium programming formulations

    Science.gov (United States)

    Scotti, Stephen J.

    1995-01-01

    Solutions to increasingly larger structural optimization problems are desired. However, computational resources are strained to meet this need. New methods will be required to solve increasingly larger problems. The present approaches to solving large-scale problems involve approximations for the constraints of structural optimization problems and/or decomposition of the problem into multiple subproblems that can be solved in parallel. An area of game theory, equilibrium programming (also known as noncooperative game theory), can be used to unify these existing approaches from a theoretical point of view (considering the existence and optimality of solutions), and be used as a framework for the development of new methods for solving large-scale optimization problems. Equilibrium programming theory is described, and existing design techniques such as fully stressed design and constraint approximations are shown to fit within its framework. Two new structural design formulations are also derived. The first new formulation is another approximation technique which is a general updating scheme for the sensitivity derivatives of design constraints. The second new formulation uses a substructure-based decomposition of the structure for analysis and sensitivity calculations. Significant computational benefits of the new formulations compared with a conventional method are demonstrated.

  14. Instanton Condensation in Field Strength Formulated QCD

    CERN Document Server

    Langfeld, K

    1993-01-01

    Field strength formulated Yang-Mills theory is confronted with the traditional formulation in terms of gauge fields. It is shown that both formulations yield the same semiclassics, in particular the same instanton physics. However, at the tree level the field strength approach is superior because it already includes a good deal of of quantum fluctuations of the standard formulation. These quantum fluctuations break the scale invariance of classical QCD and give rise to an instanton interaction and this causes the instantons to condense and form a homogeneous instanton solid. Such the instanton solids show up in the field strength approach as homogeneous (constant up to gauge transformations) vacuum solutions. A new class of SU(N) instantons is presented which are not embeddings of SU(N-1) instantons but have non-trivial SU(N) color structure and carry winding number $n=N(N^{2}-1)/6$. These instantons generate (after condensation) the lowest action solutions of the field strength approach. The statistical weig...

  15. Preparation of Copper-loaded Microcapsule Formulations

    Directory of Open Access Journals (Sweden)

    Nenad Jalšenjak

    2011-06-01

    Full Text Available Novel copper-loaded chitosan or chitosan/alginate based microcapsules formulations have been presented. It was shown that prolonged release of copper from microcapsules accompanied with possible prolonged presence of copper on leaves is useful in crop protection.

  16. Preparation of Copper-loaded Microcapsule Formulations

    Directory of Open Access Journals (Sweden)

    Nenad Jalšenjak

    2014-02-01

    Full Text Available Novel copper-loaded chitosan or chitosan/alginate based microcapsules formulations have been presented. It was shown that prolonged release of copper from microcapsules accompanied with possible prolonged presence of copper on leaves is useful in crop protection.

  17. An exact approach for aggregated formulations

    DEFF Research Database (Denmark)

    Gamst, Mette; Spoorendonk, Simon; Røpke, Stefan

    optimality cannot be guaranteed by branching on aggregated variables. We present a generic exact solution method to remedy the drawbacks of aggregation. It combines the original and aggregated formulations and applies Benders' decomposition. We apply the method to the Split Delivery Vehicle Routing Problem....

  18. Nanoparticle incorporation of melittin reduces sperm and vaginal epithelium cytotoxicity.

    Directory of Open Access Journals (Sweden)

    Andrew P Jallouk

    Full Text Available Melittin is a cytolytic peptide component of bee venom which rapidly integrates into lipid bilayers and forms pores resulting in osmotic lysis. While the therapeutic utility of free melittin is limited by its cytotoxicity, incorporation of melittin into the lipid shell of a perfluorocarbon nanoparticle has been shown to reduce its toxicity in vivo. Our group has previously demonstrated that perfluorocarbon nanoparticles containing melittin at concentrations <10 µM inhibit HIV infectivity in vitro. In the current study, we assessed the impact of blank and melittin-containing perfluorocarbon nanoparticles on sperm motility and the viability of both sperm and vaginal epithelial cells. We found that free melittin was toxic to sperm and vaginal epithelium at concentrations greater than 2 µM (p<0.001. However, melittin nanoparticles were not cytotoxic to sperm (p = 0.42 or vaginal epithelium (p = 0.48 at an equivalent melittin concentration of 10 µM. Thus, nanoparticle formulation of melittin reduced melittin cytotoxicity fivefold and prevented melittin toxicity at concentrations previously shown to inhibit HIV infectivity. Melittin nanoparticles were toxic to vaginal epithelium at equivalent melittin concentrations ≥20 µM (p<0.001 and were toxic to sperm at equivalent melittin concentrations ≥40 µM (p<0.001. Sperm cytotoxicity was enhanced by targeting of the nanoparticles to the sperm surface antigen sperm adhesion molecule 1. While further testing is needed to determine the extent of cytotoxicity in a more physiologically relevant model system, these results suggest that melittin-containing nanoparticles could form the basis of a virucide that is not toxic to sperm and vaginal epithelium. This virucide would be beneficial for HIV serodiscordant couples seeking to achieve natural pregnancy.

  19. Optical properties of nanoparticles

    DEFF Research Database (Denmark)

    Bendix, Pól Martin

    2015-01-01

    At the NBI I am involved in projects relating to optical properties of metallic nanoparticles in particular with respect to plasmonic heating with direct applications to photothermal cancer therapy. For this purpose we have developed heating assays that can be used to measure the heating of any...... nanoscopic heat source like an irradiated nanoparticle...

  20. Microbial surfactants: fundamentals and applicability in the formulation of nano-sized drug delivery vectors.

    Science.gov (United States)

    Rodrigues, Ligia R

    2015-07-01

    Microbial surfactants, so-called biosurfactants, comprise a wide variety of structurally distinct amphipathic molecules produced by several microorganisms. Besides exhibiting surface activity at the interfaces, these molecules present powerful characteristics including high biodegradability, low toxicity and special biological activities (e.g. antimicrobial, antiviral, anticancer, among others), that make them an alternative to their chemical counterparts. Several medical-related applications have been suggested for these molecules, including some reports on their potential use in the formulation of nano-sized drug delivery vectors. However, despite their promises, due to the generalized lack of knowledge on microbial surfactants phase behavior and stability under diverse physicochemical conditions, these applications remain largely unexplored, thus representing an exciting field of research. These nano-sized vectors are a powerful approach towards the current medical challenges regarding the development of efficient and targeted treatments for several diseases. In this review, a special emphasis will be given to nanoparticles and microemulsions. Nanoparticles are very auspicious as their size, shape and stability can be manipulated by changing the environmental conditions. On the other hand, the easiness of formulation, as well as the broad possibilities of administration justifies the recent popularity of the microemulsions. Notwithstanding, both vector types still require further developments to overcome some critical limitations related with toxicity and costs, among others. Such developments may include the search for other system components, as the microbial surfactants, that can display improved features. PMID:25655712

  1. Nanoparticles - A paradigm for topical drug delivery

    Directory of Open Access Journals (Sweden)

    Yogesh S Chaudhari

    2012-01-01

    Full Text Available Topical drug delivery is still a challenge due to the difficulties in controlling the active pharmaceutical ingredient (API fate within the skin. Due to the safety of the component material and controlled release abilities, nanoparticles offer an excellent opportunity for the rational delivery of drugs to the desired target site and hence these carrier systems are effectively used for topical delivery of variety of active principles for both pharmaceutical as well as cosmetic purposes. Recently, solid lipid nanoparticles (SLNs have shown a great potential as carriers for topical administration of active substances, principally owing to the possible targeting effect and controlled release in different skin strata. Also, nanostructured lipid carriers (NLCs are a new type of topical delivery system offering improved performance in terms of drug loading and long-term stability with the ability to form highly concentrated dispersions. Another invention in the field of topical drug delivery is the use of micellar nanoparticles (MNPs that offer a potentially fast and inexpensive pharmaceutical development model by using drugs already proven safe and effective to create new proprietary formulations. These novel drug delivery systems have gained much interest as they combine both the technology of lipid sciences and nanosciences, and hence may be better alternative carriers.

  2. Dead Sea Minerals loaded polymeric nanoparticles.

    Science.gov (United States)

    Dessy, Alberto; Kubowicz, Stephan; Alderighi, Michele; Bartoli, Cristina; Piras, Anna Maria; Schmid, Ruth; Chiellini, Federica

    2011-10-15

    Therapeutic properties of Dead Sea Water (DSW) in the treatment of skin diseases such as atopic dermatitis, psoriasis and photo aging UV damaged skin have been well established. DSW is in fact rich in minerals such as calcium, magnesium, sodium, potassium, zinc and strontium which are known to exploit anti-inflammatory effects and to promote skin barrier recovery. In order to develop a Dead Sea Minerals (DSM) based drug delivery system for topical therapy of skin diseases, polymeric nanoparticles based on Poly (maleic anhydride-alt-butyl vinyl ether) 5% grafted with monomethoxy poly(ethyleneglycol) 2000 MW (PEG) and 95% grafted with 2-methoxyethanol (VAM41-PEG) loaded with DSM were prepared by means of a combined miniemulsion/solvent evaporation process. The resulting nanoparticles were characterized in terms of dimension, morphology, biocompatibility, salt content and release. Cytocompatible spherical nanoparticles possessing an average diameter of about 300 nm, a time controlled drug release profile and a high formulation yield were obtained. PMID:21676600

  3. Therapeutic nanoparticles from novel multiblock engineered polyesterurethanes

    Energy Technology Data Exchange (ETDEWEB)

    Mattu, C., E-mail: clara.mattu@polito.it; Boffito, M.; Sartori, S. [Dipartimento di Ingegneria Meccanica e Aerospaziale, Politecnico di Torino (Italy); Ranzato, E. [Universita del Piemonte Orientale, DiSIT-Dipartimento di Scienze e Innovazione Tecnologica (Italy); Bernardi, E.; Sassi, M. P. [INRIM-Istituto Nazionale di Ricerca Metrologica (Italy); Di Rienzo, A. M.; Ciardelli, G. [Dipartimento di Ingegneria Meccanica e Aerospaziale, Politecnico di Torino (Italy)

    2012-12-15

    A novel biodegradable material belonging to the class of polyester-urethanes (PURs), based on poly({epsilon}-caprolactone) (PCL) blocks, was proposed as matrix-forming material for the preparation of nanoparticles by the solvent displacement method. This method has been widely applied to prepare nanoparticles with reproducible, small size with commercially available polyesters or polyester-polyether copolymers. These carriers often displayed fast and poorly controllable release rates. In response to these problems we proposed the insertion of polyesters into a more complex microstructure, such as that of polyurethanes, characterized by the alternation of hard and soft segments, in order to modulate and control the degradation rate and release profiles. PCL-based PUR (C-BC2000) was synthesized according to a two step synthesis procedure. Commercial PCL and poly(d, l lactide) (PLA) were used as controls; and paclitaxel, a potent anti-neoplastic drug, was encapsulated inside all carriers. Carriers prepared with the new material showed no intrinsic cytotoxicity (A-431 cells), with similar size in the range 211-226 nm and surface charge as the commercial controls. Moreover, C-BC2000 nanoparticles exhibited a slightly faster degradation rate, a much higher encapsulation efficiency (89 % against 24 % and 18 % for PLA and PCL, respectively) and a longer and more controlled release profile. This study highlighted the possibility to successfully employ biodegradable polyurethanes to prepare particles for controlled drug delivery, suggesting further and extensive investigation on the introduction of different PUR formulations in this field.

  4. Energy breathing of nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Dynich, Raman A., E-mail: dynich@solo.by [Institute of Social Educational Technologies (Belarus)

    2015-06-15

    The paper considers the energy exchange process of the electromagnetic wave with a spherical metal nanoparticle. Based on the account of the temporal dependencies of electric and magnetic fields, the author presents an analytical dependence of the energy flow passing through the spherical surface. It is shown that the electromagnetic energy, localized in metal nanoparticles, is not a stationary value and periodically varies with time. A consequence of the energy nonstationarity is a nonradiating exit of the electromagnetic energy out of the nanoparticle. During the time equal to the period of wave oscillations, the electromagnetic energy is penetrating twice into the particle and quits it twice. The particle warms up because of the difference in the incoming and outgoing energies. Such “energy breathing” is presented for spherical Ag and Au nanoparticles with radii of 10 and 33 nm, respectively. Calculations were conducted for these nanoparticles embedded into the cell cytoplasm near the frequencies of their surface plasmon resonances.

  5. Magnetic interactions between nanoparticles

    Directory of Open Access Journals (Sweden)

    Steen Mørup

    2010-12-01

    Full Text Available We present a short overview of the influence of inter-particle interactions on the properties of magnetic nanoparticles. Strong magnetic dipole interactions between ferromagnetic or ferrimagnetic particles, that would be superparamagnetic if isolated, can result in a collective state of nanoparticles. This collective state has many similarities to spin-glasses. In samples of aggregated magnetic nanoparticles, exchange interactions are often important and this can also lead to a strong suppression of superparamagnetic relaxation. The temperature dependence of the order parameter in samples of strongly interacting hematite nanoparticles or goethite grains is well described by a simple mean field model. Exchange interactions between nanoparticles with different orientations of the easy axes can also result in a rotation of the sub-lattice magnetization directions.

  6. Industrial applications of nanoparticles.

    Science.gov (United States)

    Stark, W J; Stoessel, P R; Wohlleben, W; Hafner, A

    2015-08-21

    Research efforts in the past two decades have resulted in thousands of potential application areas for nanoparticles - which materials have become industrially relevant? Where are sustainable applications of nanoparticles replacing traditional processing and materials? This tutorial review starts with a brief analysis on what makes nanoparticles attractive to chemical product design. The article highlights established industrial applications of nanoparticles and then moves to rapidly emerging applications in the chemical industry and discusses future research directions. Contributions from large companies, academia and high-tech start-ups are used to elucidate where academic nanoparticle research has revolutionized industry practice. A nanomaterial-focused analysis discusses new trends, such as particles with an identity, and the influence of modern instrument advances in the development of novel industrial products.

  7. Single Nanoparticle Plasmonic Sensors

    Directory of Open Access Journals (Sweden)

    Manish Sriram

    2015-10-01

    Full Text Available The adoption of plasmonic nanomaterials in optical sensors, coupled with the advances in detection techniques, has opened the way for biosensing with single plasmonic particles. Single nanoparticle sensors offer the potential to analyse biochemical interactions at a single-molecule level, thereby allowing us to capture even more information than ensemble measurements. We introduce the concepts behind single nanoparticle sensing and how the localised surface plasmon resonances of these nanoparticles are dependent upon their materials, shape and size. Then we outline the different synthetic approaches, like citrate reduction, seed-mediated and seedless growth, that enable the synthesis of gold and silver nanospheres, nanorods, nanostars, nanoprisms and other nanostructures with tunable sizes. Further, we go into the aspects related to purification and functionalisation of nanoparticles, prior to the fabrication of sensing surfaces. Finally, the recent developments in single nanoparticle detection, spectroscopy and sensing applications are discussed.

  8. Coefficient strengthening : a tool for formulating mixed integer programs

    OpenAIRE

    Andersen, Kent; Pochet, Yves

    2007-01-01

    Providing a good formulation is an important part of solving a mixed integer program. We suggest to measure the quality of a formulation by whether it is possible to strengthen the coefficients of the formulation. Sequentially strengthening coefficients can then be used as a tool for improving formulations. We believe this method could be useful for analyzing and producing tight formulations of problems that arise in practice. We illustrate the use of the approach on a problem in production s...

  9. Dry Powder form of Polymeric Nanoparticles for Pulmonary Drug Delivery.

    Science.gov (United States)

    Shiehzadeh, Farideh; Tafaghodi, Mohsen

    2016-01-01

    Delivery to the lungs is an efficient way to deliver drugs directly to the site of action or to the blood circulation. Because of limitations of direct administration of free drugs, particulate drug delivery systems such as DPI formulations based on nanoparticles (NPs) have been of interest for pulmonary drug delivery. The prolonged residence of NPs in the lungs due to ability to escape from the clearance mechanisms such as mucociliary escalator, macrophage uptake (a size of 1-2 µm is ideal for macrophage phagocytosis), and translocation to the systemic circulation is amongst the key advantages of NPs. By this approach, the controlled pulmonary delivery of drugs, peptides, proteins, genes, siRNA, and vaccines is possible. Both natural (albumin, gelatin, alginate, collagen, cyclodextrin, and chitosan) and synthetic (poly (lactide-co-glycolide) (PLGA), polyacrylates and polyanhydrides) polymers have been used in formulation of pulmonary nanovectors. As direct pulmonary administration of NPs is not feasible, by using the safe excipients, NPs could be converted to dry powder inhaler (DPI) formulations. These can provide a promising deposition and stability of NPs. In this article, the DPI formulations based on polymeric nanoparticles have been reviewed and categorized based on the polymer type used for preparation of NPs. PMID:26818872

  10. Pharmacologic sensitivity of paclitaxel to its delivery vehicles drives distinct clinical outcomes of paclitaxel formulations.

    Science.gov (United States)

    Li, Yan; Chen, Nianhang; Palmisano, Maria; Zhou, Simon

    2015-04-01

    Paclitaxel, an effective antitumor agent, is formulated in various vehicles serving as carriers to deliver the hydrophobic paclitaxel to tissue. The approved formulations in the U.S. are paclitaxel formulated in Cremophor EL (currently known as Kolliphor EL) and nanoparticle albumin-bound paclitaxel (nab-paclitaxel). Despite having the same active ingredient (paclitaxel), different formulations produce distinct products with unique efficacy and safety profiles. A semimechanistic model was developed to describe the pharmacologic sensitivity of paclitaxel under different formulations. Circulating paclitaxel concentration data from patients treated with nab-paclitaxel or Cremophor EL-paclitaxel were analyzed in NONMEM using a semimechanistic model with simultaneous disposition of paclitaxel-carrier complexes and the total paclitaxel released from the complexes. The key factors driving paclitaxel exposure in circulation and peripheral tissues were explored via sensitivity analysis. The rapid decline of total paclitaxel concentration following intravenous administration of nab-paclitaxel and Cremophor EL-paclitaxel was attributed to rapid tissue distribution of the paclitaxel-carrier complexes, with minor contribution of free and protein-bound paclitaxel. Distribution of nab-paclitaxel to peripheral tissue was 4-fold faster and 10-fold more extensive than that of Cremophor EL-paclitaxel micelles, resulting in distinct tissue paclitaxel profiles. Sensitivity analyses showed the plasma paclitaxel-time profile was insensitive to the rapid rates of tissue distribution and decomposition of paclitaxel-carrier complexes but that the tissue distribution profile of paclitaxel was highly sensitive. Tissue distribution of paclitaxel is carrier complex system-dependent. Different delivery systems result in distinct tissue paclitaxel profiles but similar paclitaxel concentration-time profiles in plasma or blood, rendering the paclitaxel plasma profile a poor surrogate for its

  11. Inclusion of the helper lipid dioleoyl-phosphatidylethanolamine in solid lipid nanoparticles inhibits their transfection efficiency

    NARCIS (Netherlands)

    de Jesus, Marcelo B.; Radaic, Allan; Hinrichs, Wouter L J; Ferreira, Carmen V; de Paula, Eneida; Hoekstra, Dirk; Zuhorn, Inge S

    2014-01-01

    Solid lipid nanoparticles (SLNs) are a promising system for the delivery of lipophilic and hydrophilic drugs. They consist of a solid lipid core that is stabilized by a layer of surfactants. By the incorporation of cationic lipids in the formulation, positively charged SLNs can be generated, that ar

  12. Microemulsion Synthesis of Nanoparticles

    Directory of Open Access Journals (Sweden)

    Gotić, M.

    2013-11-01

    Full Text Available Nanoparticles and nanomaterials have wide applications in electronics, physics, material design, being also utilized as sensors, catalysts, and more and more in biomedicine. Microemulsions are an exceptionally suitable medium for the synthesis of nanoparticles due to their thermodynamical stability, great solubility of both polar and nonpolar components, as well as their ability to control the size, dispersity and shape of the particles. This review presents microemulsion techniques for the synthesis of inorganic nanoparticles. It takes place in water-in-oil microemulsions by mixing one microemulsion with a cationic precursor, and the other with a precipitating or reducing agent, or by direct addition of reducing agents or gas (O2, NH3 ili CO2 into microemul sion (Fig. 1. Metal nanoparticles are used as catalysts, sensors, ferrofluids etc. They are produced by reducing the metal cation with a suitable reducing agent. In a similar way, one can prepare nanoparticles of alloys from the metal salts, provided that the metals are mutually soluble. The microemulsion technique is also suitable for depositing nanoparticles onto various surfaces. Highly active catalysts made from nanoparticles of Pt, Pd, Rh and other noble metals may be obtained in this way. Metal oxides and hydroxides may be prepared by hydrolysis or precipitation in the water core of microemulsion. Precipitation can be initiated by adding the base or precipitating agent into the microemulsion with water solution of metal ions. Similarly, nanoparticles may be prepared of sulphides, halogenides, cyanides, carbonates, sulphates and other insoluble metal salts. To prevent oxidation of nanoparticles, especially Fe, the particles are coated with inert metals, oxides, various polymers etc. Coating may provide additional functionality; e.g. coating with gold allows subsequent functionalization with organic compounds containing sulphur, due to the strong Au–S bond. Polymer coatings decrease

  13. Exploring the Preparation of Albendazole-Loaded Chitosan-Tripolyphosphate Nanoparticles

    Directory of Open Access Journals (Sweden)

    Bong-Seok Kang

    2015-02-01

    Full Text Available The objective of this study was to improve the solubility of albendazole and optimize the preparation of an oral nanoparticle formulation, using β-cyclodextrin (βCD and chitosan-tripolyphosphate (TPP nanoparticles. The solubility of albendazole in buffers, surfactants, and various concentrations of acetic acid solution was investigated. To determine drug loading, the cytotoxic effects of the albendazole concentration in human hepatocellular carcinoma cells (HepG2 were investigated. The formulations were prepared by mixing the drug solution in Tween 20 with the chitosan solution. TPP solution was added dropwise with sonication to produce a nanoparticle through ionic crosslinking. Then the particle size, polydispersity index, and zeta potential of the nanoparticles were investigated to obtain an optimal composition. The solubility of albendazole was greater in pH 2 buffer, Tween 20, and βCD depending on the concentration of acetic acid. Drug loading was determined as 100 µg/mL based on the results of cell viability. The optimized ratio of Tween 20, chitosan/hydroxypropyl βCD, and TPP was 2:5:1, which resulted in smaller particle size and proper zeta positive values of the zeta potential. The chitosan-TPP nanoparticles increased the drug solubility and had a small particle size with homogeneity in formulating albendazole as a potential anticancer agent.

  14. Formulation of Pine Tar Antidandruff Shampoo Assessment and Comparison With Some Commercial Formulations

    Directory of Open Access Journals (Sweden)

    M. Gharavi

    1990-07-01

    Full Text Available In this study a pine tar shampoo as a new antidandruff formulation is presented. Assessment of antidandruff preparations has been hampered by the lack of standardized schedules, and reliable methods of evaluation.Some antidandruff agents such as : Zinc pyri-thione pine tar, selenium sulphide and (sulfure were used in shampoos. Samples were coded as numbers 1,2 formulated by us and 3,4 formulated commercially. The grading scheme based on 10 point scale, and corneocyte count was carried out on 50 selected volunte¬ers. Corneocyte count and fungal study proved that pine tor shampoo is effective against pityrosporum ovale. Draize lest was used for determination of the irritancy potential of the samples. Results showed that samples numbered 1,2 were relatively innocous in comparison with the others. I urthermore,s kin sensitination test on rabbit also confirmed the results obtained by Draize test. Consumer judgments proved that all formulations were acceptable.

  15. The Use of chitosan in The Formation of Silver Nanoparticles, Chitosanic Nanoparticles and Fibrous Structures

    Science.gov (United States)

    Abdelgawad, Abdelrahman Mohamed

    Nanoscale materials have attracted much attention in the last two decades due to their unique properties. The size effect attains new chemical and physical properties to these materials. Nanoparticles and nanofiber are major component of nanomaterials and they have heavily investigated in the literature for different applications. Nanoparticles could be produced from both metals as well as polymers. Chitosan, which is a natural polymer, can be used as capping agent in the preparation of metallic nanoparticles and itself, can produce nanoparticles. The utilization of nanoparticles and nanofibers for wound dressing materials is a very popular approach. Acquiring antibacterial properties to the wound dressing materials could be obtained either by formulation of nanomaterials composites or direct chemical modification of the substance. To improve the antibacterial properties of chitosan two approaches were applied. First, is through the formulation of chitosan with silver nanoparticles and the formation of nanofiber mats. In this study, the concepts of green chemistry were applied and silver nanoparticles were prepared in high concentration using chitosan as a capping polymer and glucose as a reducing agent. Nanofiber mats of polyvinyl alcohol/chitosan/silvernanoparticles were produced via electrospinning. The antibacterial activity of these fibers shows bactericidal effect against E. coli at low concentrations of Ag-NPs. In the second approach, direct chemical modification of chitosan was performed by grafting of Iodoacetic acid to the amino group at carbon-2. The chemical structure of chitosan Iodoacetamide derivative (CIA) was confirmed by FTIR and H1-NMR. The derivative was amorphous and water soluble at neutral pH. The minimum inhibitory concentration of CIA, against E. coli, was 400ig/mL and the derivative was bacteriostatic after 4h of treatment. Nanofiber mats of polyvinyl alcohol/chitosan/chitosan Iodoacetamide were produced via electrospinning. The

  16. Flexible continuous manufacturing platforms for solid dispersion formulations

    Science.gov (United States)

    Karry-Rivera, Krizia Marie

    In 2013 16,000 people died in the US due to overdose from prescription drugs and synthetic narcotics. As of that same year, 90% of new molecular entities in the pharmaceutical drug pipeline are classified as poor water-soluble. The work in this dissertation aims to design, develop and validate platforms that solubilize weak acids and can potentially deter drug abuse. These platforms are based on processing solid dispersions via solvent-casting and hot-melt extrusion methods to produce oral transmucosal films and melt tablets. To develop these platforms, nanocrystalline suspensions and glassy solutions were solvent-casted in the form of films after physicochemical characterizations of drug-excipient interactions and design of experiment approaches. A second order model was fitted to the emulsion diffusion process to predict average nanoparticle size and for process optimization. To further validate the manufacturing flexibility of the formulations, glassy solutions were also extruded and molded into tablets. This process included a systematic quality-by-design (QbD) approach that served to identify the factors affecting the critical quality attributes (CQAs) of the melt tablets. These products, due to their novelty, lack discriminatory performance tests that serve as predictors to their compliance and stability. Consequently, Process Analytical Technology (PAT) tools were integrated into the continuous manufacturing platform for films. Near-infrared (NIR) spectroscopy, including chemical imaging, combined with deconvolution algorithms were utilized for a holistic assessment of the effect of formulation and process variables on the product's CQAs. Biorelevant dissolution protocols were then established to improve the in-vivo in-vitro correlation of the oral transmucosal films. In conclusion, the work in this dissertation supports the delivery of poor-water soluble drugs in products that may deter abuse. Drug nanocrystals ensured high bioavailability, while glassy

  17. pACC1 peptide loaded chitosan nanoparticles induces apoptosis via reduced fatty acid synthesis in MDA-MB-231 cells

    Science.gov (United States)

    Kaliaperumal, Jagatheesh; Hari, Natarajan; Pavankumar, Padarthi; Elangovan, Namasivayam

    2016-06-01

    The development of formulations with therapeutic peptides has been restricted to poor cell penetration and in this attempt; we developed pACC1 peptide loaded chitosan nanoparticles. The prepared nanoparticles were characterized with FT-IR, XRD, SEM and TEM. In addition, the suitable formulation was evaluated for hemocompatibility, plasma stability and embryo toxicity using Danio rerio embryo model. The results showed that pACC1 peptide loaded chitosan nanoparticles were compatible with plasma. They possess sustained release pattern and also found to be safe up to 300 mg/L in embryo toxicity tests. Cytotoxicity assays with MDA-MB-231 cell lines suggested that, pACC1 peptide loaded chitosan nanoparticles were capable of enhanced cellular penetration and reduced palmitic acid content, which was confirmed by H1 NMR. Hence, these nanoparticles could be employed as excellent adjuvant therapeutics while treating solid tumors with multi-drug resistance.

  18. Formulation and evaluation of nitrendipine buccal films

    Directory of Open Access Journals (Sweden)

    Nappinnai M

    2008-01-01

    Full Text Available A mucoadhesive drug delivery system for systemic delivery of nitrendipine, a calcium channel blocker through buccal route was formulated. Mucoadhesive polymers like hydroxypropylmethylcellulose K-100, hydroxypropylcellulose, sodium carboxymethylcellulose, sodium alginate, polyvinyl alcohol, polyvinyl pyrrolidone K-30 and carbopol-934P were used for film fabrication. The films were evaluated for their weight, thickness, percentage moisture absorbed and lost, surface pH, folding endurance, drug content uniformity, In vitro residence time, In vitro release and ex vivo permeation. Based on the evaluation of these results, it was concluded that buccal films made of hydroxylpropylcellulose and sodium carboxymethylcellulose (5±2% w/v; F-4, which showed moderate drug release (50% w/w at the end of 2 h and satisfactory film characteristics could be selected as the best among the formulations studied.

  19. Consistency of canonical formulation of Horava gravity

    Energy Technology Data Exchange (ETDEWEB)

    Soo, Chopin, E-mail: cpsoo@mail.ncku.edu.tw [Department of Physics, National Cheng Kung University, Tainan, Taiwan (China)

    2011-09-22

    Both the non-projectable and projectable version of Horava gravity face serious challenges. In the non-projectable version, the constraint algebra is seemingly inconsistent. The projectable version lacks a local Hamiltonian constraint, thus allowing for an extra graviton mode which can be problematic. A new formulation (based on arXiv:1007.1563) of Horava gravity which is naturally realized as a representation of the master constraint algebra (instead of the Dirac algebra) studied by loop quantum gravity researchers is presented. This formulation yields a consistent canonical theory with first class constraints; and captures the essence of Horava gravity in retaining only spatial diffeomorphisms as the physically relevant non-trivial gauge symmetry. At the same time the local Hamiltonian constraint is equivalently enforced by the master constraint.

  20. Dual Foliation Formulations of General Relativity

    CERN Document Server

    Hilditch, David

    2015-01-01

    A dual foliation treatment of General Relativity is presented. The basic idea of the construction is to consider two foliations of a spacetime by spacelike hypersurfaces and relate the two geometries. The treatment is expected to be useful in various situations, and in particular whenever one would like to compare objects represented in different coordinates. Potential examples include the construction of initial data and the study of trapped tubes. It is common for studies in mathematical relativity to employ a double-null gauge. In such studies local well-posedness is treated by referring back, for example, to the generalized harmonic formulation, global properties of solutions being treated in a separate formalism. As a first application of the dual foliation formulation we find that one can in fact obtain local well-posedness in the double-null coordinates directly, which should allow their use in numerical relativity with standard methods. With due care it is expected that practically any coordinates can...

  1. Spinor Formulations for Gravitational Energy-Momentum

    CERN Document Server

    Chen, C M; Tung, R S; Chen, Chiang-Mei; Nester, James M.; Tung, Roh-Suan

    2004-01-01

    We first describe a class of spinor-curvature identities (SCI) which have gravitational applications. Then we sketch the topic of gravitational energy-momentum, its connection with Hamiltonian boundary terms and the issues of positivity and (quasi)localization. Using certain SCIs several spinor expressions for the Hamiltonian have been constructed. One SCI leads to the celebrated Witten positive energy proof and the Dougan-Mason quasilocalization. We found two other SCIs which give alternate positive energy proofs and quasilocalizations. In each case the spinor field has a different role. These neat expressions for gravitational energy-momentum have much appeal. However it seems that such spinor formulations just have no room for angular momentum; which leads us to doubt that spinor formulations can really correctly capture the elusive gravitational energy-momentum.

  2. Principles of ration formulation for ruminants

    International Nuclear Information System (INIS)

    Feeding standards as practiced in developed countries could be misleading when non-conventional feed resources are used in formulating rations for ruminant livestock in developing countries. They tend to reject the poor quality feeds that are available in vast quantities. The non-availability of good quality forage throughout the year and the need to optimise the efficiency of utilisation of locally available feed resources have lead to the application of basic nutritional principles when considering ration formulation. The alternative approach to the use of feeding standards would be to ensure that the production system matches the available resources. The development of feed supplementation strategies based on locally available feed resources require the understanding of the relative roles and nutrient needs of the two-compartment system represented by the micro-organisms in the rumen and the host animal. (author)

  3. Gauge-Invariant Formulation of Circular Dichroism.

    Science.gov (United States)

    Raimbault, Nathaniel; de Boeij, Paul L; Romaniello, Pina; Berger, J A

    2016-07-12

    Standard formulations of magnetic response properties, such as circular dichroism spectra, are plagued by gauge dependencies, which can lead to unphysical results. In this work, we present a general gauge-invariant and numerically efficient approach for the calculation of circular dichroism spectra from the current density. First we show that in this formulation the optical rotation tensor, the response function from which circular dichroism spectra can be obtained, is independent of the origin of the coordinate system. We then demonstrate that its trace is independent of the gauge origin of the vector potential. We also show how gauge invariance can be retained in practical calculations with finite basis sets. As an example, we explain how our method can be applied to time-dependent current-density-functional theory. Finally, we report gauge-invariant circular dichroism spectra obtained using the adiabatic local-density approximation. The circular dichroism spectra we thus obtain are in good agreement with experiment. PMID:27295541

  4. Formulation and characterization of rifampicin microcapsules

    Directory of Open Access Journals (Sweden)

    Md.Sarfaraz

    2010-01-01

    Full Text Available Rifampicin biodegradable microcapsules were prepared by feasible emulsification-ionic gelation method for a novel controlled release product. Sodium alginate and Carbopol 974P were used as coating polymers in different ratios 1:1, 1:2, 1:3 and 1:4 to obtain elegant microcapsules. The formulations were characterized for encapsulation efficiency, drug loading, sieve analysis, scanning electron microscopy and in vitro release studies. The microcapsules were discrete, large, almost spherical and free flowing with encapsulation efficiency in the range of 75% to 89%, drug loading 75% to 86% and size 440 µm to 500 µm. Rifampicin release from these microcapsules was slow and extended over longer periods of time depending on the polymer coat. Drug release was diffusion controlled and followed first order kinetics. The formulation MC1 with a coating ratio of 1:1 (Sodium alginate: Carbopol 974P was found to be suitable for oral controlled release.

  5. Improved efficacy of cisplatin in combination with a nano-formulation of pentacyclic triterpenediol.

    Science.gov (United States)

    Alam, Noor; Qayum, Arem; Kumar, Ashok; Khare, Vaibhav; Sharma, Parduman Raj; Andotra, Samar Singh; Singh, Shashank K; Koul, Surinder; Gupta, Prem N

    2016-11-01

    Cisplatin is widely used for the treatment of various cancers including cervical, ovarian, lung and head and neck, however, its clinical success is limited owing to the dose-dependent adverse effects, mainly nephrotoxicity and neurotoxicity. In order to address this limitation, the present study was undertaken to investigate growth inhibitory effect of cisplatin in combination with a triterpenediol (3a, 24-dihydroxyurs-12-ene and 3a, 24-dihydroxyolean-12-ene, TPD) on human ovarian cancer cell line. Poly(dl-lactic-co-glycolic) acid nanoparticles loaded with TPD (TPD-PLGA-NPs) were successfully developed by emulsion solvent evaporation method. The TPD-PLGA-NPs were characterized for size distribution and zeta potential which was in order of 152.56±3.01nm and -17.36±0.37mV respectively. The morphological evaluation was carried out by transmission electron microscopy and the formulation was also characterized using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The drug loading of the optimized formulation was 51.03±1.52μg/mg and the formulation exhibited sustained drug release profile. The in vitro cellular uptake study of coumarin-6 loaded PLGA nanoparticles in OVCAR-5 cells demonstrated a time dependent increase in uptake efficiency. Further, growth inhibitory effect of cisplatin was investigated in combination with TPD-PLGA-NPs. The combination index (CI) was <1, indicating a synergistic interaction. Further, at 75% of cell growth inhibition (ED75) the dose of cisplatin was reduced to 3.8 folds using this combination. The results indicated the potential of cisplatin and TPD-PLGA-NPs combination in order to reduce to dose limiting toxicities of the former. PMID:27524002

  6. Policy formulation and enactment: Linked up thinking?

    OpenAIRE

    McLaren, Susan

    2015-01-01

    This chapter explores the challenges, issues and potential of Design and Technology Education as an active contributor in transformational change working towards a sustainable future. The focus is on the process of policy formulation, through translation, into practice and implementation in Design and Technology education in schools. Overall, the aim is to examine what is central to change, the key stakeholders, and what might be considered the inhibitors to enactment of policy and practice c...

  7. Chemical-Based Formulation Design: Virtual Experimentation

    OpenAIRE

    Conte, Elisa; Gani, Rafiqul

    2011-01-01

    This paper presents a software, the virtual Product-Process Design laboratory (virtual PPD-lab) and the virtual experimental scenarios for design/verification of consumer oriented liquid formulated products where the software can be used. For example, the software can be employed for the design of the active ingredient-solvent mixture and/or their verification in terms of the product function. These consumer products are still primarily designed, developed and/or tested through experiment-bas...

  8. Ising formulations of many NP problems

    Science.gov (United States)

    Lucas, Andrew

    2014-02-01

    We provide Ising formulations for many NP-complete and NP-hard problems, including all of Karp's 21 NP-complete problems. This collects and extends mappings to the Ising model from partitioning, covering and satisfiability. In each case, the required number of spins is at most cubic in the size of the problem. This work may be useful in designing adiabatic quantum optimization algorithms.

  9. Critical Review of Path Integral Formulation

    OpenAIRE

    Fujita, Takehisa

    2008-01-01

    The path integral formulation in quantum mechanics corresponds to the first quantization since it is just to rewrite the quantum mechanical amplitude into many dimensional integrations over discretized coordinates $x_n$. However, the path integral expression cannot be connected to the dynamics of classical mechanics, even though, superficially, there is some similarity between them. Further, the field theory path integral in terms of many dimensional integrations over fields does not correspo...

  10. Evaluation of vaginal antifungal formulations in vivo.

    Science.gov (United States)

    McRipley, R. J.; Erhard, P. J.; Schwind, R. A.; Whitney, R. R.

    1979-01-01

    Relatively simple and rapid procedures have been developed for evaluating the local efficacy of vaginal antifungal agents in vivo in a vaginal candidiasis model in ovariectomized rats. The results of this investigation indicate that the model and methods described are quite suitable for screening potential antifungal substances and for assessing the chemotherapeutic effectiveness of new antifungal agents and formulations before carrying out clinical studies. PMID:392480

  11. Conservative formulation for compressible multiphase flows

    OpenAIRE

    Romenski, Evgeniy; Belozerov, Alexander A.; Peshkov, Ilya M.

    2014-01-01

    Derivation of governing equations for multiphase flow on the base of thermodynamically compatible systems theory is presented. The mixture is considered as a continuum in which the multiphase character of the flow is taken into account. The resulting governing equations of the formulated model belong to the class of hyperbolic systems of conservation laws. In order to examine the reliability of the model, the one-dimensional Riemann problem for the four phase flow is studied numerically with ...

  12. Multibody Dynamics Formulations Based on Variational Principle

    Institute of Scientific and Technical Information of China (English)

    孙右烈

    2003-01-01

    The formulation of multibody dynamics was studied based on variational principle. The body coonection matrix was intro-duced to define the connection configuration. The expression for the system kinematics was obtained by using the body connection ma-trix. From variational principle the general dynamical equations for multibody system were derived and the dynamical equations were given for multibody system subjected to the constraints.

  13. Prepotential Formulation of Lattice Gauge Theory

    OpenAIRE

    Raychowdhury, Indrakshi; Anishetty, Ramesh

    2014-01-01

    Within the Hamiltonian formulation of Lattice gauge theories, prepotentials, belonging to the fundamental representation of the gauge group and defined locally at each site of the lattice, enables us to construct local loop operators and loop states. We propose a set of diagrammatic rules for the action of local gauge invariant operators on arbitrary loop states. Moreover We propose a new set of fusion variables within the prepotential aproach suitable for approaching the weak coupling limit.

  14. Gurson's Model: ALE Formulation and Strain Localization

    Science.gov (United States)

    da Cunda, Luiz A. B.; Creus, Guillermo J.

    2007-05-01

    This paper presents a brief review of Gurson's damage model, employed to describes the strength degradation in ductile metals submitted to large plastic deformations. The damage model is applied using finite elements and an Arbitrary Lagrangian-Eulerian formulation (ALE), to ensure a better quality to the finite elements mesh. The study of the combined application of ALE and Gurson approach to damage modeling and strain localization is the object of this paper.

  15. FORMULATION DEVELOPMENT OF ENTERAL NUTRITION PRODUCTS

    OpenAIRE

    Mirajkar Reshma Nilesh; Patil Amol Vilas; Jamadar Shahaji Ambadas; Mirajkar Nilesh Sharadchandra

    2011-01-01

    This review mainly deals with the Formulation Development of Enteral Nutrition Products. Nutrition plays an important role in the prevention and management of many diseases. Chronic illness is associated with many complications such as anorexia, hypermetabolism, malabsorption, atrophy of muscles, liver, kidney, gastrointestinal tract heart, and impaired cell mediated immunity, susceptibility to infection, poor wound healing, anaemia, death. Hence it is important to correct caloric and nutrien...

  16. Gravity and Mirror Gravity in Plebanski Formulation

    OpenAIRE

    Bennett, D. L.; Laperashvili, L. V.; Nielsen, H. B.; Tureanu, A.

    2012-01-01

    We present several theories of four-dimensional gravity in the Plebanski formulation, in which the tetrads and the connections are the independent dynamical variables. We consider the relation between different versions of gravitational theories: Einstenian, dual, 'mirror' gravities and gravity with torsion. According to Plebanski's assumption, our world, in which we live, is described by the self-dual left-handed gravity. We propose that if the Mirror World exists in Nature, then the 'mirror...

  17. Food formulation comprising spent coffee grounds

    OpenAIRE

    Castillo, M. Dolores del; Martínez Sáez, Nuria; Ullate, Mónica

    2014-01-01

    [EN] The invention relates to a novel food formulation comprising a combination of spent coffee grounds as a source of antioxidant insoluble dietary fibre and a source of proteins, together with other additional ingredients, used to make healthy solid food for bakeries, pastry shops, and confectioner's, including bread, pastries, biscuits, breakfast cereals and appetisers, for the general population and for people with special nutritional requirements.

  18. Potential vorticity formulation of compressible magnetohydrodynamics.

    Science.gov (United States)

    Arter, Wayne

    2013-01-01

    Compressible ideal magnetohydrodynamics is formulated in terms of the time evolution of potential vorticity and magnetic flux per unit mass using a compact Lie bracket notation. It is demonstrated that this simplifies analytic solution in at least one very important situation relevant to magnetic fusion experiments. Potentially important implications for analytic and numerical modelling of both laboratory and astrophysical plasmas are also discussed. PMID:23383802

  19. Nanocrystal formulation for poorly soluble drugs

    OpenAIRE

    Liu, Peng

    2013-01-01

    Poorly soluble drugs are often a challenging problem in drug formulation. Reducing the particle size of the drug to a nano-scale leads to an increased surface area-to-volume ratio, increased dissolution velocity and adhesiveness, and improved in vivo performance of poorly soluble drugs. Wet media milling is one of the most popular techniques to prepare the nanocrystals. The aim of this thesis was to optimize the preparation conditions and characterization methods of nanosuspensions for poorly...

  20. Consistent formulation of the spacelike axial gauge

    Energy Technology Data Exchange (ETDEWEB)

    Burnel, A.; Van der Rest-Jaspers, M.

    1983-12-15

    The usual formulation of the spacelike axial gauge is afflicted with the difficulty that the metric is indefinite while no ghost is involved. We solve this difficulty by introducing a ghost whose elimination is such that the metric becomes positive for physical states. The technique consists in the replacement of the gauge condition nxA = 0 by the weaker one partial/sub 0/nxAroughly-equal0.

  1. A Novel Docetaxel-Loaded Poly (ɛ-Caprolactone)/Pluronic F68 Nanoparticle Overcoming Multidrug Resistance for Breast Cancer Treatment

    Science.gov (United States)

    Mei, Lin; Zhang, Yangqing; Zheng, Yi; Tian, Ge; Song, Cunxian; Yang, Dongye; Chen, Hongli; Sun, Hongfan; Tian, Yan; Liu, Kexin; Li, Zhen; Huang, Laiqiang

    2009-12-01

    Multidrug resistance (MDR) in tumor cells is a significant obstacle to the success of chemotherapy in many cancers. The purpose of this research is to test the possibility of docetaxel-loaded poly (ɛ-caprolactone)/Pluronic F68 (PCL/Pluronic F68) nanoparticles to overcome MDR in docetaxel-resistance human breast cancer cell line. Docetaxel-loaded nanoparticles were prepared by modified solvent displacement method using commercial PCL and self-synthesized PCL/Pluronic F68, respectively. PCL/Pluronic F68 nanoparticles were found to be of spherical shape with a rough and porous surface. The nanoparticles had an average size of around 200 nm with a narrow size distribution. The in vitro drug release profile of both nanoparticle formulations showed a biphasic release pattern. There was an increased level of uptake of PCL/Pluronic F68 nanoparticles in docetaxel-resistance human breast cancer cell line, MCF-7 TAX30, when compared with PCL nanoparticles. The cytotoxicity of PCL nanoparticles was higher than commercial Taxotere® in the MCF-7 TAX30 cell culture, but the differences were not significant ( p > 0.05). However, the PCL/Pluronic F68 nanoparticles achieved significantly higher level of cytotoxicity than both of PCL nanoparticles and Taxotere® ( p multidrug resistance in human breast cancer cells and therefore have considerable potential for treatment of breast cancer.

  2. On the spectral formulation of Granger causality.

    Science.gov (United States)

    Chicharro, D

    2011-12-01

    Spectral measures of causality are used to explore the role of different rhythms in the causal connectivity between brain regions. We study several spectral measures related to Granger causality, comprising the bivariate and conditional Geweke measures, the directed transfer function, and the partial directed coherence. We derive the formulation of dependence and causality in the spectral domain from the more general formulation in the information-theory framework. We argue that the transfer entropy, the most general measure derived from the concept of Granger causality, lacks a spectral representation in terms of only the processes associated with the recorded signals. For all the spectral measures we show how they are related to mutual information rates when explicitly considering the parametric autoregressive representation of the processes. In this way we express the conditional Geweke spectral measure in terms of a multiple coherence involving innovation variables inherent to the autoregressive representation. We also link partial directed coherence with Sims' criterion of causality. Given our results, we discuss the causal interpretation of the spectral measures related to Granger causality and stress the necessity to explicitly consider their specific formulation based on modeling the signals as linear Gaussian stationary autoregressive processes.

  3. Phytoconstituents as photoprotective novel cosmetic formulations

    Directory of Open Access Journals (Sweden)

    S Saraf

    2010-01-01

    Full Text Available Phytoconstituents are gaining popularity as ingredients in cosmetic formulations as they can protect the skin against exogenous and endogenous harmful agents and can help remedy many skin conditions. Exposure of skin to sunlight and other atmospheric conditions causes the production of reactive oxygen species, which can react with DNA, proteins, and fatty acids, causing oxidative damage and impairment of antioxidant system. Such injuries damage regulation pathways of skin and lead to photoaging and skin cancer development. The effects of aging include wrinkles, roughness, appearance of fine lines, lack of elasticity, and de- or hyperpigmentation marks. Herbal extracts act on these areas and produce healing, softening, rejuvenating, and sunscreen effects. We have selected a few photoprotective phytoconstituents, such as curcumin, resveratrol, tea polyphenols, silymarin, quercetin and ascorbic acid, and have discussed the considerations to be undertaken for the development of herbal cosmetic formulations that could reduce the occurrence of skin cancer and delay the process of photoaging. This article is aimed at providing specific and compiled knowledge for the successful preparation of photoprotective herbal cosmetic formulations.

  4. Calixarene cleansing formulation for uranium skin contamination.

    Science.gov (United States)

    Phan, Guillaume; Semili, Naïma; Bouvier-Capely, Céline; Landon, Géraldine; Mekhloufi, Ghozlene; Huang, Nicolas; Rebière, François; Agarande, Michelle; Fattal, Elias

    2013-10-01

    An oil-in-water cleansing emulsion containing calixarene molecule, an actinide specific chelating agent, was formulated in order to improve the decontamination of uranium from the skin. Commonly commercialized cosmetic ingredients such as surfactants, mineral oil, or viscosifying agents were used in preparing the calixarene emulsion. The formulation was characterized in terms of size and apparent viscosity measurements and then was tested for its ability to limit uranyl ion permeation through excoriated pig-ear skin explants in 24-h penetration studies. Calixarene emulsion effectiveness was compared with two other reference treatments consisting of DTPA and EHBP solutions. Application of calixarene emulsion induced the highest decontamination effect with an 87% decrease in uranium diffusion flux. By contrast, EHBP and DTPA solutions only allowed a 50% and 55% reduction of uranium permeation, respectively, and had the same effect as a simple dilution of the contamination by pure water. Uranium diffusion decrease was attributed to uranyl ion-specific chelation by calixarene within the formulation, since no significant effect was obtained after application of the same emulsion without calixarene. Thus, calixarene cleansing emulsion could be considered as a promising treatment in case of accidental contamination of the skin by highly diffusible uranium compounds. PMID:23982616

  5. Do surface active parenteral formulations cause inflammation?

    Science.gov (United States)

    Söderberg, Lars; Engblom, Johan; Lanbeck, Peter; Wahlgren, Marie

    2015-04-30

    Local irritation and inflammation at the site of administration are a common side effect following administration of parenteral formulations. Biological effects of surface (interfacial) activity in solutions are less well investigated than effects caused by other physico-chemical parameters such as pH and osmolality. The interfacial activity in different systems, including human plasma, typical amphiphilic substances with fundamental biological relevance such as free fatty acids, anesthetic depot formulations and six different antibiotics was measured. The relative interfacial pressure, and/or concentration of active substance, required to obtain 50% of the maximal attainable effect in terms of interfacial pressure were calculated. The aim was to test the hypothesis that these parameters would allow comparison to biological effects reported in in vivo studies on the investigated substances. The highest interfacial activity was found in a triglyceride/plasma system. Among the antibiotic tested, the highest interfacial activities were found in erythromycin and dicloxacillin, which is in accordance with previous clinical findings of a high tendency of infusion phlebitis and cell toxicity. Independently of investigated system, biological effects were minimal below a 15% relative increase of interfacial activity. Above 35-45% the effects were severe. Interfacial activity in parenteral formulations may well cause damages to tissues followed by inflammation. PMID:25708007

  6. Formulation of benzoporphyrin derivatives in Pluronics.

    Science.gov (United States)

    Chowdhary, Rubinah K; Chansarkar, Namrata; Sharif, Isha; Hioka, Noboru; Dolphin, David

    2003-03-01

    This study investigates the potential of Pluronics for the formulation of tetrapyrrole-based photosensitizers, with a particular focus on B-ring benzoporphyrin derivatives. The B-ring derivatives have a high tendency to aggregate in aqueous solutions, and this poses a significant formulation problem. Pluronics are ABA-type triblock copolymers composed of a central hydrophobic polypropylene oxide section with two hydrophilic polyethylene oxide sections of equal length at either end. Out of a range of different commercially available block copolymers studied, it was found that the longer the hydrophobic block, the better the stabilization of tetrapyrrolic drugs in monomeric form in aqueous suspensions. Of these the best performance was observed in the micelle-forming Pluronic P123. Micelle size determination by laser light scattering confirmed that particle size in stable Pluronic formulations was around 20 nm. Pluronics such as L122 formed emulsions spontaneously without the need for emulsion stabilizers; emulsions were highly stable at ambient temperatures over several days and also highly effective as potential drug delivery agents. PMID:12685658

  7. HERBAL LIPSTICK FORMULATION: A NEW APPROACH

    Directory of Open Access Journals (Sweden)

    Meher Deepali Avinash

    2011-06-01

    Full Text Available Coloring skin particularly skin of face and lips is an ancient practice going back to prehistoric period. In present days the use of such product has increased and choice of shades of color, texture and luster have been changed and become wider. This can be observed from the fact that lipsticks are marked in hundreds of shades of colors to satisfy the demand of women. The present investigation was done to formulate herbal lipstick, since lipsticks are one of the key cosmetics to be used by the women. Attempt was also made to evaluate the formulated herbal lipstick. The word herbal is a symbol of safety in contrast to the synthetic one which has adverse effects on human health. Herbal preparations viz., herbal tablets, herbal tonics, herbal paste, herbal shampoo, herbal sindhur, herbal contraceptives and herbal lipstick has become popular among the consumer herbal medicines represent the fastest growing segment to heal the various ailments. Human being have been using herbs for different purpose like food, medicine, beatifying with advancement of science & technology use of natural things including plant has been reduced except for food, vegetarian takes plant& plant only. However there is resurgence of use of herbs both as drug and cosmetics. Due to various adverse effects of available synthetic preparation the present work was conceived by us to formulate a herbal lipstick having minimal or no side effects which will extensively used by the women of our communities with great surety and satisfaction.

  8. Formulation and evaluation of antihelminthic polyherbal tablets

    Directory of Open Access Journals (Sweden)

    Dinesh Puri

    2011-01-01

    Full Text Available From time immemorial, man has been depending on plants as medicine. Helminthes infections are among the most common infections in man, affecting a large proportion of the world′s population. These helminthic diseases can be treated by various herbal drugs. The purpose of the present work was to formulate antihelminthic tablets. In this work, a spray dried-powder was used, which was obtained from the extract of different part of seven plants that were used in helminthic disease. The different tablets were prepared by using different types of disintegrating agents and various excipients. All parameters related to physicochemical property, trace metal and microbial examination of the spray-dried powder showed that these were within limits and could be used for the tablet formulation. The granules of the spray-dried powder were prepared by a wet granulation technique using isopropyl alcohol. The blends were evaluated for flow properties and for compressibility, which were found to be good. The tablets were prepared using a single rotatory punching machine, in which the punch size was 11 mm×8 mm, and formulated caplet-type tablets. These tablets were evaluated for the colour, odor, thickness and diameter, with visual inspection for any defects, weight variation, hardness, friability and in vitro disintegration time.

  9. Nanoparticle-based Sensors

    Directory of Open Access Journals (Sweden)

    V.K. Khanna

    2008-09-01

    Full Text Available Nanoparticles exhibit several unique properties that can be applied to develop chemical and biosensorspossessing desirable features like enhanced sensitivity and lower detection limits. Gold nanoparticles arecoated with sugars tailored to recognise different biological substances. When mixed with a weak solution ofthe sugar-coated nanoparticles, the target substance, e.g., ricin or E.coli, attaches to the sugar, thereby alteringits properties and changing the colour. Spores of bacterium labeled with carbon dots have been found to glowupon illumination when viewed with a confocal microscope. Enzyme/nanoparticle-based optical sensors forthe detection of organophosphate (OP compounds employ nanoparticle-modified fluorescence of an inhibitorof the enzyme to generate the signal for the OP compound detection. Nanoparticles shaped as nanoprisms,built of silver atoms, appear red on exposure to light. These nanoparticles are used as diagnostic labels thatglow when target DNA, e.g., those of anthrax or HIV, are present. Of great importance are tools like goldnanoparticle-enhanced surface-plasmon resonance sensor and silver nanoparticle surface-enhanced portableRaman integrated tunable sensor. Nanoparticle metal oxide chemiresistors using micro electro mechanical systemhotplate are very promising devices for toxic gas sensing. Chemiresistors comprising thin films of nanogoldparticles, encapsulated in monomolecular layers of functionalised alkanethiols, deposited on interdigitatedmicroelectrodes, show resistance changes through reversible absorption of vapours of harmful gases. Thispaper reviews the state-of-the-art sensors for chemical and biological terror agents, indicates their capabilitiesand applications, and presents the future scope of these devices.Defence Science Journal, 2008, 58(5, pp.608-616, DOI:http://dx.doi.org/10.14429/dsj.58.1683

  10. Design of chitosan-based nanoparticles functionalized with gallic acid.

    Science.gov (United States)

    Lamarra, J; Rivero, S; Pinotti, A

    2016-10-01

    Active nanoparticles based on chitosan could be applied as a support for the modulation of gallic acid delivery. In this sense, these nanostructures could be employed in different fields such as food, packaging, and pharmaceutical areas. The design parameters of chitosan-based nanoparticles functionalized with gallic acid (GA) were optimized through RSM by means of the analysis of zeta potential (ZP) and percentage encapsulation efficiency (PEE). The nanoparticles were prepared by ionotropic gelation using tripolyphosphate (TPP), at different combinations of chitosan (CH) concentration, CH:TPP ratio and GA. Global desirability methodology allowed finding the optimum formulation that included CH 0.76% (w/w), CH:TPP ratio of 5 and 37mgGA/gCH leading to ZP of +50mV and 82% of PEE. Analysis through QuickScan and turbidity demonstrated that the most stable nanoparticle suspensions were achieved combining concentrations of chitosan ranging between 0.5 and 0.75% with CH:TPP ratios higher than 3. These suspensions had high stability confirmed by means ZP and transmittance values which were higher than +25mV and 0.21 on average, respectively, as well as nanoparticle diameters of about 140nm. FTIR revealed the occurrence of both hydrogen bond and ionic interactions of CH-TPP which allowed the encapsulation and the improvement of the stability of the active agent. PMID:27287172

  11. Recent advancement of gelatin nanoparticles in drug and vaccine delivery.

    Science.gov (United States)

    Sahoo, Nityananda; Sahoo, Ranjan Ku; Biswas, Nikhil; Guha, Arijit; Kuotsu, Ketousetuo

    2015-11-01

    Novel drug delivery system using nanoscale materials with a broad spectrum of applications provides a new therapeutic foundation for technological integration and innovation. Nanoparticles are suitable drug carrier for various routes of administration as well as rapid recognition by the immune system. Gelatin, the biological macromolecule is a versatile drug/vaccine delivery carrier in pharmaceutical field due to its biodegradable, biocompatible, non-antigenicity and low cost with easy availability. The surface of gelatin nanoparticles can be modified with site-specific ligands, cationized with amine derivatives or, coated with polyethyl glycols to achieve targeted and sustained release drug delivery. Compared to other colloidal carriers, gelatin nanoparticles are better stable in biological fluids to provide the desired controlled and sustained release of entrapped drug molecules. The current review highlights the different formulation aspects of gelatin nanoparticles which affect the particle characteristics like zeta potential, polydispersity index, entrapment efficacy and drug release properties. It has also given emphasis on the major applications of gelatin nanoparticles in drug and vaccine delivery, gene delivery to target tissues and nutraceutical delivery for improving the poor bioavailabity of bioactive phytonutrients.

  12. Gas Phase Nanoparticle Synthesis

    Science.gov (United States)

    Granqvist, Claes; Kish, Laszlo; Marlow, William

    This book deals with gas-phase nanoparticle synthesis and is intended for researchers and research students in nanomaterials science and engineering, condensed matter physics and chemistry, and aerosol science. Gas-phase nanoparticle synthesis is instrumental to nanotechnology - a field in current focus that raises hopes for environmentally benign, resource-lean manufacturing. Nanoparticles can be produced by many physical, chemical, and even biological routes. Gas-phase synthesis is particularly interesting since one can achieve accurate manufacturing control and hence industrial viability.

  13. Curcumin-Loaded Apotransferrin Nanoparticles Provide Efficient Cellular Uptake and Effectively Inhibit HIV-1 Replication In Vitro

    OpenAIRE

    Upendhar Gandapu; R K Chaitanya; Golla Kishore; Reddy, Raju C; Kondapi, Anand K

    2011-01-01

    BACKGROUND: Curcumin (diferuloylmethane) shows significant activity across a wide spectrum of conditions, but its usefulness is rather limited because of its low bioavailability. Use of nanoparticle formulations to enhance curcumin bioavailability is an emerging area of research. METHODOLOGY/PRINCIPAL FINDINGS: In the present study, curcumin-loaded apotransferrin nanoparticles (nano-curcumin) prepared by sol-oil chemistry and were characterized by electron and atomic force microscopy. Confoca...

  14. Human in vivo and in vitro studies on gastrointestinal absorption of titanium dioxide nanoparticles.

    Science.gov (United States)

    Jones, Kate; Morton, Jackie; Smith, Ian; Jurkschat, Kerstin; Harding, Anne-Helen; Evans, Gareth

    2015-03-01

    The study was designed to conduct human in vivo and in vitro studies on the gastrointestinal absorption of nanoparticles, using titanium dioxide as a model compound, and to compare nanoparticle behaviour with that of larger particles. A supplier's characterisation data may not fully describe a particle formulation. Most particles tested agreed with their supplied characterisation when assessed by particle number but significant proportions of 'nanoparticle formulations' were particles >100nm when assessed by particle weight. Oral doses are measured by weight and it is therefore important that the weight characterisation is taken into consideration. The human volunteer studies demonstrated that very little titanium dioxide is absorbed gastrointestinally after an oral challenge. There was no demonstrable difference in absorption for any of the three particle sizes tested. All tested formulations were shown to agglomerate in simulated gastric fluid, particularly in the smaller particle formulations. Further agglomeration was observed when dispersing formulations in polymeric or elemental foods. Virtually no translocation of titanium dioxide particles across the cell layer was demonstrated. This study found no evidence that nanoparticulate titanium dioxide is more likely to be absorbed in the gut than micron-sized particles.

  15. Lipid nanoparticles based on butyl-methoxydibenzoylmethane: in vitro UVA blocking effect

    Science.gov (United States)

    Niculae, G.; Lacatusu, I.; Badea, N.; Meghea, A.

    2012-08-01

    The aim of the present study was to obtain efficient lipid nanoparticles loaded with butyl-methoxydibenzoylmethane (BMDBM) in order to develop cosmetic formulations with enhanced UVA blocking effect. For this purpose, two adequate liquid lipids (medium chain triglycerides and squalene) have been used in combination with two solid lipids (cetyl palmitate and glyceryl stearate) in order to create appropriate nanostructured carriers with a disordered lipid network able to accommodate up to 1.5% BMDBM. The lipid nanoparticles (LNs) were characterized in terms of particle size, zeta potential, entrapment efficiency, loading capacity and in vitro UVA blocking effect. The efficiency of lipid nanoparticles in developing some cosmetic formulations has been evaluated by determining the in vitro erythemal UVA protection factor. In order to quantify the photoprotective effect, some selected cream formulations based on BMDBM-LNs and a conventional emulsion were exposed to photochemical UV irradiation at a low energy to simulate the solar energy during the midday. The results obtained demonstrated the high ability of cream formulations based on BMDBM-LNs to absorb more than 96% of UVA radiation. Moreover, the developed cosmetic formulations manifest an enhanced UVA blocking effect, the erythemal UVA protection factor being four times higher than those specific to conventional emulsions.

  16. Lipid nanoparticles based on butyl-methoxydibenzoylmethane: in vitro UVA blocking effect

    International Nuclear Information System (INIS)

    The aim of the present study was to obtain efficient lipid nanoparticles loaded with butyl-methoxydibenzoylmethane (BMDBM) in order to develop cosmetic formulations with enhanced UVA blocking effect. For this purpose, two adequate liquid lipids (medium chain triglycerides and squalene) have been used in combination with two solid lipids (cetyl palmitate and glyceryl stearate) in order to create appropriate nanostructured carriers with a disordered lipid network able to accommodate up to 1.5% BMDBM. The lipid nanoparticles (LNs) were characterized in terms of particle size, zeta potential, entrapment efficiency, loading capacity and in vitro UVA blocking effect. The efficiency of lipid nanoparticles in developing some cosmetic formulations has been evaluated by determining the in vitro erythemal UVA protection factor. In order to quantify the photoprotective effect, some selected cream formulations based on BMDBM-LNs and a conventional emulsion were exposed to photochemical UV irradiation at a low energy to simulate the solar energy during the midday. The results obtained demonstrated the high ability of cream formulations based on BMDBM-LNs to absorb more than 96% of UVA radiation. Moreover, the developed cosmetic formulations manifest an enhanced UVA blocking effect, the erythemal UVA protection factor being four times higher than those specific to conventional emulsions. (paper)

  17. Formulation of essential oil-loaded chitosan–alginate nanocapsules

    Directory of Open Access Journals (Sweden)

    Dheebika Natrajan

    2015-09-01

    Full Text Available Naturally occurring polymers such as alginate (AL and chitosan (CS are widely used in biomedical and pharmaceutical fields in various forms such as nanoparticles, capsules, and emulsions. These polymers have attractive applications in drug delivery because of their biodegradability, biocompatibility, and nontoxic nature. The pharmaceutical applications of essential oils such as turmeric oil and lemongrass oil are well-known, and their active components, ar-turmerone and citral, respectively, are known for their antibacterial, antifungal, antioxidant, antimutagenic, and anticarcinogenic properties. However, these essential oils are unstable, volatile, and insoluble in water, which limits their use for new formulations. Therefore, this study focuses on developing a CS–AL nanocarrier for the encapsulation of essential oils. The effects of process parameters such as the effect of heat and the concentrations of AL and CS were investigated. Various physicochemical characterization techniques such as scanning electron microscopy, Fourier transform infrared spectroscopy, and ultraviolet–visible spectroscopy were performed. Results of characterization studies showed that 0.3 mg/mL AL and 0.6 mg/mL CS produced minimum-sized particles (<300 nm with good stability. It was also confirmed that the oil-loaded nanocapsules were hemocompatible, suggesting their use for future biomedical and pharmaceutical applications. Furthermore, the antiproliferative activity of turmeric oil- and lemongrass oil-loaded nanocapsules was estimated using 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide assay in A549 cell lines and it was found that both the nanoformulations had significant antiproliferative properties than the bare oil.

  18. Dynamics of two polarized nanoparticles

    Institute of Scientific and Technical Information of China (English)

    段晓勇; 王治国

    2015-01-01

    The intrinsic dynamics of two interacting electric polarized nanorods is theoretically investigated. The relative motion between them caused by electric dipole–dipole interaction is derived based on the generalized Lagrangian formulation. The results show that the relative translation and rotation are nonlinear and closely dependent on the initial configuration of the two nanorods. Furthermore, the general conditions of the initial configuration, which determine the two nanorods to repel or attract each other at the initial time, are obtained. The two-dimensional relative motion of the two nanorods shows that the antiparallel and head-to-tail ordering stable self-assembly are respectively formed in two planar initial configurations. For different three-dimensional initial configurations, the interesting dynamic relative attraction, repulsion, and oscillation with rotation are respectively realized. Finally, the theoretical schemes which realize the relaxing, direct head-to-tail ordering, and direct antiparallel ordering stable self-assembly are presented according to the different modes of the motion of the nanoparticles. Some of our results agree well with the results of experiments and simulations.

  19. Coping with antibiotic resistance: combining nanoparticles with antibiotics and other antimicrobial agents.

    Science.gov (United States)

    Allahverdiyev, Adil M; Kon, Kateryna Volodymyrivna; Abamor, Emrah Sefik; Bagirova, Malahat; Rafailovich, Miriam

    2011-11-01

    The worldwide escalation of bacterial resistance to conventional medical antibiotics is a serious concern for modern medicine. High prevalence of multidrug-resistant bacteria among bacteria-based infections decreases effectiveness of current treatments and causes thousands of deaths. New improvements in present methods and novel strategies are urgently needed to cope with this problem. Owing to their antibacterial activities, metallic nanoparticles represent an effective solution for overcoming bacterial resistance. However, metallic nanoparticles are toxic, which causes restrictions in their use. Recent studies have shown that combining nanoparticles with antibiotics not only reduces the toxicity of both agents towards human cells by decreasing the requirement for high dosages but also enhances their bactericidal properties. Combining antibiotics with nanoparticles also restores their ability to destroy bacteria that have acquired resistance to them. Furthermore, nanoparticles tagged with antibiotics have been shown to increase the concentration of antibiotics at the site of bacterium-antibiotic interaction, and to facilitate binding of antibiotics to bacteria. Likewise, combining nanoparticles with antimicrobial peptides and essential oils generates genuine synergy against bacterial resistance. In this article, we aim to summarize recent studies on interactions between nanoparticles and antibiotics, as well as other antibacterial agents to formulate new prospects for future studies. Based on the promising data that demonstrated the synergistic effects of antimicrobial agents with nanoparticles, we believe that this combination is a potential candidate for more research into treatments for antibiotic-resistant bacteria. PMID:22029522

  20. Characterization of abrasion-induced nanoparticle release from paints into liquids and air

    Science.gov (United States)

    Golanski, L.; Gaborieau, A.; Guiot, A.; Uzu, G.; Chatenet, J.; Tardif, F.

    2011-07-01

    Two standard methods for the characterization of the abrasion nanoparticle release into air and liquid from coatings containing nanoparticles were developed. Details of the abrasion processes and the measurement methods are shown. Paints were formulated in an industrial facility. Standard abrasion conditions in wet environments were simulated. The size distribution of the particles abraded into liquid was analyzed by a laser granulometer: submicrometric and micrometric particles were observed, but no nanometric particles. The nanoparticles released in liquid were deposited on filters for SEM (Scanning Electron Microscopy) analysis. No free or agglomerated nanoparticles were observed by SEM: nanoparticles seem to remain embedded in the paint matrix. The same coatings were abraded in the air using another standard method. The ELPI (Electrical Low Pressure Impactor) was used to determine the number size distribution of the dust generated. Abrasion is found to produce submicrometric and micrometric particles in the air but no nanoparticles. Further characterizations by SEM confirmed that no free or agglomerated nanoparticles were emitted: nanoparticles seem to remain embedded in the paint matrix.

  1. Streptomycin-loaded PLGA-alginate nanoparticles: preparation, characterization, and assessment

    Science.gov (United States)

    Asadi, Asadollah

    2014-04-01

    The aim of this study was to formulate and characterize streptomycin-loaded PLGA-alginate nanoparticles for their potential therapeutic use in Salmonella subsp. enterica ATCC 14028 infections. The streptomycin nanoparticle was prepared by solvent diffusion method, and the other properties such as size, zeta potential, loading efficacy, release kinetics, and antimicrobial strength were evaluated. The survey shows that nanoparticles may serve as a carrier of streptomycin and may provide localized antibacterial activity in the treatment of Salmonellosis. Electron microscopy showed spherical particles with indentations. The average size of the nanoparticles was 90 nm. At pH 7.2, the release kinetics of streptomycin from the nanoparticles was successfully illustrated as an initial burst defined by a first order equation that after this stage, it has a drastic tendency to obtain steady state. Nevertheless, nanoparticles showed loading efficacy nearly about 70-75 %. In addition, the tendency of concentration of streptomycin released from nanoparticles to reach antibacterial activity was similar to that of free streptomycin against PLGA-alginate, but it had threefold more antimicrobial strength in comparison with free streptomycin. This work shows the potential use of streptomycin-loaded PLGA-alginate nanoparticles and its capability.

  2. Towards a rational design of solid drug nanoparticles with optimised pharmacological properties

    Science.gov (United States)

    Martin, Phillip; Smith, Darren; Curley, Paul; McDonald, Tom; Giardiello, Marco; Liptrott, Neill; Rannard, Steve; Owen, Andrew

    2016-01-01

    Abstract Solid drug nanoparticles (SDNs) are a nanotechnology with favourable characteristics to enhance drug delivery and improve the treatment of several diseases, showing benefit for improved oral bioavailability and injectable long‐acting medicines. The physicochemical properties and composition of nanoformulations can influence the absorption, distribution, and elimination of nanoparticles; consequently, the development of nanoparticles for drug delivery should consider the potential role of nanoparticle characteristics in the definition of pharmacokinetics. The aim of this study was to investigate the pharmacological behaviour of efavirenz SDNs and the identification of optimal nanoparticle properties and composition. Seventy‐seven efavirenz SDNs were included in the analysis. Cellular accumulation was evaluated in HepG2 (hepatic) and Caco‐2 (intestinal), CEM (lymphocyte), THP1 (monocyte), and A‐THP1 (macrophage) cell lines. Apparent intestinal permeability (Papp) was measured using a monolayer of Caco‐2 cells. The Papp values were used to evaluate the potential benefit on pharmacokinetics using a physiologically based pharmacokinetic model. The generated SDNs had an enhanced intestinal permeability and accumulation in different cell lines compared to the traditional formulation of efavirenz. Nanoparticle size and excipient choice influenced efavirenz apparent permeability and cellular accumulation, and this appeared to be cell line dependent. These findings represent a valuable platform for the design of SDNs, giving an empirical background for the selection of optimal nanoparticle characteristics and composition. Understanding how nanoparticle components and physicochemical properties influence pharmacological patterns will enable the rational design of SDNs with desirable pharmacokinetics. PMID:27774308

  3. Enhanced oral bioavailability and in vivo antioxidant activity of chlorogenic acid via liposomal formulation.

    Science.gov (United States)

    Feng, Yingshu; Sun, Congyong; Yuan, Yangyang; Zhu, Yuan; Wan, Jinyi; Firempong, Caleb Kesse; Omari-Siaw, Emmanuel; Xu, Yang; Pu, Zunqin; Yu, Jiangnan; Xu, Ximing

    2016-03-30

    In the present study, a formulation system consisting of cholesterol and phosphatidyl choline was used to prepare an effective chlorogenic acid-loaded liposome (CAL) with an improved oral bioavailability and an increased antioxidant activity. The developed liposomal formulation produced regular, spherical and multilamellar-shaped distribution nanoparticles. The pharmacokinetic analysis of CAL compared with chlorogenic acid (CA), showed a higher value of Cmax(6.42 ± 1.49 min versus 3.97 ± 0.39 min) and a delayed Tmax(15 min versus 10 min), with 1.29-fold increase in relative oral bioavailability. The tissue distribution in mice also demonstrated that CAL predominantly accumulated in the liver which indicated hepatic targeting potential of the drug. The increased activities of antioxidant enzymes (Total Superoxide Dismutase (T-SOD) and Glutathione Peroxidase (GSH-Px)) and total antioxidant capacity (T-AOC), in addition to decreased level of malondialdehyde (MDA) in CCl4-induced hepatotoxicity study further revealed that CAL exhibited significant hepatoprotective and antioxidant effects. Collectively, these findings present a liposomal formulation with significantly improved oral bioavailability and an increased in vivo antioxidant activity of CA. PMID:26861689

  4. PEGylated cyclodextrins as novel siRNA nanosystems: correlations between polyethylene glycol length and nanoparticle stability.

    Science.gov (United States)

    Godinho, Bruno M D C; Ogier, Julien R; Quinlan, Aoife; Darcy, Raphael; Griffin, Brendan T; Cryan, John F; O'Driscoll, Caitriona M

    2014-10-01

    Silencing disease-related genes in the central nervous system (CNS) using short interfering RNA (siRNA) holds great promise for treating neurological disorders. Yet, delivery of RNAi therapeutics to the brain poses major challenges to non-viral systems, especially when considering systemic administration. Cationic nanoparticles have been widely investigated for siRNA delivery, but the tendency of these to aggregate in physiological environments limits their intravenous application. Thus, strategies to increase the stability of nanoparticles have been developed. Here, we investigated the ability of modified cationic amphiphilic or PEGylated amphiphilic cyclodextrins (CD) to formulate stable CD.siRNA nanoparticles. To this end, we describe a simple method for post-modification of pre-formed cationic CD.siRNA nanoparticles at their surface using PEGylated CDs of different PEG lengths. PEGylated CD.siRNA nanoparticles presented reduced surface charges and increased stability in physiological salt conditions. Stability of PEGylated CD.siRNA nanoparticles in vitro increased with both PEG length and PEG density at the surface. Furthermore, in a comparative pharmacokinetic study, increased systemic exposure and reduced clearance were achieved with CD-formulations when compared to naked siRNAs. However, no significant differences were observed among non-PEGylated and PEGylated CD.siRNAs suggesting that longer PEG lengths might be required for improving stability in vivo. PMID:24992319

  5. The Role of Nanoparticle in Brain Permeability: An in-vitro BBB Model.

    Science.gov (United States)

    Nikandish, Niusha; Hosseinzadeh, Leila; Hemati Azandaryani, Abbas; Derakhshandeh, Katayoun

    2016-01-01

    Membrane permeability and P-glycoprotein (P-gp) efflux system are regulating factors in the drug brain penetration. Recently, some drug delivery systems have been developed to overcome these limitations. In this study, Metoclopramid has been encapsulated in PLGA nanoparticles using the emulsification/solvent evaporation technique for in-viro evaluation of the effect of PLGA nanoparticles on BBB permeability. Subsequently, prepared nanoparticles were characterized using PCS, TEM, FT-IR, DSC and XRD techniques and in-viro cell permeability of optimum formulation was evaluated using MDCK cell line as BBB model. Data investigation showed that prepared nanoparticles have the entrapment efficiency of 50 %. PCS investigation showed that prepared nanoparticles have an average size of approximately 150 ± 14 nm and a relatively monodisperse distribution. TEM micrographs of the samples showed spherical shape and smooth surface with a particle size of nanometric range. Through DSC thermograms and XRD diffractograms analysis, it was demonstrated that there was no crystalline form of the drug in the loaded formulation. Moreover, our results showed that the greater crossing of metoclopramide in the form of nanoparticle in comparison with the free form. The widely used rhodamine-123 transport assay performed in the MDCK cells demonstrated the presence of P-glycoprotein in this model. PMID:27642311

  6. Shaped gold and silver nanoparticles

    Science.gov (United States)

    Sun, Yugang; An, Changhua

    2011-03-01

    Advance in the synthesis of shaped nanoparticles made of gold and silver is reviewed in this article. This review starts with a new angle by analyzing the relationship between the geometrical symmetry of a nanoparticle shape and its internal crystalline structures. According to the relationship, the nanoparticles with well-defined shapes are classified into three categories: nanoparticles with single crystallinity, nanoparticles with angular twins, and nanoparticles with parallel twins. Discussion and analysis on the classical methods for the synthesis of shaped nanoparticles in each category are also included and personal perspectives on the future research directions in the synthesis of shaped metal nanoparticles are briefly summarized. This review is expected to provide a guideline in designing the strategy for the synthesis of shaped nanoparticles and analyzing the corresponding growth mechanism.

  7. Dual Agent Loaded PLGA Nanoparticles Enhanced Antitumor Activity in a Multidrug-Resistant Breast Tumor Eenograft Model

    Directory of Open Access Journals (Sweden)

    Yan Chen

    2014-02-01

    Full Text Available Multidrug-resistant breast cancers have limited and ineffective clinical treatment options. This study aimed to develop PLGA nanoparticles containing a synergistic combination of vincristine and verapamil to achieve less toxicity and enhanced efficacy on multidrug-resistant breast cancers. The 1:250 molar ratio of VCR/VRP showed strong synergism with the reversal index of approximately 130 in the multidrug-resistant MCF-7/ADR cells compared to drug-sensitive MCF-7 cells. The lyophilized nanoparticles could get dispersed quickly with the similar size distribution, zeta potential and encapsulation efficiency to the pre-lyophilized nanoparticles suspension, and maintain the synergistic in vitro release ratio of drugs. The co-encapsulated nanoparticle formulation had lower toxicity than free vincristine/verapamil combinations according to the acute-toxicity test. Furthermore, the most effective tumor growth inhibition in the MCF-7/ADR human breast tumor xenograft was observed in the co-delivery nanoparticle formulation group in comparison with saline control, free vincristine, free vincristine/verapamil combinations and single-drug nanoparticle combinations. All the data demonstrated that PLGANPs simultaneously loaded with chemotherapeutic drug and chemosensitizer might be one of the most potential formulations in the treatment of multidrug-resistant breast cancer in clinic.

  8. Nanoparticles: Uncertainty Risk Analysis

    DEFF Research Database (Denmark)

    Grieger, Khara Deanne; Hansen, Steffen Foss; Baun, Anders

    2012-01-01

    approaches. To date, there have been a number of different approaches to assess uncertainty of environmental risks in general, and some have also been proposed in the case of nanoparticles and nanomaterials. In recent years, others have also proposed that broader assessments of uncertainty are also needed......Scientific uncertainty plays a major role in assessing the potential environmental risks of nanoparticles. Moreover, there is uncertainty within fundamental data and information regarding the potential environmental and health risks of nanoparticles, hampering risk assessments based on standard...... in order to handle the complex potential risks of nanoparticles, including more descriptive characterizations of uncertainty. Some of these approaches are presented and discussed herein, in which the potential strengths and limitations of these approaches are identified along with further challenges...

  9. Metallic Magnetic Nanoparticles

    Directory of Open Access Journals (Sweden)

    A. Hernando

    2005-01-01

    Full Text Available In this paper, we reviewed some relevant aspects of the magnetic properties of metallic nanoparticles with small size (below 4 nm, covering the size effects in nanoparticles of magnetic materials, as well as the appearance of magnetism at the nanoscale in materials that are nonferromagnetic in bulk. These results are distributed along the text that has been organized around three important items: fundamental magnetic properties, different fabrication procedures, and characterization techniques. A general introduction and some experimental results recently obtained in Pd and Au nanoparticles have also been included. Finally, the more promising applications of magnetic nanoparticles in biomedicine are indicated. Special care was taken to complete the literature available on the subject.

  10. Predicting toxicity of nanoparticles

    OpenAIRE

    BURELLO ENRICO; Worth, Andrew

    2011-01-01

    A statistical model based on a quantitative structure–activity relationship accurately predicts the cytotoxicity of various metal oxide nanoparticles, thus offering a way to rapidly screen nanomaterials and prioritize testing.

  11. Nanoparticles deliver RNAi therapy

    Directory of Open Access Journals (Sweden)

    Martin C. Woodle

    2005-08-01

    Full Text Available Nanotechnology-based advanced materials are rapidly expanding development of better medicines. Long-standing efforts with lipid and polymer colloidal delivery systems, i.e. nanoparticles, have yielded better imaging and therapy. These benefits of nanotechnology, though limited, have driven efforts to develop advanced nanoparticles. This is particularly the case for targeted nucleic acid (gene therapeutics based on short interfering ribonucleic acid (siRNA, which is a new gene inhibitor that is highly potent and selective. Here, we evaluate the use of modular conjugates to construct targeted nanoparticle therapeutics for nucleic acids. These nanoparticles are beginning to emulate the sophistication of virus particles – nature's own nanoscale assemblies for nucleic acids. For medicine, they promise the creation of a new generation of ‘targeted’ therapeutics that can offer multiple levels of selectivity.

  12. Functionalized diamond nanoparticles

    KAUST Repository

    Beaujuge, Pierre M.

    2014-10-21

    A diamond nanoparticle can be functionalized with a substituted dienophile under ambient conditions, and in the absence of catalysts or additional reagents. The functionalization is thought to proceed through an addition reaction.

  13. METALIC NANOPARTICLES AND NANOSTRUCTURES

    OpenAIRE

    Nohavica, Dušan

    2010-01-01

    A brief overview of the field of metallic nanoparticles and nanocrystalline materials preparation and their properties is presented. Dependence of the chemical potential on surface curvature is important for particles solubility in the melt, vapour pressure of liquids as a function of droplet radius, Ostwald ripening and sintering of the individual particles. Melting point and lattice constant depends on the radius of nanoparticles as well. The major processing for nanocrystalline materials ...

  14. Towards a methodology to formulate sustainable diets for livestock: accounting for environmental impact in diet formulation.

    Science.gov (United States)

    Mackenzie, S G; Leinonen, I; Ferguson, N; Kyriazakis, I

    2016-05-28

    The objective of this study was to develop a novel methodology that enables pig diets to be formulated explicitly for environmental impact objectives using a Life Cycle Assessment (LCA) approach. To achieve this, the following methodological issues had to be addressed: (1) account for environmental impacts caused by both ingredient choice and nutrient excretion, (2) formulate diets for multiple environmental impact objectives and (3) allow flexibility to identify the optimal nutritional composition for each environmental impact objective. An LCA model based on Canadian pig farms was integrated into a diet formulation tool to compare the use of different ingredients in Eastern and Western Canada. By allowing the feed energy content to vary, it was possible to identify the optimum energy density for different environmental impact objectives, while accounting for the expected effect of energy density on feed intake. A least-cost diet was compared with diets formulated to minimise the following objectives: non-renewable resource use, acidification potential, eutrophication potential, global warming potential and a combined environmental impact score (using these four categories). The resulting environmental impacts were compared using parallel Monte Carlo simulations to account for shared uncertainty. When optimising diets to minimise a single environmental impact category, reductions in the said category were observed in all cases. However, this was at the expense of increasing the impact in other categories and higher dietary costs. The methodology can identify nutritional strategies to minimise environmental impacts, such as increasing the nutritional density of the diets, compared with the least-cost formulation.

  15. Towards a methodology to formulate sustainable diets for livestock: accounting for environmental impact in diet formulation.

    Science.gov (United States)

    Mackenzie, S G; Leinonen, I; Ferguson, N; Kyriazakis, I

    2016-05-28

    The objective of this study was to develop a novel methodology that enables pig diets to be formulated explicitly for environmental impact objectives using a Life Cycle Assessment (LCA) approach. To achieve this, the following methodological issues had to be addressed: (1) account for environmental impacts caused by both ingredient choice and nutrient excretion, (2) formulate diets for multiple environmental impact objectives and (3) allow flexibility to identify the optimal nutritional composition for each environmental impact objective. An LCA model based on Canadian pig farms was integrated into a diet formulation tool to compare the use of different ingredients in Eastern and Western Canada. By allowing the feed energy content to vary, it was possible to identify the optimum energy density for different environmental impact objectives, while accounting for the expected effect of energy density on feed intake. A least-cost diet was compared with diets formulated to minimise the following objectives: non-renewable resource use, acidification potential, eutrophication potential, global warming potential and a combined environmental impact score (using these four categories). The resulting environmental impacts were compared using parallel Monte Carlo simulations to account for shared uncertainty. When optimising diets to minimise a single environmental impact category, reductions in the said category were observed in all cases. However, this was at the expense of increasing the impact in other categories and higher dietary costs. The methodology can identify nutritional strategies to minimise environmental impacts, such as increasing the nutritional density of the diets, compared with the least-cost formulation. PMID:26987378

  16. Immunosensing using nanoparticles

    Directory of Open Access Journals (Sweden)

    Alfredo de la Escosura-Muñiz

    2010-07-01

    Full Text Available Immunosensing technology is taking advantage of the lastest developments in materials science and inparticular from the nanomaterials field. Because of their unprecedented optical tunability as well as electrical and electrochemical qualities, we are seeing significant developments in the design of novel immunoassays; various conventional optical and electrical platforms which allow for future applications in several fields are being used. Properties of nanoparticles such as light absorption and dispersion are bringing interesting immunosensing alternatives. Nanoparticles are improving the sensitivity of existing techniques used for protein detection in immunoassays based on Surface Plasmon Resonance, Quartz Crystal Microbalance, Fluorescence spectroscopy etc. Electrochemical techniques are also taking advantage of electrical properties of nanoparticles. Redox properties of metal based nanoparticles, surface impedance change and conductance changes once nanoparticles are present as labelling tags or modifiers of transducer surfaces are also improving the technology. In most of the examples nanoparticle based biosensing systems are being offered as excellent screening and superior alternatives to existing conventional strategies/assays with interest for fields in clinical analysis, food quality, safety and security.

  17. Imaging through plasmonic nanoparticles

    Science.gov (United States)

    Tanzid, Mehbuba; Sobhani, Ali; DeSantis, Christopher J.; Cui, Yao; Hogan, Nathaniel J.; Samaniego, Adam; Veeraraghavan, Ashok; Halas, Naomi J.

    2016-05-01

    The optical properties of metallic nanoparticles with plasmon resonances have been studied extensively, typically by measuring the transmission of light, as a function of wavelength, through a nanoparticle suspension. One question that has not yet been addressed, however, is how an image is transmitted through such a suspension of absorber-scatterers, in other words, how the various spatial frequencies are attenuated as they pass through the nanoparticle host medium. Here, we examine how the optical properties of a suspension of plasmonic nanoparticles affect the transmitted image. We use two distinct ways to assess transmitted image quality: the structural similarity index (SSIM), a perceptual distortion metric based on the human visual system, and the modulation transfer function (MTF), which assesses the resolvable spatial frequencies. We show that perceived image quality, as well as spatial resolution, are both dependent on the scattering and absorption cross-sections of the constituent nanoparticles. Surprisingly, we observe a nonlinear dependence of image quality on optical density by varying optical path length and nanoparticle concentration. This work is a first step toward understanding the requirements for visualizing and resolving objects through media consisting of subwavelength absorber-scatterer structures, an approach that should also prove useful in the assessment of metamaterial or metasurface-based optical imaging systems.

  18. Magnetic interactions between nanoparticles

    DEFF Research Database (Denmark)

    Mørup, Steen; Hansen, Mikkel Fougt; Frandsen, Cathrine

    2010-01-01

    We present a short overview of the influence of inter-particle interactions on the properties of magnetic nanoparticles. Strong magnetic dipole interactions between ferromagnetic or ferrimagnetic particles, that would be superparamagnetic if isolated, can result in a collective state of nanoparti......We present a short overview of the influence of inter-particle interactions on the properties of magnetic nanoparticles. Strong magnetic dipole interactions between ferromagnetic or ferrimagnetic particles, that would be superparamagnetic if isolated, can result in a collective state...... of nanoparticles. This collective state has many similarities to spin-glasses. In samples of aggregated magnetic nanoparticles, exchange interactions are often important and this can also lead to a strong suppression of superparamagnetic relaxation. The temperature dependence of the order parameter in samples...... of strongly interacting hematite nanoparticles or goethite grains is well described by a simple mean field model. Exchange interactions between nanoparticles with different orientations of the easy axes can also result in a rotation of the sub-lattice magnetization directions....

  19. Chitosan-based formulations of drugs, imaging agents and biotherapeutics

    NARCIS (Netherlands)

    Amidi, M.; Hennink, W.E.

    2010-01-01

    This preface is part of the Advanced Drug Delivery Reviews theme issue on “Chitosan-Based Formulations of Drugs, Imaging Agents and Biotherapeutics”. This special Advanced Drug Delivery Reviews issue summarizes recent progress and different applications of chitosanbased formulations.

  20. HERBAL LIPSTICK FORMULATION: A NEW APPROACH

    OpenAIRE

    Meher Deepali Avinash; Alai Manoj Hari; Nikam Shreya Pradeep

    2011-01-01

    Coloring skin particularly skin of face and lips is an ancient practice going back to prehistoric period. In present days the use of such product has increased and choice of shades of color, texture and luster have been changed and become wider. This can be observed from the fact that lipsticks are marked in hundreds of shades of colors to satisfy the demand of women. The present investigation was done to formulate herbal lipstick, since lipsticks are one of the key cosmetics to be used by th...

  1. Conservative formulation for compressible multiphase flows

    CERN Document Server

    Romenski, Evgeniy; Peshkov, Ilya M

    2014-01-01

    Derivation of governing equations for multiphase flow on the base of thermodynamically compatible systems theory is presented. The mixture is considered as a continuum in which the multiphase character of the flow is taken into account. The resulting governing equations of the formulated model belong to the class of hyperbolic systems of conservation laws. In order to examine the reliability of the model, the one-dimensional Riemann problem for the four phase flow is studied numerically with the use of the MUSCL-Hancock method in conjunction with the GFORCE flux.

  2. Sensitivity studies of a new energetic formulation

    Science.gov (United States)

    Wilson, W. H.; Forbes, J. W.; Liddiard, T. P.; Doherty, R. M.

    1994-07-01

    The shock sensitivity of a new pressed formulation based upon CL-20 has been studied. Samples were made from a biomodal particle size distribution of the CL-20 ɛpolymorph and an EVA binder, pressed to an average 97% of theoretical maximum density. The material exhibited an anomalous reversal in slope of shock sensitivity vs. input stress. Over a limited stress range near the first reaction threshold, the level of reaction decreased with increasing input stress. Within this range of input shock it was observed that break-out of reaction was delayed, and was concentrated near the sample centerline.

  3. Gradient Elasticity Formulations for Micro/Nanoshells

    Directory of Open Access Journals (Sweden)

    Bohua Sun

    2014-01-01

    Full Text Available The focus of this paper is on illustrating how to extend the second author’s gradient theory of elasticity to shells. Three formulations are presented based on the implicit gradient elasticity constitutive relation 1 -ld2∇2σij=Cijkl(1-ls2∇2εkl and its two approximations 1+ls2∇2-ld2∇2σij=Cijklεkl and σij=Cijkl(1+ld2∇2-ls2∇2εkl.

  4. Relativistic formulation of the Voigt profile

    Science.gov (United States)

    Wcisło, P.; Amodio, P.; Ciuryło, R.; Gianfrani, L.

    2015-02-01

    The relativistic formulation of the Voigt profile is reported for the spontaneous emission from an atomic or molecular cloud, in coincidence with a given spectral line. We considered the simultaneous occurrence of homogeneous broadening and thermal broadening, this latter being determined by the relativistic Doppler effect. Our formula for the relativistic Voigt profile reproduces those characterizing the two available limit cases, namely, the relativistic Gaussian profile and the classical Voigt convolution. The relativistic deformation of the Voigt profile was carefully quantified at different temperatures, in the case of the molecular hydrogen spectrum.

  5. Formulations of a hydromechanical interface element

    Institute of Scientific and Technical Information of China (English)

    Zhong-Zhi Fu; Si-Hong Liu

    2011-01-01

    A hydromechanical interface element is proposed for the consideration of the hydraulic-mechanical coupling effect along the interface.The fully coupled governing equations and the relevant finite element formulations are derived in detail for the interface element.All the involved matrices are of the same form as those of a solid element,which makes the incorporation of the model into a finite element program straightforward.Three examples are then numerically simulated using the interface element.Reasonable results confirm the correctness of the proposed model and motivate its application in hydromechanical contact problems in the future.

  6. Quality Evaluation of Pharmaceutical Formulations Containing Hydrochlorothiazide

    Directory of Open Access Journals (Sweden)

    Marcelo Antonio de Oliveira

    2014-10-01

    Full Text Available Hydrochlorothiazide is a diuretic used to treat hypertension that belongs to class IV of the Biopharmaceutics Classification System. The drug was evaluated by quality control, thermal characterization tests, and pharmaceutical formulation compatibility studies. It was concluded that the generic drug, Lab 2, was not a pharmaceutical equivalent. The compounded drugs, Lab 5 and Lab 6, produced unsatisfactory but expected results, since there is no requirement for dissolution and dissolution profile testing for the commercialization of these products. In a compatibility study, lactose and mannitol were shown to be incompatible with HCTZ, which may explain the lack of equivalence of the generic pharmaceutical product, associated with other situations.

  7. Gravitation: Global Formulation and Quantum Effects

    CERN Document Server

    Aldrovandi, R; Vu, K H

    2004-01-01

    A nonintegrable phase-factor global approach to gravitation is developed by using the similarity of teleparallel gravity with electromagnetism. The phase shifts of both the COW and the gravitational Aharonov-Bohm effects are obtained. It is then shown, by considering a simple slit experiment, that in the classical limit the global approach yields the same result as the gravitational Lorentz force equation of teleparallel gravity. It represents, therefore, the quantum mechanical version of the classical description provided by the gravitational Lorentz force equation. As teleparallel gravity can be formulated independently of the equivalence principle, it will consequently require no generalization of this principle at the quantum level.

  8. TANK 50 BATCH 0 SALTSTONE FORMULATION CONFIRMATION

    Energy Technology Data Exchange (ETDEWEB)

    Langton, C.

    2006-06-05

    Savannah River National Laboratory (SRNL) personnel were requested to confirm the Tank 50 Batch 0 grout formulation per Technical Task Request, SSF-TTR-2006-0001 (task 1 of 2) [1]. Earlier Batch 0 formulation testing used a Tank 50 sample collected in September 2005 and is described elsewhere [2]. The current testing was performed using a sample of Tank 50 waste collected in May 2006. This work was performed according to the Technical Task and Quality Assurance Plan (TT/QAP), WSRC-RP-2006-00594 [3]. The salt solution collected from Tank 50 in May 2006 contained approximately 3 weight percent more solids than the sample collected in September 2005. The insoluble solids took longer to settle in the new sample which was interpreted as indicating finer particles in the current sample. The saltstone formulation developed for the September 2005 Tank 50 Batch 0 sample was confirmed for the May 2006 sample with one minor exception. Saltstone prepared with the Tank 50 sample collected in May 2006 required 1.5 times more Daratard 17 set retarding admixture than the saltstone prepared with the September In addition, a sample prepared with lower shear mixing (stirring with a spatula) had a higher plastic viscosity (57 cP) than samples made with higher shear mixing in a blender (23cP). The static gel times of the saltstone slurries made with low shear mixing were also shorter ({approx}32 minutes) than those for comparable samples made in the blender ({approx}47 minutes). The addition of the various waste streams (ETP, HEU-HCAN, and GPE-HCAN) to Tank 50 from September 2005 to May 2006 has increased the amount of set retarder, Daratard 17, required for processing saltstone slurries through the Saltstone facility. If these streams are continued to be added to Tank 50, the quantity of admixtures required to maintain the same processing conditions for the Saltstone facility will probably change and additional testing is recommended to reconfirm the Tank 50 Saltstone formulation.

  9. Multiple-Scale Approach to Understanding Formulated Product Production

    OpenAIRE

    Rodgers, Thomas Lawrence

    2011-01-01

    Consumer- and pharmaceutical-based products are a major component of the chemicalindustry. In the personal care industry, formulations often consist of a mixture ofsurfactants and fatty alcohols. The addition of surfactants aids the stability of the formulation.The formulated product microstructure depends upon the preparation conditionsas well as the ingredients. Controlling which microstructures form during the productionof a formulated product is important as different microstructures can ...

  10. Development and Evaluation of Polyherbal Formulations for Hair Growth Potential

    OpenAIRE

    Vaishali Rathi; Jagdish Chandra Rathi; Sengodan Tamizharasi

    2009-01-01

    The present study is an effort to formulate and evaluate hair growth promoting activity of three polyherbal formulations. Polyherbal formulations were prepared using extract of Cicer arietinum Linn., Ocimum sanctum Linn. and Cyperus rotundus Linn. in various ratios to obtained the best formulation The extract incorporated into cream were applied topically on shaved skin of rats and primary skin irritation test, hair growth initiation time, completion time, hair length and diameter were record...

  11. Heteroaggregation of cerium oxide nanoparticles and nanoparticles of pyrolyzed biomass

    Science.gov (United States)

    Heteroaggregation with indigenous particles is an important process controlling the mobility of engineered nanomaterials in the environment. We studied heteroaggregation of cerium oxide nanoparticles (n-CeO2), which are widely used commercially, with nanoparticles of pyrogenic carbonaceous material ...

  12. Multi criteria decision making to select the suitable method for the preparation of nanoparticles using an analytical hierarchy process.

    Science.gov (United States)

    Velmurugan, R; Selvamuthukumar, S; Manavalan, R

    2011-11-01

    Selecting the right method for the preparation of nanoparticles is a crucial decision. A wrong decision can result in the product having to be formulated and developed again. One tool that can be useful in determining the most appropriate method is the Analytical Hierarchy Process (AHP). AHP has been employed in almost all areas related to decision-making problems. In this paper, the results of a case study illustrate that the AHP concept can assist designers in the effective evaluation of various methods available for the preparation of nanoparticles. This paper presents the methodology of selecting the most suitable method for preparing nanoparticles using the analytical hierarchy process.

  13. Simultaneously Exploiting Two Formulations: an Exact Benders Decomposition Approach

    DEFF Research Database (Denmark)

    Lusby, Richard Martin; Gamst, Mette; Spoorendonk, Simon

    linear programs and propose an approach based on Benders decomposition to exploit the advantages of two different formulations when solving a problem. We propose to apply Benders decomposition to a combined formulation,comprised of two separate formulations, augmented with linking constraints to ensure...

  14. Formulation and method for preparing gels comprising hydrous aluminum oxide

    Science.gov (United States)

    Collins, Jack L.

    2014-06-17

    Formulations useful for preparing hydrous aluminum oxide gels contain a metal salt including aluminum, an organic base, and a complexing agent. Methods for preparing gels containing hydrous aluminum oxide include heating a formulation to a temperature sufficient to induce gel formation, where the formulation contains a metal salt including aluminum, an organic base, and a complexing agent.

  15. A displacement based FE formulation for steady state problems

    NARCIS (Netherlands)

    Yu, Yuhong

    2005-01-01

    In this thesis a new displacement based formulation is developed for elasto-plastic deformations in steady state problems. In this formulation the displacements are the primary variables, which is in contrast to the more common formulations in terms of the velocities as the primary variables. In a s

  16. The role of formulation on the pharmacokinetics of antiretroviral drugs

    NARCIS (Netherlands)

    Bastiaans, Diane E T; Cressey, Tim R; Vromans, Herman; Burger, David M

    2014-01-01

    INTRODUCTION: A multitude of antiretroviral drug formulations are now available for HIV-infected adults and children. These formulations include individual and co-formulated drugs, many of which are also supplied in generic versions. Many antiretroviral drugs have a low aqueous solubility and poor b

  17. Algebraic formulation of quantum theory, particle identity and entanglement

    Science.gov (United States)

    Govindarajan, T. R.

    2016-08-01

    Quantum theory as formulated in conventional framework using statevectors in Hilbert spaces misses the statistical nature of the underlying quantum physics. Formulation using operators 𝒞∗ algebra and density matrices appropriately captures this feature in addition leading to the correct formulation of particle identity. In this framework, Hilbert space is an emergent concept. Problems related to anomalies and quantum epistemology are discussed.

  18. A comparative review of four formulations of noncommutative quantum mechanics

    Science.gov (United States)

    Gouba, Laure

    2016-07-01

    Four formulations of quantum mechanics on noncommutative Moyal phase spaces are reviewed. These are the canonical, path-integral, Weyl-Wigner and systematic formulations. Although all these formulations represent quantum mechanics on a phase space with the same deformed Heisenberg algebra, there are mathematical and conceptual differences which we discuss.

  19. Evaluation of biocompatible stabilised gelled soya bean oil nanoparticles as new hydrophobic reservoirs.

    Science.gov (United States)

    Boudier, Ariane; Kirilov, Plamen; Franceschi-Messant, Sophie; Belkhelfa, Haouaria; Hadioui, Laila; Roques, Christine; Perez, Emile; Rico-Lattes, Isabelle

    2010-01-01

    Based on the organogel concept, in which an oil is trapped in a network of low-molecular-mass organic gelator fibres creating a gel, a formulation of gelled soya bean oil nanoparticles was evaluated for its capacity to form biocompatible hydrophobic reservoirs. The aqueous dispersions of nanoparticles were prepared by hot emulsification (T° > Tgel) and cooling at room temperature in the presence of polyethyleneimine (PEI). The dispersions were stabilised by the electrostatic interactions between the positively charged amino groups of the PEI and the negatively charged carboxylates of the gelator fibres present at the surface of the particles. The aqueous dispersions were highly stable (several months) and the gelled particles were able to entrap a hydrophobic fluorescent model molecule (Nile red), allowing testing in cells. The gelled oil nanoparticles were found to be biocompatible with the tested cells (keratinocytes) and had the ability to become rapidly internalised. Thus, organogel-based nanoparticles are a promising hydrophobic drug delivery system.

  20. Fabrication of autofluorescent porous silica nanoparticles for redox-responsive drug release.

    Science.gov (United States)

    Cao, Na; Zhao, Yanbao; Sang, Bin; Wang, Zhihua; Cao, Liuqin; Sun, Lei; Zou, Xueyan

    2016-12-01

    Porous silica nanoparticles were prepared by emulsion-condensation route. The silica nanoparticles with diameter of 50nm have both accessible center-radial large pore channels (19.9nm) and small pore size of 3.5nm. The hierarchical porous structure endows them large pore volume for loading drugs and sustained release property. The silica nanoparticles were further modified with glucose-oxidized glutathione. The formulated Schiff base and disulfide bonds render the silica nanoparticles auto-fluorescent and redox-responsive properties. The cleavage of disulfide bonds caused by reactive thiols facilitates aminomethylbenzoic acid (AMA) release. The release of drug leads to the loss of fluorescence, which would be used to monitor the drug delivery and carrier distribution. PMID:27612720

  1. A Novel M2e Based Flu Vaccine Formulation for Dogs

    Science.gov (United States)

    Leclerc, Denis; Rivest, Marie; Babin, Cindy; López-Macias, Constantino; Savard, Pierre

    2013-01-01

    Background The USA 2004 influenza virus outbreak H3N8 in dogs heralded the emergence of a new disease in this species. A new inactivated H3N8 vaccine was developed to control the spread of the disease but, as in humans and swine, it is anticipated that the virus will mutate shift and drift in the dog population. Therefore, there is a need for a vaccine that can trigger a broad protection to prevent the spread of the virus and the emergence of new strains. Methodology and Principal Findings The universal M2e peptide is identical in almost all the H3N8 influenza strains sequenced to date and known to infect dogs. This epitope is therefore a good choice for development of a vaccine to provide broad protection. Malva mosaic virus (MaMV) nanoparticles were chosen as a vaccine platform to improve the stability of the M2e peptide and increase its immunogenicity in animals. The addition of an adjuvant (OmpC) purified from Salmonella typhi membrane in the vaccine formulation increased the immune response directed to the M2e peptide significantly and enlarged the protection to include the heterosubtypic strain of influenza in a mouse model. An optimal vaccine formulation was also shown to be immunogenic in dogs. Conclusions and Significance The MaMV vaccine platform triggered an improved immune response directed towards the universal M2e peptide. The adjuvant OmpC increased the immune response to the M2e peptide and protection to a heterosubtypic influenza strain that harbors a different M2e peptide in a mouse model. Antibodies generated by the vaccine formulation showed cross-reactivity with M2e peptides derived from influenza strains H9N2, H5N1 and H1N1. The vaccine formulation shows a potential for commercialization of a new M2e based vaccine in dogs. PMID:24098576

  2. Formulating tumor-homing peptides as regular nanoparticles enhances receptor-mediated cell penetrability

    OpenAIRE

    Xu, Zhikun; Unzueta Elorza, Ugutz; Roldán, Mónica; Mangues, Ramón; Sánchez Chardi, Alejandro; Ferrer Miralles, Neus; Villaverde Corrales, Antonio; Vázquez Gómez, Esther

    2015-01-01

    The authors acknowledge the financial support granted to E.V. (PI12/00327) and R.M. (PI12/01861) from FIS, to E.V. (TV32013-133930) and to R.M. and A.V. (TV32013-132031) from La Marató de TV3 (416/C/2013), to A.V. from MINECO (Grant BIO2013-41019-P) and from the Centro de Investigación Biomédica en Red (CIBER) de Bioingeniería, Biomateriales y Nanomedicina (NANOPROTHER and NANOCOMETS projects). We are grateful to the Protein Production Platform (CIBER-BBN-UAB) for protein production and purif...

  3. Nanoparticle Formulation Increases Oral Bioavailability of Poorly Soluble Drugs: Approaches Experimental Evidences and Theory

    OpenAIRE

    Jia, Lee

    2005-01-01

    The increasing frequency at which poorly soluble new chemical entities are being discovered raises concerns in the pharmaceutical industry about drugability associated with erratic dissolution and low bioavailability of these hydrophobic compounds. Nanonization provides a plausible pharmaceutical basis for enhancing oral bioavailability and therapeutic effectiveness of these compounds by increasing their surface area. This paper surveys methods available to pharmaceutical manufacturing nanopa...

  4. Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion

    OpenAIRE

    Harsha SN; Aldhubiab BE; Nair AB; Alhaider IA; Attimarad M; Venugopala KN; Srinivasan S; Gangadhar N; Asif AH

    2015-01-01

    Sree N Harsha,1 Bander E Aldhubiab,1 Anroop B Nair,1 Ibrahim Abdulrahman Alhaider,1 Mahesh Attimarad,1 Katharigatta N Venugopala,1  Saminathan Srinivasan,2 Nagesh Gangadhar,2 Afzal Haq Asif3 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2Department of Pharmaceutics, East Point College of Pharmacy, Bangalore, India; 3Department of Pharmacy Practice, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Sa...

  5. Nanoparticle formulation by Büchi B-90 Nano Spray Dryer for oral mucoadhesion

    OpenAIRE

    Harsha, Sree

    2015-01-01

    Sree N Harsha,1 Bander E Aldhubiab,1 Anroop B Nair,1 Ibrahim Abdulrahman Alhaider,1 Mahesh Attimarad,1 Katharigatta N Venugopala,1  Saminathan Srinivasan,2 Nagesh Gangadhar,2 Afzal Haq Asif3 1Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia; 2Department of Pharmaceutics, East Point College of Pharmacy, Bangalore, India; 3Department of Pharmacy Practice, College of Clinical Pharmacy, King Faisal University, Al-...

  6. Liposomal flucytosine capped with gold nanoparticle formulations for improved ocular delivery

    OpenAIRE

    Salem, Heba

    2016-01-01

    Heba F Salem,1 Sayed M Ahmed,2 Mahmoud M Omar3 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 2Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt; 3Department of Industrial Pharmacy, Faculty of Pharmacy, Deraya University, El-Minia, Egypt Abstract: Nanoliposomes have an organized architecture that provides versatile functions. In this study, liposomes were used as an ocular car...

  7. Enhanced bioavailability of orally administered flurbiprofen by combined use of hydroxypropyl-cyclodextrin and poly(alkyl-cyanoacrylate) nanoparticles.

    Science.gov (United States)

    Zhao, Xiaoyun; Li, Wei; Luo, Qiuhua; Zhang, Xiangrong

    2014-03-01

    Flurbiprofen was formulated into nanoparticle suspension to improve its oral bioavailability. Hydroxypropyl-β-cyclodextrin inclusion-flurbiprofen complex (HP-β-CD-FP) was prepared, then incorporating this complex into poly(alkyl-cyanoacrylate) (PACA) nanoparticles. HP-β-CD-FP-PACA nanoparticle was prepared by the emulsion solvent polymerization method. The zeta potential was -26.8 mV, the mean volume particle diameter was 134 nm, drug encapsulation efficiency was 53.3 ± 3.6 % and concentration was 1.5 mg/mL. The bioavailability of flurbiprofen from optimized nanoparticles was assessed in male Wistar rats at a dose of 15 mg/kg. As compared to the flurbiprofen suspension, 211.6 % relative bioavailability was observed for flurbiprofen nanoparticles. The reduced particle size and increased surface area may contribute to improve oral bioavailability of flurbiprofen.

  8. Formulation and picture of quantum phase

    Institute of Scientific and Technical Information of China (English)

    YAO ZhiXin; ZHONG JianWei; PAN BaiLiang

    2009-01-01

    Based on the concept of classical phase, we formulate a new explanation for the quantum phase from the quantum mechanical point of view. The quantum phase is the canonically conjugate variable of an angular momentum operator, which corresponds to the angular position φ in an actual physical space with a classical reference frame, but it takes a complex exponential form e~(iφ)-cosφ+i sinφin the abstract Hilbert space of a quantum reference frame. This formulation is simply the famous Euler formula in a complex number field. In particular, when φ= π/2, the correlative quantum phase is a unitary pure imaginary number e~(iπ/2)=cos(π/2)+i sin(π/2) = i. By using a photon state-vector function that is the general solution of photon Schrodinger equation and can completely describe a photon's behavior, we discuss the relationship between the angular momentum of a photon and the phase of the photon; we also analyze the intrinsic relationship between the macroscopic light wave phase and the microscopic photon phase.

  9. Formulation and picture of quantum phase

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    Based on the concept of classical phase,we formulate a new explanation for the quantum phase from the quantum mechanical point of view. The quantum phase is the canonically conjugate variable of an angular momentum operator,which corresponds to the angular position θ in an actual physical space with a classical reference frame,but it takes a complex exponential form eiθ≡cosθ +i sinθ in the abstract Hilbert space of a quantum reference frame. This formulation is simply the famous Euler formula in a complex number field. In particular,when θ = π/2,the correlative quantum phase is a unitary pure imaginary number eiπ/2 ≡cos(π/2)+i sin(π/2) ≡ i. By using a photon state-vector function that is the general solution of photon Schrdinger equation and can completely describe a photon’s behavior,we discuss the relationship between the angular momentum of a photon and the phase of the photon; we also analyze the intrinsic relationship between the macroscopic light wave phase and the microscopic photon phase.

  10. Formulation of elastic multi-structures

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    Based on the creative and groundbreaking work done by Feng and Shi, some further work has been carried out comprehensively by the first author on the formulation of elastic multi-structures. The main contribution of this paper can be summarized as follows: The work of Feng and Shi has been extended to an elastic multi-structures with nonlinear structural element: shell in both linear and nonlinear case. Three general combinations of multi-structures have been formulated, that is, Case 1: linear elements of 3-D body, 1-D bar/beam, 2-D plates and 2-D shell; Case 2: nonlinear elements of 3-D body, 1-D bar/beam, 2-D plates and 2-D shell; and Case 3: the linear-nonlinear mix problem of 3-D body (nonlinear), 1-D bar/beam (linear), 2-D plates (linear) and 2-D shell (linear). From the investigation, it has proved that the higher dimensional element will have a strong influence on the lower one with the inner linkage boundaries, and also proved that solution uniqueness of elastic multi-structures is different from a single 3-D body.

  11. New formulation of leading order anisotropic hydrodynamics

    Science.gov (United States)

    Tinti, Leonardo

    2015-05-01

    Anisotropic hydrodynamics is a reorganization of the relativistic hydrodynamics expansion, with the leading order already containing substantial momentum-space anisotropies. The latter are a cause of concern in the traditional viscous hydrodynamics, since large momentum anisotropies generated in ultrarelativistic heavy-ion collisions are not consistent with the hypothesis of small deviations from an isotropic background, i.e., from the local equilibrium distribution. We discuss the leading order of the expansion, presenting a new formulation for the (1+1)- dimensional case, namely, for the longitudinally boost invariant and cylindrically symmetric flow. This new approach is consistent with the well established framework of Israel and Stewart in the close to equilibrium limit (where we expect viscous hydrodynamics to work well). If we consider the (0+1)-dimensional case, that is, transversally homogeneous and longitudinally boost invariant flow, the new form of anisotropic hydrodynamics leads to better agreement with known solutions of the Boltzmann equation than the previous formulations, especially when we consider massive particles.

  12. Factors for formulating strategies for environmental restoration

    International Nuclear Information System (INIS)

    This publication focusses on factors which are important for formulating a strategy for environmental restoration. In parallel to this effort, the IAEA has conducted activities in related areas which have been reported in companion reports dealing with (1) the characterization of radioactively contaminated sites for remediation purposes and (2) available technology for cleanup and remediation of radioactively contaminated sites. Additionally, follow-up activities will focus on two other areas, viz. planning and management options for cleanup of contaminated groundwater, and post-restoration monitoring of decommissioned sites. In a separate initiative the IAEA has developed preliminary guidance on radiological criteria for determining when cleanup action is needed and for deciding on when areas have been cleaned up to a sufficient extent. It is also concerned with radioactive contamination of soils, groundwaters, structures and biota which may have the potential for harm to people. It is intended that it will serve as an important source of information and data on the key factors to be considered in the formulation of an environmental restoration strategy

  13. FORMULATION DEVELOPMENT OF ENTERAL NUTRITION PRODUCTS

    Directory of Open Access Journals (Sweden)

    Mirajkar Reshma Nilesh

    2011-03-01

    Full Text Available This review mainly deals with the Formulation Development of Enteral Nutrition Products. Nutrition plays an important role in the prevention and management of many diseases. Chronic illness is associated with many complications such as anorexia, hypermetabolism, malabsorption, atrophy of muscles, liver, kidney, gastrointestinal tract heart, and impaired cell mediated immunity, susceptibility to infection, poor wound healing, anaemia, death. Hence it is important to correct caloric and nutrient deficiencies whenever possible. The term enteral means “within or by the way of gastrointestinal tract”. The nutrition product given by enteral route called as enteral nutrition product. The different types of enteral nutrition are classified as Short term and long term enteral nutrition. Enteral tubes are made of PVC, Polyurethane etc. The selection of the enteral formula is patient specific thus its nutritional requirements, the ingredients used in it are taken into consideration. The classification of formulas is also done on the basis of the patient’s needs and ingredients used in it. The enteral feeds can be given in the form of solutions and powders which require reconstitution. The quality control test like Osmolality, pH, etc is also taken into consideration. Thus, the purpose here is to point out explicitly the formulation development of enteral nutrition products.

  14. FEED FORMULATION AND FEEDING TECHNOLOGY FOR FISHES

    Directory of Open Access Journals (Sweden)

    Govind Pandey

    2013-03-01

    Full Text Available Most fish farmers and ornamental fish hobbyists buy the bulk of their feed from commercial manufacturers. However, small quantities of specialized feeds are often needed for experimental purposes, feeding difficult-to maintain aquarium fishes, larval or small juvenile fishes, brood fish conditioning, or administering medication to sick fish. Small ornamental fish farms with an assortment of fish require small amounts of various diets with particular ingredients. It is not cost effective for commercial manufacturers to produce very small quantities of specialized feeds. Most feed mills will only produce custom formulations in quantities of more than one ton, and medicated feeds are usually sold in 50-pound bags. Small fish farmers, hobbyists and laboratory technicians are, therefore, left with the option of buying large quantities of expensive feed, which often goes to waste. Small quantities of fish feeds can be made quite easily in the laboratory, classroom, or at home, with common ingredients and simple kitchen or laboratory equipment. Hence, this review provides the knowledge about the fish feed formulation and feeding technology concerned with the live feed for fish larvae, fish feeds, fish feed ingredients, common fish feed stuffs, animal and plant sources of feeds for culture fish, and fish feeding methods.

  15. Science Formulation of Global Precipitation Mission (GPM)

    Science.gov (United States)

    Smith, Eric A.; Mehta, Amita; Shepherd, Marshall; Starr, David O. (Technical Monitor)

    2002-01-01

    In late 2001, the Global Precipitation Measurement (GPM) mission was approved as a new start by the National Aeronautics and Space Administration (NASA). The new mission, which is now in its formulation phase, is motivated by a number of scientific questions that are posed over a range of space and time scales that generally fall within the discipline of the global water and energy cycle (GWEC), although not restricted to that branch of research. Recognizing that satellite rainfall datasets are now a foremost tool for understanding global climate variability out to decadal scales and beyond, for improving weather forecasting, and for producing better predictions of hydrometeorological processes including short-term hazardous flooding and seasonal fresh water resources assessment, a comprehensive and internationally sanctioned global measuring strategy has led to the GPM mission. The GPM mission plans to expand the scope of rainfall measurement through use of a multi-member satellite constellation that will be contributed by a number of world nations. This talk overviews the GPM scientific research program that has been fostered within NASA, then focuses on scientific progress that is being made in various areas in the course of the mission formulation phase that are of interest to the Natural Hazards scientific community. This latter part of the talk addresses research issues that have become central to the GPM science implementation plan concerning the rate of the global water cycling, cloud macrophysical-microphysical processes of flood-producing storms, and the general improvement in measuring precipitation at the fundamental microphysical level.

  16. FORMULATION STRATEGY FOR DISSOLUTION ENHANCEMENT OF SIMVASTATIN

    Directory of Open Access Journals (Sweden)

    Neha Parmar et al

    2012-10-01

    Full Text Available The present work aim was “Formulation Strategy for Dissolution Enhancement of Simvastatin”. Simvastatin is lipid lowering drug which is known as HMG CoA reductase. The objective of this study was to increase the solubility of poorly water soluble drug, namely simvastatin, by the formation of solid dispersion and complex and also using the microwave induction technique on these formations. For solid dispersion method dispersion carrier used were poloxamer 407 and gelucire 44/14. The fusion method was used to prepare the dispersions. For inclusion complexation method β-cyclodextrin derivative of cyclodextrin was used to prepare complex with drug. Kneading method was used for formulation. After completion of these two techniques these polymers were used for the microwave induced fusion method. All the ratio of drug and polymer were used to heat for different time interval. These samples were used for solubility measurement. In the solid dispersion technique, simvastatin show higher increase in solubility with gelucire 44/14 in the ratio of 1:5 as compare to poloxamer 407. In the microwave induced fusion method simvastatin show higher solubility with simvastatin with gelucire 44/14 after 10 mins time interval as compare to poloxamer 407 and β-cyclodextrin. Solubility of simvastatin increased higher with gelucire 44/14 by using microwave induced fusion method as compare to other technique. By using gelucire 44/14 with simvastatin it show 94% increase in solubility of simvastatin as compare to pure drug in water.

  17. Clinical evaluation of seven anticalculus dentifrice formulations.

    Science.gov (United States)

    Scruggs, R R; Stewart, P W; Samuels, M S; Stamm, J W

    1991-01-01

    One hundred ninety-two subjects completed a clinical trial to determine the effects of seven dentifrice formulations on calculus inhibition. The double-blind study involved a ten-day control phase and a ten-day experimental phase. For the control phase, subjects were evaluated for calculus present, received a prophylaxis and had pre-weighed mylar strips attached to the lingual surfaces of the mandibular incisors to harvest mineral deposits. Subjects were then assigned the placebo dentifrice for unsupervised twice-daily use and were required to report once a day for a supervised mouthrinse using a 1:3 dilution of the dentrifice. The experimental phase was identical except that subjects were allocated the experimental dentifices using a stratified random assignment based on age, gender and the initial presence of calculus. Simple linear regression analyses of the dry and ash log weights obtained from the strips were performed. The results showed no statistically significant differences among the test products; however, two formulations containing zinc citrate showed some calculus inhibition-potential suggesting that further research and development of such products may be warranted.

  18. Projecting India's energy requirements for policy formulation

    International Nuclear Information System (INIS)

    Energy policy has to have a long-term perspective. To formulate it one needs to know the contours of energy requirements and options. Different approaches have been followed in literature, each with their own problems. A top down econometric approach provides little guidance on policies, while a bottom up approval requires too much knowledge and too many assumptions. Using top-down econometric approach for aggregate overall benchmarking and a detailed activity analysis model, Integrated Energy System Model, for a few large sectors, provides a unique combination for easing the difficulties of policy formulation. The model is described in this paper. Eleven alternate scenarios are built, designed to map out extreme points of feasible options. Results show that even after employing all domestic energy resource to their full potential, there will be a continued rise of fossil fuel use, continued importance of coal, and continued rise of import dependence. Energy efficiency emerges as a major option with a potential to reduce energy requirement by as much as 17%. Scenario results point towards pushing for development of alternative sources.

  19. Projecting India's energy requirements for policy formulation

    International Nuclear Information System (INIS)

    Energy policy has to have a long-term perspective. To formulate it one needs to know the contours of energy requirements and options. Different approaches have been followed in literature, each with their own problems. A top down econometric approach provides little guidance on policies, while a bottom up approval requires too much knowledge and too many assumptions. Using top-down econometric approach for aggregate overall benchmarking and a detailed activity analysis model, Integrated Energy System Model, for a few large sectors, provides a unique combination for easing the difficulties of policy formulation. The model is described in this paper. Eleven alternate scenarios are built, designed to map out extreme points of feasible options. Results show that even after employing all domestic energy resource to their full potential, there will be a continued rise of fossil fuel use, continued importance of coal, and continued rise of import dependence. Energy efficiency emerges as a major option with a potential to reduce energy requirement by as much as 17%. Scenario results point towards pushing for development of alternative sources. (author)

  20. Immunoglobulin: production, mechanisms of action and formulations

    Directory of Open Access Journals (Sweden)

    Marcia Cristina Zago Novaretti

    2011-10-01

    Full Text Available Human immunoglobulin (Ig began to be applied in the clinical practice with the treatment of primary immunodeficiencies. Quickly, applications of Ig increased, as its anti-inflammatory and immunomodulatory functions were elucidated. Currently, Ig is the most commonly used blood product. Ig is obtained by processing plasma; methods, in particular, techniques to reduce plasma viral loads have been evolving over the years and include: pasteurization, solvent/ detergent treatment, caprylic acid treatment and nanofiltration. These methods contribute to increased safety and quality of blood products. The mechanisms of action of Ig not only involve the blockade of Fc receptors of phagocytes, but also control complement pathways, idiotype-anti-idiotype dimer formation, blockage of superantigen binding to T cells, inhibition of dendritic cells and stimulation of regulatory T cells (Tregs. There are several formulations of Ig available, each one with its own peculiar characteristics. In Brazil, there is stringent legislation regulating the quality of Ig. Only Ig products that completely fulfill the quality control criteria are released for use. These standards involve different tests from visual inspection to determination of anti-complementary activity. This paper will further review the history and current status of Ig, including its production and mechanisms of action. The formulations available in Brazil and also the criteria of quality control currently applied will be presented.