Calcium carbonate microspheres as carriers for the anticancer drug camptothecin

Energy Technology Data Exchange (ETDEWEB)

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

2012-12-01

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

Promotion of the transdermal delivery of protein drugs by N-trimethyl chitosan nanoparticles combined with polypropylene electret.

Science.gov (United States)

Tu, Ye; Wang, Xinxia; Lu, Ying; Zhang, He; Yu, Yuan; Chen, Yan; Liu, Junjie; Sun, Zhiguo; Cui, Lili; Gao, Jing; Zhong, Yanqiang

We recently reported that electret, which was prepared by a corona charging system with polypropylene film, could enhance the transdermal delivery of several drugs of low molecular weight. The aim of this study was to investigate whether electret could enhance the transdermal delivery of protein drugs by N -trimethyl chitosan nanoparticles (TMC NPs) prepared by an ionic gelation method. A series of experiments were performed, including in vitro skin permeation assays and anti-inflammatory effects, to evaluate the transdermal delivery of protein drugs by TMC NPs in the presence of electret. The results showed that in the presence of electret, the transdermal delivery of protein drugs in TMC NPs was significantly enhanced, as demonstrated by in vitro permeation studies and confocal laser scanning microscopy. Notably, superoxide dismutase-loaded TMC NPs combined with electret exhibited the best inhibitory effect on the edema of the mouse ear. TMC NPs combined with electret represent a novel platform for the transdermal delivery of protein drugs.

Polyphosphonate induced coacervation of chitosan: Encapsulation of proteins/enzymes and their biosensing

International Nuclear Information System (INIS)

Liu, Hailing; Cui, Yanyun; Li, Pan; Zhou, Yiming; Chen, Yu; Tang, Yawen; Lu, Tianhong

2013-01-01

Graphical abstract: Based on the coacervation of chitosan via the ionotropic crosslinking interaction, proteins/enzymes can be encapsulated in situ into chitosan matrix. -- Highlights: •The ionotropic crosslinking interactions result in the coacervation of chitosan. •A phosphonate-assisted encapsulation of proteins in chitosan matrix is introduced. •The encapsulated proteins retain their bioactivity. •The encapsulation method can be used to fabricate various chitosan-based biosensors. -- Abstract: Based on the polyphosphonate-assisted coacervation of chitosan, a simple and versatile procedure for the encapsulation of proteins/enzymes in chitosan–carbon nanotubes (CNTs) composites matrix was developed. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS), energy dispersive spectrum (EDS) mapping demonstrated the hemoglobin (Hb) uniformly distributed into chitosan–CNTs composites matrix. Raman measurements indicated the CNTs in composites matrix retained the electronic and structural integrities of the pristine CNTs. Fourier transform infrared (FT-IR), ultraviolet–visible (UV–vis) and circular dichroism (CD) spectroscopy displayed the encapsulated Hb preserved their near-native structure, indicating the polyphosphonate–chitosan–CNTs composites possessed excellent biocompatibility for the encapsulation of proteins/enzymes. Electrochemical measurements indicated the encapsulated Hb could directly exchange electron with the substrate electrode. Moreover, the modified electrode showed excellent bioelectrocatalytic activity for the reduction of hydrogen peroxide. Under optimum experimental conditions, the fabricated electrochemical sensor displayed the fast response (less than 3 s), wide linear range (7.0 × 10 −7 to 2.0 × 10 −3 M) and low detection limit (4.0 × 10 −7 M) for the determination of hydrogen peroxide. This newly developed protocol was simple and mild and would certainly

Polyphosphonate induced coacervation of chitosan: Encapsulation of proteins/enzymes and their biosensing

Energy Technology Data Exchange (ETDEWEB)

Liu, Hailing; Cui, Yanyun; Li, Pan; Zhou, Yiming; Chen, Yu, E-mail: ndchenyu@yahoo.cn; Tang, Yawen; Lu, Tianhong

2013-05-07

Graphical abstract: Based on the coacervation of chitosan via the ionotropic crosslinking interaction, proteins/enzymes can be encapsulated in situ into chitosan matrix. -- Highlights: •The ionotropic crosslinking interactions result in the coacervation of chitosan. •A phosphonate-assisted encapsulation of proteins in chitosan matrix is introduced. •The encapsulated proteins retain their bioactivity. •The encapsulation method can be used to fabricate various chitosan-based biosensors. -- Abstract: Based on the polyphosphonate-assisted coacervation of chitosan, a simple and versatile procedure for the encapsulation of proteins/enzymes in chitosan–carbon nanotubes (CNTs) composites matrix was developed. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS), energy dispersive spectrum (EDS) mapping demonstrated the hemoglobin (Hb) uniformly distributed into chitosan–CNTs composites matrix. Raman measurements indicated the CNTs in composites matrix retained the electronic and structural integrities of the pristine CNTs. Fourier transform infrared (FT-IR), ultraviolet–visible (UV–vis) and circular dichroism (CD) spectroscopy displayed the encapsulated Hb preserved their near-native structure, indicating the polyphosphonate–chitosan–CNTs composites possessed excellent biocompatibility for the encapsulation of proteins/enzymes. Electrochemical measurements indicated the encapsulated Hb could directly exchange electron with the substrate electrode. Moreover, the modified electrode showed excellent bioelectrocatalytic activity for the reduction of hydrogen peroxide. Under optimum experimental conditions, the fabricated electrochemical sensor displayed the fast response (less than 3 s), wide linear range (7.0 × 10{sup −7} to 2.0 × 10{sup −3} M) and low detection limit (4.0 × 10{sup −7} M) for the determination of hydrogen peroxide. This newly developed protocol was simple and mild and

Surface modification of protein enhances encapsulation in chitosan nanoparticles

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Koyani, Rina D.; Andrade, Mariana; Quester, Katrin; Gaytán, Paul; Huerta-Saquero, Alejandro; Vazquez-Duhalt, Rafael

2018-04-01

Chitosan nanoparticles have a huge potential as nanocarriers for environmental and biomedical purposes. Protein encapsulation in nano-sized chitosan provides protection against inactivation, proteolysis, and other alterations due to environmental conditions, as well as the possibility to be targeted to specific tissues by ligand functionalization. In this work, we demonstrate that the chemical modification of the protein surface enhances the protein loading in chitosan nanocarriers. Encapsulation of green fluorescent protein and the cytochrome P450 was studied. The increase of electrostatic interactions between the free amino groups of chitosan and the increased number of free carboxylic groups in the protein surface enhance the protein loading, protein retention, and, thus, the enzymatic activity of chitosan nanoparticles. The chemical modification of protein surface with malonic acid moieties reduced drastically the protein isoelectric point increasing the protein interaction with the polycationic biomaterial and chitosan. The chemical modification of protein does not alter the morphology of chitosan nanoparticles that showed an average diameter of 18 nm, spheroidal in shape, and smooth surfaced. The strategy of chemical modification of protein surface, shown here, is a simple and efficient technique to enhance the protein loading in chitosan nanoparticles. This technique could be used for other nanoparticles based on polycationic or polyanionic materials. The increase of protein loading improves, doubtless, the performance of protein-loaded chitosan nanoparticles for biotechnological and biomedical applications.

Improvement of Stability and Antioxidant Activities by Using Phycocyanin - Chitosan Encapsulation Technique

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Suzery, Meiny; Hadiyanto; Majid, Dian; Setyawan, Deny; Sutanto, Heri

2017-02-01

Encapsulation is a coating process to improve the stability of bioactive compounds. Phycocyanin with high antioxidant activity has been encapsulated with chitosan in microcapsules form. In this study aims to determine the best conditions in the encapsulation process using the extrusion method, characterization of the physicochemical properties of the microcapsules, antioxidant activity test using DPPH, in vitro release performance and evaluate the storage stability against temperature. The results of the encapsulation process is obtained: Na-TPP is better than Na-citrate as crosslinker and chitosan content 3% as a coating with ratio of chitosan to phycocyanin ratio 1: 1. Test of antioxidant activity also showed encapsulation with chitosan content 3% has the highest antioxidant activity. Morphological analysis microcapsules were found to have compact spherical shape with diameter range 900-1000 µm. In vitro release testing showed a quick release in an acidic environment (SGF) for 2 hours and slowly release under alkaline conditions (SIF) for 8 hours under mechanical stirring at 37°C. Phycocyanin much more stable against temperature during storage in microcapsules.

Silk sericin-alginate-chitosan microcapsules: hepatocytes encapsulation for enhanced cellular functions.

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Nayak, Sunita; Dey, Sanchareeka; Kundu, Subhas C

2014-04-01

The encapsulation based technology permits long-term delivery of desired therapeutic products in local regions of body without the need of immunosuppressant drugs. In this study microcapsules composed of sericin and alginate micro bead as inner core and with an outer chitosan shell are prepared. This work is proposed for live cell encapsulation for potential therapeutic applications. The sericin protein is obtained from cocoons of non-mulberry silkworm Antheraea mylitta. The sericin-alginate micro beads are prepared via ionotropic gelation under high applied voltage. The beads further coated with chitosan and crosslinked with genipin. The microcapsules developed are nearly spherical in shape with smooth surface morphology. Alamar blue assay and confocal microscopy indicate high cell viability and uniform encapsulated cell distribution within the sericin-alginate-chitosan microcapsules indicating that the microcapsules maintain favourable microenvironment for the cells. The functional analysis of encapsulated cells demonstrates that the glucose consumption, urea secretion rate and intracellular albumin content increased in the microcapsules. The study suggests that the developed sericin-alginate-chitosan microcapsule contributes towards the development of cell encapsulation model. It also offers to generate enriched population of metabolically and functionally active cells for the future therapeutics especially for hepatocytes transplantation in acute liver failure. Copyright © 2014 Elsevier B.V. All rights reserved.

Chitosan/siRNA nanoparticles encapsulated in PLGA nanofibers for siRNA delivery

DEFF Research Database (Denmark)

Chen, Menglin; Gao, Shan; Dong, Mingdong

2012-01-01

Composite nanofibers of biodegradable poly(d,l-lactic-co-glycolic acid) (PLGA) encapsulating chitosan/siRNA nanoparticles (NPs) were prepared by electrospinning. Acidic/alkaline hydrolysis and a bulk/surface degradation mechanism were investigated in order to achieve an optimized release profile...... for prolonged and efficient gene silencing. Thermo-controlled AFM in situ imaging not only revealed the integrity of the encapsulated chitosan/siRNA polyplex but also shed light on the decreasing Tg of PLGA on the fiber surfaces during release. A triphasic release profile based on bulk erosion was obtained at p......RNA transfection, where the encapsulated chitosan/siRNA NPs exhibited up to 50% EGFP gene silencing activity after 48 h post-transfection on H1299 cells....

Development of chitosan-pullulan composite nanoparticles for nasal delivery of vaccines: in vivo studies.

Science.gov (United States)

Cevher, Erdal; Salomon, Stefan K; Somavarapu, Satyanarayana; Brocchini, Steve; Alpar, H Oya

2015-01-01

Here, we aimed at developing chitosan/pullulan composite nanoparticles and testing their potential as novel systems for the nasal delivery of diphtheria toxoid (DT). All the chitosan derivatives [N-trimethyl (TMC), chloride and glutamate] and carboxymethyl pullulan (CMP) were synthesised and antigen-loaded composites were prepared by polyion complexation of chitosan and pullulan derivatives (particle size: 239-405 nm; surface charge: +18 and +27 mV). Their immunological effects after intranasal administration to mice were compared to intramuscular route. Composite nanoparticles induced higher levels of IgG responses than particles formed with chitosan derivative and antigen. Nasally administered TMC-pullulan composites showed higher DT serum IgG titre when compared with the other composites. Co-encapsulation of CpG ODN within TMC-CMP-DT nanoparticles resulted in a balanced Th1/Th2 response. TMC/pullulan composite nanoparticles also induced highest cytokine levels compared to those of chitosan salts. These findings demonstrated that TMC-CMP-DT composite nanoparticles are promising delivery system for nasal vaccination.

Drug permeability and mucoadhesion properties of thiolated trimethyl chitosan nanoparticles in oral insulin delivery.

Science.gov (United States)

Yin, Lichen; Ding, Jieying; He, Chunbai; Cui, Liming; Tang, Cui; Yin, Chunhua

2009-10-01

Trimethyl chitosan-cysteine conjugate (TMC-Cys) was synthesized in an attempt to combine the mucoadhesion and the permeation enhancing effects of TMC and thiolated polymers related to different mechanisms for oral absorption. TMC-Cys with various molecular weights (30, 200, and 500 kDa) and quaternization degrees (15 and 30%) was allowed to form polyelectrolyte nanoparticles with insulin through self-assembly, which demonstrated particle size of 100-200 nm, zeta potential of +12 to +18 mV, and high encapsulation efficiency. TMC-Cys/insulin nanoparticles (TMC-Cys NP) showed a 2.1-4.7-fold increase in mucoadhesion compared to TMC/insulin nanoparticles (TMC NP), which might be partly attributed to disulfide formation between TMC-Cys and mucin as evidenced by DSC measurement. Compared to insulin solution and TMC NP, TMC-Cys NP induced increased insulin transport through rat intestine by 3.3-11.7 and 1.7-2.6 folds, promoted Caco-2 cell internalization by 7.5-12.7 and 1.7-3.0 folds, and augmented uptake in Peyer's patches by 14.7-20.9 and 1.7-5.0 folds, respectively. Such results were further confirmed by in vivo experiment with the optimal TMC-Cys NP. Biocompatibility assessment revealed lack of toxicity of TMC-Cys NP. Therefore, self-assembled nanoparticles between TMC-Cys and protein drugs could be an effective and safe oral delivery system.

Exploring advantages/disadvantages and improvements in overcoming gene delivery barriers of amino acid modified trimethylated chitosan.

Science.gov (United States)

Zheng, Hao; Tang, Cui; Yin, Chunhua

2015-06-01

Present study aimed at exploring advantages/disadvantages of amino acid modified trimethylated chitosan in conquering multiple gene delivery obstacles and thus providing comprehensive understandings for improved transfection efficiency. Arginine, cysteine, and histidine modified trimethyl chitosan were synthesized and employed to self-assemble with plasmid DNA (pDNA) to form nanocomplexes, namely TRNC, TCNC, and THNC, respectively. They were assessed by structural stability, cellular uptake, endosomal escape, release behavior, nuclear localization, and in vitro and in vivo transfection efficiencies. Besides, sodium tripolyphosphate (TPP) was added into TRNC to compromise certain disadvantageous attributes for pDNA delivery. Optimal endosomal escape ability failed to bring in satisfactory transfection efficiency of THNC due to drawbacks in structural stability, cellular uptake, pDNA liberation, and nuclear distribution. TCNC evoked the most potent gene expression owing to multiple advantages including sufficient stability, preferable uptake, efficient pDNA release, and high nucleic accumulation. Undesirable stability and insufficient pDNA release adversely affected TRNC-mediated gene transfer. However, incorporation of TPP could improve such disadvantages and consequently resulted in enhanced transfection efficiencies. Coordination of multiple contributing effects to conquer all delivery obstacles was necessitated for improved transfection efficiency, which would provide insights into rational design of gene delivery vehicles.

Novel chitosan film embedded with liposome-encapsulated phage for biocontrol of Escherichia coli O157:H7 in beef.

Science.gov (United States)

Cui, Haiying; Yuan, Lu; Lin, Lin

2017-12-01

In recent years, phages used for the reduction of pathogenic bacteria have fostered many attentions, but they are liable to lost bioactivity in food due to the presence of acidic compounds, enzymes and evaporite materials. To improve the stability of phages, a chitosan edible film containing liposome-encapsulated phage was engineered in the present study. The characteristics of liposome-encapsulated phage and the chitosan film containing liposome-encapsulated phage were investigated. The encapsulation efficiency of phages in liposome reached 57.66±0.12%. Besides, the desirable physical properties of chitosan film were obtained. The chitosan film embedded with liposome-encapsulated phage exhibited high antibacterial activity against Escherichia coli O157:H7, without the impact on the sensory properties of beef. Hence, chitosan film containing liposome-encapsulated phage could be a promising antibacterial packaging for beef preservation. Copyright © 2017 Elsevier Ltd. All rights reserved.

5-Fluorouracil Encapsulated Chitosan Nanoparticles for pH-Stimulated Drug Delivery: Evaluation of Controlled Release Kinetics

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R. Seda Tığlı Aydın

2012-01-01

Full Text Available Nanoparticles consisting of human therapeutic drugs are suggested as a promising strategy for targeted and localized drug delivery to tumor cells. In this study, 5-fluorouracil (5-FU encapsulated chitosan nanoparticles were prepared in order to investigate potentials of localized drug delivery for tumor environment due to pH sensitivity of chitosan nanoparticles. Optimization of chitosan and 5-FU encapsulated nanoparticles production revealed 148.8±1.1 nm and 243.1±17.9 nm particle size diameters with narrow size distributions, which are confirmed by scanning electron microscope (SEM images. The challenge was to investigate drug delivery of 5-FU encapsulated chitosan nanoparticles due to varied pH changes. To achieve this objective, pH sensitivity of prepared chitosan nanoparticle was evaluated and results showed a significant swelling response for pH 5 with particle diameter of ∼450 nm. In vitro release studies indicated a controlled and sustained release of 5-FU from chitosan nanoparticles with the release amounts of 29.1–60.8% due to varied pH environments after 408 h of the incubation period. pH sensitivity is confirmed by mathematical modeling of release kinetics since chitosan nanoparticles showed stimuli-induced release. Results suggested that 5-FU encapsulated chitosan nanoparticles can be launched as pH-responsive smart drug delivery agents for possible applications of cancer treatments.

A step-by-step approach to study the influence of N-acetylation on the adjuvanticity of N,N,N-trimethyl chitosan (TMC) in an intranasal nanoparticulate influenza virus vaccine.

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Verheul, Rolf J; Hagenaars, Niels; van Es, Thomas; van Gaal, Ethlinn V B; de Jong, Pascal H J L F; Bruijns, Sven; Mastrobattista, Enrico; Slütter, Bram; Que, Ivo; Heldens, Jacco G M; van den Bosch, Han; Glansbeek, Harrie L; Hennink, Wim E; Jiskoot, Wim

2012-03-12

Recently we reported that reacetylation of N,N,N-trimethyl chitosan (TMC) reduced the adjuvant effect of TMC in mice after intranasal (i.n.) administration of whole inactivated influenza virus (WIV) vaccine. The aim of the present study was to elucidate the mechanism of this lack of adjuvanticity. Reacetylated TMC (TMC-RA, degree of acetylation 54%) was compared with TMC (degree of acetylation 17%) at six potentially critical steps in the induction of an immune response after i.n. administration in mice. TMC-RA was degraded in a nasal wash to a slightly larger extent than TMC. The local i.n. distribution and nasal clearance of WIV were similar for both TMC types. Fluorescently labeled WIV was taken up more efficiently by Calu-3 cells when formulated with TMC-RA compared to TMC and both TMCs significantly reduced transport of WIV over a Calu-3 monolayer. Murine bone-marrow derived dendritic cell activation was similar for plain WIV, and WIV formulated with TMC-RA or TMC. The inferior adjuvant effect in mice of TMC-RA over that of TMC might be caused by a slightly lower stability of TMC-RA-WIV in the nasal cavity, rather than by any of the other factors studied in this paper. Copyright © 2011 Elsevier B.V. All rights reserved.

Characterization and obtainment of thin films based on N,N,N-trimethyl chitosan and heparin through the technical layer-by-layer; Caracterizacao e obtencao de filmes finos de N,N,N-trimetil quitosana e heparina atraves da tecnica layer-by-layer

Energy Technology Data Exchange (ETDEWEB)

NONE

2011-07-01

Thin films of Heparin (HP) and N,N,N-trimethyl chitosan (TMC) with a high degree of quaternization (DQ) were obtained at pH 7.4 through the layer-by-layer (LbL) technique. Polystyrene (PS) was oxidized with aqueous solution of sodium persulfate and subsequently employed as substrate. The characterization of TMC and the respective determination of DQ were performed through {sup 1}H NMR spectroscopy. The thin films de TMC/HP were characterized by FTIR-ATR and AFM. Both techniques confirmed the adsorption of TMC and HP in surface of the PS. The increasing of the bilayers provides a decrease of the projections and/or roughness, further of minimizing the depressions at the surface of the films. Studies of thin films the base of TMC/HP prepared from the LbL technique has not been reported in the literature. It is expected that the thin films of TMC/HP present anti-adhesive and antimicrobial properties. (author)

Controlling chitosan-based encapsulation for protein and vaccine delivery

Science.gov (United States)

Koppolu, Bhanu prasanth; Smith, Sean G.; Ravindranathan, Sruthi; Jayanthi, Srinivas; Kumar, Thallapuranam K.S.; Zaharoff, David A.

2014-01-01

Chitosan-based nano/microencapsulation is under increasing investigation for the delivery of drugs, biologics and vaccines. Despite widespread interest, the literature lacks a defined methodology to control chitosan particle size and drug/protein release kinetics. In this study, the effects of precipitation-coacervation formulation parameters on chitosan particle size, protein encapsulation efficiency and protein release were investigated. Chitosan particle sizes, which ranged from 300 nm to 3 μm, were influenced by chitosan concentration, chitosan molecular weight and addition rate of precipitant salt. The composition of precipitant salt played a significant role in particle formation with upper Hofmeister series salts containing strongly hydrated anions yielding particles with a low polydispersity index (PDI) while weaker anions resulted in aggregated particles with high PDIs. Sonication power had minimal effect on mean particle size, however, it significantly reduced polydispersity. Protein loading efficiencies in chitosan nano/microparticles, which ranged from 14.3% to 99.2%, was inversely related to the hydration strength of precipitant salts, protein molecular weight and directly related to the concentration and molecular weight of chitosan. Protein release rates increased with particle size and were generally inversely related to protein molecular weight. This study demonstrates that chitosan nano/microparticles with high protein loading efficiencies can be engineered with well-defined sizes and controllable release kinetics through manipulation of specific formulation parameters. PMID:24560459

Smart AS1411-aptamer conjugated pegylated PAMAM dendrimer for the superior delivery of camptothecin to colon adenocarcinoma in vitro and in vivo.

Science.gov (United States)

Alibolandi, Mona; Taghdisi, Seyed Mohammad; Ramezani, Pouria; Hosseini Shamili, Fazileh; Farzad, Sara Amel; Abnous, Khalil; Ramezani, Mohammad

2017-03-15

In the current study camptothecin-loaded pegylated PAMAM dendrimer were synthesized and were functionalized with AS1411 anti-nucleolin aptamers for site-specific targeting against colorectal cancer cells which over expresses nucleolin receptors. The morphological properties and size dispersity of the prepared nanoparticles were evaluated using transmission electron microscope (TEM) and DLS. The drug-loading content and encapsulation efficiency were obtained 8.1% and 93.67% respectively. The in vitro release of camptothecin from the formulation was provided the sustained release of encapsulated camptothecin during 4days. Comparative in vitro cytotoxicity experiments demonstrated that the targeted camptothecin loaded-pegylated dendrimers had higher antiproliferation activity, towards nucleolin-positive HT29 and C26 colorectal cancer cells than nucleolin-negative CHO cell line. Fluorscence microscopy and flow cytometry also confirmed the enhanced cellular uptake of AS1411 targeted pegylated-dendrimer. In vivo study in C26 tumor-bearing BALB/C mice revealed that the AS1411-functionalized camptothecin loaded pegylated dendrimers improved antitumor activity and survival rate of the encapsulated camptothecin. Conjugation of AS1411 aptamer to the camptothecin loaded-pegylated dendrimer surface provides site-specific delivery of camptothecin, inhibit C26 tumor growth in vivo and significantly decrease systemic toxicity. These results suggested that the new nucleolin-targeted pegylated PAMAM dendrimer as a delivery system for camptothecin have the potential for the treatment of nucleolin-overexpressed colorectal cancer. Copyright © 2017 Elsevier B.V. All rights reserved.

Antiproliferative effect of Antrodia camphorata polysaccharides encapsulated in chitosan-silica nanoparticles strongly depends on the metabolic activity type of the cell line

Energy Technology Data Exchange (ETDEWEB)

Kong, Zwe-Ling, E-mail: kongzl@mail.ntou.edu.tw; Chang, Jenq-Sheng; Chang, Ke Liang B. [National Taiwan Ocean University, Department of Food Science (China)

2013-09-15

Chitosan molecules interact with silica and encapsulate the Antrodia camphorata extract (ACE) polysaccharides to form composite nanoparticles. The nanoparticle suspensions of ACE polysaccharides encapsulated in silica-chitosan and silica nanoparticles approach an average particle size of 210 and 294 nm in solution, respectively. The encapsulation efficiencies of ACE polysaccharides are 66 and 63.5 %, respectively. Scanning electron micrographs confirm the formation of near-spherical nanoparticles. ACE polysaccharides solution had better antioxidative capability than ACE polysaccharides encapsulated in silica or silica-chitosan nanoparticles suspensions. The antioxidant capacity of nanoparticles increases with increasing dissolution time. The antitumor effects of ACE polysaccharides, ACE polysaccharides encapsulated in silica, or silica-chitosan nanoparticles increased with increasing concentration of nanoparticles. This is the first report demonstrating the potential of ACE polysaccharides encapsulated in chitosan-silica nanoparticles for cancer chemoprevention. Furthermore, this study suggests that antiproliferative effect of nanoparticle-encapsulated bioactive could significantly depend on the metabolic activity type of the cell line.

Antiproliferative effect of Antrodia camphorata polysaccharides encapsulated in chitosan-silica nanoparticles strongly depends on the metabolic activity type of the cell line

Science.gov (United States)

Kong, Zwe-Ling; Chang, Jenq-Sheng; Chang, Ke Liang B.

2013-09-01

Chitosan molecules interact with silica and encapsulate the Antrodia camphorata extract (ACE) polysaccharides to form composite nanoparticles. The nanoparticle suspensions of ACE polysaccharides encapsulated in silica-chitosan and silica nanoparticles approach an average particle size of 210 and 294 nm in solution, respectively. The encapsulation efficiencies of ACE polysaccharides are 66 and 63.5 %, respectively. Scanning electron micrographs confirm the formation of near-spherical nanoparticles. ACE polysaccharides solution had better antioxidative capability than ACE polysaccharides encapsulated in silica or silica-chitosan nanoparticles suspensions. The antioxidant capacity of nanoparticles increases with increasing dissolution time. The antitumor effects of ACE polysaccharides, ACE polysaccharides encapsulated in silica, or silica-chitosan nanoparticles increased with increasing concentration of nanoparticles. This is the first report demonstrating the potential of ACE polysaccharides encapsulated in chitosan-silica nanoparticles for cancer chemoprevention. Furthermore, this study suggests that antiproliferative effect of nanoparticle-encapsulated bioactive could significantly depend on the metabolic activity type of the cell line.

Amidase encapsulated O-carboxymethyl chitosan nanoparticles for vaccine delivery.

Science.gov (United States)

Smitha, K T; Sreelakshmi, M; Nisha, N; Jayakumar, R; Biswas, Raja

2014-02-01

This work reports the development of amidase encapsulated O-carboxymethyl chitosan nanoparticles (Ami-O-CMC NPs) of 300±50 nm size by ionic cross-linking method. The prepared Ami-O-CMC NPs had an encapsulation efficiency of 55.39%. Haemolysis assay and cytotoxicity studies proved the hemocompatibility and cytocompatibility of the prepared NPs. The sustained release of Ami from the NPs is expected to prolong its immunogenicity and in turn lead to development of better protective immunity against Staphylococcus aureus infections. Copyright © 2013 Elsevier B.V. All rights reserved.

Preparation of N, N, N-trimethyl chitosan-functionalized retinoic acid ...

African Journals Online (AJOL)

encapsulated solid lipid nanoparticles for the effective treatment of glioma. Methods: Retinoic acid-loaded solid lipid nanoparticles (R-SLNs) were prepared using homogenization followed by sonication. R-SLN surfaces were functionalized electrostatically ...

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

Injectable and microporous scaffold of densely-packed, growth factor-encapsulating chitosan microgels.

Science.gov (United States)

Riederer, Michael S; Requist, Brennan D; Payne, Karin A; Way, J Douglas; Krebs, Melissa D

2016-11-05

In this work, an emulsion crosslinking method was developed to produce chitosan-genipin microgels which acted as an injectable and microporous scaffold. Chitosan was characterized with respect to pH by light scattering and aqueous titration. Microgels were characterized with swelling, light scattering, and rheometry of densely-packed microgel solutions. The results suggest that as chitosan becomes increasingly deprotonated above the pKa, repulsive forces diminish and intermolecular attractions cause pH-responsive chain aggregation; leading to microgel-microgel aggregation as well. The microgels with the most chitosan and least cross-linker showed the highest yield stress and a storage modulus of 16kPa when condensed as a microgel paste at pH 7.4. Two oppositely-charged growth factors could be encapsulated into the microgels and endothelial cells were able to proliferate into the 3D microgel scaffold. This work motivates further research on the applications of the chitosan microgel scaffold as an injectable and microporous scaffold in regenerative medicine. Copyright © 2016 Elsevier Ltd. All rights reserved.

Long-term Efficacy and Biocompatibility of Encapsulated Islet Transplantation With Chitosan-Coated Alginate Capsules in Mice and Canine Models of Diabetes.

Science.gov (United States)

Yang, Hae Kyung; Ham, Dong-Sik; Park, Heon-Seok; Rhee, Marie; You, Young Hye; Kim, Min Jung; Shin, Juyoung; Kim, On-You; Khang, Gilson; Hong, Tae Ho; Kim, Ji-Won; Lee, Seung-Hwan; Cho, Jae-Hyoung; Yoon, Kun-Ho

2016-02-01

Clinical application of encapsulated islet transplantation is hindered by low biocompatibility of capsules leading to pericapsular fibrosis and decreased islet viability. To improve biocompatibility, we designed a novel chitosan-coated alginate capsules and compared them to uncoated alginate capsules. Alginate capsules were formed by crosslinking with BaCl2, then they were suspended in chitosan solution for 10 minutes at pH 4.5. Xenogeneic islet transplantation, using encapsulated porcine islets in 1,3-galactosyltransferase knockout mice, and allogeneic islet transplantation, using encapsulated canine islets in beagles, were performed without immunosuppressants. The chitosan-alginate capsules showed similar pore size, islet viability, and insulin secretory function compared to alginate capsules, in vitro. Xenogeneic transplantation of chitosan-alginate capsules demonstrated a trend toward superior graft survival (P = 0.07) with significantly less pericapsular fibrosis (cell adhesion score: 3.77 ± 0.41 vs 8.08 ± 0.05; P transplantation. Allogeneic transplantation of chitosan-alginate capsules normalized the blood glucose level up to 1 year with little evidence of pericapsular fibrotic overgrowth on graft explantation. The efficacy and biocompatibility of chitosan-alginate capsules were demonstrated in xenogeneic and allogeneic islet transplantations using small and large animal models of diabetes. This capsule might be a potential candidate applicable in the treatment of type 1 diabetes mellitus patients, and further studies in nonhuman primates are required.

Properties of Lactobacillus reuteri chitosan-calcium-alginate encapsulation under simulated gastrointestinal conditions.

Science.gov (United States)

Huang, Hui-Ying; Tang, Yi-Ju; King, V An-Erl; Chou, Jen-Wei; Tsen, Jen-Horng

2015-03-01

The protective effects of encapsulation on the survival of Lactobacillus reuteri and the retention of the bacterium's probiotic properties under simulated gastrointestinal conditions were investigated. Viable counts and the remaining probiotic properties of calcium (Ca)-alginate encapsulated (A group), chitosan-Ca-alginate encapsulated (CA group), and unencapsulated, free L. reuteri (F group) were determined. Encapsulation improved the survival of L. reuteri subjected to simulated gastrointestinal conditions, with the greatest protective effect achieved in the CA group. The degree of cell membrane injury increased with increasing bile salt concentrations at constant pH, but the extent of injury was less in the encapsulated than in the free cells. Adherence rates were, in descending order: CA (0.524%)>A (0.360%)>F (0.275%). Lactobacillus reuteri cells retained their antagonistic activity toward Listeria monocytogenes even after incubation of the lactobacilli under simulated gastrointestinal conditions. Displacement of the pathogen by cells released from either of the encapsulation matrices was higher than that by free cells. The safety of L. reuteri was demonstrated in an in vitro invasion assay. Copyright© by the Spanish Society for Microbiology and Institute for Catalan Studies.

A pH-responsive chitosan-b-poly(p-dioxanone) nanocarrier: formation and efficient antitumor drug delivery

International Nuclear Information System (INIS)

Tang Daolu; Song Fei; Chen Cheng; Wang Xiuli; Wang Yuzhong

2013-01-01

Increasing attention has recently been paid to the fabrication of drug delivery systems with excellent cell internalization and intracellular drug release properties. In this study, an amphiphilic block copolymer of chitosan was synthesized for the first time, which can self-assemble into micelles in a neutral aqueous solution but partially disassemble in an acidic endosomal/lysosomal environment. The antitumor drug, camptothecin (CPT), was encapsulated in the cores of the micelles for tumor cell therapy. In vitro drug release studies demonstrated that the micelles presented a much faster release of CPT at pH 5.0 than at pH 7.4. Blank micelles were found to be nontoxic in preliminary in vitro cytotoxicity assays. Cell experiments showed that the CPT-loaded micelles could be effectively internalized by Hela cells and accomplished a potent antitumor cell efficacy, indicating that the chitosan-based micelles might be an attractive new platform for efficient intracellular drug delivery. (paper)

Intranasal delivery of Huperzine A to the brain using lactoferrin-conjugated N-trimethylated chitosan surface-modified PLGA nanoparticles for treatment of Alzheimer’s disease

Directory of Open Access Journals (Sweden)

Meng QQ

2018-02-01

Full Text Available Qingqing Meng,1,* Aiping Wang,1,2,* Hongchen Hua,1 Ying Jiang,1 Yiyun Wang,1 Hongjie Mu,1 Zimei Wu,1 Kaoxiang Sun1 1School of Pharmacy, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, People’s Republic of China; 2State Key Laboratory of Long-Acting and Targeting Drug Delivery System, Shandong Luye Pharmaceutical Co., Ltd, Yantai, People’s Republic of China *These authors contributed equally to this work Background: Safe and effective delivery of therapeutic drugs to the brain is important for successful therapy of Alzheimer’s disease (AD.Purpose: To develop Huperzine A (HupA-loaded, mucoadhesive and targeted polylactide-co-glycoside (PLGA nanoparticles (NPs with surface modification by lactoferrin (Lf-conjugated N-trimethylated chitosan (TMC (HupA Lf-TMC NPs for efficient intranasal delivery of HupA to the brain for AD treatment.Methods: HupA Lf-TMC NPs were prepared using the emulsion–solvent evaporation method and optimized using the Box–Behnken design. The particle size, zeta potential, drug entrapment efficiency, adhesion and in vitro release behavior were investigated. The cellular uptake was investigated by fluorescence microscopy and flow cytometry. MTT assay was used to evaluate the cytotoxicity of the NPs. In vivo imaging system was used to investigate brain targeting effect of NPs after intranasal administration. The biodistribution of Hup-A NPs after intranasal administration was determined by liquid chromatography–tandem mass spectrometry.Results: Optimized HupA Lf-TMC NPs had a particle size of 153.2±13.7 nm, polydispersity index of 0.229±0.078, zeta potential of +35.6±5.2 mV, drug entrapment efficiency of 73.8%±5.7%, and sustained release in vitro over a 48 h period. Adsorption of mucin onto Lf-TMC NPs was 86.9%±1.8%, which was significantly higher than that onto PLGA NPs (32.1%±2.5%. HupA Lf-TMC NPs showed lower toxicity

Cyclodextrin based ternary system of modafinil: Effect of trimethyl chitosan and polyvinylpyrrolidone as complexing agents.

Science.gov (United States)

Patel, Parth; Agrawal, Y K; Sarvaiya, Jayrajsinh

2016-03-01

Modafinil is an approved drug for the treatment of narcolepsy and have a strong market presence in many countries. The drug is widely consumed for off-label uses and currently listed as a restricted drug. Modafinil has very low water solubility. To enhance the aqueous solubility of modafinil by the formation of a ternary complex with Hydroxypropyl-β-cyclodextrin and two hydrophilic polymers was the main objective of the present study. Pyrrolidone (PVP K30) and a water soluble chitosan derivative, trimethyl chitosan (TMC) were studied by solution state and solid state characterization methods for their discriminatory efficiency in solubility enhancement of modafinil. Phase solubility study depicted the highest complexation efficiency (2.22) of cyclodextrin derivative in the presence of TMC compared to the same in the presence of PVP K30 (0.08) and in the absence of any polymer (0.92). FT-IR analysis of binary and ternary complex expressed comparable contribution of both polymers in formation of inclusion complex. The thermal behaviour of binary and ternary complex, involving individual polymers disclosed the influence of TMC on polymorphism of the drug. DSC study revealed efficiency of TMC to prevent conversion of metastable polymorphic form to stable polymorphic form. Ternary complex, involving TMC enhanced water solubility of the drug 1.5 times more compared to the binary complex of the drug whereas PVP K30 reduced the Solubility. Copyright © 2015 Elsevier B.V. All rights reserved.

Lyophilized insulin nanoparticles prepared from quaternized N-aryl derivatives of chitosan as a new strategy for oral delivery of insulin: in vitro, ex vivo and in vivo characterizations.

Science.gov (United States)

Mahjub, Reza; Radmehr, Moojan; Dorkoosh, Farid Abedin; Ostad, Seyed Naser; Rafiee-Tehrani, Morteza

2014-12-01

The purpose of this research was the development, in vitro, ex vivo and in vivo characterization of lyophilized insulin nanoparticles prepared from quaternized N-aryl derivatives of chitosan. Insulin nanoparticles were prepared from methylated N-(4-N,N-dimethylaminobenzyl), methylated N-(4 pyridinyl) and methylated N-(benzyl). Insulin nanoparticles containing non-modified chitosan and also trimethyl chiotsan (TMC) were also prepared as control. The effects of the freeze-drying process on physico-chemical properties of nanoparticles were investigated. The release of insulin from the nanoparticles was studied in vitro. The mechanism of the release of insulin from different types of nanoparticles was determined using curve fitting. The secondary structure of the insulin released from the nanoparticles was analyzed using circular dichroism and the cell cytotoxicity of nanoparticles on a Caco-2 cell line was determined. Ex vivo studies were performed on excised rat jejunum using Frantz diffusion cells. In vivo studies were performed on diabetic male Wistar rats and blood glucose level and insulin serum concentration were determined. Optimized nanoparticles with proper physico-chemical properties were obtained. The lyophilization process was found to cause a decrease in zeta potential and an increase in PdI as well as and a decrease in entrapment efficiency (EE%) and loading efficiency (LE%) but conservation in size of nanoparticles. Atomic force microscopy (AFM) images showed non-aggregated, stable and spherical to sub-spherical nanoparticles. The in vitro release study revealed higher release rates for lyophilized compared to non-lyophilized nanoparticles. Cytotoxicity studies on Caco-2 cells revealed no significant cytotoxicity for prepared nanoparticles after 3-h post-incubation but did show the concentration-dependent cytotoxicity after 24 h. The percentage of cumulative insulin determined from ex vivo studies was significantly higher in nanoparticles prepared

Antidiabetic Activity from Gallic Acid Encapsulated Nanochitosan

Science.gov (United States)

Purbowatiningrum; Ngadiwiyana; Ismiyarto; Fachriyah, E.; Eviana, I.; Eldiana, O.; Amaliyah, N.; Sektianingrum, A. N.

2017-02-01

Diabetes mellitus (DM) has become a health problem in the world because it causes death. One of the phenolic compounds that have antidiabetic activity is gallic acid. However, the use of this compound still provides unsatisfactory results due to its degradation during the absorption process. The solution offered to solve the problem is by encapsulated it within chitosan nanoparticles that serve to protect the bioactive compound from degradation, increases of solubility and delivery of a bioactive compound to the target site by using freeze-drying technique. The result of chitosan nanoparticle’s Scanning Electron Microscopy (SEM) showed that chitosan nanoparticle’s size is uniform and it is smaller than chitosan. The value of encapsulation efficiency (EE) of gallic acid which encapsulated within chitosan nanoparticles is about 50.76%. Inhibition test result showed that gallic acid-chitosan nanoparticles at 50 ppm could inhibite α-glucosidase activity in 28.87% with 54.94 in IC50. So it can be concluded that gallic acid can be encapsulated in nanoparticles of chitosan and proved that it could inhibit α-glucosidase.

Optimizing indomethacin-loaded chitosan nanoparticle size, encapsulation, and release using Box-Behnken experimental design.

Science.gov (United States)

Abul Kalam, Mohd; Khan, Abdul Arif; Khan, Shahanavaj; Almalik, Abdulaziz; Alshamsan, Aws

2016-06-01

Indomethacin chitosan nanoparticles (NPs) were developed by ionotropic gelation and optimized by concentrations of chitosan and tripolyphosphate (TPP) and stirring time by 3-factor 3-level Box-Behnken experimental design. Optimal concentration of chitosan (A) and TPP (B) were found 0.6mg/mL and 0.4mg/mL with 120min stirring time (C), with applied constraints of minimizing particle size (R1) and maximizing encapsulation efficiency (R2) and drug release (R3). Based on obtained 3D response surface plots, factors A, B and C were found to give synergistic effect on R1, while factor A has a negative impact on R2 and R3. Interaction of AB was negative on R1 and R2 but positive on R3. The factor AC was having synergistic effect on R1 and on R3, while the same combination had a negative effect on R2. The interaction BC was positive on the all responses. NPs were found in the size range of 321-675nm with zeta potentials (+25 to +32mV) after 6 months storage. Encapsulation, drug release, and content were in the range of 56-79%, 48-73% and 98-99%, respectively. In vitro drug release data were fitted in different kinetic models and pattern of drug release followed Higuchi-matrix type. Copyright © 2016 Elsevier B.V. All rights reserved.

Encapsulation of rat bone marrow stromal cells using a poly-ion complex gel of chitosan and succinylated poly(Pro-Hyp-Gly).

Science.gov (United States)

Kusumastuti, Yuni; Shibasaki, Yoshiaki; Hirohara, Shiho; Kobayashi, Mime; Terada, Kayo; Ando, Tsuyoshi; Tanihara, Masao

2017-03-01

Encapsulation of stem cells into a three-dimensional (3D) scaffold is necessary to achieve tissue regeneration. Prefabricated 3D scaffolds, such as fibres or porous sponges, have limitations regarding homogeneous cell distribution. Hydrogels that can encapsulate cells such as animal-derived collagen gels need adjustment of the pH and/or temperature upon cell mixing. In this report, we fabricated a poly-ion complex (PIC) hydrogel of chitosan and succinylated poly(Pro-Hyp-Gly) and assessed its effect on cell viability after encapsulation of rat bone marrow stromal cells. PIC hydrogels were obtained successfully with a concentration of each precursor as low as 3.0-3.8 mg/ml. The maximum gelation and swelling ratios were achieved with an equal molar ratio (1:1) of anionic and cationic groups. Using chitosan acetate as a cationic precursor produced a PIC hydrogel with both a significantly greater gelation ratio and a better swelling ratio than chitosan chloride. Ammonium succinylated poly(Pro-Hyp-Gly) as an anionic precursor gave similar gelation and swelling ratios to those of sodium succinylated poly(Pro-Hyp-Gly). Cell encapsulation was also achieved successfully by mixing rat bone marrow stromal cells with the PIC hydrogel simultaneously during its formation. The PIC hydrogel was maintained in the culture medium for 7 days at 37°C and the encapsulated cells survived and proliferated in it. Although it is necessary to improve its functionality, this PIC hydrogel has the potential to act as a 3D scaffold for cell encapsulation and tissue regeneration. Copyright © 2015 John Wiley & Sons, Ltd. Copyright © 2015 John Wiley & Sons, Ltd.

New type of chitosan/2-hydroxypropyl-β-cyclodextrin composite membrane for gallic acid encapsulation and controlled release.

Science.gov (United States)

Paun, Gabriela; Neagu, Elena; Tache, Andreia; Radu, G L

2014-01-01

A new type of chitosan/2-hydroxypropyl-β-cyclodextrin composite membrane have been developed for the encapsulation and controlled release of gallic acid. The morphology of the composite membrane was investigated by infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM), whereas swelling gallic acid and release properties were investigated by UV-visible spectroscopy. The release behavior with pH changes was also explored. The composite membrane based on chitosan/2-hydroxypropyl-β-cyclodextrin with gallic acid included showed improved antioxidant capacities compared to plain chitosan membrane. The information obtained in this study will facilitate the design and preparation of composite membrane based on chitosan and could open a wide range of applications, particularly its use as an antioxidant in food, food packaging, biomedical (biodegradable soft porous scaffolds for enhance the surrounding tissue regeneration), pharmaceutical and cosmetics industries.

Cytotoxicity and metal ions removal using antibacterial biodegradable hydrogels based on N-quaternized chitosan/poly(acrylic acid).

Science.gov (United States)

Mohamed, Riham R; Elella, Mahmoud H Abu; Sabaa, Magdy W

2017-05-01

Physically crosslinked hydrogels resulted from interaction between N,N,N-trimethyl chitosan chloride (N-Quaternized Chitosan) (NQC) and poly(acrylic acid) (PAA) were synthesized in different weight ratios (3:1), (1:1) and (1:3) taking the following codes Q3P1, Q1P1 and Q1P3, respectively. Characterization of the mentioned hydrogels was done using several analysis tools including; FTIR, XRD, SEM, TGA, biodegradation in simulated body fluid (SBF) and cytotoxicity against HepG-2 liver cancer cells. FTIR results proved that the prepared hydrogels were formed via electrostatic and H-bonding interactions, while XRD patterns proved that the prepared hydrogels -irrespective to their ratios- were more crystalline than both matrices NQC and PAA. TGA results, on the other hand, revealed that Q1P3 hydrogel was the most thermally stable compared to the other two hydrogels (Q3P1 and Q1P1). Biodegradation tests in SBF proved that these hydrogels were more biodegradable than the native chitosan. Examination of the prepared hydrogels for their potency in heavy metal ions removal revealed that they adsorbed Fe (III) and Cd (II) ions more than chitosan, while they adsorbed Cr (III), Ni (II) and Cu (II) ions less than chitosan. Moreover, testing the prepared hydrogels as antibacterial agents towards several Gram positive and Gram negative bacteria revealed their higher antibacterial activity as compared with NQC when used alone. Evaluating the cytotoxic effect of these hydrogels on an in vitro human liver cancer cell model (HepG-2) showed their good cytotoxic activity towards HepG-2. Moreover, the inhibition rate increased with increasing the hydrogels concentration in the culture medium. Copyright © 2017 Elsevier B.V. All rights reserved.

Proteomic analysis of the increased stress tolerance of saccharomyces cerevisiae encapsulated in liquid core alginate-chitosan capsules.

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Johan O Westman

Full Text Available Saccharomyces cerevisiae CBS8066 encapsulated in semi-permeable alginate or alginate-chitosan liquid core capsules have been shown to have an enhanced tolerance towards complex dilute-acid lignocellulose hydrolysates and the lignocellulose-derived inhibitor furfural, as well as towards high temperatures. The underlying molecular reasons for these effects have however not been elucidated. In this study we have investigated the response of the encapsulation on the proteome level in the yeast cells, in comparison with cells grown freely in suspension under otherwise similar conditions. The proteomic analysis was performed on whole cell protein extracts using nLC-MS/MS with TMT® labelling and 2-D DIGE. 842 and 52 proteins were identified using each method, respectively. The abundances of 213 proteins were significantly different between encapsulated and suspended cells, with good correlation between the fold change ratios obtained by the two methods for proteins identified in both. Encapsulation of the yeast caused an up-regulation of glucose-repressed proteins and of both general and starvation-specific stress responses, such as the trehalose biosynthesis pathway, and down-regulation of proteins linked to growth and protein synthesis. The encapsulation leads to a lack of nutrients for cells close to the core of the capsule due to mass transfer limitations. The triggering of the stress response may be beneficial for the cells in certain conditions, for example leading to the increased tolerance towards high temperatures and certain inhibitors.

High molecular weight chitosan derivative polymeric micelles encapsulating superparamagnetic iron oxide for tumor-targeted magnetic resonance imaging

Directory of Open Access Journals (Sweden)

Xiao Y

2015-02-01

Full Text Available Yunbin Xiao,1,* Zuan Tao Lin,2,* Yanmei Chen,1 He Wang,1 Ya Li Deng,2 D Elizabeth Le,3 Jianguo Bin,1 Meiyu Li,1 Yulin Liao,1 Yili Liu,1 Gangbiao Jiang,2 Jianping Bin1 1State Key Laboratory of Organ Failure Research, Division of Cardiology, Nanfang Hospital, Southern Medical University, Guangzhou, People’s Republic of China; 2Department of Pharmaceutical Engineering, South China Agricultural University, Guangzhou, People’s Republic of China; 3Cardiovascular Division, Oregon Health and Science University, Portland, OR, USA *These authors contributed equally to this work Abstract: Magnetic resonance imaging (MRI contrast agents based on chitosan derivatives have great potential for diagnosing diseases. However, stable tumor-targeted MRI contrast agents using micelles prepared from high molecular weight chitosan derivatives are seldom reported. In this study, we developed a novel tumor-targeted MRI vehicle via superparamagnetic iron oxide nanoparticles (SPIONs encapsulated in self-aggregating polymeric folate-conjugated N-palmitoyl chitosan (FAPLCS micelles. The tumor-targeting ability of FAPLCS/SPIONs was demonstrated in vitro and in vivo. The results of dynamic light scattering experiments showed that the micelles had a relatively narrow size distribution (136.60±3.90 nm and excellent stability. FAPLCS/SPIONs showed low cytotoxicity and excellent biocompatibility in cellular toxicity tests. Both in vitro and in vivo studies demonstrated that FAPLCS/SPIONs bound specifically to folate receptor-positive HeLa cells, and that FAPLCS/SPIONs accumulated predominantly in established HeLa-derived tumors in mice. The signal intensities of T2-weighted images in established HeLa-derived tumors were reduced dramatically after intravenous micelle administration. Our study indicates that FAPLCS/SPION micelles can potentially serve as safe and effective MRI contrast agents for detecting tumors that overexpress folate receptors. Keywords: superparamagnetic

Encapsulation of a bioactive steroid in a polymer matrix (micro-encapsulation of DI-31 in chitosan by spray drying for various purposes)

OpenAIRE

Collado , A ,; Hernández , G.; Morejón , V.; Coll , F.; Peniche , C.

2017-01-01

International audience; DI-31 is a synthetic analog of brasinosteroids (ABR), the active ingredient (PA) of Biobras, a plant growth stimulant, which has shown positive impact on Cuban agriculture, especially in rice cultivation. However, it has the drawback of having low solubility in water and being rapidly metabolized by the plants. An alternative to overcome these limitations is its micro-encapsulation in a polymer matrix. Chitosan (CHI) has been investigated as an excellent candidate for ...

Preparation of collagen peptide functionalized chitosan nanoparticles by ionic gelation method: An effective carrier system for encapsulation and release of doxorubicin for cancer drug delivery

Energy Technology Data Exchange (ETDEWEB)

Anandhakumar, S., E-mail: rsanandhakumar@gmail.com [SRM Research Institute, SRM University, Kattankulathur, Chennai 603203 (India); Krishnamoorthy, G.; Ramkumar, K.M. [SRM Research Institute, SRM University, Kattankulathur, Chennai 603203 (India); Raichur, A.M. [Department of Materials Engineering, Indian Institute of Science, Bangalore 560012 (India)

2017-01-01

In recent years, nanoparticles (NPs) based on biopolymers or peptides are gaining popularity for the encapsulation and release of drug molecules, especially for cancer therapy, due to their ability for targeted and controlled release. The use of collagen peptide (CP) for the preparation of chitosan (CN) NPs is especially interesting as it results in NPs that are stable under physiological conditions. In this work, mono-dispersed pH responsive CPCN NPs of about 100 nm were prepared via ionic gelation method by simple and mild co-precipitation of CN and CP. Investigation of NPs with Fourier transform infra-red (FTIR) spectroscopy and dynamic light scattering (DLS) measurements reveals that hydrogen bonding and electrostatic interactions are believed to be major driving forces for NP formation and drug encapsulation, respectively. Scanning electron microscopic (SEM) investigations show that hard and fine CPCN NPs transform to soft and bigger gel like particles as a function of collagen concentration. The unique “polymeric gel” structure of NPs showed high encapsulation efficiency towards doxorubicin hydrochloride (DOX) as well as pH controlled release. Anti-proliferative and cell viability analysis revealed that DOX loaded NPs showed excellent anti-proliferative characteristics against HeLa cells with favorable biocompatibility against normal cells. Such NPs have high potential for use as smart drug delivery carriers in advanced cancer therapy. - Highlights: • Preparation of collagen peptide functionalized chitosan nanoparticles • Hydrogen bonding plays a key role in particle formation. • Electrostatic interaction plays a key role in drug encapsulation. • Functionalized chitosan particles are more stable than chitosan NPs.

Extraction and encapsulation of prodigiosin in chitosan microspheres for targeted drug delivery

Energy Technology Data Exchange (ETDEWEB)

Dozie-Nwachukwu, S.O. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Biotechnology and Genetic Engineering Advanced Laboratory, Sheda Science and Technology Complex (SHESTCO), P.M.B 186, Garki, Abuja, Federal Capital Territory (Nigeria); Danyuo, Y. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Materials Science and Engineering, Kwara State University, Malete (Nigeria); Obayemi, J.D. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Odusanya, O.S. [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Biotechnology and Genetic Engineering Advanced Laboratory, Sheda Science and Technology Complex (SHESTCO), P.M.B 186, Garki, Abuja, Federal Capital Territory (Nigeria); Malatesta, K. [Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Soboyejo, W.O., E-mail: soboyejo@princeton.edu [Department of Materials Science and Engineering, African University of Science and Technology (AUST) Abuja, Federal Capital Territory (Nigeria); Department of Mechanical and Aerospace Engineering, Princeton University, Princeton, NJ 08544 (United States); Princeton Institute of Science and Technology of Materials (PRISM), Bowen Hall, 70 Prospect Street, Princeton, NJ 08544 (United States)

2017-02-01

The encapsulation of drugs in polymeric materials has brought opportunities to the targeted delivery of chemotherapeutic agents. These polymeric delivery systems are capable of maximizing the therapeutic activity, as well as reducing the side effects of anti-cancer agents. Prodigiosin, a secondary metabolite extracted from the bacteria, Serratia marcescens, exhibits anti-cancer properties. Prodigiosin-loaded chitosan microspheres were prepared via water-in-oil (w/o) emulsion technique, using glutaraldehyde as a cross-linker. The morphologies of the microspheres were studied using scanning electron microscopy. The average sizes of the microspheres were between 40 μm and 60 μm, while the percentage yields ranged from 42 ± 2% to 55.5 ± 3%. The resulting encapsulation efficiencies were between 66.7 ± 3% and 90 ± 4%. The in-vitro drug release from the microspheres was characterized by zeroth order, first order and Higuchi and Korsmeyer-Peppas models. - Highlights: • Prodigiosin of ~ 92.8% purity was extracted from locally isolated Serratia marcescens. • This approach reduces the cost and ensure availability of drugs for cancer treatment. • High encapsulation efficiency which increased with increasing drug:polymer ratio • The percentage yield was generally poor due to the recovery process. • Prodigiosin greatly reduced the viability of the breast cancer cell line (MDA-MB-231).

Extraction and encapsulation of prodigiosin in chitosan microspheres for targeted drug delivery

International Nuclear Information System (INIS)

Dozie-Nwachukwu, S.O.; Danyuo, Y.; Obayemi, J.D.; Odusanya, O.S.; Malatesta, K.; Soboyejo, W.O.

2017-01-01

The encapsulation of drugs in polymeric materials has brought opportunities to the targeted delivery of chemotherapeutic agents. These polymeric delivery systems are capable of maximizing the therapeutic activity, as well as reducing the side effects of anti-cancer agents. Prodigiosin, a secondary metabolite extracted from the bacteria, Serratia marcescens, exhibits anti-cancer properties. Prodigiosin-loaded chitosan microspheres were prepared via water-in-oil (w/o) emulsion technique, using glutaraldehyde as a cross-linker. The morphologies of the microspheres were studied using scanning electron microscopy. The average sizes of the microspheres were between 40 μm and 60 μm, while the percentage yields ranged from 42 ± 2% to 55.5 ± 3%. The resulting encapsulation efficiencies were between 66.7 ± 3% and 90 ± 4%. The in-vitro drug release from the microspheres was characterized by zeroth order, first order and Higuchi and Korsmeyer-Peppas models. - Highlights: • Prodigiosin of ~ 92.8% purity was extracted from locally isolated Serratia marcescens. • This approach reduces the cost and ensure availability of drugs for cancer treatment. • High encapsulation efficiency which increased with increasing drug:polymer ratio • The percentage yield was generally poor due to the recovery process. • Prodigiosin greatly reduced the viability of the breast cancer cell line (MDA-MB-231).

Interaction of PLGA and trimethyl chitosan modified PLGA nanoparticles with mixed anionic/zwitterionic phospholipid bilayers studied using molecular dynamics simulations

Science.gov (United States)

Novak, Brian; Astete, Carlos; Sabliov, Cristina; Moldovan, Dorel

2012-02-01

Poly(lactic-co-glycolic acid) (PLGA) is a biodegradable polymer. Nanoparticles of PLGA are commonly used for drug delivery applications. The interaction of the nanoparticles with the cell membrane may influence the rate of their uptake by cells. Both PLGA and cell membranes are negatively charged, so adding positively charged polymers such as trimethyl chitosan (TMC) which adheres to the PLGA particles improves their cellular uptake. The interaction of 3 nm PLGA and TMC-modified-PLGA nanoparticles with lipid bilayers composed of mixtures of phosphatidylcholine and phosphatidylserine lipids was studied using molecular dynamics simulations. The free energy profiles as function of nanoparticles position along the normal direction to the bilayers were calculated, the distribution of phosphatidylserine lipids as a function of distance of the particle from the bilayer was calculated, and the time scale for particle motion in the directions parallel to the bilayer surface was estimated.

Recent advances in chitosan-based nanoparticulate pulmonary drug delivery

Science.gov (United States)

Islam, Nazrul; Ferro, Vito

2016-07-01

The advent of biodegradable polymer-encapsulated drug nanoparticles has made the pulmonary route of administration an exciting area of drug delivery research. Chitosan, a natural biodegradable and biocompatible polysaccharide has received enormous attention as a carrier for drug delivery. Recently, nanoparticles of chitosan (CS) and its synthetic derivatives have been investigated for the encapsulation and delivery of many drugs with improved targeting and controlled release. Herein, recent advances in the preparation and use of micro-/nanoparticles of chitosan and its derivatives for pulmonary delivery of various therapeutic agents (drugs, genes, vaccines) are reviewed. Although chitosan has wide applications in terms of formulations and routes of drug delivery, this review is focused on pulmonary delivery of drug-encapsulated nanoparticles of chitosan and its derivatives. In addition, the controversial toxicological effects of chitosan nanoparticles for lung delivery will also be discussed.

Synthesis of N-oleyl O-sulfate chitosan from methyl oleate with O-sulfate chitosan as edible film material

Science.gov (United States)

Daniel; Sihaloho, O.; Saleh, C.; Magdaleni, A. R.

2018-04-01

The research on the synthesis of N-oleyl O-sulfate chitosan through sulfonation reaction on chitosan with ammonium sulfate and followed by amidation reaction using methyl oleate has been done. In this study, chitosan was chemically modified into N-oleyl O-sulfatechitosan as an edible film making material. N-oleyl O-sulfate chitosan was synthesized by reaction between methyl oleate and O-sulfate chitosan. Wherein the depleted chitosan of O-sulfate chitosan into O-sulfate chitosan was obtained by reaction of sulfonation between ammonium sulfate and chitosan aldimine. While chitosan aldimine was obtained through reaction between chitosan with acetaldehyde. The structure of N-oleyl O-sulfate chitosan was characterized by FT-IR analysis which showed vibration uptake of C-H sp3 group, S=O group, and carbonyl group C=O of the ester. The resulting of N-oleyl O-sulfate chitosan yielded a percentage of 93.52%. Hydrophilic-Lipophilic Balance (HLB) test results gave a value of 6.68. In the toxicity test results of N-oleyl O-sulfate chitosan obtained LC50 value of 3738.4732 ppm. In WVTR (Water Vapor Transmission Rate) test results for chitosan film was 407.625 gram/m2/24 hours and N-oleylO-sulfate chitosan film was 201.125 gram/m2/24 hours.

40 CFR 721.7270 - 1-propanaminium, 3-amino-, N,N,N-trimethyl-N-soya acyl derivs., chloride.

Science.gov (United States)

2010-07-01

...-trimethyl-N-soya acyl derivs., chloride. 721.7270 Section 721.7270 Protection of Environment ENVIRONMENTAL...-soya acyl derivs., chloride. (a) Chemical substance and significant new uses subject to reporting. (1...., chloride (PMN P-01-646; CAS No. 391232-99-8) is subject to reporting under this section for the significant...

Development of chitosan/montmorillonite nanocomposites with encapsulated α-tocopherol.

Science.gov (United States)

Dias, Marali Vilela; Machado Azevedo, Viviane; Borges, Soraia Vilela; Soares, Nilda de Fátima Ferreira; de Barros Fernandes, Regiane Victória; Marques, João José; Medeiros, Eber Antonio Alves

2014-12-15

Nanocomposites of chitosan (CS) were developed and characterized in a full factorial design with varying levels of montmorillonite (MMTNa) and encapsulated tocopherol (toc-encap). The structural properties (XRD, FTIR), morphology (TEM), hygroscopic properties (water vapour permeability, hydrophobicity, sorption isotherms) and optical properties (haze, CIELab parameters) of the resulting materials were evaluated. Toc-encap contents up to 10% influenced the intercalation of MMTNa in the CS matrix, resulting in films with reduced water vapour permeability (3.48×10(-11)(g/msPa)), increased hydrophobicity (ΔGHydroph |7.93-59.54|mJm(-2)) and lower equilibrium moisture content (EMC), thus showing potential for active food packaging materials. At levels above 10%, toc-encap agglomerates occurred, which deteriorated the properties of the resulting films, as shown with the TEM. As the toc-encap content increased, the films became slightly more yellow, more irregular and less transparent, with a higher haze index. Copyright © 2014 Elsevier Ltd. All rights reserved.

Effects of pore forming agents of potassium bicarbonate and drug loading method against dissolution mechanisms of amoxicillin drugs encapsulated in hydrogel full-Ipn chitosan-poly(N-vinylcaprolactam) as a floating drug delivery system

Science.gov (United States)

Aini, Nurul; Rahayu, Dyah Utami Cahyaning; Budianto, Emil

2018-04-01

The limitation of amoxicillin trihydrate in the treatment of H. pylori bacteria is relatively short retention time in the stomach. The FDDS (Floating Drug Delivery System) amoxicillin trihydrate into a chitosan-poly(N-vinylcaprolactam) full-Ipn hydrogel matrix using a pore-forming agent KHCO3 is expected to overcome these limitations. The pore-forming agent to be used is 15% KHCO3 compound. Chemical kinetics approach is performed to determine the dissolution mechanism of amoxicillin trihydrate from K-PNVCL hydrogel in vitro on gastric pH and characterization using SEM performed to confirm the dissolution mechanism. Hydrogels with the addition of pore-forming agents will be loading in situ loading and post loading. Fourier Transform Infra Red (FTIR) spectroscopy was used to characterize K-PNVCL and UV-Vis hydrogels used to calculate the efficiency of encapsulation and drug dissolution rate in K-PNVCL hydrogel. Hydrogel K-PNVCL / KHCO3 that encapsulated by in situ loading method resulted in an encapsulation efficiency of 93.5% and dissolution of 93.4%. While the Hydrogel K-PNVCL / KHCO3 which is drug encapsulation resulted in an encapsulation efficiency of 87.2% with dissolution of 81.5%. Chemical kinetics approach to in situ encapsulation of loading and post loading shows the dissolution mechanism occurring in the K-PNVCL / KHCO3 hydrogel matrix occurs by diffusion. Observation using optical microscope and SEM showed the mechanism of drug dissolution in Hydrogel K-PNVCL occurred by diffusion.

Quaternized Chitosan-Capped Mesoporous Silica Nanoparticles as Nanocarriers for Controlled Pesticide Release.

Science.gov (United States)

Cao, Lidong; Zhang, Huirong; Cao, Chong; Zhang, Jiakun; Li, Fengmin; Huang, Qiliang

2016-06-28

Nanotechnology-based pesticide formulations would ensure effective utilization of agricultural inputs. In the present work, mesoporous silica nanoparticles (MSNs) with particle diameters of ~110 nm and pore sizes of ~3.7 nm were synthesized via a liquid crystal templating mechanism. A water-soluble chitosan (CS) derivative ( N -(2-hydroxyl)propyl-3-trimethyl ammonium CS chloride, HTCC) was successfully capped on the surface of pyraclostrobin-loaded MSNs. The physicochemical and structural analyses showed that the electrostatic interactions and hydrogen bonding were the major forces responsible for the formation of HTCC-capped MSNs. HTCC coating greatly improved the loading efficiency (LC) (to 40.3%) compared to using bare MSNs as a single encapsulant (26.7%). The microstructure of the nanoparticles was revealed by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The pyraclostrobin-loaded nanoparticles showed an initial burst and subsequent sustained release behavior. HTCC-capped MSNs released faster than bare MSNs in the initial stage. Pyraclostrobin-loaded HTCC-capped MSNs with half doses of pyraclostrobin technical demonstrated almost the same fungicidal activity against Phomopsis asparagi (Sacc.), which obviously reduced the applied pesticide and enhanced the utilization efficiency. Therefore, HTCC-decorated MSNs demonstrated great potential as nanocarriers in agrochemical applications.

Antidiabetic activity from cinnamaldydhe encapsulated by nanochitosan

Science.gov (United States)

Purbowatingrum; Ngadiwiyana; Fachriyah, E.; Ismiyarto; Ariestiani, B.; Khikmah

2018-04-01

Diabetes mellitus (DM) is a disease characterized by chronic hyperglycemia and metabolic disorders of carbohydrates, proteins, and fats due to reduced function of insulin. Treatment of diabetes can be done by insulin therapy or hypoglycemic drugs. Hypoglycemic drugs usually contain compounds that can inhibit the action of α-glucosidase enzymes that play a role in breaking carbohydrates into blood sugar. Cinnamaldehyde has α-glucosidase inhibit activity because it has a functional group of alkene that is conjugated with a benzene ring and a carbonyl group. However, the use of this compound still provides unsatisfactory results due to its degradation during the absorption process. The solution offered to solve the problem is by encapsulated it within chitosan nanoparticles that serve to protect the bioactive compound from degradation, increases of solubility and delivery of a bioactive compound to the target site by using freeze-drying technique. The value of encapsulation efficiency (EE) of cinnamaldyhde which encapsulated within chitosan nanoparticles is about 74%. Inhibition test result showed that cinnamaldehyde-chitosan nanoparticles at 100 ppm could inhibit α-glucosidase activity in 23.9% with 134,13 in IC50. So it can be concluded that cinnamaldehyde can be encapsulated in nanoparticles of chitosan and proved that it could inhibit α-glucosidase.

Preparation of an Environmentally Friendly Formulation of the Insecticide Nicotine Hydrochloride through Encapsulation in Chitosan/Tripolyphosphate Nanoparticles.

Science.gov (United States)

Yang, Ying; Cheng, Jiagao; Garamus, Vasil M; Li, Na; Zou, Aihua

2018-02-07

Insecticide nicotine hydrochloride (NCT) was formulated as nanoparticles composed of chitosan (CS) and sodium tripolyphosphate (TPP) to undermine its adverse impacts on human health and reinforce its physicochemical stability. The study investigated the preparation and characterization of chitosan/tripolyphosphate nanoparticles (CS/TPP NPs) with good encapsulation efficiency (55%), uniform morphology, and physicochemical stability (45 days) through dynamic light scattering (DLS), transmission electron microscopy (TEM), and small-angle X-ray scattering (SAXS) measurements. A bioassay against Musca domestica NCT CS/TPP NPs exhibited good bioactivity and thermal stability. The effect of the monovalent salt (NaCl) on manipulating the formation and size distribution of ionically cross-linked nanoparticles was demonstrated as well. The formulation of NCT CS/TPP NPs could be a utility candidate in public health and agriculture.

Effect of drug loading method against the dissolution mechanism of encapsulated amoxicillin trihidrate drug in matrix of semi-IPN chitosan-poly (N-vinyl pyrrolidone) hydrogel with pore forming agent CaCO3

Science.gov (United States)

Nurjannah, Yanah; Budianto, Emil

2018-04-01

Heliobacter pylori (H.pylori) is a type of bacteria that causes inflammation in the lining of the stomach. The treatment of the bacterial infection by using conventional medicine which is amoxicillin trihidrate has a very short retention time in the stomach which is about 1-1,5 hours. Floating drug delivery system is expected to have a long retention time in the stomach so the efficiency of drug can be achieved. In this study, has been synthesized matrix of semi-IPN chitosan-Poly(N-vinil pyrrolidone) hydrogel with a pore-forming agent of CaCO3 under optimum conditions. Amoxicillin is encapsulated in a matrix hydrogel to be applied as a floating drug delivery system by in situ loading and post loading methods. The encapsulation efficiency and dissolution of in situ loading and post loading hydrogels are performed in vitro on gastric pH. In situ loading hydrogel shows higer percentage of encapsulation efficiency and dissolution compared to post loading hydrogel. The encapsulation efficiency of in situ and post loading hydrogels were 92,1% and 89,4%, respectively. The aim of drug dissolution by mathematical equation model is to know kinetics and the mecanism of dissolution. The kinetics release of in situ hydrogel tends to follow first order kinetics, while the post loading hydrogel follow the Higuchi model. The dissolution mecanism of hydrogels is erosion.

Synthesis of camptothecin-loaded gold nanomaterials

International Nuclear Information System (INIS)

Xing Zhimin; Liu Zhiguo; Zu Yuangang; Fu Yujie; Zhao Chunjian; Zhao Xiuhua; Meng Ronghua; Tan Shengnan

2010-01-01

Camptothecin-loaded gold nanomaterials have been synthesized by the sodium borohydride reduction method under a strong basic condition. The obtained gold nanomaterials have been characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM) and UV-vis absorption spectroscopy. The camptothecin-loaded gold colloidal solution was very stable and can be stored for more than two months at room temperature without obvious changes. The color of the colloidal solution can change from wine red to purple and blue during the acidifying process. It was revealed that the release of camptothecin and the aggregation of gold nanoparticles can be controlled by tuning the solution pH. The present study implied that the gold nanomaterials can be used as the potential carrier for CPT delivery.

Synthesis of camptothecin-loaded gold nanomaterials

Energy Technology Data Exchange (ETDEWEB)

Xing Zhimin [Key Laboratory of Forest Plant Ecology of Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Liu Zhiguo, E-mail: zguoliu@yahoo.com.cn [Key Laboratory of Forest Plant Ecology of Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Zu Yuangang, E-mail: nefunano@yahoo.com.cn [Key Laboratory of Forest Plant Ecology of Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Fu Yujie; Zhao Chunjian; Zhao Xiuhua; Meng Ronghua; Tan Shengnan [Key Laboratory of Forest Plant Ecology of Ministry of Education, Northeast Forestry University, Harbin 150040 (China); Engineering Research Center of Forest Bio-preparation, Ministry of Education, Northeast Forestry University, Harbin 150040 (China)

2010-04-01

Camptothecin-loaded gold nanomaterials have been synthesized by the sodium borohydride reduction method under a strong basic condition. The obtained gold nanomaterials have been characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM) and UV-vis absorption spectroscopy. The camptothecin-loaded gold colloidal solution was very stable and can be stored for more than two months at room temperature without obvious changes. The color of the colloidal solution can change from wine red to purple and blue during the acidifying process. It was revealed that the release of camptothecin and the aggregation of gold nanoparticles can be controlled by tuning the solution pH. The present study implied that the gold nanomaterials can be used as the potential carrier for CPT delivery.

Chitosan-thioglycolic acid as a versatile antimicrobial agent.

Science.gov (United States)

Geisberger, Georg; Gyenge, Emina Besic; Hinger, Doris; Käch, Andres; Maake, Caroline; Patzke, Greta R

2013-04-08

As functionalized chitosans hold great potential for the development of effective and broad-spectrum antibiotics, representative chitosan derivatives were tested for antimicrobial activity in neutral media: trimethyl chitosan (TMC), carboxy-methyl chitosan (CMC), and chitosan-thioglycolic acid (TGA; medium molecular weight: MMW-TGA; low molecular weight: LMW-TGA). Colony forming assays indicated that LMW-TGA displayed superior antimicrobial activity over the other derivatives tested: a 30 min incubation killed 100% Streptococcus sobrinus (Gram-positive bacteria) and reduced colony counts by 99.99% in Neisseria subflava (Gram-negative bacteria) and 99.97% in Candida albicans (fungi). To elucidate LMW-TGA effects at the cellular level, microscopic studies were performed. Use of fluorescein isothiocyanate (FITC)-labeled chitosan derivates in confocal microscopy showed that LMW-TGA attaches to microbial cell walls, while transmission electron microscopy indicated that this derivative severely affects cell wall integrity and intracellular ultrastructure in all species tested. We therefore propose LMW-TGA as a promising and effective broad-band antimicrobial compound.

Microencapsulation of Lactobacillus Acidophilus by Xanthan-Chitosan and Its Stability in Yoghurt

Directory of Open Access Journals (Sweden)

Guowei Shu

2017-12-01

Full Text Available Microencapsulations of Lactobacillus acidophilus in xanthan-chitosan (XC and xanthan-chitosan-xanthan (XCX polyelectrolyte complex (PEC gels were prepared in this study. The process of encapsulation was optimized with the aid of response surface methodology (RSM. The optimum condition was chitosan of 0.68%, xanthan of 0.76%, xanthan-L. acidophilus mixture (XLM/chitosan of 1:2.56 corresponding to a high viable count (1.31 ± 0.14 × 1010 CFU·g−1, and encapsulation yield 86 ± 0.99%, respectively. Additionally, the application of a new encapsulation system (XC and XCX in yoghurt achieved great success in bacterial survival during the storage of 21 d at 4 °C and 25 °C, respectively. Specially, pH and acidity in yogurt were significantly influenced by the new encapsulation system in comparison to free suspension during 21 d storage. Our study provided a potential encapsulation system for probiotic application in dairy product which paving a new way for functional food development.

Chitosan and Its Derivatives for Application in Mucoadhesive Drug Delivery Systems

Directory of Open Access Journals (Sweden)

Twana Mohammed M. Ways

2018-03-01

Full Text Available Mucoadhesive drug delivery systems are desirable as they can increase the residence time of drugs at the site of absorption/action, provide sustained drug release and minimize the degradation of drugs in various body sites. Chitosan is a cationic polysaccharide that exhibits mucoadhesive properties and it has been widely used in the design of mucoadhesive dosage forms. However, its limited mucoadhesive strength and limited water-solubility at neutral and basic pHs are considered as two major drawbacks of its use. Chemical modification of chitosan has been exploited to tackle these two issues. In this review, we highlight the up-to-date studies involving the synthetic approaches and description of mucoadhesive properties of chitosan and chitosan derivatives. These derivatives include trimethyl chitosan, carboxymethyl chitosan, thiolated chitosan, chitosan-enzyme inhibitors, chitosan-ethylenediaminetetraacetic acid (chitosan-EDTA, half-acetylated chitosan, acrylated chitosan, glycol chitosan, chitosan-catechol, methyl pyrrolidinone-chitosan, cyclodextrin-chitosan and oleoyl-quaternised chitosan. We have particularly focused on the effect of chemical derivatization on the mucoadhesive properties of chitosan. Additionally, other important properties including water-solubility, stability, controlled release, permeation enhancing effect, and in vivo performance are also described.

IGF-1 release kinetics from chitosan microparticles fabricated using environmentally benign conditions

Energy Technology Data Exchange (ETDEWEB)

Mantripragada, Venkata P. [Biomedical Engineering Program, The University of Toledo, Toledo, OH 43614-5807 (United States); Jayasuriya, Ambalangodage C., E-mail: a.jayasuriya@utoledo.edu [Biomedical Engineering Program, The University of Toledo, Toledo, OH 43614-5807 (United States); Department of Orthopaedic Surgery, The University of Toledo, Toledo, OH 43614-5807 (United States)

2014-09-01

The main objective of this study is to maximize growth factor encapsulation efficiency into microparticles. The novelty of this study is to maximize the encapsulated growth factors into microparticles by minimizing the use of organic solvents and using relatively low temperatures. The microparticles were fabricated using chitosan biopolymer as a base polymer and cross-linked with tripolyphosphate (TPP). Insulin like-growth factor-1 (IGF-1) was encapsulated into microparticles to study release kinetics and bioactivity. In order to authenticate the harms of using organic solvents like hexane and acetone during microparticle preparation, IGF-1 encapsulated microparticles prepared by the emulsification and coacervation methods were compared. The microparticles fabricated by emulsification method have shown a significant decrease (p < 0.05) in IGF-1 encapsulation efficiency, and cumulative release during the two-week period. The biocompatibility of chitosan microparticles and the bioactivity of the released IGF-1 were determined in vitro by live/dead viability assay. The mineralization data observed with von Kossa assay, was supported by mRNA expression levels of osterix and runx2, which are transcription factors necessary for osteoblasts differentiation. Real time RT-PCR data showed an increased expression of runx2 and a decreased expression of osterix over time, indicating differentiating osteoblasts. Chitosan microparticles prepared in optimum environmental conditions are a promising controlled delivery system for cells to attach, proliferate, differentiate and mineralize, thereby acting as a suitable bone repairing material. - Highlights: • Coacervation chitosan microparticles were biocompatible and biodegradable. • IGF-1 encapsulation efficiency increased with coacervation chitosan microparticles. • Coacervation chitosan microparticles support osteoblast attachment and differentiation. • Coacervation chitosan microparticles support osteoblast mineralization.

IGF-1 release kinetics from chitosan microparticles fabricated using environmentally benign conditions

International Nuclear Information System (INIS)

Mantripragada, Venkata P.; Jayasuriya, Ambalangodage C.

2014-01-01

The main objective of this study is to maximize growth factor encapsulation efficiency into microparticles. The novelty of this study is to maximize the encapsulated growth factors into microparticles by minimizing the use of organic solvents and using relatively low temperatures. The microparticles were fabricated using chitosan biopolymer as a base polymer and cross-linked with tripolyphosphate (TPP). Insulin like-growth factor-1 (IGF-1) was encapsulated into microparticles to study release kinetics and bioactivity. In order to authenticate the harms of using organic solvents like hexane and acetone during microparticle preparation, IGF-1 encapsulated microparticles prepared by the emulsification and coacervation methods were compared. The microparticles fabricated by emulsification method have shown a significant decrease (p < 0.05) in IGF-1 encapsulation efficiency, and cumulative release during the two-week period. The biocompatibility of chitosan microparticles and the bioactivity of the released IGF-1 were determined in vitro by live/dead viability assay. The mineralization data observed with von Kossa assay, was supported by mRNA expression levels of osterix and runx2, which are transcription factors necessary for osteoblasts differentiation. Real time RT-PCR data showed an increased expression of runx2 and a decreased expression of osterix over time, indicating differentiating osteoblasts. Chitosan microparticles prepared in optimum environmental conditions are a promising controlled delivery system for cells to attach, proliferate, differentiate and mineralize, thereby acting as a suitable bone repairing material. - Highlights: • Coacervation chitosan microparticles were biocompatible and biodegradable. • IGF-1 encapsulation efficiency increased with coacervation chitosan microparticles. • Coacervation chitosan microparticles support osteoblast attachment and differentiation. • Coacervation chitosan microparticles support osteoblast mineralization

Development of carboxymethyl cellulose-chitosan hybrid micro- and macroparticles for encapsulation of probiotic bacteria.

Science.gov (United States)

Singh, P; Medronho, B; Alves, L; da Silva, G J; Miguel, M G; Lindman, B

2017-11-01

Novel carboxymethyl cellulose-chitosan (CMC-Cht) hybrid micro- and macroparticles were successfully prepared in aqueous media either by drop-wise addition or via nozzle-spray methods. The systems were either physically or chemically crosslinked using genipin as the reticulation agent. The macroparticles (ca. 2mm) formed are found to be essentially of the core-shell type, while the microparticles (ca. 5μm) are apparently homogeneous. The crosslinked particles are robust, thermally resistant and less sensitive to pH changes. On the other hand, the physical systems are pH sensitive presenting a remarkable swelling at pH 7.4, while little swelling is observed at pH 2.4. Furthermore, model probiotic bacteria (Lactobacillus rhamnosus GG) was for the first time successfully encapsulated in the CMC-Cht based particles with acceptable viability count. Overall, the systems developed are highly promising for probiotic encapsulation and potential delivery in the intestinal tract with the purpose of modulating gut microbiota and improving human health. Copyright © 2017 Elsevier Ltd. All rights reserved.

Synthesis and characterization of PEG-conjugated quaternized chitosan and its application as a gene vector.

Science.gov (United States)

Zhang, Xi; Yao, Juan; Zhang, Lihong; Fang, Jianguo; Bian, Fengling

2014-03-15

Poly(ethylene glycol)-conjugated N-(2-hydroxy) propyl-3-trimethyl ammonium chitosan chloride (PHTAC) derivatives were prepared by incorporating PEG molecules onto quaternized chitosan backbone. The copolymers were characterized by FTIR, (1)H NMR and XRD. Agarose gel retardation assay indicated that PHTAC had good plasmid DNA (pDNA) binding capability and the particle sizes of PHTAC/pDNA complexes determined by DLS were about 200 nm. Cytotoxicity assays in HeLa and 293T cells showed that PHTAC had low cytotoxicity. In vitro luciferase assay showed that PHTAC with PEGylation degree of 9% (PHTAC-1) had good transfection efficiency about 5.3-fold higher than quaternized chitosan, which was comparable with PEI (25 kDa). These results suggest that PHTAC-1 is a promising candidate as an efficient nonviral gene vector. Copyright © 2013 Elsevier Ltd. All rights reserved.

Quaternized Chitosan-Capped Mesoporous Silica Nanoparticles as Nanocarriers for Controlled Pesticide Release

Directory of Open Access Journals (Sweden)

Lidong Cao

2016-06-01

Full Text Available Nanotechnology-based pesticide formulations would ensure effective utilization of agricultural inputs. In the present work, mesoporous silica nanoparticles (MSNs with particle diameters of ~110 nm and pore sizes of ~3.7 nm were synthesized via a liquid crystal templating mechanism. A water-soluble chitosan (CS derivative (N-(2-hydroxylpropyl-3-trimethyl ammonium CS chloride, HTCC was successfully capped on the surface of pyraclostrobin-loaded MSNs. The physicochemical and structural analyses showed that the electrostatic interactions and hydrogen bonding were the major forces responsible for the formation of HTCC-capped MSNs. HTCC coating greatly improved the loading efficiency (LC (to 40.3% compared to using bare MSNs as a single encapsulant (26.7%. The microstructure of the nanoparticles was revealed by scanning electron microscopy (SEM and transmission electron microscopy (TEM. The pyraclostrobin-loaded nanoparticles showed an initial burst and subsequent sustained release behavior. HTCC-capped MSNs released faster than bare MSNs in the initial stage. Pyraclostrobin-loaded HTCC-capped MSNs with half doses of pyraclostrobin technical demonstrated almost the same fungicidal activity against Phomopsis asparagi (Sacc., which obviously reduced the applied pesticide and enhanced the utilization efficiency. Therefore, HTCC-decorated MSNs demonstrated great potential as nanocarriers in agrochemical applications.

Amphiphilic chitosan derivatives as carrier agents for rotenone

Science.gov (United States)

Kamari, Azlan; Aljafree, Nurul Farhana Ahmad

2017-08-01

In the present study, the feasibility of amphiphilic chitosan derivatives, namely oleoyl carboxymethyl chitosan (OCMCs), N,N-dimethylhexadecyl carboxymethyl chitosan (DCMCs) and deoxycholic acid carboxymethyl chitosan (DACMCs) as carrier agents for rotenone in water-insoluble pesticide formulations was investigated. Fourier Transform Infrared (FTIR) Spectrometer, CHN-O Elemental Analyser (CHN-O) and Transmission Electron Microscope (TEM) were used to characterise amphiphilic chitosan derivatives. The critical micelle concentration (CMC) of amphiphilic chitosan derivatives was determined using a Fluorescence Spectrometer. A High Performance Liquid Chromatography (HPLC) was used to determine the ability of OCMCs, DCMCs and DACMCs to load and release rotenone in an in vitro system. Based on TEM analysis, results have shown that amphiphilic chitosan derivatives formed self-assembly and exhibited spherical shape. The CMC values determined for OCMCs, DCMCs and DACMCs were 0.093, 0.098 and 0.468 mg/mL, respectively. The encapsulation efficiency (EE) values for the materials were more than 97.0%, meanwhile the loading capacity (LC) values were greater than 0.90%. OCMCs, DCMCs and DACMCs micelles exhibited an excellent ability to control the release of rotenone, of which 90.0% of rotenone was released within 40 to 52 h. In conclusion, OCMCs, DCMCs and DACMCs possess several key features to act as effective carrier agents for rotenone. Overall, amphiphilic chitosan derivatives produced in this study were successfully increased the solubility of rotenone by 49.0 times higher than free rotenone.

Camptothecin disrupts androgen receptor signaling and suppresses prostate cancer cell growth

International Nuclear Information System (INIS)

Liu, Shicheng; Yuan, Yiming; Okumura, Yutaka; Shinkai, Norihiro; Yamauchi, Hitoshi

2010-01-01

The androgen receptor (AR) is the main therapeutic target for treatment of metastatic prostate cancers. The present study demonstrates that the topoisomerase I inhibitor camptothecin selectively inhibits androgen-responsive growth of prostate cancer cells. Camptothecin strikingly inhibited mutated and wild-type AR protein expression in LNCaP and PC-3/AR cells. This inhibition coincided with decreased androgen-mediated AR phosphorylation at Ser 81 and reduced androgen-mediated AR transcriptional activity in a dose-dependent manner. Additionally, camptothecin disrupted the association between AR and heat shock protein 90 and impeded binding of the synthetic androgen [ 3 H]R1881 to AR in LNCaP cells. Camptothecin also blocked androgen-induced AR nuclear translocation, leading to downregulation of the AR target gene PSA. In addition to decreasing the intracellular and secreted prostate-specific antigen (PSA) levels, camptothecin markedly inhibited androgen-stimulated PSA promoter activity. Collectively, our data reveal that camptothecin not only serves as a traditional genotoxic agent but, by virtue of its ability to target and disrupt AR, may also be a novel candidate for the treatment of prostate cancer.

Chitosan encapsulation of essential oil "cocktails" with well-defined binary Zn(II)-Schiff base species targeting antibacterial medicinal nanotechnology.

Science.gov (United States)

Halevas, Eleftherios; Nday, Christiane M; Chatzigeorgiou, Evanthia; Varsamis, Vasileios; Eleftheriadou, Despoina; Jackson, Graham E; Litsardakis, Georgios; Lazari, Diamanto; Ypsilantis, Konstantinos; Salifoglou, Athanasios

2017-11-01

The advent of biodegradable nanomaterials with enhanced antibacterial activity stands as a challenge to the global research community. In an attempt to pursue the development of novel antibacterial medicinal nanotechnology, we herein a) synthesized ionic-gelated chitosan nanoparticles, b) compared and evaluated the antibacterial activity of essential oils extracted from nine different herbs (Greek origin) and their combinations with a well-defined antibacterial Zn(II)-Schiff base compound, and c) encapsulated the most effective hybrid combination of Zn(II)-essential oils inside the chitosan matrix, thereby targeting well-formulated nanoparticles of distinct biological impact. The empty and loaded chitosan nanoparticles were physicochemically characterized by FT-IR, Thermogravimetric Analysis (TGA), Scanning Electron Microscopy (SEM), with the entrapment and drug release studies being conducted through UV-Visible and atomic absorption techniques. The antimicrobial properties of the novel hybrid materials were demonstrated against Gram positive (S. aureus, B. subtilis, and B. cereus) and Gram negative (E. coli and X. campestris) bacteria using modified agar diffusion methods. The collective physicochemical profile of the hybrid Zn(II)-essential oil cocktails, formulated so as to achieve optimal activity when loaded to chitosan nanoparticles, signifies the importance of design in the development of efficient nanomedicinal pharmaceuticals a) based on both natural products and biogenic metal ionic cofactors, and b) targeting bacterial infections and drug resistance. Copyright © 2017 Elsevier Inc. All rights reserved.

Preparation and in vitro evaluation of amoxicillin encapsulated in ...

African Journals Online (AJOL)

Purpose: To optimize and characterize amoxicillin encapsulated in mucoadhesive alginate-coated chitosan microparticles for the treatment of gastric and duodenal ulcers caused by Helicobacter pylori. Methods: Eighteen batches of various ratios of chitosan, sodium alginate and calcium chloride were prepared by ...

Chitosan-solid lipid nanoparticles as carriers for topical delivery of tretinoin.

Science.gov (United States)

Ridolfi, Daniela M; Marcato, Priscyla D; Justo, Giselle Z; Cordi, Lívia; Machado, Daisy; Durán, Nelson

2012-05-01

Tretinoin (TRE) or all-trans retinoic acid is employed in the topical treatment of various skin diseases including acne and psoriasis. However, its use is strongly limited by side effects and high chemical instability. TRE encapsulation in nanostructured systems reduces these problems. Chitosan is a biopolymer that exhibits a number of interesting properties such as bioadhesion and antibacterial activity. The aim of this work was to prepare and characterize solid lipid nanoparticles (SLN) containing TRE, with and without addition of chitosan, to assess their in vitro cytotoxicity in keratinocytes and to evaluate their antibacterial activity against bacteria related to acne. SLN without (SLN-TRE) and with (SLN-chitosan-TRE) chitosan were prepared by hot high pressure homogenization. The hydrodynamic mean diameter and zeta potential were 162.7±1.4 nm and -31.9±2.0 mV for SLN-TRE, and 284.8±15.0 nm and 55.9±3.1 mV for SLN-chitosan-TRE. The SLN-chitosan-TRE exhibited high encapsulation efficiency, high physical stability in the tested period (one year), were not cytotoxic to keratinocytes and showed high antibacterial activity against P. acnes and S. aureus. Therefore chitosan-SLN can be good candidates to encapsulate TRE and to increase its therapeutic efficacy in the topical treatment of acne. Copyright © 2011 Elsevier B.V. All rights reserved.

Human bone marrow stem cell-encapsulating calcium phosphate scaffolds for bone repair

Science.gov (United States)

Weir, Michael D.; Xu, Hockin H.K.

2010-01-01

Due to its injectability and excellent osteoconductivity, calcium phosphate cement (CPC) is highly promising for orthopedic applications. However, a literature search revealed no report on human bone marrow mesenchymal stem cell (hBMSC) encapsulation in CPC for bone tissue engineering. The aim of this study was to encapsulate hBMSCs in alginate hydrogel beads and then incorporate them into CPC, CPC–chitosan and CPC–chitosan–fiber scaffolds. Chitosan and degradable fibers were used to mechanically reinforce the scaffolds. After 21 days, that the percentage of live cells and the cell density of hBMSCs inside CPC-based constructs matched those in alginate without CPC, indicating that the CPC setting reaction did not harm the hBMSCs. Alkaline phosphate activity increased by 8-fold after 14 days. Mineral staining, scanning electron microscopy and X-ray diffraction confirmed that apatitic mineral was deposited by the cells. The amount of hBMSC-synthesized mineral in CPC–chitosan–fiber matched that in CPC without chitosan and fibers. Hence, adding chitosan and fibers, which reinforced the CPC, did not compromise hBMSC osteodifferentiation and mineral synthesis. In conclusion, hBMSCs were encapsulated in CPC and CPC–chitosan–fiber scaffolds for the first time. The encapsulated cells remained viable, osteodifferentiated and synthesized bone minerals. These self-setting, hBMSC-encapsulating CPC-based constructs may be promising for bone tissue engineering applications. PMID:20451676

Synthesize and Characterization of Hydroxypropyl-N-octanealkyl Chitosan Ramification

Science.gov (United States)

Tan, Fu-neng

2018-03-01

A new type of amphiphilic ramification, hydroxypropyl-N-octanealkyl chitosan was prepared from chitosan via hydrophilic group and hydrophobic group were introduced. We could protect the amino group of chitosan via the reaction of chitosan and benzaldehyde could get Schiff base structure. Structures of the products were characterized with FT-IR, elemental analysis, themogrammetry (TG) analysis and X-ray diffraction. The degree of substitution of hydrophobic group was studied by elemental analysis. The result showed this chitosan ramification was soluble, biocompatible, biodegradable and nontoxic.

Antiproliferative effect of Antrodia camphorata polysaccharides encapsulated in chitosan–silica nanoparticles strongly depends on the metabolic activity type of the cell line

International Nuclear Information System (INIS)

Kong, Zwe-Ling; Chang, Jenq-Sheng; Chang, Ke Liang B.

2013-01-01

Chitosan molecules interact with silica and encapsulate the Antrodia camphorata extract (ACE) polysaccharides to form composite nanoparticles. The nanoparticle suspensions of ACE polysaccharides encapsulated in silica–chitosan and silica nanoparticles approach an average particle size of 210 and 294 nm in solution, respectively. The encapsulation efficiencies of ACE polysaccharides are 66 and 63.5 %, respectively. Scanning electron micrographs confirm the formation of near-spherical nanoparticles. ACE polysaccharides solution had better antioxidative capability than ACE polysaccharides encapsulated in silica or silica–chitosan nanoparticles suspensions. The antioxidant capacity of nanoparticles increases with increasing dissolution time. The antitumor effects of ACE polysaccharides, ACE polysaccharides encapsulated in silica, or silica–chitosan nanoparticles increased with increasing concentration of nanoparticles. This is the first report demonstrating the potential of ACE polysaccharides encapsulated in chitosan–silica nanoparticles for cancer chemoprevention. Furthermore, this study suggests that antiproliferative effect of nanoparticle-encapsulated bioactive could significantly depend on the metabolic activity type of the cell line

Electrochemical Studies of Camptothecin and Its Interaction with Human Serum Albumin

OpenAIRE

Zhao, Jing; Zheng, Xiaofeng; Xing, Wei; Huang, Junyi; Li, Genxi

2007-01-01

Camptothecin, an anticancer component from Camptotheca acuminate, may interact with human serum albumin (HSA) at the subdomain IIA (site I), and then convert to its inactive form(carboxylate form). In this paper, the detailed electrochemical behaviors of camptothecin at a pyrolytic graphite electrode is presented. The interaction between camptothecin and HSA is also studied by electrochemical technique. By comparing with bovine serum albumin (BSA), which is highly homologous to HSA, we prove ...

Effect of stiffness of chitosan-hyaluronic acid dialdehyde hydrogels on the viability and growth of encapsulated chondrocytes.

Science.gov (United States)

V Thomas, Lynda; Vg, Rahul; D Nair, Prabha

2017-11-01

Substrate elasticity or stiffness can influence the phenotypic and functional characteristics of chondrocytes. This work aimed to study the effect of varying stiffness compositions of a two-component injectable hydrogel based on chitosan (CH) and oxidized hyaluronic acid (HDA) on the growth and functionality of encapsulated chondrocytes. Three different ratios of the gel were prepared (10:1,10:3 and 10:5 CH-HDA) and characterized. The stiffness of the gels was evaluated from the force displacement curves using force spectroscopy AFM analysis. Rabbit articular chondrocytes were harvested and the cells from Passage 2 to 4 were used for the encapsulation study. The viability and ECM production of encapsulated chondrocytes were assessed at 7day, 14day and 28day post culture. The results of the study show that as the ratio of hyaluronic acid dialdehyde component was increased, the stiffness of the gels increased from 130.78±19.83kPa to 181.47±19.77kPa which was also evidenced from the decrease in gelling time. Although there was an increase in the percentage of viable encapsulated cells which also maintained the spherical phenotype in the less stiff gels, decreased expression of ECM markers- Collagen type II and Glycosaminoglycans was observed compared to the stiffer gels. These findings indicate that gel stiffness strongly impacts the chondrocyte microenvironment both in maintenance of phenotypic integrity and ECM production. Copyright © 2017. Published by Elsevier B.V.

Synthesis and evaluation of PEG-O-chitosan nanoparticles for delivery of poor water soluble drugs: Ibuprofen

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Hassani Najafabadi, Alireza [Department of Chemistry, Amirkabir University of Technology, P.O. Box 1587-4413, Tehran (Iran, Islamic Republic of); Abdouss, Majid, E-mail: phdabdouss44@aut.ac.ir [Department of Chemistry, Amirkabir University of Technology, P.O. Box 1587-4413, Tehran (Iran, Islamic Republic of); Faghihi, Shahab [Tissue Engineering and Biomaterials Division, National Institute of Genetic Engineering and Biotechnology, Tehran 14965/161 (Iran, Islamic Republic of)

2014-08-01

Current methods for preparation of PEGylated chitosan have limitations such as harsh de protecting step and several purification cycles. In the present study, a facile new method for conjugating methoxy polyethylene glycol (mPEG) to chitosan under mild condition is introduced to improve water solubility of chitosan and control the release of poor water soluble drugs. The method consists of chitosan modification by grafting the C6 position of chitosan to mPEG which is confirmed by Fourier transformed-infrared (FT-IR) and proton nuclear magnetic resonance ({sup 1}HNMR) analyses. The amine groups at the C2 position of chitosan are protected using sodium dodecylsulfate (SDS) which is removed by dialyzing the precipitation against Tris solution. The chemical structure of the prepared polymer is characterized by FTIR and {sup 1}HNMR. The synthesized polymer is then employed to prepare nanoparticles which are characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM), scanning electron microscopy (SEM), and dynamic light scattering (DLS) for their size and morphology. The nanoparticles are used for encapsulation of ibuprofen followed by in vitro release investigation in gastrointestinal and simulated biological fluids. The chitosan nanoparticles are used as control. The PEGylated nanoparticles show a particle size of 80 nm with spherical morphology. The results clearly show that drug release from PEGylated chitosan nanoparticles is remarkably slower than chitosan. In addition, drug encapsulation and encapsulation efficiency in PEGylated nanoparticles are dependent on the amount of drug added to the formulation being significantly higher than chitosan nanoparticles. This study provides an efficient, novel, and facile method for preparing a nano carrier system for delivery of water insoluble drugs. - Highlights: • A facile novel method for conjugating methoxy polyethylene glycol (mPEG) to chitosan is introduced. • Fabricated PEG

Synthesis and evaluation of PEG-O-chitosan nanoparticles for delivery of poor water soluble drugs: Ibuprofen

International Nuclear Information System (INIS)

Hassani Najafabadi, Alireza; Abdouss, Majid; Faghihi, Shahab

2014-01-01

Current methods for preparation of PEGylated chitosan have limitations such as harsh de protecting step and several purification cycles. In the present study, a facile new method for conjugating methoxy polyethylene glycol (mPEG) to chitosan under mild condition is introduced to improve water solubility of chitosan and control the release of poor water soluble drugs. The method consists of chitosan modification by grafting the C6 position of chitosan to mPEG which is confirmed by Fourier transformed-infrared (FT-IR) and proton nuclear magnetic resonance ( 1 HNMR) analyses. The amine groups at the C2 position of chitosan are protected using sodium dodecylsulfate (SDS) which is removed by dialyzing the precipitation against Tris solution. The chemical structure of the prepared polymer is characterized by FTIR and 1 HNMR. The synthesized polymer is then employed to prepare nanoparticles which are characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM), scanning electron microscopy (SEM), and dynamic light scattering (DLS) for their size and morphology. The nanoparticles are used for encapsulation of ibuprofen followed by in vitro release investigation in gastrointestinal and simulated biological fluids. The chitosan nanoparticles are used as control. The PEGylated nanoparticles show a particle size of 80 nm with spherical morphology. The results clearly show that drug release from PEGylated chitosan nanoparticles is remarkably slower than chitosan. In addition, drug encapsulation and encapsulation efficiency in PEGylated nanoparticles are dependent on the amount of drug added to the formulation being significantly higher than chitosan nanoparticles. This study provides an efficient, novel, and facile method for preparing a nano carrier system for delivery of water insoluble drugs. - Highlights: • A facile novel method for conjugating methoxy polyethylene glycol (mPEG) to chitosan is introduced. • Fabricated PEG-grafted chitosan

PEGylated versus non-PEGylated magnetic nanoparticles as camptothecin delivery system

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Paula M. Castillo

2014-08-01

Full Text Available Camptothecin (CPT; (S-(+-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-(4H,12H-dione is a highly cytotoxic natural alkaloid that has not yet found use as chemotherapeutic agent due to its poor water-solubility and chemical instability and, as a consequence, no effective administration means have been designed. In this work, camptothecin has been successfully loaded into iron oxide superparamagnetic nanoparticles with an average size of 14 nm. It was found that surface modification of the nanoparticles by polyethylene glycol enables loading a large amount of camptothecin. While the unloaded nanoparticles do not induce apoptosis in the H460 lung cancer cell line, the camptothecin-loaded nanoparticle formulations exhibit remarkable pro-apoptotic activity. These results indicate that camptothecin retains its biological activity after loading onto the magnetic nanoparticles. The proposed materials represent novel materials based on naturally occurring bioactive molecules loaded onto nanoparticles to be used as chemotherapeutic formulations. The procedure seems apt to be extended to other active molecules extracted from natural products. In addition, these materials offer the potential of being further implemented for combined imaging and therapeutics, as magnetic nanoparticles are known to be multifunctional tools for biomedicine.

Intranasal delivery of Huperzine A to the brain using lactoferrin-conjugated N-trimethylated chitosan surface-modified PLGA nanoparticles for treatment of Alzheimer's disease.

Science.gov (United States)

Meng, Qingqing; Wang, Aiping; Hua, Hongchen; Jiang, Ying; Wang, Yiyun; Mu, Hongjie; Wu, Zimei; Sun, Kaoxiang

2018-01-01

Safe and effective delivery of therapeutic drugs to the brain is important for successful therapy of Alzheimer's disease (AD). To develop Huperzine A (HupA)-loaded, mucoadhesive and targeted polylactide-co-glycoside (PLGA) nanoparticles (NPs) with surface modification by lactoferrin (Lf)-conjugated N-trimethylated chitosan (TMC) (HupA Lf-TMC NPs) for efficient intranasal delivery of HupA to the brain for AD treatment. HupA Lf-TMC NPs were prepared using the emulsion-solvent evaporation method and optimized using the Box-Behnken design. The particle size, zeta potential, drug entrapment efficiency, adhesion and in vitro release behavior were investigated. The cellular uptake was investigated by fluorescence microscopy and flow cytometry. MTT assay was used to evaluate the cytotoxicity of the NPs. In vivo imaging system was used to investigate brain targeting effect of NPs after intranasal administration. The biodistribution of Hup-A NPs after intranasal administration was determined by liquid chromatography-tandem mass spectrometry. Optimized HupA Lf-TMC NPs had a particle size of 153.2±13.7 nm, polydispersity index of 0.229±0.078, zeta potential of +35.6±5.2 mV, drug entrapment efficiency of 73.8%±5.7%, and sustained release in vitro over a 48 h period. Adsorption of mucin onto Lf-TMC NPs was 86.9%±1.8%, which was significantly higher than that onto PLGA NPs (32.1%±2.5%). HupA Lf-TMC NPs showed lower toxicity in the 16HBE cell line compared with HupA solution. Qualitative and quantitative cellular uptake experiments indicated that accumulation of Lf-TMC NPs was higher than nontargeted analogs in 16HBE and SH-SY5Y cells. In vivo imaging results showed that Lf-TMC NPs exhibited a higher fluorescence intensity in the brain and a longer residence time than nontargeted NPs. After intranasal administration, Lf-TMC NPs facilitated the distribution of HupA in the brain, and the values of the drug targeting index in the mouse olfactory bulb, cerebrum (with hippocampus

Identification and replication of loci involved in camptothecin-induced cytotoxicity using CEPH pedigrees.

Directory of Open Access Journals (Sweden)

Venita Gresham Watson

2011-05-01

Full Text Available To date, the Centre d'Etude Polymorphism Humain (CEPH cell line model has only been used as a pharmacogenomic tool to evaluate which genes are responsible for the disparity in response to a single drug. The purpose of this study was demonstrate the model's ability to establish a specific pattern of quantitative trait loci (QTL related to a shared mechanism for multiple structurally related drugs, the camptothecins, which are Topoisomerase 1 inhibitors. A simultaneous screen of six camptothecin analogues for in vitro sensitivity in the CEPH cell lines resulted in cytotoxicity profiles and orders of potency which were in agreement with the literature. For all camptothecins studied, heritability estimates for cytotoxic response averaged 23.1 ± 2.6%. Nonparametric linkage analysis was used to identify a relationship between genetic markers and response to the camptothecins. Ten QTLs on chromosomes 1, 3, 5, 6, 11, 12, 16 and 20 were identified as shared by all six camptothecin analogues. In a separate validation experiment, nine of the ten QTLs were replicated at the significant and suggestive levels using three additional camptothecin analogues. To further refine this list of QTLs, another validation study was undertaken and seven of the nine QTLs were independently replicated for all nine camptothecin analogues. This is the first study using the CEPH cell lines that demonstrates that a specific pattern of QTLs could be established for a class of drugs which share a mechanism of action. Moreover, it is the first study to report replication of linkage results for drug-induced cytotoxicity using this model. The QTLs, which have been identified as shared by all camptothecins and replicated across multiple datasets, are of considerable interest; they harbor genes related to the shared mechanism of action for the camptothecins, which are responsible for variation in response.

Cost-effective alternative to nano-encapsulation: Amorphous curcumin-chitosan nanoparticle complex exhibiting high payload and supersaturation generation.

Science.gov (United States)

Nguyen, Minh Hiep; Yu, Hong; Kiew, Tie Yi; Hadinoto, Kunn

2015-10-01

While the wide-ranging therapeutic activities of curcumin have been well established, its successful delivery to realize its true therapeutic potentials faces a major challenge due to its low oral bioavailability. Even though nano-encapsulation has been widely demonstrated to be effective in enhancing the bioavailability of curcumin, it is not without drawbacks (i.e. low payload and costly preparation). Herein we present a cost-effective bioavailability enhancement strategy of curcumin in the form of amorphous curcumin-chitosan nanoparticle complex (or curcumin nanoplex in short) exhibiting a high payload (>80%). The curcumin nanoplex was prepared by a simple yet highly efficient drug-polysaccharide complexation method that required only mixing of the curcumin and chitosan solutions under ambient condition. The effects of (1) pH and (2) charge ratio of chitosan to curcumin on the (i) physical characteristics of the nanoplex (i.e. size, colloidal stability and payload), (ii) complexation efficiency, and (iii) production yield were investigated from which the optimal preparation condition was determined. The nanoplex formation was found to favor low acidic pH and charge ratio below unity. At the optimal condition (i.e. pH 4.4. and charge ratio=0.8), stable curcumin nanoplex (≈260nm) was prepared at >90% complexation efficiency and ≈50% production yield. The amorphous state stability, colloidal stability, and in vitro non-cytotoxicity of the nanoplex were successfully established. The curcumin nanoplex produced prolonged supersaturation (3h) in the presence of hydroxypropyl methylcellulose (HPMC) at five times of the saturation solubility of curcumin. In addition, curcumin released from the nanoplex exhibited improved chemical stability owed to the presence of chitosan. Both results (i.e. high supersaturation and improved chemical stability) bode well for the ability of the curcumin nanoplex to enhance the bioavailability of curcumin clinically. Copyright © 2015

Curcumin drug delivery by vanillin-chitosan coated with calcium ferrite hybrid nanoparticles as carrier.

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Kamaraj, Sriram; Palanisamy, Uma Maheswari; Kadhar Mohamed, Meera Sheriffa Begum; Gangasalam, Arthanareeswaran; Maria, Gover Antoniraj; Kandasamy, Ruckmani

2018-04-30

The aim of the present investigation is the development, optimization and characterization of curcumin-loaded hybrid nanoparticles of vanillin-chitosan coated with super paramagnetic calcium ferrite. The functionally modified vanillin-chitosan was prepared by the Schiff base reaction to enhance the hydrophobic drug encapsulation efficiency. Calcium ferrite (CFNP) nano particles were added to the vanillin modified chitosan to improve the biocompatibility. The vanillin-chitosan-CFNP, hybrid nanoparticle carrier was obtained by ionic gelation method. Characterizations of the hybrid materials were performed by XRD, FTIR, 1 H NMR, TGA, AFM and SEM techniques to ensure the modifications on the chitosan material. Taguchi method was applied to optimize the drug (curcumin) encapsulation efficiency by varying the drug to chitosan-vanillin, CFNP to chitosan-vanillin and TPP (sodium tripolyphospate) to chitosan-vanillin ratios. The maximum encapsulation efficiency was obtained as 98.3% under the conditions of 0.1, 0.75 and 1.0 for the drug to chitosan-vanillin, CFNP to chitosan-vanillin and TPP to chitosan-vanillin ratios, respectively. The curcumin release was performed at various pH, initial drug loading concentrations and magnetic fields. The drug release mechanism was predicted by fitting the experimental kinetic data with various drug release models. The drug release profiles showed the best fit with Higuchi model under the most of conditions. The drug release mechanism followed both non-Fickian diffusion and case II transport mechanism for chitosan, however the non-Fickian diffusion mechanism was followed for the vanillin modified chitosan. The biocompatibility of the hybrid material was tested using L929 fibroblast cells. The cytotoxicity test was performed against MCF-7 breast cancer cell line to check the anticancer property of the hybrid nano carrier with the curcumin drug. Copyright © 2018 Elsevier B.V. All rights reserved.

Cyclodextrin-insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery.

Science.gov (United States)

Sajeesh, S; Sharma, Chandra P

2006-11-15

Present investigation was aimed at developing an oral insulin delivery system based on hydroxypropyl beta cyclodextrin-insulin (HPbetaCD-I) complex encapsulated polymethacrylic acid-chitosan-polyether (polyethylene glycol-polypropylene glycol copolymer) (PMCP) nanoparticles. Nanoparticles were prepared by the free radical polymerization of methacrylic acid in presence of chitosan and polyether in a solvent/surfactant free medium. Dynamic light scattering (DLS) experiment was conducted with particles dispersed in phosphate buffer (pH 7.4) and size distribution curve was observed in the range of 500-800 nm. HPbetaCD was used to prepare non-covalent inclusion complex with insulin and complex was analyzed by Fourier transform infrared (FTIR) and fluorescence spectroscopic studies. HPbetaCD complexed insulin was encapsulated into PMCP nanoparticles by diffusion filling method and their in vitro release profile was evaluated at acidic/alkaline pH. PMCP nanoparticles displayed good insulin encapsulation efficiency and release profile was largely dependent on the pH of the medium. Enzyme linked immunosorbent assay (ELISA) study demonstrated that insulin encapsulated inside the particles was biologically active. Trypsin inhibitory effect of PMCP nanoparticles was evaluated using N-alpha-benzoyl-L-arginine ethyl ester (BAEE) and casein as substrates. Mucoadhesive studies of PMCP nanoparticles were conducted using freshly excised rat intestinal mucosa and the particles were found fairly adhesive. From the preliminary studies, cyclodextrin complexed insulin encapsulated mucoadhesive nanoparticles appear to be a good candidate for oral insulin delivery.

New and highly efficient column chromatographic extraction and simple purification of camptothecin from Camptotheca acuminata and Nothapodytes pittosporoides.

Science.gov (United States)

Zeng, Xue-Hua; Li, Yue-Hong; Wu, Shan-Shan; Hao, Rui-Lin; Li, Hui; Ni, He; Han, Han-Bing; Li, Hai-Hang

2013-01-01

Camptothecin, a widely used natural anti-cancer drug, is difficult to extract and purify effectively from plants. To develop new and highly efficient extraction and purification methods for analysis and production of camptothecin from leaves and fruits of Camptotheca acuminata and Nothapodytes pittosporoides roots. Dried materials were loaded in empty columns with fivefold 60% ethanol for leaves or 70% ethanol for fruits of C. acumnata, and sixfold 70% ethanol for N. pittosporoides roots. The columns were eluted with the same solvents at room temperature. Eluent was collected as extraction solution. Extraction solution from leaves and fruits of C. acuminata was vacuum-evaporated to remove ethanol, precipitated at pH 8.0 to remove alkaline insolubles and fractionated with chloroform at pH 3.0, which yields a crude product with 70% purity. Extraction solution from N. pittosporoides roots was concentrated to 1/10 volume and precipitated at pH 3.0, which yields a crude product with 60% purity. All crude products were purified by crystallisation. All steps were monitored by HPLC. Camptothecin was extracted from the three plant materials at a 98% rate with 15- or 18-fold solvent for content analysis, or at a 97% rate with five- or sixfold solvent for production. All crude products were purified to 98%. The overall recovery rates of camptothecin from plant materials to purified products reached 92% or higher. The new procedures are simple and highly efficient, and have multiple advantages for quantitative analysis and large production of camptothecin from plants. Copyright © 2013 John Wiley & Sons, Ltd.

Effects of pore forming agents on chitosan-graft-poly(N-vinylpyrrolidone) hydrogel properties for use as a matrix for floating drug delivery

Science.gov (United States)

Budianto, E.; Al-Shidqi, M. F.; Cahyana, A. H.

2017-07-01

Eradicating H. pylori-based infection by using conventional oral dosage form of amoxicillin trihydrate finds difficulties to overcome rapid gastric retention time. Encapsulating amoxicillin trihydrate in floating drug delivery system may solve the problem. In this research, the floating drug delivery system of amoxicillin trihydrate encapsulated in floating chitosan-graft-poly(N-vinyl pyrrolidone) hydrogels containing CaCO3 and NaHCO3 as pore forming agents has been successfully prepared. Pore forming agents used was varied with the ratio of 10 to 25% pore forming agents to total mass of the used materials. The hydrogel were characterizedusing FTIR spectrophotometer and stereo microscope. As pore forming agents compositions increased, the porosity (%) and floating properties increased but followed by decrease in drug entrapment efficiency. Most of the floating hydrogels possessed floating ability longer than 180 min and the highest porosity was found in hydrogel containing 25% NaHCO3. Hydrogel containing CaCO3 showed sustained drug release profile than hydrogel containing NaHCO3. However, the optimum formulation was achieved at composition of 10% NaHCO3 with 57% of drug entrapped within the hydrogel and 43% drug released. The results of these studies show that NaHCO3 is an effective pore forming agents for chitosan-graft-poly(N-vinyl pyrrolidone) hydrogel preparation as compare to CaCO3.

Intranasal delivery of Huperzine A to the brain using lactoferrin-conjugated N-trimethylated chitosan surface-modified PLGA nanoparticles for treatment of Alzheimer’s disease

Science.gov (United States)

Hua, Hongchen; Jiang, Ying; Wang, Yiyun; Mu, Hongjie; Wu, Zimei

2018-01-01

Background Safe and effective delivery of therapeutic drugs to the brain is important for successful therapy of Alzheimer’s disease (AD). Purpose To develop Huperzine A (HupA)-loaded, mucoadhesive and targeted polylactide-co-glycoside (PLGA) nanoparticles (NPs) with surface modification by lactoferrin (Lf)-conjugated N-trimethylated chitosan (TMC) (HupA Lf-TMC NPs) for efficient intranasal delivery of HupA to the brain for AD treatment. Methods HupA Lf-TMC NPs were prepared using the emulsion–solvent evaporation method and optimized using the Box–Behnken design. The particle size, zeta potential, drug entrapment efficiency, adhesion and in vitro release behavior were investigated. The cellular uptake was investigated by fluorescence microscopy and flow cytometry. MTT assay was used to evaluate the cytotoxicity of the NPs. In vivo imaging system was used to investigate brain targeting effect of NPs after intranasal administration. The biodistribution of Hup-A NPs after intranasal administration was determined by liquid chromatography–tandem mass spectrometry. Results Optimized HupA Lf-TMC NPs had a particle size of 153.2±13.7 nm, polydispersity index of 0.229±0.078, zeta potential of +35.6±5.2 mV, drug entrapment efficiency of 73.8%±5.7%, and sustained release in vitro over a 48 h period. Adsorption of mucin onto Lf-TMC NPs was 86.9%±1.8%, which was significantly higher than that onto PLGA NPs (32.1%±2.5%). HupA Lf-TMC NPs showed lower toxicity in the 16HBE cell line compared with HupA solution. Qualitative and quantitative cellular uptake experiments indicated that accumulation of Lf-TMC NPs was higher than nontargeted analogs in 16HBE and SH-SY5Y cells. In vivo imaging results showed that Lf-TMC NPs exhibited a higher fluorescence intensity in the brain and a longer residence time than nontargeted NPs. After intranasal administration, Lf-TMC NPs facilitated the distribution of HupA in the brain, and the values of the drug targeting index in the mouse

Design, characterisation and application of alginate-based encapsulated pig liver esterase.

Science.gov (United States)

Pauly, Jan; Gröger, Harald; Patel, Anant V

2018-06-05

Encapsulation of hydrolases in biopolymer-based hydrogels often suffers from low activities and encapsulation efficiencies along with high leaching and unsatisfactory recycling properties. Exemplified for the encapsulation of pig liver esterase the coating of alginate and chitosan beads have been studied by creating various biopolymer hydrogel beads. Enzyme activity and encapsulation efficiency were notably enhanced by chitosan coating of alginate beads while leaching remained nearly unchanged. This was caused by the enzymatic reaction acidifying the matrix, which increased enzyme retention through enhanced electrostatic enzyme-alginate interaction but decreased activity through enzyme deactivation. A practical and ready-to-use method for visualising pH in beads during reaction by co-encapsulation of a conventional pH indicator was also found. Our method proves that pH control inside the beads can only be realised by buffering. The resulting beads provided a specific activity of 0.267 μmol ∙ min -1 ∙ mg -1 , effectiveness factor 0.88, encapsulation efficiency of 88%, 5% leaching and good recycling properties. This work will contribute towards better understanding and application of encapsulated hydrolases for enzymatic syntheses. Copyright © 2018 Elsevier B.V. All rights reserved.

Multilayer emulsions as a strategy for linseed oil and α-lipoic acid micro-encapsulation: study on preparation and in vitro characterization.

Science.gov (United States)

Huang, Juan; Wang, Qiang; Li, Tong; Xia, Nan; Xia, Qiang

2018-01-04

Linseed oil and α-lipoic acid are bioactive ingredients, which play an important role in human nutrition and health. However, their application in functional foods is limited because of their instabilities and poor solubilities in hydrophilic matrices. Multilayer emulsions are particularly useful to protect encapsulated bioactive ingredients. The aim of this study was to fabricate multilayer emulsions by a high-pressure homogenization method to encapsulate linseed oil and α-lipoic acid simultaneously. Tween 20 and lecithin were used as surfactants to stabilize the oil droplets of primary emulsions. Multilayer emulsions were produced by using an electrostatic layer-by-layer deposition process of lecithin-chitosan membranes. Thermal treatment exhibited that chitosan encapsulation could improve the thermal stability of primary emulsions. During in vitro digestion, it was found that chitosan encapsulation had little effect on the lipolysis of linseed oil and bioaccessibility of α-lipoic acid. The oxidation stability of linseed oil in multilayer emulsions was improved effectively by chitosan encapsulation and α-lipoic acid. Chitosan encapsulation could inhibit the degradation of α-lipoic acid. A physical stability study indicated that multilayer emulsions had good centrifugal, dilution and storage stabilities. Multilayer emulsion is an effective delivery system to incorporate linseed oil and α-lipoic acid into functional foods and beverages. © 2018 Society of Chemical Industry. © 2018 Society of Chemical Industry.

Poly(amido amine) dendrimers as absorption enhancers for oral delivery of camptothecin.

Science.gov (United States)

Sadekar, S; Thiagarajan, G; Bartlett, K; Hubbard, D; Ray, A; McGill, L D; Ghandehari, H

2013-11-01

Oral delivery of camptothecin has a treatment advantage but is limited by low bioavailability and gastrointestinal toxicity. Poly(amido amine) or PAMAM dendrimers have shown promise as intestinal penetration enhancers, drug solubilizers and drug carriers for oral delivery in vitro and in situ. There have been very limited studies in vivo to evaluate PAMAM dendrimers for oral drug delivery. In this study, camptothecin (5 mg/kg) was formulated and co-delivered with cationic, amine-terminated PAMAM dendrimer generation 4.0 (G4.0) (100 and 300 mg/kg) and anionic, carboxylate-terminated PAMAM generation 3.5 (G3.5) (300 and 1000 mg/kg) in CD-1 mice. Camptothecin associated to a higher extent with G4.0 than G3.5 in the formulation, attributed to an electrostatic interaction on the surface of G4.0. Both PAMAM G4.0 and G3.5 increased camptothecin solubilization in simulated gastric fluid and caused a 2-3 fold increase in oral absorption of camptothecin when delivered at 2 h. PAMAM G4.0 and G3.5 did not increase mannitol transport suggesting that the oral absorption of camptothecin was not due to tight junction modulation. Histologic observations of the epithelial layer of small intestinal segments of the gastrointestinal tract (GIT) at 4 h post dosing supported no evidence of toxicity at the evaluated doses of PAMAM dendrimers. This study demonstrates that both cationic (G.4) and anionic (G3.5) PAMAM dendrimers were effective in enhancing the oral absorption of camptothecin. Results suggest that drug inclusion in PAMAM interior controlled solubilization in simulated gastric and intestinal fluids, and increased oral bioavailability. Copyright © 2013 Elsevier B.V. All rights reserved.

Effects of extraction parameters on physicochemical and functional characteristics of chitosan from Penaeus monodon shell

Directory of Open Access Journals (Sweden)

Jubril Olayinka Akolade

2016-11-01

Full Text Available Objective: To investigate the effect of extraction parameters with particular interest during the microwave deacetylation process on the characteristics of chitosan produced from Penaeus monodon (P. monodon sourced within the coastal region of Lagos, Nigeria for applications of controlled release systems for pharmaceutical industries. Methods: Chitosan was extracted from shrimp (P. monodon shell and evaluated as a controlled release system for curcumin. Effects of relevant processing parameters on physicochemical and functional characteristics of the extracted chitosan were assessed. The crude chitosan was purified and used to prepare controlled release formulations for curcumin via ionic gelation with tripolyphosphate. Results: Data from the study showed that increasing time and temperature during deproteinization significantly improved the removal of protein bound to the shell matrix. Also, the ratio of the weight of the deproteinized sample to the volume of HCl used for demineralization influenced the process. During microwave-assisted production of chitosan from chitin, increase in the concentration of the deacetylating medium significantly increased solubility, viscosity and degree of deacetylation, whereas increasing temperature and time during deacetylation of chitin degraded the biopolymer to give low molecular weight chitosan. Optimized extraction and purification process yielded absolutely soluble medium to low molecular weight chitosan. The encapsulation efficiency, loading capacity, percentage yield, release efficiencies in simulated gastric and intestinal fluids of curcumin loaded in the formulations of chitosan from P. monodon were compared favorably to encapsulation and release characteristics of the encapsulated curcumin in commercially available chitosan used as the reference. Conclusions: Valorization of shrimp waste into pharmaceutically graded medium molecular weight chitosan was achieved. The chitosan obtained can be used as

Chitosan microparticles for sustaining the topical delivery of minoxidil sulphate.

Science.gov (United States)

Gelfuso, Guilherme Martins; Gratieri, Taís; Simão, Patrícia Sper; de Freitas, Luís Alexandre Pedro; Lopez, Renata Fonseca Vianna

2011-01-01

Given the hypothesis that microparticles can penetrate the skin barrier along the transfollicular route, this work aimed to obtain and characterise chitosan microparticles loaded with minoxidil sulphate (MXS) and to study their ability to sustain the release of the drug, attempting a further application utilising them in a targeted delivery system for the topical treatment of alopecia. Chitosan microparticles, containing different proportions of MXS/polymer, were prepared by spray drying and were characterised by yield, encapsulation efficiency, size and morphology. Microparticles selected for further studies showed high encapsulation efficiency (∼82%), a mean diameter of 3.0 µm and a spherical morphology without porosities. When suspended in an ethanol/water solution, chitosan microparticles underwent instantaneous swelling, increasing their mean diameter by 90%. Release studies revealed that the chitosan microparticles were able to sustain about three times the release rate of MXS. This feature, combined with suitable size, confers to these microparticles the potential to target and improve topical therapy of alopecia with minoxidil.

IR 820 dye encapsulated in polycaprolactone glycol chitosan: Poloxamer blend nanoparticles for photo immunotherapy for breast cancer

International Nuclear Information System (INIS)

Kumar, Piyush; Srivastava, Rohit

2015-01-01

In the present study, we have fabricated biocompatible and biodegradable monodisperse IR 820 encapsulated polycaprolactone (PCL) glycol chitosan (GC): Poloxamer blend nanoparticles (PP-IR NPs) for imaging and effective photo-immunotherapy. IR 820 has been used as an imaging and photothermal agent whereas glycol chitosan (GC) as an immunostimulatory agent. The combination of IR 820, poloxamer, and GC can be used effectively for photoimmunotherapy for cancer, drug-resistant and TNF-α resistant estrogen positive breast cancer. PP-IR NPs are stable in aqueous solution. The uniform size of 100–220 nm with a high zeta value of + 38 ± 2 mV led them to accumulate in cancer cells. Laser treatment did not affect the morphology of PP-IR NPs as observed under the transmission electron microscope (TEM). In vitro cytotoxicity studies on MCF-7 cells showed enhanced toxicity upon laser treatment. Further, we validated the cell death by reactive oxygen species (ROS) production. Our studies thus showed that PP-IR NPs are effective in suppressing metastatic cancer as the combinational therapy leads to the formation of apoptotic bodies in MCF-7 cells. - Highlights: • PPIR nanoparticles for photoimmunotherapy for cancer • IR 820/GC serves as theranostic and immunostimulatory. • Photoimmunotherapy enhances cytotoxicity by reactive oxygen species production

IR 820 dye encapsulated in polycaprolactone glycol chitosan: Poloxamer blend nanoparticles for photo immunotherapy for breast cancer

Energy Technology Data Exchange (ETDEWEB)

Kumar, Piyush; Srivastava, Rohit, E-mail: rsrivasta@iitb.ac.in

2015-12-01

In the present study, we have fabricated biocompatible and biodegradable monodisperse IR 820 encapsulated polycaprolactone (PCL) glycol chitosan (GC): Poloxamer blend nanoparticles (PP-IR NPs) for imaging and effective photo-immunotherapy. IR 820 has been used as an imaging and photothermal agent whereas glycol chitosan (GC) as an immunostimulatory agent. The combination of IR 820, poloxamer, and GC can be used effectively for photoimmunotherapy for cancer, drug-resistant and TNF-α resistant estrogen positive breast cancer. PP-IR NPs are stable in aqueous solution. The uniform size of 100–220 nm with a high zeta value of + 38 ± 2 mV led them to accumulate in cancer cells. Laser treatment did not affect the morphology of PP-IR NPs as observed under the transmission electron microscope (TEM). In vitro cytotoxicity studies on MCF-7 cells showed enhanced toxicity upon laser treatment. Further, we validated the cell death by reactive oxygen species (ROS) production. Our studies thus showed that PP-IR NPs are effective in suppressing metastatic cancer as the combinational therapy leads to the formation of apoptotic bodies in MCF-7 cells. - Highlights: • PPIR nanoparticles for photoimmunotherapy for cancer • IR 820/GC serves as theranostic and immunostimulatory. • Photoimmunotherapy enhances cytotoxicity by reactive oxygen species production.

Development of Cy5.5-Labeled Hydrophobically Modified Glycol Chitosan Nanoparticles for Protein Delivery

Science.gov (United States)

Chin, Amanda

Therapeutic proteins are often highly susceptible to enzymatic degradation, thus restricting their in vivo stability. To overcome this limitation, delivery systems designed to promote uptake and reduce degradation kinetics have undergone a rapid shift from macro-scale systems to nanomaterial based carriers. Many of these nanomaterials, however, elicit immune responses and may have cytotoxic effects both in vitro and in vivo. The naturally derived polysaccharide chitosan has emerged as a promising biodegradable material and has been utilized for many biomedical applications; nevertheless, its function is often constrained by poor solubility. Glycol chitosan, a derivative of chitosan, can be hydrophobically modified to impart amphiphilic properties that enable the self-assembly into nanoparticles in aqueous media at neutral pH. This nanoparticle system has shown initial success as a therapeutic agent in several model cell culture systems, but little is known about its stability against enzymatic degradation. Therefore, the goal of this research was to investigate the resistance of hydrophobically modified glycol chitosan against enzyme-catalyzed degradation using an in vivo simulated system containing lysozyme. To synthesize the nanoparticles, hydrophobic cholanic acid was first covalently conjugated to glycol chitosan using of N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (EDC) and N-hydroxysuccinimide (NHS). Conjugates were purified by dialysis, lyophilized, and ultra-sonicated to form nanoparticles. Fourier transform infrared (FT-IR) spectroscopy confirmed the binding of 5beta-cholanic acid to the glycol chitosan. Particle size and stability over time were determined with dynamic light scattering (DLS), and particle morphology was evaluated by transmission electron microscopy (TEM). The average diameter of the nanoparticles was approximately 200 nm, which remained stable at 4°C for up to 10 days. Additionally, a near infrared fluorescent (NIRF) dye

Immunological evaluation of chitosan nanoparticles loaded with tetanus toxoid.

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Ghalavand, M; Saadati, M; Ahmadi, A; Abbasi, E; Salimian, J

2018-01-01

The present study was aimed at comparing tetanus toxoid (TT)‑loaded-chitosan nanoparticles with aluminum hydroxide as a common vaccine adjuvant. Tetanus remains to be a major public health problem. Nanoparticles have been extensively used as immune adjuvants. Tetanus toxoid (TT) encapsulated in chitosan nanoparticles is considered to be a promising tetanus vaccine candidate. TT‑loaded chitosan nanoparticles were prepared by the ionic gelation method. The nanoparticles were studied by SEM for their size and morphology. In vivo study was conducted to evaluate the immunity response using mice divided into 4 groups and injected with encapsulated toxoid. The immune responses were then measured using indirect ELISA. The purity and integrity of antigen were confirmed by SDS-PAGE electrophoresis. The size of nanoparticles was estimated at 100 nm. As a result, the IgG antibody levels were 1.9, 1.76, and 0.87 in chitosan nanoparticles, aluminum hydroxide, and TT alone groups, respectively. Also, the immune responses were significantly higher in immunized groups compared to control groups vaccinated with free adjuvant vaccines (p chitosan nanoparticles were reasonable. It enhanced the immune responses as much as aluminum hydroxide adjuvant does and thus may be a good alternative candidate (Tab. 1, Fig. 3, Ref. 16).

Graft copolymerization of N-maleoyl-N-phthaloyl-chitosan (MAPHCS) and acrylic acid via γ-ray irradiation

International Nuclear Information System (INIS)

Mu Qing; Fang Yue'e

2006-01-01

Chitosan is a well-known abundant natural polymer with good biodegradability, biocompatibility and bioactivity. But its insolubility in common organic solvents of chitosan have hindered its utilization and basic research. N-maleoyl-N-phthaloyl-chitosan (MAPHCS), soluble in DMF or DMSO, was synthesized and characterized by Fourier transform infrared spectra analysis (FT-IR) and 1 H-NMR. The graft copolymerization of acrylic acid onto chitosan was carried out with N-maleoyl-N-phthaloyl-chitosan as intermediate in homogeneous system and initiated by γ-irradiation. The double bond of MAPHCS may be the grafting site because the grafting field was much higher than that of the graft copolymerization of acrylic acid and phthaloylchitosan via γ-ray irradiation. The chemical structure of the graft copolymer was characterized by FT-IR and 1 H-NMR. As indicated in FTIR spectra, the evidence of the stronger absorbance at 2800-3000 cm -1 for C-H and at 1720 cm -1 for carboxyl group implied significantly the successful introduction of the poly (acrylic acid) on the chitosan chain. Differential scanning calorimetry (DSC) and thermal gravimetric analysis (TGA) were also used to characterize the copolymer. Effects of synthesis variables on the graft copolymerization were studied in light of the grafting percentage. The grafting percentage increased with the dose at lower doses, and then decreased. The maximum grafting percentage was up to 132%. (authors)

Synthesis and evaluation of PEG-O-chitosan nanoparticles for delivery of poor water soluble drugs: ibuprofen.

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Hassani Najafabadi, Alireza; Abdouss, Majid; Faghihi, Shahab

2014-08-01

Current methods for preparation of PEGylated chitosan have limitations such as harsh de protecting step and several purification cycles. In the present study, a facile new method for conjugating methoxy polyethylene glycol (mPEG) to chitosan under mild condition is introduced to improve water solubility of chitosan and control the release of poor water soluble drugs. The method consists of chitosan modification by grafting the C6 position of chitosan to mPEG which is confirmed by Fourier transformed-infrared (FT-IR) and proton nuclear magnetic resonance ((1)HNMR) analyses. The amine groups at the C2 position of chitosan are protected using sodium dodecylsulfate (SDS) which is removed by dialyzing the precipitation against Tris solution. The chemical structure of the prepared polymer is characterized by FTIR and (1)HNMR. The synthesized polymer is then employed to prepare nanoparticles which are characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM), scanning electron microscopy (SEM), and dynamic light scattering (DLS) for their size and morphology. The nanoparticles are used for encapsulation of ibuprofen followed by in vitro release investigation in gastrointestinal and simulated biological fluids. The chitosan nanoparticles are used as control. The PEGylated nanoparticles show a particle size of 80 nm with spherical morphology. The results clearly show that drug release from PEGylated chitosan nanoparticles is remarkably slower than chitosan. In addition, drug encapsulation and encapsulation efficiency in PEGylated nanoparticles are dependent on the amount of drug added to the formulation being significantly higher than chitosan nanoparticles. This study provides an efficient, novel, and facile method for preparing a nano carrier system for delivery of water insoluble drugs. Copyright © 2014 Elsevier B.V. All rights reserved.

The Effects of Biopolymer Encapsulation on Total Lipids and Cholesterol in Egg Yolk during in Vitro Human Digestion

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Si-Kyung Lee

2013-08-01

Full Text Available The purpose of this study was to examine the effect of biopolymer encapsulation on the digestion of total lipids and cholesterol in egg yolk using an in vitro human digestion model. Egg yolks were encapsulated with 1% cellulose, pectin, or chitosan. The samples were then passed through an in vitro human digestion model that simulated the composition of mouth saliva, stomach acid, and the intestinal juice of the small intestine by using a dialysis tubing system. The change in digestion of total lipids was monitored by confocal fluorescence microscopy. The digestion rate of total lipids and cholesterol in all egg yolk samples dramatically increased after in vitro human digestion. The digestion rate of total lipids and cholesterol in egg yolks encapsulated with chitosan or pectin was reduced compared to the digestion rate of total lipids and cholesterol in other egg yolk samples. Egg yolks encapsulated with pectin or chitosan had lower free fatty acid content, and lipid oxidation values than samples without biopolymer encapsulation. Moreover, the lipase activity decreased, after in vitro digestion, in egg yolks encapsulated with biopolymers. These results improve our understanding of the effects of digestion on total lipids and cholesterol in egg yolk within the gastrointestinal tract.

The Effects of Biopolymer Encapsulation on Total Lipids and Cholesterol in Egg Yolk during in Vitro Human Digestion

Science.gov (United States)

Hur, Sun-Jin; Kim, Young-Chan; Choi, Inwook; Lee, Si-Kyung

2013-01-01

The purpose of this study was to examine the effect of biopolymer encapsulation on the digestion of total lipids and cholesterol in egg yolk using an in vitro human digestion model. Egg yolks were encapsulated with 1% cellulose, pectin, or chitosan. The samples were then passed through an in vitro human digestion model that simulated the composition of mouth saliva, stomach acid, and the intestinal juice of the small intestine by using a dialysis tubing system. The change in digestion of total lipids was monitored by confocal fluorescence microscopy. The digestion rate of total lipids and cholesterol in all egg yolk samples dramatically increased after in vitro human digestion. The digestion rate of total lipids and cholesterol in egg yolks encapsulated with chitosan or pectin was reduced compared to the digestion rate of total lipids and cholesterol in other egg yolk samples. Egg yolks encapsulated with pectin or chitosan had lower free fatty acid content, and lipid oxidation values than samples without biopolymer encapsulation. Moreover, the lipase activity decreased, after in vitro digestion, in egg yolks encapsulated with biopolymers. These results improve our understanding of the effects of digestion on total lipids and cholesterol in egg yolk within the gastrointestinal tract. PMID:23965957

Sol-gel encapsulation of pullulanase in the presence of hybrid magnetic (Fe3O4-chitosan) nanoparticles improves thermal and operational stability.

Science.gov (United States)

Long, Jie; Li, Xingfei; Zhan, Xiaobei; Xu, Xueming; Tian, Yaoqi; Xie, Zhengjun; Jin, Zhengyu

2017-06-01

Pullulanase was sol-gel encapsulated in the presence of magnetic chitosan/Fe 3 O 4 nanoparticles. The resulting immobilized pullulanase was characterized by scanning electron microscopy, vibrating sample magnetometry, Fourier transform infrared spectroscopy and thermogravimetric analysis. The results showed that the addition of pullulanase created a more regular surface on the sol-gel matrix and an enhanced magnetic response to an applied magnetic field. The maximal activity retention (83.9%) and specific activity (291.7 U/mg) of the immobilized pullulanase were observed under optimized conditions including an octyltriethoxysilane:tetraethoxysilane (OTES:TEOS) ratio of 1:2 and enzyme concentration of 0.484 mg/mL sol. The immobilized enzyme exhibited good thermal stability. When the temperature was above 60 °C, the immobilized pullulanase showed significantly higher activity than the free enzyme (p sol-gel encapsulation and co-immobilized by crosslinking-encapsulation retained 52 and 69% of their initial activity after 5 h at 62 °C, respectively, compared to 11% for the free enzyme. Moreover, the stability of the pullulanase was improved by crosslinking-encapsulation, as the enzyme retained more than 85 and 81% of its original activity after 5 and 6 consecutive reuses, respectively, compared to 80 and 72% of its original activity for simple sol-gel encapsulated enzymes. This indicated the leakage of enzyme molecules through the pores of the gel was substantially abated by cross-linking. Such immobilized pullulanase provides high stability and ease of enzyme recovery, characteristics that are advantageous for applications in the food industry that involve continuous starch processing.

Brain targeting effect of camptothecin-loaded solid lipid nanoparticles in rat after intravenous administration

DEFF Research Database (Denmark)

Martins, S. M.; Sarmento, B.; Nunes, C.

2013-01-01

studies against glioma and macrophage human cell lines revealed that camptothecin-loaded SLN induced cell death with the lowest maximal inhibitory concentration (IC50) values, revealing higher antitumour activity of camptothecin-loaded SLN against gliomas. Furthermore, in vivo biodistribution studies...

Characteristics of eugenol loaded chitosan-tripolyphosphate particles as affected by initial content of eugenol and their in-vitro release characteristic

Science.gov (United States)

Cahyono, B.; A’yun, Qurrotu; Suzery, M.; Hadiyanto

2018-04-01

The aim of this research was to determine encapsulation efficiency, loading capacity and controlled release of eugenol loaded chitosan-tpp products which prepared by coaservation method. The characteristic of eugenol-loaded chitosan showed that %EE and % LC increased by increasing the initial eugenol content. The optimum of %EE (72.63%) and %LC (43.96%) were obtained at the ratio of chitosan to eugenol of 1:1.5. The FTIR spectrum showed the characteristic peaks of eugenol appearing on spectrum of eugenol encapsulated and blue-shift in the hydroxyl band from 3425.58 cm-1 in chitosan-tpp to 3417.86 cm-1 and 3394.72 cm-1 in eugenol loaded chitosan-tpp indicating that eugenol was successfully encapsulated. The surface morphologies of freeze-dried particles with the optimum %EE showed that more surface roughness and porosity than plain particles. Furthermore, the in vitro release of particles with minimum and optimum %EE were also investigated in acid (Simulated Gastric Fluid) and base (Simulated Intestinal Fluid) medium at ambient temperature.

Chitosan nanoparticles as drug delivery carriers for biomedical engineering

International Nuclear Information System (INIS)

Shi, L.E.S.; Chen, M.; XINF, L.Y.; Guo, X.F.; Zhao, L.M.

2011-01-01

Chitosan is a rather abundant material, which has been widely used in food industrial and bioengineering aspects, including in encapsulating active food ingredients, in enzyme immobilization, and as a carrier for drug delivery, due to its significant biological and chemical properties such as biodegradable, biocompatible, bioactive and polycationic. This review discussed preparation and applications of chitosan nanoparticles in the biomedical engineering field, namely as a drug delivery carrier for biopharmaceuticals. (author)

Camptothecin-Based Regimens for Treatment of Ewing Sarcoma: sPast Studies and Future Directions

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Lars Wagner

2011-01-01

Full Text Available New therapies are needed to improve survival for patients with Ewing sarcoma. Over the past decade, camptothecin agents such as topotecan and irinotecan have demonstrated activity against Ewing sarcoma, especially in combination with alkylating agents. Previous studies have shown camptothecin-based combinations to be tolerable outpatient strategies that are attractive for salvage therapy. This paper highlights important issues related to drug dosing, schedule of administration, pharmacokinetics, toxicity, and activity of commonly used camptothecin-based regimens. Also discussed are strategies for incorporating these regimens into therapy for newly diagnosed patients, including several potential possibilities for combination with targeted agents.

Effect drug loading process on dissolution mechanism of encapsulated amoxicillin trihydrate in hydrogel semi-IPN chitosan methyl cellulose with pore forming agent KHCO3 as a floating drug delivery system

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Fithawati, Garnis; Budianto, Emil

2018-04-01

Common treatment for Helicobacter pylori by repeated oral consumption of amoxicillin trihydrate is not effective. Amoxicillin trihydrate has a very short residence time in stomach which leads into its ineffectiveness. Residence time of amoxicillin trihydrate can be improved by encapsulating amoxicillin trihydrate into a floating drug delivery system. In this study, amoxicillin trihydrate is encapsulated into hydrogel semi-IPN chitosan methyl cellulose matrix as a floating drug delivery system and then treated with 20% KHCO3 as pore forming agent. Drug loading process used are in-situ loading and post loading. In-situ loading process has higher efficiency percentage and dissolution percentage than post loading process. In-situ loading process resulted 100% efficiency with 92,70% dissolution percentage. Post loading process resulted 98,7% efficiency with 90,42% dissolution percentage. Mechanism of drug dissolution study by kinetics approach showed both in-situ loading process and post loading process are diffusion and degradation process (n=0,4913) and (n=0,4602) respectively. These results are supported by characterization data from optical microscope and scanning electron microscopy (SEM). Data from optical microscope showed both loading process resulted in coarser hydrogel surface. Characterization using SEM showed elongated pores in both loading process after dissolution test.

Polyphenon-E encapsulated into chitosan nanoparticles inhibited proliferation and growth of Ehrlich solid tumor in mice

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Azza I. Othman

2018-03-01

Full Text Available Limited bioavailability of green tea polyphenols hampered their delivery to tumor and hence therapeutic effectiveness. This study investigated the antitumor activity of polyphenon-E (PE encapsulated into chitosan nanoparticles (CSNPs in Ehrlich solid tumor in mice. CSNPs-PE, with a particle size of 53–69 nm showed 83% entrapment efficiency and a sustained release of PE in pH = 7.4 at 37 °C. The data demonstrated a higher percentage of released drug in case of less crosslinked formulations. Ehrlich ascites carcinoma (EAC cells (2.5 × 106/0.2 ml/mouse were injected subcutaneously in the back of mice. Oral administration of CSNPs-PE for 30 days produced a significant decrease in tumor volume (53% and weight (60% compared with free PE and voids CSNPs (72%. Compared with free PE and control, cell cycle revealed G0/G1 arrest associated with decrease in proliferating cell nuclear antigen (PCNA. In tumor tissue of CSNPs-PE treated mice, compared with free PE, there were; 1 induction of Bax and p53, 2 activation of caspases-3,-8 and -9, and CD95, 3 decrease in Bcl-2 expression of 4 inhibition of VEGF and CD31 expressions in tumor tissue. In conclusion, encapsulation of PE into CSNPs provided a good platform for cancer chemotherapy and raised existing application of different polyphenols for nanochemotherapy/prevention.

Effects of storage and yogurt matrix on the stability of tocotrienols encapsulated in chitosan-alginate microcapsules.

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Tan, Phui Yee; Tan, Tai Boon; Chang, Hon Weng; Tey, Beng Ti; Chan, Eng Seng; Lai, Oi Ming; Baharin, Badlishah Sham; Nehdi, Imededdine Arbi; Tan, Chin Ping

2018-02-15

Tocotrienol microcapsules (TM) were formed by firstly preparing Pickering emulsion containing tocotrienols, which was then gelled into microcapsules using alginate and chitosan. In this study, we examined the stability of TM during storage and when applied into a model food system, i.e. yogurt. During storage at 40°C, TM displayed remarkably lower tocotrienols loss (50.8%) as compared to non-encapsulated tocotrienols in bulk oil (87.5%). When the tocotrienols were incorporated into yogurt, the TM and bulk oil forms showed a loss of 23.5% and 81.0%, respectively. Generally, the tocotrienols were stable in the TM form and showed highest stability when these TM were added into yogurt. δ-Tocotrienol was the most stable isomer in both forms during storage and when incorporated into yogurt. The addition of TM into yogurt caused minimal changes in the yogurt's color and texture but slightly altered the yogurt's viscosity. Copyright © 2017 Elsevier Ltd. All rights reserved.

Phosphatidylcholine nanovesicles coated with chitosan or chondroitin sulfate as novel devices for bacteriocin delivery

Science.gov (United States)

da Silva, Indjara Mallmann; Boelter, Juliana Ferreira; da Silveira, Nádya Pesce; Brandelli, Adriano

2014-07-01

There is increased interest on the use of natural antimicrobial peptides in biomedicine and food preservation technologies. In this study, the antimicrobial activity of nisin encapsulated into nanovesicles containing polyanionic polysaccharides was investigated. Nisin was encapsulated in phosphatidylcholine (PC) liposomes containing chitosan or chondroitin sulfate by the thin-film hydration method and tested for antimicrobial activity against Listeria spp. The mean particle size of PC liposomes was 145 nm and varied to 210 and 134 nm with the incorporation of chitosan and chondroitin sulfate, respectively. Nisin-containing nanovesicles with and without incorporation of polysaccharides had a zeta potential values around -20 mV, showing mostly spherical structures when observed by transmission electron microscopy. Encapsulated nisin had similar efficiency as free nisin in inhibiting Listeria spp. isolated from bovine carcass, and greater efficiency in inhibiting Listeria monocytogenes. The formulation containing chitosan was more stable and more efficient in inhibiting L. monocytogenes when compared to the other nanovesicles tested. After 24 h, the viable cell counts were 2 log lower as compared with the other treatments and 7 log comparing to controls.

Chitosan/dextran multilayer microcapsules for polyphenol co-delivery

International Nuclear Information System (INIS)

Paini, Marco; Aliakbarian, Bahar; Casazza, Alessandro A.; Perego, Patrizia; Ruggiero, Carmelina; Pastorino, Laura

2015-01-01

Polysaccharide-based nanostructured polymeric microcapsules were fabricated by the electrostatic layer-by-layer self-assembly technique and used to encapsulate mixtures of four different polyphenols in order to achieve their controlled release. The real-time fabrication of the dextran/chitosan multilayer was monitored by quartz crystal microbalance with dissipation monitoring, and the morphology of the nanostructured polymeric capsules was characterized by scanning electron microscopy. The polyphenol encapsulation was obtained by reversible permeability variation of the capsule shell in ethanol:water mixtures. The loading efficiency in different water:ethanol mixtures and the release rate in acidic conditions were characterized by UV spectroscopy and HPLC. The higher loading efficiency was obtained with an ethanol:water 35:65 phenolic solution, equal to 42.0 ± 0.6%, with a total release of 11.5 ± 0.7 mg of total polyphenols per 11.3 μL of microcapsules after 240 min of incubation in acidic environment. The results suggest that polysaccharide-based capsules can be successfully used to encapsulate and release low water-soluble molecules, such as polyphenols. - Highlights: • Chitosan/dextran nanocapsules were made by layer-by-layer self-assembly technique. • Different ethanol:water mixtures of four polyphenols were encapsulated. • An encapsulation efficiency of 42.0 ± 0.6% was obtained using ethanol:water 35:65. • Release profiles in acidic environment were monitored by UV spectroscopy and HPLC. • Nanocapsules had shown a complete release after 60 min in acidic environment

Chitosan/dextran multilayer microcapsules for polyphenol co-delivery

Energy Technology Data Exchange (ETDEWEB)

Paini, Marco, E-mail: marco.paini@unige.it [Department of Civil, Chemical and Environmental Engineering, University of Genoa, via Opera Pia 15, 16145 Genoa (Italy); Research Center for Biologically Inspired Engineering in Vascular Medicine and Longevity (BELONG), Via Montallegro 1, 16145 Genoa (Italy); Aliakbarian, Bahar; Casazza, Alessandro A.; Perego, Patrizia [Department of Civil, Chemical and Environmental Engineering, University of Genoa, via Opera Pia 15, 16145 Genoa (Italy); Research Center for Biologically Inspired Engineering in Vascular Medicine and Longevity (BELONG), Via Montallegro 1, 16145 Genoa (Italy); Ruggiero, Carmelina; Pastorino, Laura [Department of Informatics, Bioengineering, Robotics and Systems Engineering, University of Genoa, Via Opera Pia 13, 16145 Genoa (Italy)

2015-01-01

Polysaccharide-based nanostructured polymeric microcapsules were fabricated by the electrostatic layer-by-layer self-assembly technique and used to encapsulate mixtures of four different polyphenols in order to achieve their controlled release. The real-time fabrication of the dextran/chitosan multilayer was monitored by quartz crystal microbalance with dissipation monitoring, and the morphology of the nanostructured polymeric capsules was characterized by scanning electron microscopy. The polyphenol encapsulation was obtained by reversible permeability variation of the capsule shell in ethanol:water mixtures. The loading efficiency in different water:ethanol mixtures and the release rate in acidic conditions were characterized by UV spectroscopy and HPLC. The higher loading efficiency was obtained with an ethanol:water 35:65 phenolic solution, equal to 42.0 ± 0.6%, with a total release of 11.5 ± 0.7 mg of total polyphenols per 11.3 μL of microcapsules after 240 min of incubation in acidic environment. The results suggest that polysaccharide-based capsules can be successfully used to encapsulate and release low water-soluble molecules, such as polyphenols. - Highlights: • Chitosan/dextran nanocapsules were made by layer-by-layer self-assembly technique. • Different ethanol:water mixtures of four polyphenols were encapsulated. • An encapsulation efficiency of 42.0 ± 0.6% was obtained using ethanol:water 35:65. • Release profiles in acidic environment were monitored by UV spectroscopy and HPLC. • Nanocapsules had shown a complete release after 60 min in acidic environment.

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

Energy Technology Data Exchange (ETDEWEB)

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

2016-01-15

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

Design and Evaluation of Chitosan-Based Novel pHSensitive Drug ...

African Journals Online (AJOL)

Design and Evaluation of Chitosan-Based Novel pHSensitive Drug Carrier for Sustained ... Scanning electron microscopy(SEM),Raman spectroscopy for particle size analysis. Swelling ratio, Effect of drug loading on encapsulation efficiency

Chitosan nanoparticles enhances the anti-quorum sensing activity of kaempferol.

Science.gov (United States)

Ilk, Sedef; Sağlam, Necdet; Özgen, Mustafa; Korkusuz, Feza

2017-01-01

Quorum sensing (QS) is a cell density dependent expression of species in bacteria mediated by compounds called autoinducers (AI). Several processes responsible for successful establishment of bacterial infection are mediated by QS. Inhibition of QS is therefore being considered as a new target for antimicrobial chemotherapy. Flavonoid compounds are strong antioxidant and antimicrobial agents but their applications are limited due to their poor dissolution and bioavailability. Our objective was to investigate the effect of kaempferol loaded chitosan nanoparticles on modulating QS mediated by AI in model bioassay test systems. For this purpose, kaempferol loaded nanoparticles were synthesized and characterized in terms of hydrodynamic diameter, hydrogen bonding, amorphous transformation and antioxidant activity. QS inhibition in time dependent manner of nanoparticles was measured in violacein pigment producing using the biosensor strain Chromobacterium violaceum CV026 mediated by AI known as acylated homoserine lactone (AHL). Our results indicated that the average kaempferol loaded chitosan/TPP nanoparticle size and zeta potential were 192.27±13.6nm and +35mV, respectively. The loading and encapsulation efficiency of kaempferol into chitosan/TPP nanoparticles presented higher values between 78 and 93%. Kaempferol loaded chitosan/TPP nanoparticle during the 30 storage days significantly inhibited the production of violacein pigment in Chromobacterium violaceum CV026. The observation that kaempferol encapsulated chitosan nanoparticles can inhibit QS related processes opens up an exciting new strategy for antimicrobial chemotherapy as stable QS-based anti-biofilm agents. Copyright © 2016 Elsevier B.V. All rights reserved.

Ferritin glycosylated by chitosan as a novel EGCG nano-carrier: Structure, stability, and absorption analysis.

Science.gov (United States)

Yang, Rui; Liu, Yuqian; Gao, Yunjing; Wang, Yongjin; Blanchard, Chris; Zhou, Zhongkai

2017-12-01

Ferritin is a shell-like carrier protein with an 8nm diameter cavity which endows a natural space to encapsulate food and drug components. In this work, phytoferritin was unprecedentedly glycosylated by chitosan to fabricate ferritin-chitosan Maillard reaction products (FCMPs) (grafting degree of 26.17%, 24h, 55°C). Results indicated that the amide I and II bands of ferritin were altered due to the chitosan grafting, whereas the ferritin spherical structure were retained. Simulated digestion analysis showed that the FCMPs were more resistant to pepsin and trypsin digestion as compared with ferritin alone. Furthermore, FCMPs were employed as carrier to encapsulate epigallocatechin gallate (EGCG) molecules with an encapsulation ratio of 12.87% (w/w), and the resulting FCMPs-EGCG complexes showed a slow release of EGCG in simulated gastrointestinal tract. Interestingly, different types of food components displayed different effects in EGCG release behavior from the FCMPs, wherein proanthocyanidin, milk and soy protein inhibited the EGCG release. In addition, the absorption of EGCG encapsulated in FCMPs in Caco-2 monolayer model was significantly improved as compared with free EGCG. This work provides a novel nano-vehicle for fabricating core-shell systems in food and drug delivery domain. Copyright © 2017 Elsevier B.V. All rights reserved.

Preparing and Characterizing Chitosan Nanoparticles Containing Hemiscorpius lepturus Scorpion Venom as an Antigen Delivery System

Directory of Open Access Journals (Sweden)

Mohammadpour Dounighi, N.

2012-11-01

Full Text Available In recent years, chitosan nanoparticles have been studied widely for protein delivery. In this study, Hemiscorpius lepturus (HL venom was encapsulated in chitosan nanoparticles. The aim of the present work was to carry out a systematic study for preparing biocompatible and biodegradable nanoparticles for loading HL scorpion venom and to evaluate their potential as an antigen delivery system. In this study, HL venom loaded chitosan nanoparticles fabricated by ionic gelation of chitosan and tripolyphosphate and the factors which may be influenced in the preparation of nanoparticles were analyzed. Also, their physicochemical properties and in vitro release behavior were studied. The optimum encapsulation efficiency and capacity were observed when the chitosan concentration and HL venom were 2mg/ml and 500µg/ml, respectively. The HL venom loaded nanoparticles were in the size range of 130-160nm (polydispersity index values of 0.423 and exhibited the positive zeta potential. Transmission electron microscope imaging showed spherical and smooth surface of nanoparticles. The profiles of the release exhibited a burst releases about 50% in the first 4 hr and then slowed down at a constant rate. The obtained results suggested that the chitosan nanoparticles prepared in this work had the potential for antigen delivery.

Thiolated Chitosan Masked Polymeric Microspheres with Incorporated Mesocellular Silica Foam (MCF for Intranasal Delivery of Paliperidone

Directory of Open Access Journals (Sweden)

Stavroula Nanaki

2017-11-01

Full Text Available In this study, mesocellular silica foam (MCF was used to encapsulate paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. MCF with the drug adsorbed was further encapsulated into poly(lactic acid (PLA and poly(lactide-co-glycolide (PLGA 75/25 w/w microspheres and these have been coated with thiolated chitosan. As found by TEM analysis, thiolated chitosan formed a thin layer on the polymeric microspheres’ surface and was used in order to enhance their mucoadhesiveness. These microspheres aimed at the intranasal delivery of paliperidone. The DSC and XRD studies showed that paliperidone was encapsulated in amorphous form inside the MCF silica and for this reason its dissolution profile was enhanced compared to the neat drug. In coated microspheres, thiolated chitosan reduced the initial burst effect of the paliperidone dissolution profile and in all cases sustained release formulations have been prepared. The release mechanism was also theoretically studied and three kinetic models were proposed and successfully fitted for a dissolution profile of prepared formulations to be found.

ESI(+-MS and GC-MS Study of the Hydrolysis of N-Azobenzyl Derivatives of Chitosan

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Fernanda S. Pereira

2014-10-01

Full Text Available New N-p-chloro-, N-p-bromo-, and N-p-nitrophenylazobenzylchitosan derivatives, as well as the corresponding azophenyl and azophenyl-p-sulfonic acids, were synthesized by coupling N-benzylvchitosan with aryl diazonium salts. The synthesized molecules were analyzed by UV-Vis, FT-IR, 1H-NMR and 15N-NMR spectroscopy. The capacity of copper chelation by these materials was studied by AAS. Chitosan and the derivatives were subjected to hydrolysis and the products were analyzed by ESI(+-MS and GC-MS, confirming the formation of N-benzyl chitosan. Furthermore, the MS results indicate that a nucleophilic aromatic substitution (SnAr reaction occurs under hydrolysis conditions, yielding chloroaniline from N-p-bromo-, and N-p-nitrophenylazo-benzylchitosan as well as bromoaniline from N-p-chloro-, and N-p-nitrophenylazobenzyl-chitosan.

Hydrophobic lapatinib encapsulated dextran-chitosan nanoparticles using a toxic solvent free method: fabrication, release property & in vitro anti-cancer activity

Energy Technology Data Exchange (ETDEWEB)

Mobasseri, Rezvan [Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Center for Nanofibers & Nanotechnology, Department of Mechanical Engineering, National University of Singapore, 117576 (Singapore); Karimi, Mahdi [Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Tian, Lingling, E-mail: lingling_tian@nus.edu.sg [Center for Nanofibers & Nanotechnology, Department of Mechanical Engineering, National University of Singapore, 117576 (Singapore); Naderi-Manesh, Hossein, E-mail: naderman@modares.ac.ir [Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Department of Biophysics, Faculty of Biological Sciences, Tarbiat Modares University, Tehran (Iran, Islamic Republic of); Ramakrishna, Seeram [Center for Nanofibers & Nanotechnology, Department of Mechanical Engineering, National University of Singapore, 117576 (Singapore); Guangdong-Hongkong-Macau Institute of CNS Regeneration (GHMICR), Jinan University, Guangzhou 510632 (China)

2017-05-01

Dextran sulfate-chitosan (DS-CS) nanoparticles, which possesses properties such as nontoxicity, biocompatibility and biodegradability have been employed as drug carriers in cancer therapy. In this study, DS-CS nanoparticles were synthesized and their sizes were controlled by a modification of the divalent cations cross-linkers (Ca{sup 2+}, Zn{sup 2+} or Mg{sup 2+}). Based on the optimized processing parameters, lapatinib encapsulated nanoparticles were developed and characterized by Dynamics Light Scattering (DLS) measurements, Fourier Transform Infrared Spectroscopy (FT-IR) and Scanning Electron Microscopy (SEM). Calcium chloride (CaCl{sub 2}) facilitated the formation of bare (100.3 ± 0.80 nm) and drug-loaded nanoparticles (134.3 ± 1.3 nm) with narrow size distributions being the best cross-linker. The surface potential of drug-loaded nanoparticles was − 16.8 ± 0.47 mV and its entrapment and loading efficiency were 76.74 ± 1.73% and 47.36 ± 1.27%, respectively. Cellular internalization of nanoparticles was observed by fluorescence microscopy and MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) assay was used to determine cytotoxicity of bare and drug-loaded nanoparticles in comparison to the free drug lapatinib. The MTT assay showed that drug-loaded nanoparticles had comparable anticancer activity to free drug within a duration of 48 h. The aforementioned results showed that the DS-CS nanoparticles were able to entrap, protect and release the hydrophobic drug, lapatinib in a controlled pattern and could further serve as a suitable drug carrier for cancer therapy. - Highlights: • The best condition to prepare best size (about 100 nm) dextran-chitosan nanoparticles is proposed. • Divalent cationic cross-linker can act as hardener and compress the particles. • Drug/dextran mixing in a toxic solvent free method provides hydrophobic drug encapsulation within a hydrophilic system. • High entrapment efficiency of Lapatinib in polymeric

Preparation, Characterization and in Vivo Antimycobacterial Studies of Panchovillin-Chitosan Nanocomposites

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Edward Rwegasila

2016-09-01

Full Text Available Chitosan (CS, molecular weight 20.2 kDa, degree of deacylation (DD 73.31% was successfully obtained by deacetylation of chitin extracted from shrimp (Litopenaeus vannamei shell wastes. The encapsulation of the bioactive natural product, panchovillin (PANV, isolated from Erythrina schliebenii, on a chitosan-tripolyphosphate (CS/TPP nano-framework was achieved by ionotropic gelation. Characterization of pure CS, CS/TPP and PANV-CS/TPP nanocomposites was performed by FTIR, SEM and XRD. The molecular weight of chitosan and the thermal stability of the materials were determined by MALDI-TOF-MS and simultaneous thermal analyzer (STA/DTG, respectively. The respective encapsulation efficiency and loading capacity of the PANV were found to be 70% and 0.36%. The in vitro release studies showed an initial burst of 42% of PANV in the first six hours. This was followed by a slow and sustained release up to 72 h. The in vivo antimycobacterial activities of both PANV and PANV-CS/TPP nanocomposite against Mycobacterium indicus pranii (MIP using Galleria mellonella larvae as an in vivo infection model are reported in this paper.

The role of chitosan on oral delivery of peptide-loaded nanoparticle formulation.

Science.gov (United States)

Wong, Chun Y; Al-Salami, Hani; Dass, Crispin R

2017-12-01

Therapeutic peptides are conventionally administered via subcutaneous injection. Chitosan-based nanoparticles are gaining increased attention for their ability to serve as a carrier for oral delivery of peptides and vaccination. They offered superior biocompatibiltiy, controlled drug release profile and facilitated gastrointestinal (GI) absorption. The encapsulated peptides can withstand enzymatic degradation and various pH. Chitosan-based nanoparticles can also be modified by ligand conjugation to the surface of nanoparticle for transcellular absorption and specific-targeted delivery of macromolecules to the tissue of interest. Current research suggests that chitosan-based nanoparticles can deliver therapeutic peptide for the treatment of several medical conditions such as diabetes, bacterial infection and cancer. This review summarises the role of chitosan in oral nanoparticle delivery and identifies the clinical application of peptide-loaded chitosan-based nanoparticles.

In vitro evaluation of encapsulated primary rat hepatocytes pre- and post-cryopreservation at -80°C and in liquid nitrogen.

Science.gov (United States)

Durkut, Serap; Elçin, A Eser; Elçin, Y Murat

2015-02-01

Encapsulation techniques have the potential to protect hepatocytes from cryoinjury. In this study, we comparatively evaluated the viability and metabolic function of primary rat hepatocytes encapsulated in calcium alginate microbeads, in chitosan tripolyphosphate beads, and in three-layered alginate-chitosan-alginate (ACA) microcapsules, before and after cryopreservation at -80°C and in liquid nitrogen (LN2) for 1 and 3 months. Findings demonstrated that LN2 was atop of -80°C in regard to preservation of viability (> 90%) and hepatic functions. LN2-cryopreserved hepatocytes encapsulated in ACA microcapsules retained metabolic function post-thawing, with > 90% of the albumin, total protein and urea syntheses activities, and > 80% of oxidative function.

Synthesis, characterization, bioactivity and potential application of phenolic acid grafted chitosan: A review.

Science.gov (United States)

Liu, Jun; Pu, Huimin; Liu, Shuang; Kan, Juan; Jin, Changhai

2017-10-15

In recent years, increasing attention has been paid to the grafting of phenolic acid onto chitosan in order to enhance the bioactivity and widen the application of chitosan. Here, we present a comprehensive overview on the recent advances of phenolic acid grafted chitosan (phenolic acid-g-chitosan) in many aspects, including the synthetic method, structural characterization, biological activity, physicochemical property and potential application. In general, four kinds of techniques including carbodiimide based coupling, enzyme catalyzed grafting, free radical mediated grafting and electrochemical methods are frequently used for the synthesis of phenolic acid-g-chitosan. The structural characterization of phenolic acid-g-chitosan can be determined by several instrumental methods. The physicochemical properties of chitosan are greatly altered after grafting. As compared with chitosan, phenolic acid-g-chitosan exhibits enhanced antioxidant, antimicrobial, antitumor, anti-allergic, anti-inflammatory, anti-diabetic and acetylcholinesterase inhibitory activities. Notably, phenolic acid-g-chitosan shows potential applications in many fields as coating agent, packing material, encapsulation agent and bioadsorbent. Copyright © 2017 Elsevier Ltd. All rights reserved.

pH responsive N-succinyl chitosan/Poly (acrylamide-co-acrylic acid hydrogels and in vitro release of 5-fluorouracil.

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Shahid Bashir

Full Text Available There has been significant progress in the last few decades in addressing the biomedical applications of polymer hydrogels. Particularly, stimuli responsive hydrogels have been inspected as elegant drug delivery systems capable to deliver at the appropriate site of action within the specific time. The present work describes the synthesis of pH responsive semi-interpenetrating network (semi-IPN hydrogels of N-succinyl-chitosan (NSC via Schiff base mechanism using glutaraldehyde as a crosslinking agent and Poly (acrylamide-co-acrylic acid(Poly (AAm-co-AA was embedded within the N-succinyl chitosan network. The physico-chemical interactions were characterized by Fourier transform infrared (FTIR, X-ray diffraction (XRD, thermogravimetric analysis (TGA, and field emission scanning electron microscope (FESEM. The synthesized hydrogels constitute porous structure. The swelling ability was analyzed in physiological mediums of pH 7.4 and pH 1.2 at 37°C. Swelling properties of formulations with various amounts of NSC/ Poly (AAm-co-AA and crosslinking agent at pH 7.4 and pH 1.2 were investigated. Hydrogels showed higher swelling ratios at pH 7.4 while lower at pH 1.2. Swelling kinetics and diffusion parameters were also determined. Drug loading, encapsulation efficiency, and in vitro release of 5-fluorouracil (5-FU from the synthesized hydrogels were observed. In vitro release profile revealed the significant influence of pH, amount of NSC, Poly (AAm-co-AA, and crosslinking agent on the release of 5-FU. Accordingly, rapid and large release of drug was observed at pH 7.4 than at pH 1.2. The maximum encapsulation efficiency and release of 5-FU from SP2 were found to be 72.45% and 85.99%, respectively. Kinetics of drug release suggested controlled release mechanism of 5-FU is according to trend of non-Fickian. From the above results, it can be concluded that the synthesized hydrogels have capability to adapt their potential exploitation as targeted oral drug

Synthesis and properties of new cationic polymers on 2-[(methacryloyloxy)ethyl]trimethyl ammonium chloride and N-isopropylacrylamidet base

International Nuclear Information System (INIS)

Sergaziev, A.; Khutoryanskij, V.; Bajzhumanova, T.; Fefelova, N.; Nurkeeva, Z.

2003-01-01

New water-soluble cationic polyelectrolytes were synthesized by γ-radiation copolymerization of 2-[(methacryloyloxy)ethyl]trimethyl ammonium chloride and N-isopropylacrylamide. The phase transition of aqueous solutions of copolymers was studied with temperature increase in presence and absence of inorganic salts. The copolymers complexation with potassium hexacyano ferrates (II, III) was investigated. It was shown that the poly-complexes solubility depends on concentration of interacting reagents and temperature. (author)

Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.

Science.gov (United States)

Maliepaard, M; van Gastelen, M A; Tohgo, A; Hausheer, F H; van Waardenburg, R C; de Jong, L A; Pluim, D; Beijnen, J H; Schellens, J H

2001-04-01

This study was aimed at characterizing the role of BCRP/MXR/ABCP (BCRP) in resistance of the human ovarian tumor cell lines T8 and MX3 to camptothecins more extensively and investigating whether resistance can be reversed by inhibiting BCRP by GF120918. Camptothecins studied were topotecan, CPT-11, and its active metabolite SN-38, 9-aminocamptothecin, and the novel experimental camptothecins NX211, DX8951f, and BNP1350. Notably, DX8951f and BNP1350 appeared to be very poor substrates for BCRP, with much lower resistance factors observed both in T8 and MX3 cells than observed for the other camptothecins tested. In the presence of a nontoxic dose level of GF120918, the intracellular accumulation of topotecan in the T8 and MX3 cells was completely restored to the intracellular levels observed in the sensitive IGROV1 parental cell line. This resulted in almost complete reversal of drug resistance to topotecan and to most of the other topoisomerase I drugs tested in the T8 cell line and to complete reversal in the MX3 cells. However, coincubation of DX8951f or BNP1350 with GF120918 did not affect the cytotoxicity of either of these drugs significantly. From the combined data, we conclude that the affinities of topoisomerase I drugs for BCRP are, in decreasing order: SN-38 > topotecan > 9-aminocamptothecin approximately CPT-11 > NX211 > DX8951f > BNP1350. Furthermore, GF120918 appears to be a potent reversal agent of BCRP-mediated resistance to camptothecins, with almost complete reversal noted at 100 nM. Potential BCRP-mediated resistance to topoisomerase I inhibitors can also be avoided by using the BCRP-insensitive drugs DX8951f or BNP1350. This observation may have important clinical implications for future development of novel camptothecins.

Preparation and Characterization of Novel Cationic Chitosan Derivatives Bearing Quaternary Ammonium and Phosphonium Salts and Assessment of Their Antifungal Properties.

Science.gov (United States)

Tan, Wenqiang; Li, Qing; Dong, Fang; Chen, Qiuhong; Guo, Zhanyong

2017-08-31

Chitosan is an abundant and renewable polysaccharide, its derivatives exhibit attractive bioactivities and the wide applications in various biomedical fields. In this paper, two novel cationic chitosan derivatives modified with quaternary phosphonium salts were successfully synthesized via trimethylation, chloride acetylation, and quaternization with tricyclohexylphosphine and triphenylphosphine. The structures and properties of synthesized products in the reactions were characterized by FTIR spectroscopy, ¹H-NMR, 31 P-NMR, elemental and thermogravimetric analysis. The antifungal activities of chitosan derivatives against four kinds of phytopathogens, including Phomopsis asparagi , Watermelon fusarium , Colletotrichum lagenarium , and Fusarium oxysporum were tested using the radial growth assay in vitro. The results revealed that the synthesized cationic chitosan derivatives showed significantly improved antifungal efficiency compared to chitosan. It was reasonably suggested that quaternary phosphonium groups enabled the obviously stronger antifungal activity of the synthesized chitosans. Especially, the triphenylphosphonium-functionalized chitosan derivative inhibited the growth of Phomopsis asparagi most effectively, with inhibitory indices of about 80% at 0.5 mg/mL. Moreover, the data demonstrated that the substituted groups with stronger electron-withdrawing ability relatively possessed greater antifungal activity. The results suggest the possibility that cationic chitosan derivatives bearing quaternary phosphonium salts could be effectively employed as novel antifungal biomaterials for application in the field of agriculture.

Research on the combination of chitosan encapsulated porous calcium polyphosphate and rabbit osteoblasts%壳聚糖包裹的多孔聚磷酸钙生物陶瓷复合兔成骨细胞的实验研究

Institute of Scientific and Technical Information of China (English)

郭小凡; 范长春; 曹学成; 蔡锦方

2012-01-01

Objective To investigate the preparation of chitosan encapsulated poms calcium polyphosphate ( CPP) bioceramic and its combination with osteoblasts in vitro, in order to find a kind of biomaterial which can be used in the treatment of bone defect. Methods The chitosan microsphere was produced by method of latex coagulation and was used as the porogen. The porous CPP bioceramic was produced by method of microspheres accumulation and it was encapsulated by the chitosan by infiltration method. After that, the mechanical property of the chitosan encapsulated porous CPP bioceramic was tested. The rabbits bone marrow mesenchymal stem cells were isolated and induced into osteoblasts. We combined the CPP compound with the osteoblasts. The osteoblast morphologic and functional detection were performed. Results The CPP bioceramic turned out to be good at perforation and uniform holes inside. The compressive strength of CPP was 400 Mpa. The osteoblasts showed good appearance, cellularity and function after their combination with the chitosan encapsulated porous CPP bioceramic in vitro. Conclusions The chitosan encapsulated porous CPP bioceramic is good in both appearance and mechanical properties and it showed good compatibility with rabbit osteoblasts.%目的 探讨壳聚糖包裹的多孔聚磷酸钙(CPP)生物陶瓷的制备方法及其与兔成骨细胞在体外复合的情况,以探索一种可以应用于骨缺损治疗的生物材料.方法 采用乳液凝固法合成壳聚糖微球并将其作为后续步骤的致孔剂.采用微球堆积法制备多孔CPP,并通过浸润法使壳聚糖膜包裹于其上,随后对其进行生物力学性能测试.分离培养兔骨髓间充质干细胞并诱导成为成骨细胞,将其与壳聚糖膜包裹的多孔CPP生物陶瓷复合,观察复合后的成骨细胞生长情况,检测其生理活性.结果 制备出的多孔CPP生物陶瓷孔的分布较为均匀,贯通性较好,抗压强度约为400 MPa

Curcumin-cyclodextrin encapsulated chitosan nanoconjugates with enhanced solubility and cell cytotoxicity.

Science.gov (United States)

Popat, Amirali; Karmakar, Surajit; Jambhrunkar, Siddharth; Xu, Chun; Yu, Chengzhong

2014-05-01

Curcumin (CUR), a naturally derived anti-cancer cocktail is arguably the most widely studied neutraceutical. Despite a lot of promises, it is yet to reach the market as an active anti-cancer formulation. In the present study, we have prepared highly soluble (3 mg/ml) CUR-γ-hydroxypropyl cyclodextrin (CUR-CD) hollow spheres. CUR-CD hollow spheres were prepared by a novel and scalable spray drying method. CUR-CD was then encapsulated into positively charged biodegradable chitosan (CUR-CD-CS) nanoparticles. The CUR-CD-CS nanoparticles were characterised by TEM, SEM, DLS, drug loading and in vitro release. We tested the efficacy of these CUR-CD-CS nanoparticles in SCC25 cell lines using MTT assay and investigated its cellular uptake mechanism. We also studied Oligo DNA loading in CUR-CD-CS nanoparticles and its delivery via confocal imaging and FACS analysis. Our results demonstrated that CUR-CD-CS nanoparticles showed superior in vitro release performance and higher cytotoxicity in SCC25 cell line amongst all tested formulations. The cytotoxicity results were corroborated by cell cycle analysis and apoptosis test, showing nearly 100% apoptotic cell death in the case of CUR-CD-CS nanoparticles. Compared to CS nanoparticles, CS-CD nanoformulation showed higher cellular delivery of Cy3-Oligo DNA which was tested quantitatively using flowcytometry analysis, indicating that CD not only enhanced CUR solubility but also boosted the cellular uptake. Our study shows that rationally designed bio-degradable natural biomaterials have great potential as next generation nano-carriers for hydrophobic drug delivery such as CUR with potential of dual drug-gene delivery. Copyright © 2014 Elsevier B.V. All rights reserved.

Synthesis of position-specific tritium-labeled 20(S)-camptothecin, 9-amino-20(S)-camptothecin, and 10,11-methylenedioxy-20(S)-camptothecin

International Nuclear Information System (INIS)

Nicholas, A.W.; Wani, M.C.; Wall, M.E.; Kepler, J.A.; Taylor, G.F.

1993-01-01

The synthesis is given for three ring A tritiated camptothecin (CPT) analogs as biological probes in the study of the parent compounds which are of current widespread interest as potent anticancer agents. The strategy of catalytic tritolysis of aryl halide bonds was employed, and thus the preparations of the requisite precursors 9-chloro-20(S)-CPT, 9-amino-10,12-dibromo-20(S)-CPT, and 9-chloro-10,11-methylenedioxy-20(S)-CPT are given; catalytic tritiation of these respective precursors under polar, alkaline solvent conditions using palladium/carbon provides smooth conversion to [9- 3 H]-20(S)-CPT, 9-amino-[1012 3 H]-20(S)-CPT, and [9- 3 H]-10,11-methylenedioxy-20(S)-CPT. (author)

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

that fluorescently labelled SLN were detected in the brain after i.v. administration. This study indicates that the camptothecin-loaded SLN are a promising drug brain delivery system worth to explore further for brain tumour therapy. (C) 2012 Elsevier B. V. All rights reserved.......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 stabilise the lactone ring, which is essential for its antitumour activity, and for avoiding premature loss of drug on the way to target camptothecin to the brain. A multivariate approach was used to assess the influence of the qualitative and quantitative composition on the physicochemical properties...

Oral Methylated N-Aryl Chitosan Derivatives for Inducing Immune ...

African Journals Online (AJOL)

TM-CM-CS) and methylated N-(4-pyridinylmethyl) chitosan (TM-Py-CS), with Eqiva degree (equivalent degree) were studied by in vitro absorption enhancement on the transepithelial electrical resistance (TEER) in Caco-2 cell monolayers as ...

Chitosan based metallic nanocomposite scaffolds as antimicrobial wound dressings.

Science.gov (United States)

Mohandas, Annapoorna; Deepthi, S; Biswas, Raja; Jayakumar, R

2018-09-01

Chitosan based nanocomposite scaffolds have attracted wider applications in medicine, in the area of drug delivery, tissue engineering and wound healing. Chitosan matrix incorporated with nanometallic components has immense potential in the area of wound dressings due to its antimicrobial properties. This review focuses on the different combinations of Chitosan metal nanocomposites such as Chitosan/nAg, Chitosan/nAu, Chitosan/nCu, Chitosan/nZnO and Chitosan/nTiO 2 towards enhancement of healing or infection control with special reference to the antimicrobial mechanism of action and toxicity.

Mucosal Immunity and Protective Efficacy of Intranasal Inactivated Influenza Vaccine Is Improved by Chitosan Nanoparticle Delivery in Pigs

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Santosh Dhakal

2018-05-01

Full Text Available Annually, swine influenza A virus (SwIAV causes severe economic loss to swine industry. Currently used inactivated SwIAV vaccines administered by intramuscular injection provide homologous protection, but limited heterologous protection against constantly evolving field viruses, attributable to the induction of inadequate levels of mucosal IgA and cellular immune responses in the respiratory tract. A novel vaccine delivery platform using mucoadhesive chitosan nanoparticles (CNPs administered through intranasal (IN route has the potential to elicit strong mucosal and systemic immune responses in pigs. In this study, we evaluated the immune responses and cross-protective efficacy of IN chitosan encapsulated inactivated SwIAV vaccine in pigs. Killed SwIAV H1N2 (δ-lineage antigens (KAg were encapsulated in chitosan polymer-based nanoparticles (CNPs-KAg. The candidate vaccine was administered twice IN as mist to nursery pigs. Vaccinates and controls were then challenged with a zoonotic and virulent heterologous SwIAV H1N1 (γ-lineage. Pigs vaccinated with CNPs-KAg exhibited an enhanced IgG serum antibody and mucosal secretory IgA antibody responses in nasal swabs, bronchoalveolar lavage (BAL fluids, and lung lysates that were reactive against homologous (H1N2, heterologous (H1N1, and heterosubtypic (H3N2 influenza A virus strains. Prior to challenge, an increased frequency of cytotoxic T lymphocytes, antigen-specific lymphocyte proliferation, and recall IFN-γ secretion by restimulated peripheral blood mononuclear cells in CNPs-KAg compared to control KAg vaccinates were observed. In CNPs-KAg vaccinated pigs challenged with heterologous virus reduced severity of macroscopic and microscopic influenza-associated pulmonary lesions were observed. Importantly, the infectious SwIAV titers in nasal swabs [days post-challenge (DPC 4] and BAL fluid (DPC 6 were significantly (p < 0.05 reduced in CNPs-KAg vaccinates but not in KAg vaccinates when compared

Precipitation synthesis and magnetic properties of self-assembled magnetite-chitosan nanostructures

Energy Technology Data Exchange (ETDEWEB)

Bezdorozhev, Oleksii; Kolodiazhnyi, Taras; Vasylkiv, Oleg, E-mail: oleg.vasylkiv@nims.go.jp

2017-04-15

This paper reports the synthesis and magnetic properties of unique magnetite-chitosan nanostructures synthesized by the chemical precipitation of magnetite nanoparticles in the presence of chitosan. The influence of varying synthesis parameters on the morphology of the magnetic composites is determined. Depending on the synthesis parameters, magnetite-chitosan nanostructures of spherical (9–18 nm), rice-seed-like (75–290 nm) and lumpy (75–150 nm) shapes were obtained via self-assembly. Spherical nanostructures encapsulated by a 9–15 nm chitosan layer were assembled as well. The prospective morphology of the nanostructures is combined with their excellent magnetic characteristics. It was found that magnetite-chitosan nanostructures are ferromagnetic and pseudo-single domain. Rice-seed-like nanostructures exhibited a coercivity of 140 Oe and saturation magnetization of 56.7 emu/g at 300 K. However, a drop in the magnetic properties was observed for chitosan-coated spherical nanostructures due to the higher volume fraction of chitosan. - Highlights: • Magnetite-chitosan nanostructures are synthesized via self-assembly. • Different morphology can be obtained by adjusting the synthesis parameters. • An attractive combination of magnetic properties and morphology is obtained. • Magnetite-chitosan nanostructures are ferrimagnetic and pseudo-single domain.

Precipitation synthesis and magnetic properties of self-assembled magnetite-chitosan nanostructures

International Nuclear Information System (INIS)

Bezdorozhev, Oleksii; Kolodiazhnyi, Taras; Vasylkiv, Oleg

2017-01-01

This paper reports the synthesis and magnetic properties of unique magnetite-chitosan nanostructures synthesized by the chemical precipitation of magnetite nanoparticles in the presence of chitosan. The influence of varying synthesis parameters on the morphology of the magnetic composites is determined. Depending on the synthesis parameters, magnetite-chitosan nanostructures of spherical (9–18 nm), rice-seed-like (75–290 nm) and lumpy (75–150 nm) shapes were obtained via self-assembly. Spherical nanostructures encapsulated by a 9–15 nm chitosan layer were assembled as well. The prospective morphology of the nanostructures is combined with their excellent magnetic characteristics. It was found that magnetite-chitosan nanostructures are ferromagnetic and pseudo-single domain. Rice-seed-like nanostructures exhibited a coercivity of 140 Oe and saturation magnetization of 56.7 emu/g at 300 K. However, a drop in the magnetic properties was observed for chitosan-coated spherical nanostructures due to the higher volume fraction of chitosan. - Highlights: • Magnetite-chitosan nanostructures are synthesized via self-assembly. • Different morphology can be obtained by adjusting the synthesis parameters. • An attractive combination of magnetic properties and morphology is obtained. • Magnetite-chitosan nanostructures are ferrimagnetic and pseudo-single domain.

Еvaluation of biocompatibility and antioxidant efficiency of chitosan-alginate nanoparticles loaded with quercetin.

Science.gov (United States)

Aluani, Denitsa; Tzankova, Virginia; Kondeva-Burdina, Magdalena; Yordanov, Yordan; Nikolova, Elena; Odzhakov, Feodor; Apostolov, Alexandar; Markova, Tzvetanka; Yoncheva, Krassimira

2017-10-01

The present study deals with development and evaluation of the safety profile of chitosan/alginate nanoparticles as a platform for delivery of a natural antioxidant quercetin. The nanoparticles were prepared by varying the ratios between both biopolymers giving different size and charge of the formulations. The biocompatibility was explored in vitro in cells from different origin: cultivated HepG2 cells, isolated primary rat hepatocytes, isolated murine spleen lymphocytes and macrophages. In vivo toxicological evaluation was performed after repeated 14-day oral administration to rats. The study revealed that chitosan/alginate nanoparticles did not change body weight, the relative weight of rat livers, liver histology, hematology and biochemical parameters. The protective effects of quercetin-loaded nanoparticles were investigated in the models of iron/ascorbic acid (Fe 2+ /AA) induced lipid peroxidation in microsomes and tert-butyl hydroperoxide oxidative stress in isolated rat hepatocytes. Interesting finding was that the empty chitosan/alginate nanoparticles possessed protective activity themselves. The antioxidant effects of quercetin loaded into the nanoparticles formulated with higher concentration of chitosan were superior compared to quercetin encapsulated in nanoparticles with higher amount of sodium alginate. In conclusion, chitosan/alginate nanoparticles can be considered appropriate carrier for quercetin, combining safety profile and improved protective activity of the encapsulated antioxidant. Copyright © 2017 Elsevier B.V. All rights reserved.

Polyionic hydrocolloids for the intestinal delivery of protein drugs: alginate and chitosan--a review.

Science.gov (United States)

George, Meera; Abraham, T Emilia

2006-08-10

The protein pharmaceutical market is rapidly growing, since it is gaining support from the recombinant DNA technology. To deliver these drugs via the oral route, the most preferred route, is the toughest challenge. In the design of oral delivery of peptide or protein drugs, pH sensitive hydrogels like alginate and chitosan have attracted increasing attention, since most of the synthetic polymers are immunogenic and the incorporation of proteins in to these polymers require harsh environment which may denature and inactivate the desired protein. Alginate is a water-soluble linear polysaccharide composed of alternating blocks of 1-4 linked alpha-L-guluronic and beta-D-mannuronic acid residues where as chitosan is a co polymer of D-glucosamine and N-acetyl glucosamine. The incorporation of protein into these two matrices can be done under relatively mild environment and hence the chances of protein denaturation are minimal. The limitations of these polymers, like drug leaching during preparation can be overcome by different techniques which increase their encapsulation efficiency. Alginate, being an anionic polymer with carboxyl end groups, is a good mucoadhesive agent. The pore size of alginate gel microbeads has been shown to be between 5 and 200 nm and coated beads and microspheres are found to be better oral delivery vehicles. Cross-linked alginate has more capacity to retain the entrapped drugs and mixing of alginate with other polymers such as neutral gums, pectin, chitosan, and eudragit have been found to solve the problem of drug leaching. Chitosan has only limited ability for controlling the release of encapsulated compound due to its hydrophilic nature and easy solubility in acidic medium. By simple covalent modifications of the polymer, its physicochemical properties can be changed and can be made suitable for the peroral drug delivery purpose. Ionic interactions between positively charged amino groups in chitosan and the negatively charged mucus gel layer

Mucosal delivery of liposome-chitosan nanoparticle complexes.

Science.gov (United States)

Carvalho, Edison L S; Grenha, Ana; Remuñán-López, Carmen; Alonso, Maria José; Seijo, Begoña

2009-01-01

Designing adequate drug carriers has long been a major challenge for those working in drug delivery. Since drug delivery strategies have evolved for mucosal delivery as the outstanding alternative to parenteral administration, many new drug delivery systems have been developed which evidence promising properties to address specific issues. Colloidal carriers, such as nanoparticles and liposomes, have been referred to as the most valuable approaches, but still have some limitations that can become more inconvenient as a function of the specific characteristics of administration routes. To overcome these limitations, we developed a new drug delivery system that results from the combination of chitosan nanoparticles and liposomes, in an approach of combining their advantages, while avoiding their individual limitations. These lipid/chitosan nanoparticle complexes are, thus, expected to protect the encapsulated drug from harsh environmental conditions, while concomitantly providing its controlled release. To prepare these assemblies, two different strategies have been applied: one focusing on the simple hydration of a previously formed dry lipid film with a suspension of chitosan nanoparticles, and the other relying on the lyophilization of both basic structures (nanoparticles and liposomes) with a subsequent step of hydration with water. The developed systems are able to provide a controlled release of the encapsulated model peptide, insulin, evidencing release profiles that are dependent on their lipid composition. Moreover, satisfactory in vivo results have been obtained, confirming the potential of these newly developed drug delivery systems as drug carriers through distinct mucosal routes.

Chitosan-dextran sulfate hydrogels as a potential carrier for probiotics

DEFF Research Database (Denmark)

Yucel Falco, Cigdem; Falkman, Peter; Risbo, Jens

2017-01-01

Physical and chemical (crosslinked with genipin) hydrogels based on chitosan and dextran sulfate were developed and characterized as novel bio-materials suitable for probiotic encapsulation. The swelling of the hydrogels was dependent on the composition and weakly influenced by the pH of the media...

Preparation of thermal-responsive chitosan-graft-N-isopropylacrylamide membranes via γ-ray irradiation

International Nuclear Information System (INIS)

Mu Qing; Fang Yue'e

2006-01-01

Poly(N-isopropylacrylamide) (PNIPAAm) has been attracting increasing attention because of its thermosensitivity. Many authors have studied the reaction of chitosan with NIPAAm, with most of the interest being focused on hydrogels. Few research programs, however, were about chitosan membranes grafted with NIPAAm monomer. In this study, a novel thermo-sensitive switching membrane was prepared by radiation-induced simultaneous grafting of NIPAAm onto chitosan membrane. Fourier transform infrared spectroscopy (FT-IR) was used to identify structure of the grafted membranes. Compared to FT-IR spectra of pristine chitosan, the new band at 1535 cm-1 in the grafted membrane was attributed to amide II of PNIPAAm. This indicated that NIPAAm was introduced onto the chitosan membrane. Surface morphology of the grafted membrane was different from the pristine chitosan membrane. The SEM images revealed cypress leaf-like structures adhered tightly to the grafted membrane surface, in comparison to smooth surface of the pristine chitosan membrane. Pure water flux measurements showed that the grafted membrane decreased with the increasing temperature, while water flux of pristine chitosan membrane was constant. It was found that the grafted membrane was sensitive to temperature. The effects of dose, dose rate and the concentration of NIPAAm on the grafting percentage were discussed. The graft yield increased with the monomer concentration and the absorbed dose. (authors)

Preparation of N, N, N-trimethyl chitosan-functionalized retinoic acid ...

African Journals Online (AJOL)

nanocarrier (TR-SLNs) with enhanced anti-cancer activity. ... Retinoic acid (RA), a derivative of vitamin A, is a potential ... intravenous (i.v.) administration; therefore, RA ... °C. Preparation of TMC. TMC was synthesized by reductive methylation.

Preparation of microcapsules by complex coacervation of gum Arabic and chitosan.

Science.gov (United States)

Butstraen, Chloé; Salaün, Fabien

2014-01-01

Gum Arabic-chitosan microcapsules containing a commercially available blend of triglycerides (Miglyol 812 N) as core phase were synthesized by complex coacervation. This study was conducted to clarify the influence of different parameters on the encapsulation process, i.e. during the emulsion formation steps and during the shell formation, using conductometry, zeta potential, surface and interface tension measurement and Fourier-transform infrared spectroscopy. By carefully analyzing the influencing factors including phase volume ratio, stirring rate and time, pH, reaction time, biopolymer ratio and crosslinking effect, the optimum synthetic conditions were found out. For the emulsion step, the optimum phase volume ratio chosen was 0.10 and an emulsion time of 15 min at 11,000 rpm was selected. The results also indicated that the optimum formation of these complexes appears at a pH value of 3.6 and a weight ratio of chitosan to gum Arabic mixtures of 0.25. Copyright © 2013 Elsevier Ltd. All rights reserved.

The use of cross-linked chitosan beads for nutrients (nitrate and orthophosphate) removal from a mixture of P-PO4, N-NO2 and N-NO3.

Science.gov (United States)

Jóźwiak, Tomasz; Filipkowska, Urszula; Szymczyk, Paula; Kuczajowska-Zadrożna, Małgorzata; Mielcarek, Artur

2017-11-01

A hydrogel chitosan sorbent ionically cross-linked with sodium citrate and covalently cross-linked with epichlorohydrin was used to remove nutrients from an equimolar mixture of P-PO 4 , N-NO 2 and N-NO 3 . The scope of the study included, among other things, determination of the influence of pH on nutrient sorption effectiveness, nutrient sorption kinetics as well as determination of the maximum sorption capacity of cross-linked chitosan sorbents regarding P-PO 4 (H 2 PO 4 - , HPO 4 2- ), N-NO 2 (HNO 2 , NO 2 - ), and N-NO 3 (NO 3 - ). The effect of the type of the cross-linking agent on the affinity of the modified chitosan to each nutrient was studied as well. The kinetics of nutrient sorption on the tested chitosan sorbents was best described with the pseudo-second order model. The model of intramolecular diffusion showed that P-PO 4 , N-NO 2 and N-NO3 sorption on cross-linked hydrogel chitosan beads proceeded in two phases. The best sorbent of nutrients turned out to be chitosan cross-linked covalently with epichlorohydrin; with P-PO 4 , N-NO 2 and N-NO 3 sorption capacity reaching: 1.23, 0.94 and 0.76mmol/g, respectively (total of 2.92mmol/g). For comparison, the sorption capacity of chitosan cross-linked ionically with sodium citrate was: 0.43, 0.39 and 0.39mmol/g for P-PO 4 , N-NO 2 and N-NO 3 , respectively (total of 1.21mmol/g). Copyright © 2017 Elsevier B.V. All rights reserved.

Preparation of thermally stable microcapsules with a chitosan-silica hybrid.

Science.gov (United States)

Kang, Hong-Yi; Chen, Hui-Huang

2014-09-01

Addition of microcapsules with a high dielectric constant and low specific heat capacity to a battered layer was designed to create a higher temperature in the crust than in the prefried fish nuggets to prevent the water vapor in the fish nuggets from migrating to the crust during microwave heating. Therefore, chitosan-silica hybrids and soybean oil were utilized to prepare the shell and core of the thermally stable microcapsules (MC(CS)), respectively. The MC(CS) were prepared by sol-gel coacervation from an oil-in-water emulsion. The sodium silicate was hydrolyzed and coacervated through polymerization for 24 h at pH 5. The zeta potential analysis indicated that chitosan with a positive charge and silica with a negative charge interacted through electrostatic attraction to form a hybrid shell. The volume mean particle size and encapsulation efficiency of the MC(CS) were 9.6 ± 0.2 μm and 75.6% ± 1.3%, respectively, when oil/chitosan = 0.2 and chitosan/silica = 0.5 (w/w). In addition to H-bonding and electrostatic attraction, Si-O-N bonds were formed between chitosan and silica. Dehydration of the bound water in the MC(CS) was observed in the range of 25 to 250 °C in the differential scanning calorimetry thermal analysis, with the lack of apparent thermal peaks indicating its high thermal stability. The decrease of force to cut the crust observed by texture analysis as well as the increase of hedonic score by consumer acceptance test revealed the addition of 1% MC(CS) significantly improved the crispness of the crust in the microwave-reheated nuggets. © 2014 Institute of Food Technologists®

Interactions between chitosan and cells measured by AFM

Energy Technology Data Exchange (ETDEWEB)

Hsiao, Sheng-Wen; Thien, Doan Van Hong; Ho, Ming-Hua [Department of Chemical Engineering, National Taiwan University of Science and Technology, Taipei 10617, Taiwan (China); Hsieh, Hsyue-Jen [Department of Chemical Engineering, National Taiwan University, Taipei 10617, Taiwan (China); Li, Chung-Hsing [Division of Orthodontics and Pediatric Dentistry, Department of Dentistry, Tri-Service General Hospital, Taipei, Taiwan (China); Hung, Chang-Hsiang [Department of Dentistry, Kinmen Hospital Department of Health, Taiwan (China); Li, Hsi-Hsin, E-mail: mhho@mail.ntust.edu.t [Deputy Superintendent, Kinmen Hospital Department of Health, Taiwan (China)

2010-10-01

Chitosan, a biocompatible material that has been widely used in bone tissue engineering, is believed to have a high affinity to osteoblastic cells. This research is the first to prove this hypothesis. By using atomic force microscopy (AFM) with a chitosan-modified cantilever, quantitative evaluation of the interforce between chitosan and cells was carried out. A chitosan tip functionalized with Arg-Gly-Asp (RGD) was also used to measure the interforce between RGD-chitosan and osteoblastic cells. This research concluded by examining cell adhesion and spreading of chitosan substrates as further characterization of the interactions between cells and chitosan. The force measured by AFM showed that the interforce between chitosan and osteoblasts was the highest (209 nN). The smallest adhesion force (61.8 nN) appeared between chitosan and muscle fibroblasts, which did not demonstrate any osteoblastic properties. This result proved that there was a significant interaction between chitosan and bone cells, and correlated with the observations of cell attachment and spreading. The technique developed in this research directly quantified the adhesion between chitosan and cells. This is the first study to demonstrate that specific interaction exists between chitosan and osteoblasts.

Interactions between chitosan and cells measured by AFM

International Nuclear Information System (INIS)

Hsiao, Sheng-Wen; Thien, Doan Van Hong; Ho, Ming-Hua; Hsieh, Hsyue-Jen; Li, Chung-Hsing; Hung, Chang-Hsiang; Li, Hsi-Hsin

2010-01-01

Chitosan, a biocompatible material that has been widely used in bone tissue engineering, is believed to have a high affinity to osteoblastic cells. This research is the first to prove this hypothesis. By using atomic force microscopy (AFM) with a chitosan-modified cantilever, quantitative evaluation of the interforce between chitosan and cells was carried out. A chitosan tip functionalized with Arg-Gly-Asp (RGD) was also used to measure the interforce between RGD-chitosan and osteoblastic cells. This research concluded by examining cell adhesion and spreading of chitosan substrates as further characterization of the interactions between cells and chitosan. The force measured by AFM showed that the interforce between chitosan and osteoblasts was the highest (209 nN). The smallest adhesion force (61.8 nN) appeared between chitosan and muscle fibroblasts, which did not demonstrate any osteoblastic properties. This result proved that there was a significant interaction between chitosan and bone cells, and correlated with the observations of cell attachment and spreading. The technique developed in this research directly quantified the adhesion between chitosan and cells. This is the first study to demonstrate that specific interaction exists between chitosan and osteoblasts.

Cartilaginous extracellular matrix-modified chitosan hydrogels for cartilage tissue engineering.

Science.gov (United States)

Choi, Bogyu; Kim, Soyon; Lin, Brian; Wu, Benjamin M; Lee, Min

2014-11-26

Cartilaginous extracellular matrix (ECM) components such as type-II collagen (Col II) and chondroitin sulfate (CS) play a crucial role in chondrogenesis. However, direct clinical use of natural Col II or CS as scaffolds for cartilage tissue engineering is limited by their instability and rapid enzymatic degradation. Here, we investigate the incorporation of Col II and CS into injectable chitosan hydrogels designed to gel upon initiation by exposure to visible blue light (VBL) in the presence of riboflavin. Unmodified chitosan hydrogel supported proliferation and deposition of cartilaginous ECM by encapsulated chondrocytes and mesenchymal stem cells. The incorporation of native Col II or CS into chitosan hydrogels further increased chondrogenesis. The incorporation of Col II, in particular, was found to be responsible for the enhanced cellular condensation and chondrogenesis observed in modified hydrogels. This was mediated by integrin α10 binding to Col II, increasing cell-matrix adhesion. These findings demonstrate the potential of cartilage ECM-modified chitosan hydrogels as biomaterials to promote cartilage regeneration.

Entirely S-protected chitosan: A promising mucoadhesive excipient for metronidazole vaginal tablets.

Science.gov (United States)

Lupo, Noemi; Fodor, Benjamin; Muhammad, Ijaz; Yaqoob, Muhammad; Matuszczak, Barbara; Bernkop-Schnürch, Andreas

2017-12-01

Synthesis and evaluation of an entirely S-protected chitosan as mucoadhesive excipient for vaginal drug delivery. N-acetyl-cysteine was linked to 6-mercaptonicotinamide via disulphide exchange reaction. The obtained ligand, NAC-6-MNA, was subsequently attached to chitosan by carbodiimide mediated amide bond formation in two concentrations. The synthesized S-protected chitosan was chemically characterized and mucoadhesive properties and stability against oxidation were investigated. Moreover, metronidazole tablets comprising the S-protected chitosan were evaluated regarding water uptake capacity, disintegration behaviour, residence time on vaginal mucosa, release of the encapsulated drug and antimicrobial activity. S-protected chitosan displayed 160±19 (CS-MNA-160) and 320±38 (CS-MNA-320)µmol of ligand per gram of polymer. At pH 4.2, CS-MNA-160 and CS-MNA-320 showed 5.2-fold and 6.2-fold increase in mucus viscosity in comparison to unmodified chitosan (One-way ANOVA, pchitosan remained stable against oxidation in presence of 0.5%v/v hydrogen peroxide. Metronidazole tablets consisting in S-protected chitosan showed prolonged residence time on vaginal mucosa and improved water uptake capacity and disintegration time in comparison to tablets consisting of unmodified chitosan. Moreover, CS-MNA-320 metronidazole tablets displayed prolonged drug release and antimicrobial activity. On the basis of the achieved results, entirely S-protected chitosan represents a promising excipient for the development of metronidazole vaginal tablets. S-protected thiomers are polymers modified with thiol groups protected by aromatic ligands and characterized by strong mucoadhesive properties and high stability against oxidation. Up to date, the entirely S-protection of thiol groups was achieved via the synthesis of the ligand 2-((2-amino-2-carboxyethyl)disulfanyl)nicotinic acid) which can be directly bound to the backbone of polymers bearing carboxylic moieties as pectin. However, this

Controlled release of 9-nitro-20(S)-camptothecin from methoxy poly(ethylene glycol)-poly(D,L-lactide) micelles

Energy Technology Data Exchange (ETDEWEB)

Gao, J M [College of Material Science and Engineering, Southwest Jiaotong University, Chengdu 610031 (China); Ming, J [Department of Medicament, The Second People' s Hospital of Sichuan, Chengdu 610041 (China); He, B; Gu, Z W; Zhang, X D [National Engineering Research Center for Biomaterials, Sichuan University, Chengdu 610064 (China)], E-mail: zwgu@scu.edu.cn

2008-03-01

9-nitro-20(S)-camptothecin (9-NC) is a potent topoisomerase-I inhibitor, and it was applied for clinical trials in cancer treatment. However, the applications of 9-NC were limited by its poor solubility and instability. In order to overcome these disadvantages, 9-NC was encapsulated in amphiphilic copolymer micelles composed of methoxy poly(ethylene glycol)-b-poly(D,L-lactide) (mPEG-PDLLA, PELA). Three diblock copolymers with different PDLLA chain lengths were synthesized. The critical micelle concentration was varied from 10{sup -4} g L{sup -1} to 10{sup -2} g L{sup -1}. The 9-NC loaded micelles were nanospheres with diameters ranging from 30 nm to 60 nm. The relationship between the composition of copolymers and the drug loading content was discussed. The encapsulation of micelles improved the solubility of 9-NC greatly. The solubility of 9-NC in micelle M1 was about 250 times higher than that of 9-NC in a phosphate buffer solution (PBS). The stability of 9-NC in micelles was also promoted. After being incubated in PBS for 160 min, 80% of 9-NC in micelles existed as an active lactone form, while 85% of 9-NC in PBS were transferred to an inactive carboxylate salt form. The release experiments were carried out in PBS and the results showed that the release processes were controllable.

Effect of silibinin-loaded nano-niosomal coated with trimethyl chitosan on miRNAs expression in 2D and 3D models of T47D breast cancer cell line.

Science.gov (United States)

Yazdi Rouholamini, Seyede Elmira; Moghassemi, Saeid; Maharat, Zahra; Hakamivala, Amirhossien; Kashanian, Susan; Omidfar, Kobra

2018-05-01

Silibinin is a natural flavonoid with a strong antioxidant property and weak cytotoxic activity. It has demonstrated anti-tumoural activity against many types of malignancies; however, due to its hydrophobic structure, it has poor water solubility, bioavailability and permeability across intestinal epithelial cells. To improve the effect of silibinin, we have vehiculated silibinin by a highly stable niosomal nanostructure based on a Span 60/cholesterol (CH)/N-trimethyl chitosan (TMC) system in order to study its potential application for the delivery of silibinin in T47D cultured under three-dimensional (3D) and two-dimensional (2D) conditions. To study the effect of nanodrug on miRNAs expression, we evaluated quantitative expression of miRNA-21 and miRNA-15a as well as miR-141 and miR-200c which act as oncogene and tumour suppressors by real-time PCR. Results demonstrated that the mechanism of nanodrug action as well as the response of tumour cells differed in 3D culture as compared to 2D. Delivery of silibinin-loaded niosomes coated with TMC was found to be more effective in inhibiting the growth of tumour cells and inducing apoptosis than free silibinin administration. In silibinin-treated cells, death occurred in a dose- and time- dependent manner by induction of apoptosis and alteration of the cell cycle. Real-time PCR analysis revealed a decrease in miR-21, miR-15a and miR-141while increase in miR-200c expression levels was observed in silibinin-treated cells relative to the levels in the untreated cells. The results show that nanodrug delivery was more effective than free silibinin administration in changing the level of miRNAs expression in cancer cells. Therefore, niosomal nanostructure with TMC could be a suitable vehicle for hydrophobic compounds, such as silibinin, by improving their action in cancer therapy.

Chitosan nanoparticles from marine squid protect liver cells against N-diethylnitrosoamine-induced hepatocellular carcinoma.

Science.gov (United States)

Subhapradha, Namasivayam; Shanmugam, Vairamani; Shanmugam, Annaian

2017-09-01

Rationale of this study was framed to investigate the protective effect and anti-cancer property of nanoparticles based on chitosan isolated from squid, Sepioteuthis lessoniana, on hepatic cells in N-Nitrosodiethylamine-induced hepatocellular carcinoma in rats. The results conferred that the chitosan nanoparticle supplementation had a protective effect on liver cells by reducing the levels of marker enzymes and bilirubin and thus increasing the albumin levels. The level of reduced glutathione, ascorbic acid and α-tocopherol significantly increased in both post- and pre-treatment with chitosan nanoparticles. The levels of antioxidant enzymes were enhanced and lipid peroxidation products were diminished while treating nitrosodiethylamine-induced hepatocellular carcinoma with chitosan nanoparticles. Supplementation of chitosan nanoparticles had potent anti-hyperlipidemic property that was evidenced by monitoring the serum lipid levels and its components. Animals pre-treated with chitosan nanoparticles along with nitrosodiethylamine showed a significant reduction in the total cholesterol and triglycerides levels with increase in the levels of phospholipids and free fatty acids. Chitosan nanoparticles treated rats showed significant increment in high-density lipoprotein cholesterol and reduction in low-density lipoprotein and very low-density lipoprotein cholesterol when compared with levels in nitrosodiethylamine-induced hepatocellular carcinoma. Nitrosodiethylamine-induced carcinoma changes on circulation and hepatic antioxidant defense mechanism were regulated by chitosan nanoparticles, concluding that the chitosan nanoparticles have a potent protective effect on liver cells which might be due to its robust antioxidant and anti-lipidemic property. Copyright © 2017 Elsevier Ltd. All rights reserved.

Effects of pore CaCO3 form agencies on dissolution mechanisms of amoxicillin drugs encapsulated in hydrogels full-IPN chitosan N-vinyl caprolactam

Science.gov (United States)

Budianto, Emil; Fauzia, Maghfira

2018-04-01

The administration of amoxicillin trihydrate in Helicobacter pylori infection is not effective enough because the conventional preparations used have a short retention time in the stomach. To overcome this problem, amoxicillin trihydrate was encapsulated into the floating drug delivery matrix-matrix. In this study, the full-ipn acetaldehyde crosslinked hydrogel (N-vinyl caprolactam) was synthesized with a 10% CaCO3 pore forming agent and then encapsulated on amoxicillin trihydrate and studied the mechanism of drug dissolution with its kinetic kinetics approach. The K-PNVCL Hydrogel produces optimal properties which are then loaded with amoxicillin trihydrate in situ and post loading. In this research, we have got the percentage of swelling, floating time, the efficiency of in situ and post loading 873%; 3.15 minutes; 99.8% and 99.4%. The dissolution test was performed on amoxicillin trihydrate which had been encapsulated K-PNVCL hydrogel in vitro at pH 1.2 resulting in 94.5% for in situ loading and 98.5% for post loading. Results of the kinetics of drug release for post loading and in situ loading methods tend to follow the Higuchi model kinetics. The drug release mechanism occurs by Fickian diffusion. Proof of drug release mechanism from K-PNVCL hydrogel matrix is further done by Scanning Electron Microscope (SEM) instrument.

Characterization of bioactive chitosan and sulfated chitosan from Doryteuthis singhalensis (Ortmann, 1891).

Science.gov (United States)

Ramasamy, Pasiyappazham; Subhapradha, Namasivayam; Thinesh, Thangadurai; Selvin, Joseph; Selvan, Kanagaraj Muthamizh; Shanmugam, Vairamani; Shanmugam, Annaian

2017-06-01

Chitosan was extracted from the pen of squid Doryteuthis singhalensis and characterized using FT-IR, NMR, CHN, SEM and DSC analysis. Purified chitosan was sulfated with chlorosulfonic acid in N,N-dimethylformamide and the added sulfate group was confirmed with FT-IR analysis. The molecular weight and degree of deacetylation (DDA) of chitosan was found 226.6kDa and 83.76% respectively. Chitosan exhibited potent antioxidant activity evidenced by reducing power, chelating ability on ferrous ions and scavenging activity on DPPH, superoxide and hydroxyl radicals. The anticoagulant assay using activated partial thromboplastin time (APTT) and prothrombin time (PT) showed chitosan as a strong anticoagulant. The results of this study showed possibility of using D. singhalensis pen as a non-conventional source of natural antioxidants and anticoagulant which can be incorporated in functional food formulations. Copyright © 2017 Elsevier B.V. All rights reserved.

Preparation and Adsorption Ability of Polysulfone Microcapsules Containing Modified Chitosan Gel

Institute of Scientific and Technical Information of China (English)

CHEN Fei; LUO Guangsheng; YANG Weiwei; WANG Yujun

2005-01-01

Chemically modified chitosan beads containing polyethyleneimine (PEI) were prepared to improve the metal ion adsorption capacity of the chitosan beads and their mechanical stability and to limit their biodegradability. The modified beads were encapsulated with the polymer material polysulfone by a novel surface coating method named the emulsion phase inversion method. The adsorption properties of the modified beads and the microstructures of the polysulfone coating layer were then analyzed. The experimental results showed that the PEI was successfully linked onto the chitosan beads. The density of the -NH2 groups in the modified beads was significantly increased, while the water content was reduced. The coating layer thickness was about 200 (m. The modified chitosan gel beads had excellent Cu(II) adsorption capacity, with a maximum Cu(II) adsorption capacity 1.34 times higher than that of the unmodified beads. The results show that even with the polysulfone coating the adsorption kinetics of the modified beads is still better than those of the unmodified beads. The modifications improve the mass transfer performance of the chitosan beads as well as the bead stability.

Synthesis of position-specific tritium-labeled 20(S)-camptothecin, 9-amino-20(S)-camptothecin, and 10,11-methylenedioxy-20(S)-camptothecin. [Anticancer agents

Energy Technology Data Exchange (ETDEWEB)

Nicholas, A.W.; Wani, M.C.; Wall, M.E.; Kepler, J.A.; Taylor, G.F. (Research Triangle Inst., Research Triangle Park, NC (United States))

1993-09-01

The synthesis is given for three ring A tritiated camptothecin (CPT) analogs as biological probes in the study of the parent compounds which are of current widespread interest as potent anticancer agents. The strategy of catalytic tritolysis of aryl halide bonds was employed, and thus the preparations of the requisite precursors 9-chloro-20(S)-CPT, 9-amino-10,12-dibromo-20(S)-CPT, and 9-chloro-10,11-methylenedioxy-20(S)-CPT are given; catalytic tritiation of these respective precursors under polar, alkaline solvent conditions using palladium/carbon provides smooth conversion to [9-[sup 3]H]-20(S)-CPT, 9-amino-[1012[sup 3]H]-20(S)-CPT, and [9-[sup 3]H]-10,11-methylenedioxy-20(S)-CPT. (author).

Mucosal Immunity and Protective Efficacy of Intranasal Inactivated Influenza Vaccine Is Improved by Chitosan Nanoparticle Delivery in Pigs.

Science.gov (United States)

Dhakal, Santosh; Renu, Sankar; Ghimire, Shristi; Shaan Lakshmanappa, Yashavanth; Hogshead, Bradley T; Feliciano-Ruiz, Ninoshkaly; Lu, Fangjia; HogenEsch, Harm; Krakowka, Steven; Lee, Chang Won; Renukaradhya, Gourapura J

2018-01-01

Annually, swine influenza A virus (SwIAV) causes severe economic loss to swine industry. Currently used inactivated SwIAV vaccines administered by intramuscular injection provide homologous protection, but limited heterologous protection against constantly evolving field viruses, attributable to the induction of inadequate levels of mucosal IgA and cellular immune responses in the respiratory tract. A novel vaccine delivery platform using mucoadhesive chitosan nanoparticles (CNPs) administered through intranasal (IN) route has the potential to elicit strong mucosal and systemic immune responses in pigs. In this study, we evaluated the immune responses and cross-protective efficacy of IN chitosan encapsulated inactivated SwIAV vaccine in pigs. Killed SwIAV H1N2 (δ-lineage) antigens (KAg) were encapsulated in chitosan polymer-based nanoparticles (CNPs-KAg). The candidate vaccine was administered twice IN as mist to nursery pigs. Vaccinates and controls were then challenged with a zoonotic and virulent heterologous SwIAV H1N1 (γ-lineage). Pigs vaccinated with CNPs-KAg exhibited an enhanced IgG serum antibody and mucosal secretory IgA antibody responses in nasal swabs, bronchoalveolar lavage (BAL) fluids, and lung lysates that were reactive against homologous (H1N2), heterologous (H1N1), and heterosubtypic (H3N2) influenza A virus strains. Prior to challenge, an increased frequency of cytotoxic T lymphocytes, antigen-specific lymphocyte proliferation, and recall IFN-γ secretion by restimulated peripheral blood mononuclear cells in CNPs-KAg compared to control KAg vaccinates were observed. In CNPs-KAg vaccinated pigs challenged with heterologous virus reduced severity of macroscopic and microscopic influenza-associated pulmonary lesions were observed. Importantly, the infectious SwIAV titers in nasal swabs [days post-challenge (DPC) 4] and BAL fluid (DPC 6) were significantly ( p  influenza nanovaccine may be an ideal candidate vaccine for use in pigs, and pig is a

Molecular orbital calculations for the formation of GaN layers on ultra-thin AlN/6H-SiC surface using alternating pulsative supply of gaseous trimethyl gallium (TMG) and NH sub 3

CERN Document Server

Seong, S Y

2001-01-01

The steps for the generation of very thin GaN films on ultrathin AlN/6H-SiC surface by alternating a pulsative supply (APS) of trimethyl gallium and NH sub 3 gases have been examined by ASED-MO calculations. We postulate that the gallium clusters was formed with the evaporation of CH sub 4 gases via the decomposition of trimethyl gallium (TMG), dimethyl gallium (DMG), and monomethyl gallium (MMG). During the injection of NH sub 3 gas into the reactor, the atomic hydrogens were produced from the thermal decomposition of NH sub 3 molecule. These hydrogen gases activated the Ga-C bond cleavage. An energetically stable GaN nucleation site was formed via nitrogen incorporation into the layer of gallium cluster. The nitrogen atoms produced from the thermal degradation of NH sub 3 were expected to incorporate into the edge of the gallium cluster since the galliums bind weakly to each other (0.19 eV). The structure was stabilized by 2.08 eV, as an adsorbed N atom incorporated into a tetrahedral site of the Ga cluster...

UV-screening chitosan nanocontainers: increasing the photostability of encapsulated materials and controlled release

International Nuclear Information System (INIS)

Anumansirikul, Nattaporm; Wittayasuporn, Mayura; Klinubol, Patcharawalai; Tachaprutinun, A; Wanichwecharungruang, Supason P

2008-01-01

Methyl ether terminated poly(ethylene glycol)-4-methoxycinnamoylphthaloylchitosan (PCPLC), a UV absorptive polymer, and methyl ether terminated poly(ethylene glycol)-phthaloylchitosan (PPLC) were synthesized, characterized and self-assembled into stable water-dispersible spherical nanoparticles. The encapsulation of a model compound, 2-ethylhexyl-4-methoxycinnamate (EHMC), was carried out to give particles with 67% (w/w) EHMC loading. The E to Z photoisomerization of EHMC encapsulated inside both particles was monitored and compared to non-encapsulated EHMC. Minimal E to Z photoisomerization was observed when EHMC was encapsulated in PCPLC particles prepared from a polymer with a maximum degree of 4-methoxycinnamoyl substitution. The results indicated that the grafted UVB absorptive chromophore, 4-methoxycinnamoyl moieties, situated at the shell of PCPLC nanoparticles acted as a UV-filtering barrier, protecting the encapsulated EHMC from the UVB radiation, thus minimizing its photoisomerization. In vitro experiments revealed the pH-dependent controlled release of EHMC from PCPLC and PPLC particles. Ex vivo experiments, using a Franz diffusion cell with baby mouse skin, indicated that neither PPLC nor PCPLC particles could penetrate the skin into the receptor medium after a 24 h topical application. When applied on the baby mouse skin, both EHMC-encapsulated PPLC and EHMC-encapsulated PCPLC showed comparable controlled releases of the EHMC. The released EHMC could transdermally penetrate the baby mouse skin

UV-screening chitosan nanocontainers: increasing the photostability of encapsulated materials and controlled release

Science.gov (United States)

Anumansirikul, Nattaporm; Wittayasuporn, Mayura; Klinubol, Patcharawalai; Tachaprutinun, A.; Wanichwecharungruang, Supason P.

2008-05-01

Methyl ether terminated poly(ethylene glycol)-4-methoxycinnamoylphthaloylchitosan (PCPLC), a UV absorptive polymer, and methyl ether terminated poly(ethylene glycol)-phthaloylchitosan (PPLC) were synthesized, characterized and self-assembled into stable water-dispersible spherical nanoparticles. The encapsulation of a model compound, 2-ethylhexyl-4-methoxycinnamate (EHMC), was carried out to give particles with 67% (w/w) EHMC loading. The E to Z photoisomerization of EHMC encapsulated inside both particles was monitored and compared to non-encapsulated EHMC. Minimal E to Z photoisomerization was observed when EHMC was encapsulated in PCPLC particles prepared from a polymer with a maximum degree of 4-methoxycinnamoyl substitution. The results indicated that the grafted UVB absorptive chromophore, 4-methoxycinnamoyl moieties, situated at the shell of PCPLC nanoparticles acted as a UV-filtering barrier, protecting the encapsulated EHMC from the UVB radiation, thus minimizing its photoisomerization. In vitro experiments revealed the pH-dependent controlled release of EHMC from PCPLC and PPLC particles. Ex vivo experiments, using a Franz diffusion cell with baby mouse skin, indicated that neither PPLC nor PCPLC particles could penetrate the skin into the receptor medium after a 24 h topical application. When applied on the baby mouse skin, both EHMC-encapsulated PPLC and EHMC-encapsulated PCPLC showed comparable controlled releases of the EHMC. The released EHMC could transdermally penetrate the baby mouse skin.

Thymidine selectively enhances growth suppressive effects of camptothecin/irinotecan in MSI+ cells and tumors containing a mutation of MRE11

DEFF Research Database (Denmark)

Rodriguez, Rene; Hansen, Lasse Tengbjerg; Phear, Geraldine

2008-01-01

to exploit the altered response of mismatch repair (MMR)-deficient colon cancer cells and tumors to camptothecin or irinotecan and thymidine by combining them to improve therapeutic response. EXPERIMENTAL DESIGN: A panel of colon cancer cell lines was assayed for response to camptothecin...

Chitosan microparticles: influence of the gelation process on the release profile and oral bioavailability of albendazole, a class II compound.

Science.gov (United States)

Piccirilli, Gisela N; García, Agustina; Leonardi, Darío; Mamprin, María E; Bolmaro, Raúl E; Salomón, Claudio J; Lamas, María C

2014-11-01

Encapsulation of albendazole, a class II compound, into polymeric microparticles based on chitosan-sodium lauryl sulfate was investigated as a strategy to improve drug dissolution and oral bioavailability. The microparticles were prepared by spray drying technique and further characterized by means of X-ray powder diffractometry, infrared spectroscopy and scanning electron microscopy. The formation of a novel polymeric structure between chitosan and sodium lauryl sulfate, after the internal or external gelation process, was observed by infrared spectroscopy. The efficiency of encapsulation was found to be between 60 and 85% depending on the internal or external gelation process. Almost spherically spray dried microparticles were observed using scanning electron microscopy. In vitro dissolution results indicated that the microparticles prepared by internal gelation released 8% of the drug within 30 min, while the microparticles prepared by external gelation released 67% within 30 min. It was observed that the AUC and Cmax values of ABZ from microparticles were greatly improved, in comparison with the non-encapsulated drug. In conclusion, the release properties and oral bioavailability of albendazole were greatly improved by using spraydried chitosan-sodium lauryl sulphate microparticles.

Electrospun Xanthan gum-Chitosan nanofibers as delivery carrier of hydrophobic bioactives

DEFF Research Database (Denmark)

Shekarforoush, Elhamalsadat; Ajalloueian, Fatemeh; Zeng, Guanghong

2018-01-01

Viscoelastic gels of xanthan gum-chitosan(X-Ch) were electrospun to produce nanofibers, stable in aqueous media, for the encapsulation and release of curcumin (Cu). After 120h, the nanofibers released lower amount of curcumin (∼20%) at pH 2.2 comparatively to the release in neutral media (∼50...

The sustained-release behavior and in vitro and in vivo transfection of pEGFP-loaded core-shell-structured chitosan-based composite particles

Science.gov (United States)

Wang, Yun; Lin, Fu-xing; Zhao, Yu; Wang, Mo-zhen; Ge, Xue-wu; Gong, Zheng-xing; Bao, Dan-dan; Gu, Yu-fang

2014-01-01

Novel submicron core-shell-structured chitosan-based composite particles encapsulated with enhanced green fluorescent protein plasmids (pEGFP) were prepared by complex coacervation method. The core was pEGFP-loaded thiolated N-alkylated chitosan (TACS) and the shell was pH- and temperature-responsive hydroxybutyl chitosan (HBC). pEGFP-loaded TACS-HBC composite particles were spherical, and had a mean diameter of approximately 120 nm, as measured by transmission electron microscopy and particle size analyzer. pEGFP showed sustained release in vitro for >15 days. Furthermore, in vitro transfection in human embryonic kidney 293T and human cervix epithelial cells, and in vivo transfection in mice skeletal muscle of loaded pEGFP, were investigated. Results showed that the expression of loaded pEGFP, both in vitro and in vivo, was slow but could be sustained over a long period. pEGFP expression in mice skeletal muscle was sustained for >60 days. This work indicates that these submicron core-shell-structured chitosan-based composite particles could potentially be used as a gene vector for in vivo controlled gene transfection. PMID:25364253

Molecular orbital calculations for the formation of GaN layers on ultra-thin AlN/6H-SiC surface using alternating pulsative supply of gaseous trimethyl gallium (TMG) and NH3

International Nuclear Information System (INIS)

Seong, See Yearl; Hwang, Jin Soo

2001-01-01

The steps for the generation of very thin GaN films on ultrathin AlN/6H-SiC surface by alternating a pulsative supply (APS) of trimethyl gallium and NH 3 gases have been examined by ASED-MO calculations. We postulate that the gallium clusters was formed with the evaporation of CH 4 gases via the decomposition of trimethyl gallium (TMG), dimethyl gallium (DMG), and monomethyl gallium (MMG). During the injection of NH 3 gas into the reactor, the atomic hydrogens were produced from the thermal decomposition of NH 3 molecule. These hydrogen gases activated the Ga-C bond cleavage. An energetically stable GaN nucleation site was formed via nitrogen incorporation into the layer of gallium cluster. The nitrogen atoms produced from the thermal degradation of NH 3 were expected to incorporate into the edge of the gallium cluster since the galliums bind weakly to each other (0.19 eV). The structure was stabilized by 2.08 eV, as an adsorbed N atom incorporated into a tetrahedral site of the Ga cluster. This suggests that the adhesion of the initial layer can be reinforced by the incorporation of nitrogen atom through the formation of large grain boundary GaN crystals at the early stage of GaN film growth

Transport mechanism of chitosan-N-acetylcysteine, chitosan oligosaccharides or carboxymethyl chitosan decorated coumarin-6 loaded nanostructured lipid carriers across the rabbit ocular.

Science.gov (United States)

Li, Jinyu; Tan, Guoxin; Cheng, Bingchao; Liu, Dandan; Pan, Weisan

2017-11-01

To facilitate the hydrophobic drugs modeled by coumarin-6 (Cou-6) acrossing the cornea to the anterior chamber of the rabbit eye, chitosan (CS) derivatives including chitosan-N-acetyl-l-cysteine (CS-NAC), chitosan oligosaccharides (COS) and carboxymethyl chitosan (CMCS) modified nanostructured lipid carriers (NLCs) were designed and characterized. We found that, with similar size distribution and positivecharges, different CS derivatives based on NLCs led to distinctive delivery performance. In vivo precorneal retention study on rabbits revealed that these CS derivatives coating exhibited a stronger resistant effect than Cou-6 eye drops and Cou-6-NLC (P<0.05), moreover, the AUC (0-∞) , C max and MRT (0-∞) of them followed the sequence of CMCS-Cou-6-NLC

Characterization of DNA topoisomerase-1 in Spodoptera exigua for toxicity evaluation of camptothecin and hydoxy-camptothecin.

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Lan Zhang

Full Text Available Camptothecin (CPT, a plant alkaloid originally isolated from the native Chinese tree, Camptotheca acuminate, exerts the toxic effect by targeting eukaryotic DNA topoisomerase 1 (DNA Topo1. Besides as potent anti-cancer agents, CPT and its derivatives are now being explored as potential pesticides for insect control. In this study, we assessed their toxicity to an insect homolog, the Topo1 protein from beet armyworms (Spodoptera exigua Hübner, a worldwide pest of many important crops. The S. exigua Topo1 gene contains an ORF of 2790 base pairs that is predicted to encode a polypeptide of 930 amino acids. The deduced polypeptide exhibits polymorphism at residue sites V420, L530, A653 and T729 (numbered according to human Topo1 among insect species, which are predicted to confer sensitivity to CPT. The DNA relaxation activity of this protein was subsequently examined using a truncated form that contained the residues 337-930 and was expressed in bacteria BL21 cells. The purified protein retained the ability to relax double-stranded DNA and was susceptible to CPT and its derivative hydroxy-camptothecin (HCPT in a dose-dependent manner. The same inhibitory effect was also found on the native Topo1 extracted from IOZCAS-Spex-II cells, a cell line established from beet armyworms. Additionally, CPT and HCPT treatment reduced the steady accumulation of Topo1 protein despite the increased mRNA expression in response to the treatment. Our studies provide information of the S. exigua Topo1 gene and its amino acid polymorphism in insects and uncover some clues about potential mechanisms of CPT toxicity against insect pests. These results also are useful for development of more effective Topo1-targeted CPT insecticides in the future.

Chitosan-folate decorated carbon nanotubes for site specific lung cancer delivery.

Science.gov (United States)

Singh, Rahul Pratap; Sharma, Gunjan; Sonali; Singh, Sanjay; Bharti, Shreekant; Pandey, Bajarangprasad L; Koch, Biplob; Muthu, Madaswamy S

2017-08-01

The aim of this work was to formulate chitosan-folate conjugated multi-walled carbon nanotubes for the lung cancer targeted delivery of docetaxel. The chitosan-folate conjugate was synthesized and the conjugation was confirmed by Fourier transform infrared spectroscopy. The multi-walled carbon nanotubes were characterized for their particle size, polydispersity, zeta potential, surface morphology, drug encapsulation efficiency and in vitro release study. The in vitro cellular uptake, cytotoxicity, and cell cycle analysis of the docetaxel/coumarin-6 loaded multi-walled carbon nanotubes were carried out to compare the effectiveness of the formulations. The biocompatibility and safety of chitosan-folate conjugated multi-walled carbon nanotubes was analyzed by lung histopathology in comparison with marketed docetaxel formulation (Docel™) and acylated multi-walled carbon nanotubes. The cellular internalization study shown that the chitosan-folate conjugated multi-walled carbon nanotubes could be easily internalized into the lung cancer cells through a folate receptor-mediated endocytic pathway. The IC 50 values exhibited that chitosan-folate conjugated multi-walled carbon nanotubes could be 89-fold more effective than Docel™ in human lung cancer cells (A549 cells). Copyright © 2017 Elsevier B.V. All rights reserved.

Biological evaluation of 99m Tc-N-(3-bromo-trimethyl-acetanilide)-iminodiacetic acid (99mTc mebrofenin) as hepatobiliary radiopharmaceutical

International Nuclear Information System (INIS)

Hamada, E.S.

1994-01-01

Technetium-99 m-N-(3-bromo-2,4,6-trimethyl acetanilide) iminodiacetic acid ( 99m Tc-Mebrofenin) has been described as having optimal properties as hepatobiliary radiopharmaceutical. This paper describes the synthesis, radiopharmaceutical preparation and biological distribution of new labeled compound. The biodistribution study of 99m Tc-Mebrofenin- was carried out in normal mice. The specificity for hepatobiliary excretion blood clearance and cumulative biliary excretion were evaluated in normal and cirrhotic rats. (author). 5 refs, 3 figs, 3 tabs

Determination of the parameters of binding between lipopolysaccharide and chitosan and its N-acetylated derivative using a gravimetric piezoquartz biosensor.

Science.gov (United States)

Naberezhnykh, G A; Gorbach, V I; Kalmykova, E N; Solov'eva, T F

2015-03-01

The interaction of endotoxin (lipopolysaccharide - LPS) with low molecular weight chitosan (5.5 kDa), its N-acylated derivative and chitoliposomes was studied using a gravimetric piezoelectric quartz crystal microbalance biosensor. The optimal conditions for the formation of a biolayer based on immobilized LPS on the resonator surface and its regeneration were elaborated. The association and dissociation rate constants for LPS binding to chitosans were determined and the affinity constants (Kaf) were calculated based on the data on changes in the oscillation frequency of the quartz crystal resonator. The Kaf values correlated with the ones obtained using other methods. The affinity of N-acylated chitosan binding to LPS was higher than that of the parent chitosan binding to LPS. Based on the results obtained, we suggest that water-soluble N-acylated derivatives of chitosan with low degree of substitution of amino groups could be useful compounds for endotoxin binding and neutralization. Copyright © 2015 Elsevier B.V. All rights reserved.

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

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Zhang Hu

2012-01-01

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

Formation of nanoparticles by cooperative inclusion between (S-camptothecin-modified dextrans and β-cyclodextrin polymers

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Thorbjørn Terndrup Nielsen

2015-01-01

Full Text Available Novel (S-camptothecin–dextran polymers were obtained by “click” grafting of azide-modified (S-camptothecin and alkyne-modified dextrans. Two series based on 10 kDa and 70 kDa dextrans were prepared with a degree of substitution of (S-camptothecin between 3.1 and 10.2%. The binding properties with β-cyclodextrin and β-cyclodextrin polymers were measured by isothermal titration calorimetry and fluorescence spectroscopy, showing no binding with β-cyclodextrin but high binding with β-cyclodextrin polymers. In aqueous solution nanoparticles were formed from association between the (S-camptothecin–dextran polymers and the β-cyclodextrin polymers.

Production of secondary metabolites trimethyl xanthina by Camellia sinensis L suspension culture

Science.gov (United States)

Sutini, Sodiq, Mochamad; Muslihatin, Wirdhatul; Indra, Mochamad Rasjad

2017-06-01

Bioactive trimethyl xanthina can be obtained from the plant Camellia sinensis L. To obtain bioactive plant of which there are several hurdles for instance to wait up to five years to be harvested, also it needs land at a certain height from the sea level. Therefore, the production of secondary metabolites trimethyl xanthina need to be developed with suspense culture techniques. The purpose of this study obtained the production of bioactive trimethyl xanthina way culturally suspense in large scale with a relatively short time, potentially as anti-oxidants. Research methods include: (1) initiation of callus from pieces of leaves, shoots the youngest of the plant Camellia sinensis L in the media MS with the optimization of the addition of growth regulators, (2) the subculture of callus on media and plant growth regulator that is equal to the stage of initiation, (3) initiation of suspension culture using explants of callus Camellia sinensis L, (4) Analysis of secondary metabolites trimethyl xanthina growth in suspension culture, (5) the isolation and identification of trimethyl xanthina qualitatively and quantitatively using thin layer chromatography/high performance chromatography column. The results of the study suspension cultures containing bioactive trimethyl xanthina candidates that can be used as an antioxidant.

Multiple-Site Trimethylation of Ribosomal Protein L11 by the PrmA Methyltransferase

Energy Technology Data Exchange (ETDEWEB)

Demirci,H.; Gregory, S.; Dahlberg, A.; Jogl, G.

2008-01-01

Ribosomal protein L11 is a universally conserved component of the large subunit, and plays a significant role during initiation, elongation, and termination of protein synthesis. In Escherichia coli, the lysine methyltransferase PrmA trimethylates the N-terminal a-amino group and the -amino groups of Lys3 and Lys39. Here, we report four PrmA-L11 complex structures in different orientations with respect to the PrmA active site. Two structures capture the L11 N-terminal a-amino group in the active site in a trimethylated postcatalytic state and in a dimethylated state with bound S-adenosyl-L-homocysteine. Two other structures show L11 in a catalytic orientation to modify Lys39 and in a noncatalytic orientation. The comparison of complex structures in different orientations with a minimal substrate recognition complex shows that the binding mode remains conserved in all L11 orientations, and that substrate orientation is brought about by the unusual interdomain flexibility of PrmA.

Chitosan/lecithin liposomal nanovesicles as an oral insulin delivery system.

Science.gov (United States)

Al-Remawi, Mayyas; Elsayed, Amani; Maghrabi, Ibrahim; Hamaidi, Mohammad; Jaber, Nisrein

2017-05-01

In the present work, insulin-chitosan polyelectrolyte complexes associated to lecithin liposomes were investigated as a new carrier for oral delivery of insulin. The preparation was characterized in terms of particle size, zeta potential and encapsulation efficiency. Surface tension measurements revealed that insulin-chitosan polyelectrolyte complexes have some degree of hydrophobicity and should be added to lecithin liposomal dispersion and not the vice versa to prevent their adsorption on the surface. Stability of insulin was enhanced when it was associated to liposomes. Significant reduction of blood glucose levels was noticed after oral administration of liposomal preparation to streptozotocin diabetic rats compared to control. The hypoglycemic activity was more prolonged compared to subcutaneously administered insulin.

Collagen/chitosan based two-compartment and bi-functional dermal scaffolds for skin regeneration

Energy Technology Data Exchange (ETDEWEB)

Wang, Feng [Department of Plastic Surgery and Burns, Shenzhen Second People' s Hospital, Shenzhen 518035 (China); Wang, Mingbo [Key Laboratory of Biomedical Materials and Implants, Research Institute of Tsinghua University in Shenzhen, Shenzhen 518057 (China); She, Zhending [Key Laboratory of Biomedical Materials and Implants, Research Institute of Tsinghua University in Shenzhen, Shenzhen 518057 (China); Shenzhen Lando Biomaterials Co., Ltd., Shenzhen 518057 (China); Fan, Kunwu; Xu, Cheng [Department of Plastic Surgery and Burns, Shenzhen Second People' s Hospital, Shenzhen 518035 (China); Chu, Bin; Chen, Changsheng [Key Laboratory of Biomedical Materials and Implants, Research Institute of Tsinghua University in Shenzhen, Shenzhen 518057 (China); Shi, Shengjun, E-mail: shengjunshi@yahoo.com [The Burns Department of Zhujiang Hospital, Southern Medical University, Guangzhou 510280 (China); Tan, Rongwei, E-mail: tanrw@landobiom.com [Key Laboratory of Biomedical Materials and Implants, Research Institute of Tsinghua University in Shenzhen, Shenzhen 518057 (China); Shenzhen Lando Biomaterials Co., Ltd., Shenzhen 518057 (China)

2015-07-01

Inspired from the sophisticated bilayer structures of natural dermis, here, we reported collagen/chitosan based two-compartment and bi-functional dermal scaffolds. Two functions refer to mediating rapid angiogenesis based on recombinant human vascular endothelial growth factor (rhVEGF) and antibacterial from gentamicin, which were encapsulated in PLGA microspheres. The gentamicin and rhVEGF encapsulated PLGA microspheres were further combined with collagen/chitosan mixtures in low (lower layer) and high (upper layer) concentrations, and molded to generate the two-compartment and bi-functional scaffolds. Based on morphology and pore structure analyses, it was found that the scaffold has a distinct double layered porous and connective structure with PLGA microspheres encapsulated. Statistical analysis indicated that the pores in the upper layer and in the lower layer have great variations in diameter, indicative of a two-compartment structure. The release profiles of gentamicin and rhVEGF exceeded 28 and 49 days, respectively. In vitro culture of mouse fibroblasts showed that the scaffold can facilitate cell adhesion and proliferation. Moreover, the scaffold can obviously inhibit proliferation of Staphylococcus aureus and Serratia marcescens, exhibiting its unique antibacterial effect. The two-compartment and bi-functional dermal scaffolds can be a promising candidate for skin regeneration. - Highlights: • The dermal scaffold is inspired from the bilayer structures of natural dermis. • The dermal scaffold has two-compartment structures. • The dermal scaffold containing VEGF and gentamicin encapsulated PLGA microspheres • The dermal scaffold can facilitate cell adhesion and proliferation.

Collagen/chitosan based two-compartment and bi-functional dermal scaffolds for skin regeneration

International Nuclear Information System (INIS)

Wang, Feng; Wang, Mingbo; She, Zhending; Fan, Kunwu; Xu, Cheng; Chu, Bin; Chen, Changsheng; Shi, Shengjun; Tan, Rongwei

2015-01-01

Inspired from the sophisticated bilayer structures of natural dermis, here, we reported collagen/chitosan based two-compartment and bi-functional dermal scaffolds. Two functions refer to mediating rapid angiogenesis based on recombinant human vascular endothelial growth factor (rhVEGF) and antibacterial from gentamicin, which were encapsulated in PLGA microspheres. The gentamicin and rhVEGF encapsulated PLGA microspheres were further combined with collagen/chitosan mixtures in low (lower layer) and high (upper layer) concentrations, and molded to generate the two-compartment and bi-functional scaffolds. Based on morphology and pore structure analyses, it was found that the scaffold has a distinct double layered porous and connective structure with PLGA microspheres encapsulated. Statistical analysis indicated that the pores in the upper layer and in the lower layer have great variations in diameter, indicative of a two-compartment structure. The release profiles of gentamicin and rhVEGF exceeded 28 and 49 days, respectively. In vitro culture of mouse fibroblasts showed that the scaffold can facilitate cell adhesion and proliferation. Moreover, the scaffold can obviously inhibit proliferation of Staphylococcus aureus and Serratia marcescens, exhibiting its unique antibacterial effect. The two-compartment and bi-functional dermal scaffolds can be a promising candidate for skin regeneration. - Highlights: • The dermal scaffold is inspired from the bilayer structures of natural dermis. • The dermal scaffold has two-compartment structures. • The dermal scaffold containing VEGF and gentamicin encapsulated PLGA microspheres • The dermal scaffold can facilitate cell adhesion and proliferation

Cytotoxicity study of novel water-soluble chitosan derivatives applied as membrane material of alginate microcapsules

NARCIS (Netherlands)

Sobol, Marcin; Bartkowiak, Artur; de Haan, Bart; de Vos, Paul

The majority of cell encapsulation systems applied so far are based on polyelectrolyte complexes of alginate and polyvalent metal cations. Although widely used, these systems suffer from the risk of disintegration. This can be partially solved by applying chitosan as additional outer membrane.

ANALYSIS OF THERMAL AND AQUEOUS SUSPENSION STABILITIES OF CHITOSAN BASED NANOENCAPSULATED VITAMINS

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Douglas de Britto

Full Text Available The food nutritional content is reduced as result of vitamins degradation. In order to minimize such losses, the encapsulation technique into polymeric nanoparticles (NPs could offer an additional protection, extending the stability. The crosslinking formed by the ionic gelation process of chitosan and tripolyphosphate (Chi-TPP has been widely used as an encapsulating matrix for several chemical compounds. In this way, Chi-TPP was used for encapsulation of C, B9 and B12 vitamins. The stability of the vitamins in NPs was evaluated in aqueous suspension by UV-Visible spectroscopy under different conditions: stored in dark, light exposure and effect of oxygen bubbling. The results indicated that encapsulation had a positive effect in preserving the vitamins, mainly vitamin C. The encapsulation preserved 47% of the initial concentration of vitamin C by the tenth day and around 28% after 17 days. Conversely, in non-encapsulated controls (neutral and acidic medium the losses were higher, reaching 13% by the tenth day and almost 3% after 17 days of storage in both medium. When exposed to light and O2 the protection provided by the encapsulation was even greater. By thermogravimetric analysis, the pure and the encapsulated vitamins showed distinct thermal behavior confirming Chi-TPP as a potential encapsulation material.

Synthesis and characterization of diethylenetriaminepentaacetic acid-chitosan-coated cobalt ferrite core/shell nanostructures

Energy Technology Data Exchange (ETDEWEB)

Runhua, Qin [Department of Physics, North University of China, Taiyuan 030051 (China); National Special Superfine Powder Engineering Research Center, Nanjing University Science and Technology, Xiaolingwei 200, Nanjing 210094 (China); Li Fengsheng, E-mail: qinrunh@126.com [National Special Superfine Powder Engineering Research Center, Nanjing University Science and Technology, Xiaolingwei 200, Nanjing 210094 (China); Wei, Jiang; Mingyue, Chen [National Special Superfine Powder Engineering Research Center, Nanjing University Science and Technology, Xiaolingwei 200, Nanjing 210094 (China)

2010-08-01

Special diethylenetriaminepentaacetic acid (DTPA)-chitosan-coated cobalt ferrite core/shell nanoparticles have been synthesized via a novel zero-length emulsion crosslinking process and characterized via crosslinking degree, simultaneous thermogravimetric analysis and differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectrometer, transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS) and vibration sample magnetometry. The experimental results showed that the CoFe{sub 2}O{sub 4} nanoparticles were really encapsulated with a DTPA-chitosan hybrid layer and the nanocomposites were proved to be nearly superparamagnetic with saturation magnetization of 26.6 emu g{sup -1}.

Radiation-induced changes in carboxymethylated chitosan

International Nuclear Information System (INIS)

Huang Ling; Peng Jing; Zhai Maolin; Li Jiuqiang; Wei Genshuan

2007-01-01

This study focuses on the radiation effect of γ-ray on carboxymethylated chitosan (CM-chitosan) in solid state. The changes in molecular weight of CM-chitosan with absorbed dose were monitored by viscosity method. Experimental results indicated that random chain scissions took place under irradiation. Radiation chemical yield (G d ) of CM-chitosan in solid state with N 2 -saturated was 0.49, which showed CM-chitosan has high radiation stability. Biomaterials composed of CM-chitosan can be thought to sterilize with low absorbed dose. FTIR and UV spectra showed that main chain structures of CM-chitosan were retained, carbonyl/carboxyl groups were formed and partial amino groups were eliminated in high absorbed dose. XRD patterns identified that the degradation of CM-chitosan occurred mostly in amorphous region

Physical and Oxidative Stability of Uncoated and Chitosan-Coated Liposomes Containing Grape Seed Extract

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Jochen Weiss

2013-08-01

Full Text Available Polyphenol-rich grape seed extract (0.1 w/w% was incorporated in liposomes (1 w/w% soy lecithin by high pressure homogenization (22,500 psi and coated with chitosan (0.1 w/w%. Primary liposomes and chitosan-coated secondary liposomes containing grape seed extract showed good physical stability during 98 days of storage. Most of the polyphenols were incorporated in the shell of the liposomes (85.4%, whereas only 7.6% of the polyphenols of grape seed extract were located in the interior of the liposomes. Coating with chitosan did not change the polyphenol content in the liposomes (86.6%. The uncoated liposomes without grape seed extract were highly prone to lipid oxidation. The cationic chitosan coating, however, improved the oxidative stability to some extent, due to its ability to repel pro-oxidant metals. Encapsulated grape seed extract showed high antioxidant activity in both primary and secondary liposomes, which may be attributed to its polyphenol content. In conclusion, the best chemical stability of liposomes can be achieved using a combination of grape seed extract and chitosan.

Ab initio computational study of –N-C and –O-C bonding formation : functional group modification reaction based chitosan

Science.gov (United States)

Siahaan, P.; Salimah, S. N. M.; Sipangkar, M. J.; Hudiyanti, D.; Djunaidi, M. C.; Laksitorini, M. D.

2018-04-01

Chitosan application in pharmaceutics and cosmeceutics industries is limited by its solubility issue. Modification of -NH2 and -OH fuctional groups of chitosan by adding carboxyl group has been shown to improve its solubility and application. Attempt to synthesize carboxymethyl chitosan (CMC) from monocloroacetic acid (MCAA) has been done prior this report. However no information is available wether –OH (-O-C bonding formation) or -NH2 (-N-C bonding formation) is the preference for - CH2COOH to attach. In the current study, the reaction mechanism between chitosan and MCAA reactants into carboxymethyl chitosan (CMC) was examined by computational approach. Dimer from of chitosan used as a molecular model in calculation All the molecular structure involved in the reaction mechanism was optimized by ab initio computational on the theory and basis set HF/6-31G(d,p). The results showed that the - N-C bonding formation via SN2 than the -O-C bonding formation via SN2 which have activation energy 469.437 kJ/mol and 533.219 kJ/mol respectively. However, the -O-C bonding formation more spontaneous than the -N-C bonding formation because ΔG the formation of O-CMC-2 reaction is more negative than ΔG of formation N-CMC-2 reaction is -4.353 kJ/mol and -1.095 kJ/mol respectively. The synthesis of N,O-CMC first forms -O-CH2COOH, then continues to form -NH-CH2COOH. This information is valuable to further optimize the reaction codition for CMC synthesis.

Evaluation of nano encapsulation techniques in different polymeric system for the delivery of anti-tuberculosis drugs (ATD)

CSIR Research Space (South Africa)

Swai, H

2006-02-01

Full Text Available In this study, isoniazid, one of the most potent anti-TB drugs, was successfully encapsulated in poly (D, L- lactide-co-glycolide) (PLG) and in alginate-chitosan polymeric systems using a double-emulsion method and a cation-induced gelation method...

The sustained-release behavior and in vitro and in vivo transfection of pEGFP-loaded core-shell-structured chitosan-based composite particles

Directory of Open Access Journals (Sweden)

Wang Y

2014-10-01

Full Text Available Yun Wang,1 Fu-xing Lin,2 Yu Zhao,1 Mo-zhen Wang,2 Xue-wu Ge,2 Zheng-xing Gong,1 Dan-dan Bao,1 Yu-fang Gu1 1Department of Plastic Surgery, First Affiliated Hospital of Anhui Medical University, 2CAS Key Laboratory of Soft Matter Chemistry, Department of Polymer Science and Engineering, University of Science and Technology of China, Hefei, Anhui, People’s Republic of China Abstract: Novel submicron core-shell-structured chitosan-based composite particles ­encapsulated with enhanced green fluorescent protein plasmids (pEGFP were prepared by complex coacervation method. The core was pEGFP-loaded thiolated N-alkylated chitosan (TACS and the shell was pH- and temperature-responsive hydroxybutyl chitosan (HBC. pEGFP-loaded TACS-HBC composite particles were spherical, and had a mean diameter of approximately 120 nm, as measured by transmission electron microscopy and particle size analyzer. pEGFP showed sustained release in vitro for >15 days. Furthermore, in vitro transfection in human embryonic kidney 293T and human cervix epithelial cells, and in vivo transfection in mice skeletal muscle of loaded pEGFP, were investigated. Results showed that the expression of loaded pEGFP, both in vitro and in vivo, was slow but could be sustained over a long period. pEGFP expression in mice skeletal muscle was sustained for >60 days. This work indicates that these submicron core-shell-structured chitosan-based composite particles could potentially be used as a gene vector for in vivo controlled gene transfection. Keywords: gene therapy, gene transfection, hydroxybutyl chitosan, thiolated N-alkylated chitosan, pEGFP, complex coacervation

Chitosan-catechol: a writable bioink under serum culture media.

Science.gov (United States)

Lee, Daiheon; Park, Joseph P; Koh, Mi-Young; Kim, Pureum; Lee, Junhee; Shin, Mikyung; Lee, Haeshin

2018-05-01

Mussel-inspired adhesive coatings on biomedical devices have attracted significant interest due to their unique properties such as substrate independency and high efficiency. The key molecules for mussel-inspired adhesive coatings are catechol and amine groups. Along with the understanding of catechol chemistry, chitosan-catechol has also been developed as a representative mussel-inpired adhesive polymer that contains catechol and amine groups for adhesiveness. Herein, we demonstrated the direct writability of chitosan-catechol as a bioink for 3D printing, one of the additive techniques. The use of chitosan-catechol bioink results in the formation of 3D constructs in normal culture media via rapid complexation of this bioink with serum proteins; in addition, the metal/catechol combination containing tiny amounts of vanadyl ions, in which the ratio of metal to catechol is 0.0005, dramatically enhances the mechanical strength and printability of the cell-encapsulated inks, showing a cell viability of approximately 90%. These findings for mussel-inspired bioinks will be a promising way to design a biocompatible 3D bioink cross-linked without any external stimuli.

Chitosan nanoparticles as non-viral gene delivery systems: determination of loading efficiency.

Science.gov (United States)

Carrillo, Carolina; Suñé, Josep Maria; Pérez-Lozano, Pilar; García-Montoya, Encarna; Sarrate, Rocío; Fàbregas, Anna; Miñarro, Montserrat; Ticó, Josep Ramon

2014-07-01

Chitosan has been studied for use in particle delivery systems for therapeutic purposes, since one of its most important applications is as a non-viral vector in gene therapy. Due to its positive charge, it is capable of forming DNA complexes (polyplexes) obtained through several methods and with the property of protecting nucleic acids. Two methods for obtaining the nanoparticles of chitosan-nucleic acids are reported in this study: simple complexation (of depolymerized chitosan or of different chitosan salts with plasmid) and ionic gelation (by adsorption of plasmid in the nanoparticles or by encapsulation of plasmid into nanoparticles). The determination of the loading efficiency of chitosan nanoparticles with the plasmid is carried out by electrophoretic mobility of the samples on agarose gel. Furthermore, the nanoparticles have been characterized according to their morphology, size and surface charge using AFM, TEM, laser diffraction and dynamic light scattering techniques. The polyplexes obtained have been found to be spherical and nanometric in size (between 100-230nm) with a zeta potential between 37 and 48mV. Positive results have been obtained by agarose gel electrophoresis for all studied cases: a concentration of between 20 and 30μg/mL of chitosan salts is required while for the remaining chitosan samples studied, 100% loading efficiency does not occur until a concentration equal to 100μg/mL (regardless of previous depolymerisation and the method performed). Chitosan-plasmid nanocapsules have been obtained at the polymer concentrations worked with (between 0.025 and 0.2%). Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Estabilidade de emulsões de d-limoneno em quitosana modificada Stability of d-limonene emulsions in modified chitosan

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Camila Figueiredo Borgognoni

2006-09-01

Full Text Available A quitosana é um biopolímero produzido a partir da quitina, presente na casca de crustáceos. Atualmente, o estudo de suas propriedades se deve às suas diversas utilizações nas áreas farmacêutica e alimentícia. A quitosana utilizada neste estudo foi quimicamente modificada para tornar-se solúvel em água (quitosana succinilada. Estudou-se a estabilidade de emulsões com d-limoneno para que estes dados sejam úteis na sua posterior utilização como agente de encapsulação de d-limoneno por liofilização. Sua estabilidade foi analisada por espectrofotometria, em diferentes temperaturas, e por cromatografia gasosa associada à técnica da análise do espaço livre, à temperatura ambiente. Sua caracterização foi feita por microscopia óptica. Emulsões de maltodextrina com d-limoneno foram utilizadas para comparação já que maltodextrinas são muito usadas como agentes de encapsulação de aromas. Observou-se boa estabilidade de emulsões de quitosana succinilada com d-limoneno ao longo do tempo e características muito distintas em relação às observadas em emulsões de maltodextrina com d-limoneno. Pode-se concluir neste estudo que emulsões de quitosana succinilada com d-limoneno apresentaram características favoráveis à encapsulação de aromas.Chitosan is a biopolymer derived from chitin, a component of the shells of crustaceans. Recently, special attention has been given to the study of chitosan properties as a consequence of their wide application in pharmaceutical and food areas. In this study, the chitosan used was chemically modified in order to become water soluble (succinyl chitosan. The stability of succinyl chitosan emulsion with d-limonene was studied so that these results could be useful in a subsequent use of succinyl chitosan as a d-limonene encapsulating agent by lyophilization. The stability of the emulsion was analyzed using a spectrophotometer in different temperatures and by the headspace

Development of novel encapsulated formulations using albumin-chitosan as a polymer matrix for ocular drug delivery

Science.gov (United States)

Addo, Richard Tettey

Designing formulations for ophthalmic drug delivery is one of the most challenging endeavors facing the pharmaceutical scientist due to the unique anatomy, physiology, and biochemistry of the eye. Current treatment protocols for administration of drugs in eye diseases are primarily solution formulations, gels or ointments. However, these modes of delivery have several drawbacks such as short duration of exposure, need for repeated administrations and non-specific toxicity. We hypothesize that development of ocular drugs in microparticles will overcome the deficiencies of the current modalities of treatment. We based the hypothesis on the preliminary studies conducted with encapsulated tetracaine, an anesthetic used for surgical purposes and atropine, a medication used for several ophthalmic indications including mydriatic and cycloplegic effects. However, atropine is well absorbed into the systemic circulation and has been reported to exert severe systemic side effects after ocular administration (Hoefnagel D. 1961, Morton H. G. 1939 and Lang J. C. 1995) and may lead to serious side effects including death in extreme cases with pediatric use. Based on these observations, the focus of this dissertation is to formulate microparticulate drug carrier for treatment of various conditions of the eye. Purpose: To prepare, characterize, study the in vitro and in vivo interaction of albumin-chitosan microparticles (BSA-CSN MS), a novel particulate drug carrier for ocular drug delivery. Method: Microparticle formulations were prepared by method of spray drying. The percentage drug loading and efficiency were assessed using USP (I) dissolution apparatus. Using Malvern Zeta-Sizer, we determined size and surface charge of the fabrication. Surface morphology of the microparticles was examined using Scanning Electron Microscopy. Microparticles were characterized in terms of thermal properties using Differential Scanning Calorimetry. Human corneal epithelial cells (HCET-1) were

Thermo-responsive wound dressings by grafting chitosan and poly(N-isopropylacrylamide) to plasma-induced graft polymerization modified non-woven fabrics

International Nuclear Information System (INIS)

Chen, Jyh-Ping; Kuo, Chang-Yi; Lee, Wen-Li

2012-01-01

Highlights: ► Poly(N-isopropylacrylamide) and chitosan were grafted to polypropylene non-wovens. ► An easily stripped off thermo-responsive wound dressing was developed. ► The wound dressing is biocompatible, has antibacterial and wound healing abilities. ► The bigraft non-woven will be a potential wound dressing for biomedical use. - Abstract: To obtain a chitosan wound dressings with temperature-responsive characteristics, polypropylene (PP) non-woven fabric (NWF) was modified by direct current pulsed oxygen plasma-induced grafting polymerization of acrylic acid (AAc) to improve hydrophilicity and to introduce carboxylic acid groups. Conjugation of chitosan and poly(N-isopropylacrylamide) (PNIPAAm) followed by using water-soluble carbodiimide as a coupling agent to form a novel bigraft PP-g-chitosan-g-PNIPAAm wound dressing. The amount of chitosan and PNIPAAm grafted to PP-g-chitosan-g-PNIPAAm were 83.0 ± 4.6 μg/cm 2 and 189.5 ± 8.2 μg/cm 2 , respectively. The surface chemical composition and microstructure of the NWF were studied by electron spectroscopy for chemical analysis (ESCA) and scanning electron microscopy (SEM). The linkages between AAc, chitosan, and PNIPAAm were confirmed with the formation of amide bonds. Physical properties of the NWF were characterized and potentials of these NWFs as wound dressings were evaluated using SD rat as the animal model. NWFs contained PNIPAAm were better than those contained only chitosan in wound healing rates and the wound areas covered by PP-g-chitosan-g-PNIPAAm wound dressings healed completely in 17 days.

Encapsulation of protease from Aspergillus oryzae and lipase from Thermomyces lanuginoseus using alginate and different copolymer types

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Truong Thi Mong Thu

2016-05-01

Full Text Available Although the application of enzymes in food as a food processing aid and enzyme supplement is of interest and widely used, the enzymes can be easily deactivated or lose their activity due to many causes such as pH and moisture as well as through the introduction of incompatible ingredients during food processing and storage. These problems can be solved by the encapsulation technique, especially in a gel matrix. The influences were studied of the alginate concentration, types of copolymer and their concentrations on the bead size, encapsulation yield (EY, encapsulation efficiency (EE, leakage and the retention of enzyme activity during storage period of encapsulated protease from Aspergillus oryzae and lipase from Thermomyces lanuginosus beads. A solution of purified protease or lipase was encapsulated in calcium alginate-chitosan beads (CACB, calcium alginate-xanthan gum beads (CAXB and calcium alginate-maltodextrin beads (CAMB using the extrusion method. Increasing the alginate and copolymer concentrations in the solution increased the bead size, EY, EE and the retention of enzyme activity during the storage period and reduced leakage of both the encapsulated protease and lipase. In addition, different types of copolymer significantly (p ≤ 0.05 affected these properties of both encapsulated enzymes. Furthermore, protease encapsulated using 2.0% alginate and 0.2% chitosan provided the highest EY (81.7% and EE (77.2% with a bead size of 1.85 mm and 8.1% leakage. The retention of encapsulated protease activity and the shelf-life of encapsulated enzyme which was expressed as half-life, the time required for the enzyme activity to decrease by half (thalf life were 75.8% and 27.2 wk, respectively after storage at 4 °C for 10 wk. For lipase, encapsulation using 2.0% alginate and 0.4% xanthan gum provided the highest EY (42.5% and EE (43.9% and the bead size and leakage were 1.81 mm and 6.2%, respectively. The retention of encapsulated

N,O6-partially acetylated chitosan nanoparticles hydrophobically-modified for controlled release of steroids and vitamin E

DEFF Research Database (Denmark)

Quinones, Javier Perez; Gothelf, Kurt Vesterager; Kjems, Jørgen

2013-01-01

Diosgenin, two synthetic analogs of brassinosteroids, testosterone and dl-α-tocopherol were covalently linked to synthetic water-soluble N,O6-partially acetylated chitosan, for their controlled release. Drug linking was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also character......Diosgenin, two synthetic analogs of brassinosteroids, testosterone and dl-α-tocopherol were covalently linked to synthetic water-soluble N,O6-partially acetylated chitosan, for their controlled release. Drug linking was confirmed by FTIR spectroscopy and proton NMR. Conjugates were also...

Diphtheria toxoid-containing microparticulate powder formulations for pulmonary vaccination : Preparation, characterization and evaluation in guinea pigs

NARCIS (Netherlands)

Amidi, Maryam; Pellikaan, Hubert C.; Hirschberg, Hoang; de Boerd, Anne H.; Crommelin, Daan J. A.; Hennink, Wim E.; Kersten, Gideon; Jiskoot, Wim

2007-01-01

this study, the potential of N-Trimethyl chitosan (TMC, degree of quaternization 50%) and dextran microparticles for pulmonary delivery of diphtheria toxoid (DT) was investigated. The antigen-containing microparticles were prepared by drying of an aqueous solution of polymer and DT through a

Preparation, physical characterization, and stability of Ferrous-Chitosan microcapsules using different iron sources

Science.gov (United States)

Handayani, Noer Abyor; Luthfansyah, M.; Krisanti, Elsa; Kartohardjono, Sutrasno; Mulia, Kamarza

2017-11-01

Dietary modification, supplementation and food fortification are common strategies to alleviate iron deficiencies. Fortification of food is an effective long-term approach to improve iron status of populations. Fortification by adding iron directly to food will cause sensory problems and decrease its bioavailability. The purpose of iron encapsulation is: (1) to improve iron bioavailability, by preventing oxidation and contact with inhibitors and competitors; and (2) to disguise the rancid aroma and flavor of iron. A microcapsule formulation of two suitable iron compounds (iron II fumarate and iron II gluconate) using chitosan as a biodegradable polymer will be very important. Freeze dryer was also used for completing the iron microencapsulation process. The main objective of the present study was to prepare and characterize the iron-chitosan microcapsules. Physical characterization, i.e. encapsulation efficiency, iron loading capacity, and SEM, were also discussed in this paper. The stability of microencapsulated iron under simulated gastrointestinal conditions was also investigated, as well. Both iron sources were highly encapsulated, ranging from 71.5% to 98.5%. Furthermore, the highest ferrous fumarate and ferrous gluconate loaded were 1.9% and 4.8%, respectively. About 1.04% to 9.17% and 45.17% to 75.19% of Fe II and total Fe, were released in simulated gastric fluid for two hours and in simulated intestinal fluid for six hours, respectively.

Encapsulation layer design and scalability in encapsulated vertical 3D RRAM

International Nuclear Information System (INIS)

Yu, Muxi; Fang, Yichen; Wang, Zongwei; Chen, Gong; Pan, Yue; Yang, Xue; Yin, Minghui; Yang, Yuchao; Li, Ming; Cai, Yimao; Huang, Ru

2016-01-01

Here we propose a novel encapsulated vertical 3D RRAM structure with each resistive switching cell encapsulated by dielectric layers, contributing to both the reliability improvement of individual cells and thermal disturbance reduction of adjacent cells due to the effective suppression of unwanted oxygen vacancy diffusion. In contrast to the traditional vertical 3D RRAM, encapsulated bar-electrodes are adopted in the proposed structure substituting the previous plane-electrodes, thus encapsulated resistive switching cells can be naturally formed by simply oxidizing the tip of the metal bar-electrodes. In this work, TaO x -based 3D RRAM devices with SiO 2 and Si 3 N 4 as encapsulation layers are demonstrated, both showing significant advantages over traditional unencapsulated vertical 3D RRAM. Furthermore, it was found thermal conductivity and oxygen blocking ability are two key parameters of the encapsulation layer design influencing the scalability of vertical 3D RRAM. Experimental and simulation data show that oxygen blocking ability is more critical for encapsulation layers in the relatively large scale, while thermal conductivity becomes dominant as the stacking layers scale to the sub-10 nm regime. Finally, based on the notable impacts of the encapsulation layer on 3D RRAM scaling, an encapsulation material with both excellent oxygen blocking ability and high thermal conductivity such as AlN is suggested to be highly desirable to maximize the advantages of the proposed encapsulated structure. The findings in this work could pave the way for reliable ultrahigh-density storage applications in the big data era. (paper)

Low toxic and high soluble camptothecin derivative 2–47 effectively induces apoptosis of tumor cells in vitro

International Nuclear Information System (INIS)

Zhou, Yao; Zhao, Hong-Ye; Jiang, Du; Wang, Lu-Yao; Xiang, Cen; Wen, Shao-Peng; Fan, Zhen-Chuan; Zhang, Yong-Min; Guo, Na; Teng, Yu-Ou; Yu, Peng

2016-01-01

The cytotoxic activity of camptothecin derivatives is so high that these compounds need to be further modified before their successful application as anti-cancer agents clinically. In this study, we reported the synthesis and biological evaluation of a novel camptothecin derivative called compound 2–47. The changes in structure did not reduce its activity to inhibit DNA topoisomerase I. Compound 2–47 induced apoptosis of many tumor cells including leukemia cells K562, Jurkat, HL-60, breast cancer cell BT-549, colon cancer cell HT-29 and liver cancer cell HepG2 with a half maximal inhibitory concentration (IC 50 ) of 2- to 3-fold lower than HCPT as a control. In particular, 2–47 inhibited the proliferation of Jurkat cells with an IC 50 of as low as 40 nM. By making use of Jurkat cell as a model, following treatment of Jurkat cells, compound 2–47 activated caspase-3 and PARP, resulting in a decreased Bcl-2/Bax ratio. These data showed that compound 2–47 induces Jurkat cell death through the mitochondrial apoptotic pathway. In addition, compound 2–47 showed a decreased cytotoxic activity against normal cells and an improved solubility in low-polar solvent. For example, compound 2–47 solutes in CHCl 3 130-fold higher than HCPT. Taken together, our data demonstrated that camptothecin derivative 2–47 notably inhibits the tumor cell proliferation through mitochondrial-mediated apoptosis in vitro. - Highlights: • Compound 2–47 showed a wide inhibitory effect on the tested tumor cell lines with an IC 50 of 3 times lower than that of HCPT in general. • Compound 2–47 inhibited the proliferation of the human leukemia cell Jurkat at an IC 50 of as low as 40 nM. • As compared to HCPT, compound 2–47 showed much reduced cytotoxicity on normal human cells. • As compared to others, compound 2–47 showed a hundreds-fold higher solubility in non-polar organic solution.

Chitosan-based nanoparticles for improved anticancer efficacy and bioavailability of mifepristone

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Huijuan Zhang

2016-11-01

Full Text Available In addition to its well-known abortifacient effect, mifepristone (MIF has been used as an anticancer drug for various cancers in many studies with an in-depth understanding of the mechanism of action. However, application of MIF is limited by its poor water solubility and low oral bioavailability. In this work, we developed a drug delivery system based on chitosan nanoparticles (CNs to improve its bioavailability and anticancer activity. The MIF-loaded chitosan nanoparticles (MCNs were prepared by convenient ionic gelation techniques between chitosan (Cs and tripolyphosphate (TPP. The preparation conditions, including Cs concentration, TPP concentration, Cs/MIF mass ratio, and pH value of the TPP solution, were optimized to gain better encapsulation efficiency (EE and drug loading capacity (DL. MCNs prepared with the optimum conditions resulted in spherical particles with an average size of 200 nm. FTIR and XRD spectra verified that MIF was successfully encapsulated in CNs. The EE and DL of MCNs determined by HPLC were 86.6% and 43.3%, respectively. The in vitro release kinetics demonstrated that MIF was released from CNs in a sustained-release manner. Compared with free MIF, MCNs demonstrated increased anticancer activity in several cancer cell lines. Pharmacokinetic studies in male rats that were orally administered MCNs showed a 3.2-fold increase in the area under the curve from 0 to 24 h compared with free MIF. These results demonstrated that MCNs could be developed as a potential delivery system for MIF to improve its anticancer activity and bioavailability.

The Extraction Process of Trimethyl Xanthina in Vitro Culture of Callus Camellia Sinensis with ethyl Acetate Solvent

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Sutini

2016-01-01

Full Text Available Trimethyl xanthina is one of the compounds contained bioactive culture in vitro Cammelia sinensis callus which is widely used in the field of food, beverage, agriculture and health industries. The presence of trimethyl xanthina on food, beverages and health is needed in a certain amount depending on the use which is achieved by the user. To get a certain amount of trimethyl xanthina from callus culture of Cammelia sinensis, the extraction process is performed on the water solvent, as well as non-solvent water / organic solvent such as ethyl acetate. The purpose of this study was to obtain profile of trimethyl xanthina in the extraction of Cammelia sinensis callus. The experimental methods used consisted of dissolution, filtration, extraction with water solvent and ethyl acetate, then followed by identification of trimethyl xanthina using HPLC. The results shows the profile form of trimethyl xanthina of Cammelia sinensis callus have similarities with the standard form of trimethyl xanthina.

N-mercapto acetyl-N'-octyl-O, N″-glycol chitosan as an efficiency oral delivery system of paclitaxel.

Science.gov (United States)

Huo, Meirong; Fu, Ying; Liu, Yanhong; Chen, Qinyu; Mu, Yan; Zhou, Jianping; Li, Lingchao; Xu, Wei; Yin, Tingjie

2018-02-01

Herein, thioglycolic acid modified N-octyl-O, N'-glycol chitosan (N-mercapto acetyl-N'-octyl-O, N″-glycol chitosan, abbreviated as SH-OGC) was synthesized to improve the oral bioavailability of paclitaxel (PTX). PTX was readily solubilized into the hydrophobic inner core of SH-OGC. Pharmacokinetic studies demonstrated that the bioavailability of PTX was greatly enhanced when delivered by SH-OGC compared to Taxol ® or non-sulfhydrylated OGC micelles. Caco-2 cell experiments confirmed PTX or rhodamine-123-loaded SH-OGC demonstrated effective cellular accumulation via caveola-mediated endocytosis along with the inhibition of P-gp efflux. Furthermore, Caco-2 transport studies demonstrated that the mechanistic basis of SH-OGC efficacy was attributed to P-gp inhibition, enhanced permeability of tight junctions and clathrin-mediated transcytosis across the endothelium. In addition, SH-OGC exhibited increased intestinal retention through thiol-mediated mucoadhesion compared with OGC according to results of mucoadhesion evaluation on freshly excised rat intestine. In summary, SH-OGC micelles may present as a promising delivery vehicle for enhancing the oral bioavailability of P-gp substrates. Copyright © 2017 Elsevier Ltd. All rights reserved.

Hypericum perforatum incorporated chitosan films as potential bioactive wound dressing material.

Science.gov (United States)

Güneş, Seda; Tıhmınlıoğlu, Funda

2017-09-01

Recent studies in wound dressing applications offer new therapies and promote wound healing process. The aim of this study was to develop Hypericum perforatum (St John's Wort) oil incorporated chitosan films for wound dressing applications. H. perforatum oil as a potential therapeutic agent was encapsulated in chitosan film to achieve a better wound dressing material. Oil incorporated chitosan films were successfully prepared by solvent casting method in different oil concentrations (0.25-1.5%v/v). Water vapor permeability (WVP), mechanical test, swelling behavior and surface hydrophobicity were performed in order to characterize the prepared films. Antimicrobial test was performed by disc diffusion method and the growth inhibition effects of the films including different amount of H. perforatum oil were investigated on Escherichia coli and Staphylococcus aureus. WVP increased with oil incorporation and the highest value was obtained for 0.25% oil concentration.The highest strain value was obtained in 0.25% oil content films although tensile stress decreased with increasing oil content. H. perforatum oil incorporated films had antimicrobial effect on both microorganisms. Chitosan based films had no cytotoxic effects on NIH3T3fibroblast cells and provided a good surface for cell attachment and proliferation. The results showed that the H. perforatum incorporated chitosan films seems to be a potential and novel biomaterial for wound healing applications. Copyright © 2017 Elsevier B.V. All rights reserved.

Biological significance of lysine mono-, di- and trimethylation on histone and non-histone proteins

International Nuclear Information System (INIS)

Perez-Burgos, L.

2006-01-01

Histones are the proteins that compact DNA into the repeating unit of chromatin known as the nucleosome. The N-termini of histones are subject to a series of post-translational modifications, one of which is methylation. This modification is termed 'epigenetic' because it extends the information encoded in the genome. Lysines can be mono-, di- or tri-methylated at different positions on histones H1, H3 and H4. In order to study the biological role of histone lysine methylation, antibodies were generated against mono-, di- and trimethylated H3-K9 and H3-27. Indeed, different chromatin domains in the mouse nucleus are enriched in distinct forms of histone lysine methylation, such as pericentric heterochromatin and the inactive X chromosome. Interestingly, heterochromatin in Arabidopsis thaliana is enriched in the mono- and di-, but not the trimethylated form of H3-K9. Furthermore, there exists a hierarchy of epigenetic modifications in which H3-K9 trimethylation is found to be upstream of DNA methylation on mouse major satellites. Histone lysine methylation is also involved in gene regulation upon development. One example is the chicken 61538;-globin locus, a region of facultative chromatin that undergoes a loss of di- and trimethylated H3-K27 in mature red blood cells, concomitant with expression of the 61538;-globin genes. SET-domain proteins are enzymes that methylate histones, but some of them are also able to methylate non-histone substrates. In particular, p53 is methylated by Set9 on lysine 372, G9a and Glp-1 on lysine 373 and by Smyd2 on lysine 370. Smyd2 transcript levels are greatly increased upon irradiation and dimethylated p53-370 specifically binds to 53BP1, a protein involved in recognizing DNA double-stranded breaks upon ionizing radiation. These results argue for a novel role of p53-K370 methylation in the biology of DNA damage. In summary, lysine methylation is a post-translational modification that can occur both on histone and non-histone proteins

Synthesis and Characterization of Chitosan Coated Manganese Zinc Ferrite Nanoparticles as MRI Contrast Agents

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M. Zahraei

2015-04-01

Full Text Available Manganese zinc ferrite nanoparticles (MZF NPs were synthesized by using a direct, efficient and environmental friendly hydrothermal method. To improve the colloidal stability of MZF NPs for biomedical applications, NPs were coated with chitosan by ionic gelation technique using sodium tripolyphosphate (TPP as crosslinker. The synthesized NPs were characterized by X ray diffraction (XRD analysis, inductively coupled plasma optical emission spectrometry (ICP-OES, fourier transform infrared (FTIR spectroscopy, transmission electron microscopy (TEM, vibrating sample magnetometer (VSM and the dynamic light scattering (DLS methods. The results confirmed the spinel ferrite phase formation without any calcination process after synthesis. Mean particle size of bare NPs was around 14 nm. Moreover, certain molar ratio of chitosan to TPP was required for encapsulation of NPs in chitosan. Coated NPs showed hydrodynamic size of 300 nm and polydispersity index about 0.3.

Synthesis, characterization and cytotoxicity of S-nitroso-mercaptosuccinic acid-containing alginate/chitosan nanoparticles

Science.gov (United States)

Seabra, Amedea B.; Fabbri, Giulia K.; Pelegrino, Milena T.; Silva, Letícia C.; Rodrigues, Tiago

2017-06-01

Nitric oxide (NO) is an endogenous free radical, which plays key roles in several biological processes including vasodilation, neurotransmission, inhibition of platelet adhesion, cytotoxicity against pathogens, wound healing, and defense against cancer. Due to the relative instability of NO in vivo (half-life of ca. 0.5 seconds), there is an increasing interest in the development of low molecular weight NO donors, such as S-nitrosothiols (RSNOs), which are able to prolong and preserve the biological activities of NO in vivo. In order to enhance the sustained NO release in several biomedical applications, RSNOs have been successfully allied to nanomaterials. In this context, this work describes the synthesis and characterization of the NO donor S-nitroso-mercaptosuccinic acid (S-nitroso-MSA), which belongs to the class of RSNOs, and its incorporation in polymeric biodegradable nanoparticles composed by alginate/chitosan. First, chitosan nanoparticles were obtained by gelation process with sodium tripolyphosphate (TPP), followed by the addition of the alginate layer, to enhance the nanoparticle protection. The obtained nanoparticles presented a hydrodynamic diameter of 343 ± 38 nm, polydispersity index (PDI) of 0.36 ± 0.1, and zeta potential of - 30.3 ± 0.4 mV, indicating their thermal stability in aqueous suspension. The negative zeta potential value was assigned to the presence of alginate chains on the surface of chitosan/TPP nanoparticles. The encapsulation efficiency of the NO donor into the polymeric nanoparticles was found to be 98 ± 0.2%. The high encapsulation efficiency value was attributed to the positive interactions between the NO donor and the polymeric content of the nanoparticles. Kinetics of NO release from the nanoparticles revealed a spontaneous and sustained release of therapeutic amounts of NO, for several hours under physiological temperature. The incubation of NO-releasing alginate/chitosan nanoparticles with human hepatocellular carcinoma

Structure of a Multilayer Nanofilm To Increase the Encapsulation Efficiency of Basic Fibroblast Growth Factor.

Science.gov (United States)

Han, Uiyoung; Hong, Jinkee

2018-03-05

In this study, we established the structure of a multilayer nanofilm that more efficiently encapsulates basic fibroblast growth factor (bFGF). First, a positively charged layer material was selected from biocompatible polymers such as collagen (Col), poly(beta-amino ester) (Poly2), and chitosan (Chi), while considering the film thickness. We then investigated the change in bFGF encapsulation efficiency when the multilayer structure was changed from a tetralayer to a trilayer. As a result, we obtained a highly improved bFGF encapsulation efficiency in the nanofilm using a positively charged layer formed by a blend of Col and Poly2 and a negatively charged poly(acrylic acid) (PAA) layer within a trilayered structure. In particular, we found that a significant amount of adsorbed bFGF was desorbed again during the film fabrication process of a tetralayered nanofilm. In the conventional nanofilm, bFGF was regarded as a polycation and formed a multilayer nanofilm that was composed of a tetralayered structure and was represented as (polycation/polyanion/bFGF/polyanion) n where n = number of repeated tetralayers. Here, we suggested that bFGF should not be considered a polycation, rather it should be considered as a small quantity of molecule that exists between the polyanion and polycation layers. In this case, the nanofilm is composed of repeating units of (polycation/polyanion/bFGF/polycation/polyanion), because the amount of adsorbed bFGF is considerably lower than that of other building blocks.

Antioxidant and antimutagenic activity of N-(2-carboxyethyl)chitosan

International Nuclear Information System (INIS)

Kogan, Grigorij; Skorik, Yury A.; Zitnanova, Ingrid; Krizkova, Livia; Durackova, Zdenka; Gomes, Carlos A.R.; Yatluk, Yury G.; Krajcovic, Juraj

2004-01-01

The antioxidant and antimutagenic activities of the novel carboxyethyl derivatives of chitosan with three different degrees of substitution have been assayed in vitro in the unicellular flagellate Euglena gracilis subjected to the action of genotoxic agents acridine orange and ofloxacin. It has been demonstrated that chitosan derivatives exhibit concentration-dependent protective antigenotoxic activity against both mutagens. It is suggested that different mechanisms may be involved in its protective action--antioxidant activity in case of ofloxacin-induced DNA damage, as well as possible interaction with the cell membrane that prevents acridine orange from reaching the genetic compartments and subsequent damaging DNA through intercalative binding. Direct adsorption of acridine orange on chitosan derivatives was ruled out as a possible mechanism of protection on the basis of spectrophotometric measurements. Dependence of the antimutagenic properties of the studied chitosan derivatives on the degree of substitution was reversed in experiments involving acridine orange and ofloxacin, which also indicated different mechanisms of protection involved in these two cases

Preparation of N,O-carboxymethyl chitosan coated alginate microcapsules and their application to Bifidobacterium longum BIOMA 5920

International Nuclear Information System (INIS)

Mi, Yu; Su, Ran; Fan, Dai-Di; Zhu, Xiao-Li; Zhang, Wen-Ni

2013-01-01

In order to greatly improve vitality of probiotic bacteria within the application, a novel biocompatible vehicle, N,O-carboxymethyl chitosan (NOCs) with appropriate degrees of substitution coat alginate (ALg) microparticles, was prepared by electrostatic droplet generation. The amount of chitosan (Cs) and N,O-carboxymethyl chitosan (NOCs) coated on the ALg microparticles was determined by differential scanning calorimetry. The surface morphology of ALg microparticles, Cs coated ALg microparticles and NOCs coated ALg microparticles was determined using scanning electron microscopy. The coating thickness of Cs coated ALg microparticles and that of NOCs coated ALg microparticles was directly observed with confocal laser scanning microscopy. In order to assess pH sensitivity of microparticles, the bovine serum albumin release from the microspheres was tested in acid solution (pH 2.0) for 2 h and subsequently in alkaline solution (pH 7.0) for 2 h. The survival of Bifidobacterium longum BIOMA 5920 loaded in NOCs coated with ALg microparticle was improved in simulated gastric juice (pH 2.0, for 2 h) compared to that of B. longum BIOMA 5920 loaded in ALg microparticles and Cs coated ALg microparticles. After incubation in simulated intestinal juices (pH 7.0, 2 h), the release of microencapsulated B. longum BIOMA 5920 was investigated. - Highlights: • Synthesised N,O-carboxymethyl chitosan (NOCs) coated alginate (ALg) microspheres. • Their effect on intestinal microflora was investigated in simulated gastric juices. • NOCs A coated ALg microspheres improved Bifidobacterium longum survival in SGJ. • The modified chitosan layer improved the pH-response of alginate microspheres. • NOCs A coated microspheres could be used to deliver oral bioactive compounds

Preparation of N,O-carboxymethyl chitosan coated alginate microcapsules and their application to Bifidobacterium longum BIOMA 5920

Energy Technology Data Exchange (ETDEWEB)

Mi, Yu; Su, Ran [Shaanxi R and D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University (China); Fan, Dai-Di, E-mail: fandaidi@nwu.edu.cn [Shaanxi R and D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University (China); Zhu, Xiao-Li [Shaanxi R and D Center of Biomaterials and Fermentation Engineering, School of Urban and Environmental Science, Northwest University, Taibai North Road 229, Xi' an, Shaanxi 710069 (China); Zhang, Wen-Ni [Shaanxi R and D Center of Biomaterials and Fermentation Engineering, School of Chemical Engineering, Northwest University (China); Shaanxi Key Laboratory of Degradable Biomedical Materials, School of Chemical Engineering, Northwest University (China)

2013-07-01

In order to greatly improve vitality of probiotic bacteria within the application, a novel biocompatible vehicle, N,O-carboxymethyl chitosan (NOCs) with appropriate degrees of substitution coat alginate (ALg) microparticles, was prepared by electrostatic droplet generation. The amount of chitosan (Cs) and N,O-carboxymethyl chitosan (NOCs) coated on the ALg microparticles was determined by differential scanning calorimetry. The surface morphology of ALg microparticles, Cs coated ALg microparticles and NOCs coated ALg microparticles was determined using scanning electron microscopy. The coating thickness of Cs coated ALg microparticles and that of NOCs coated ALg microparticles was directly observed with confocal laser scanning microscopy. In order to assess pH sensitivity of microparticles, the bovine serum albumin release from the microspheres was tested in acid solution (pH 2.0) for 2 h and subsequently in alkaline solution (pH 7.0) for 2 h. The survival of Bifidobacterium longum BIOMA 5920 loaded in NOCs coated with ALg microparticle was improved in simulated gastric juice (pH 2.0, for 2 h) compared to that of B. longum BIOMA 5920 loaded in ALg microparticles and Cs coated ALg microparticles. After incubation in simulated intestinal juices (pH 7.0, 2 h), the release of microencapsulated B. longum BIOMA 5920 was investigated. - Highlights: • Synthesised N,O-carboxymethyl chitosan (NOCs) coated alginate (ALg) microspheres. • Their effect on intestinal microflora was investigated in simulated gastric juices. • NOCs A coated ALg microspheres improved Bifidobacterium longum survival in SGJ. • The modified chitosan layer improved the pH-response of alginate microspheres. • NOCs A coated microspheres could be used to deliver oral bioactive compounds.

Ultrasonically synthesized organic liquid-filled chitosan microcapsules: part 2: characterization using AFM (atomic force microscopy) and combined AFM-confocal laser scanning fluorescence microscopy.

Science.gov (United States)

Mettu, Srinivas; Ye, Qianyu; Zhou, Meifang; Dagastine, Raymond; Ashokkumar, Muthupandian

2018-04-25

Atomic Force Microscopy (AFM) is used to measure the stiffness and Young's modulus of individual microcapsules that have a chitosan cross-linked shell encapsulating tetradecane. The oil filled microcapsules were prepared using a one pot synthesis via ultrasonic emulsification of tetradecane and crosslinking of the chitosan shell in aqueous solutions of acetic acid. The concentration of acetic acid in aqueous solutions of chitosan was varied from 0.2% to 25% v/v. The effect of acetic acid concentration and size of the individual microcapsules on the strength was probed. The deformations and forces required to rupture the microcapsules were also measured. Three dimensional deformations of microcapsules under large applied loads were obtained by the combination of Laser Scanning Confocal Microscopy (LSCM) with Atomic Force Microscopy (AFM). The stiffness, and hence the modulus, of the microcapsules was found to decrease with an increase in size with the average stiffness ranging from 82 to 111 mN m-1 and average Young's modulus ranging from 0.4 to 6.5 MPa. The forces required to rupture the microcapsules varied from 150 to 250 nN with deformations of the microcapsules up to 62 to 110% relative to their radius, respectively. Three dimensional images obtained using laser scanning confocal microscopy showed that the microcapsules retained their structure and shape after being subjected to large deformations and subsequent removal of the loads. Based on the above observations, the oil filled chitosan crosslinked microcapsules are an ideal choice for use in the food and pharmaceutical industries as they would be able to withstand the process conditions encountered.

Folic Acid Conjugated Chitosan for Targeted Delivery of siRNA to Activated Macrophages in vitro and in vivo

DEFF Research Database (Denmark)

Yang, Chuanxu; Gao, Shan; Kjems, Jørgen

2014-01-01

was conjugated to chitosan (FA–CS) and used to formulate siRNA into nanoparticles capable of cell specific delivery. The physiochemical properties of the nanoparticles, including size, zeta-potential and encapsulation efficiency, were characterized and the intracellular uptake and gene silencing efficiency were...

Drug-polymer interaction studies of cytarabine loaded chitosan nanoparticles

International Nuclear Information System (INIS)

Madni, A.; Kashif, P.M.; Nazir, I.; Rehman, M.

2017-01-01

Assessment of possible incompatibilities between drug and excipients is an important parameter of preformulation stage during the pharmaceutical product development of active pharmaceutical ingredient (API). The potential physical and chemical interaction among the components of a delivery system can affect the chemical nature, bioavailability, stability, and subsequently therapeutic efficacy of drugs. In this study, ATR-FTIR spectroscopy was employed to investigate the possible intermolecular interaction of Cytarabine with deacetylated chitosan and tripolyphosphate in the resulting physical blends and crosslinked nanoparticulate system. Two different strategies, physical blending and ionotropic gelation, were adopted to prepare binary or tertiary mixtures and nanoparticulate formulation, respectively. The IR spectra of CB showed characteristic peaks at 3438.27 cm-1 (primary amine), 3264.74 cm-1 (hydroxyl group) and 1654.98 cm-1 (C=O stretch in cyclic ring); CS at 3361.47 cm-1 (N-H stretching), 1646.18 cm-1 (C=O of Amide I), 1582.36 cm-1 (C=O of Amide II), and sTPP at 1135.77 cm-1 (P=O). CS-sTPP chemical interaction was confirmed from the shift in the absorption band of carbonyl groups (amide I, II) to 1634.66 cm-1 and 1541.17 cm-1 in blank chitosan nanoparticles, and 1636.87 cm-1, 1543.33 cm-1 in CSNP1 (2:6:1), and at 1646.15 cm-1 and 1557.04 cm-1 in CSNP2 (1:3:1). The characteristic peaks of CB were also present in chitosan formulation with a slight shift in the amino group at 3429.43 cm-1 and 3423.21 cm-1, in the hydroxyl group at 3274.54 cm-1 and 3270.73 cm-1, CSNP1 and CSNP2, respectively. The findings counseled no significant interaction in IR absorption pattern of cytarabine functional groups after encapsulation in CS-sTPP complex, which projected the potential of chitosan nanoparticulate system to entrap cytarabine. (author)

Spanish Broom (Spartium junceum L.) fibers impregnated with vancomycin-loaded chitosan nanoparticles as new antibacterial wound dressing: Preparation, characterization and antibacterial activity.

Science.gov (United States)

Cerchiara, Teresa; Abruzzo, Angela; Ñahui Palomino, Rogers Alberto; Vitali, Beatrice; De Rose, Renata; Chidichimo, Giuseppe; Ceseracciu, Luca; Athanassiou, Athanassia; Saladini, Bruno; Dalena, Francesco; Bigucci, Federica; Luppi, Barbara

2017-03-01

In this work, we propose as new wound dressing, the Spanish Broom fibers impregnated with vancomycin (VM) loaded chitosan nanoparticles. Spanish Broom fibers were extracted by patented method DiCoDe and the morphological, physical and mechanical properties were investigated. Chitosan nanoparticles were prepared by ionic gelation using different weight ratios between chitosan (CH) and tripolyphosphate (TPP). Nanoparticles were characterized in terms of size, zeta potential, yield, encapsulation efficiency, stability and drug release. Finally, the antibacterial activity against Staphylococcus aureus as well as in vitro cytotoxicity on HaCaT cells were evaluated. The best formulation CH/TPP 4:1 was selected based on the encapsulation efficiency and yield. Spanish Broom fibers impregnated with loaded nanoparticles showed an increased antibacterial activity against S. aureus compared to the same fibers containing VM without nanoparticles. Moreover, these fibers were not toxic to HaCaT keratinocytes cells. In conclusion, Spanish Broom fibers impregnated with VM loaded CH/TPP nanoparticles would appear to be a promising candidate for wound dressing application. Copyright © 2016 Elsevier B.V. All rights reserved.

Development of diclofenac sodium loaded magnetic nanocarriers of pectin interacted with chitosan for targeted and sustained drug delivery.

Science.gov (United States)

Dutta, Raj Kumar; Sahu, Saurabh

2012-09-01

A novel spherical magnetic nanocarrier of 100-150 nm dimensions made of pectin interacted with chitosan (MPCh-DS0.05) resulted in 99.5% encapsulation efficiency of diclofenac sodium (DS) as a model drug. Similarly, magnetic nanocarrier made of only pectin crosslinked with Ca(2+) (MPDS-0.05) resulted in only 60.6% encapsulation efficiency of DS. The increase in drug encapsulation efficiency (%) in MPCh-DS0.05 batch was due to synergistic drug encapsulation properties of pectin and chitosan. The structural and morphological features of these magnetic nanocarriers were studied by X-ray diffractometry (XRD), Fourier transform infrared-spectrometry (FT-IR), thermogravimetry, electron microscopy and dynamic light scattering (DLS) measurements. The magnetic properties were measured by vibrating sample magnetometer (VSM) and superconducting quantum unit interference device measurements (SQUID). The in vitro drug release was pH sensitive and exhibited sustained release sequentially in simulated gastric fluid (negligible release in 0-2h), simulated intestinal fluid (~69% release in 2-5h), simulated colonic fluid (5-60 h) and also in phosphate buffer at pH 7.4 (0-48 h). The drug release profile in phosphate buffer solution at pH 7.4 was in good agreement with swelling controlled mechanism on the basis of Korsemeyer-Peppas model. Copyright © 2012 Elsevier B.V. All rights reserved.

Microencapsulation of Purified Amylase Enzyme from Pitaya (Hylocereus polyrhizus Peel in Arabic Gum-Chitosan using Freeze Drying

Directory of Open Access Journals (Sweden)

Mehrnoush Amid

2014-03-01

Full Text Available Amylase is one of the most important enzymes in the world due to its wide application in various industries and biotechnological processes. In this study, amylase enzyme from Hylocereus polyrhizus was encapsulated for the first time in an Arabic gum-chitosan matrix using freeze drying. The encapsulated amylase retained complete biocatalytic activity and exhibited a shift in the optimum temperature and considerable increase in the pH and temperature stabilities compared to the free enzyme. Encapsulation of the enzyme protected the activity in the presence of ionic and non-ionic surfactants and oxidizing agents (H2O2 and enhanced the shelf life. The storage stability of amylase is found to markedly increase after immobilization and the freeze dried amylase exhibited maximum encapsulation efficiency value (96.2% after the encapsulation process. Therefore, the present study demonstrated that the encapsulation of the enzyme in a coating agent using freeze drying is an efficient method to keep the enzyme active and stable until required in industry.

Chitosan films incorporated with nettle (Urtica dioica L.) extract-loaded nanoliposomes: I. Physicochemical characterisation and antimicrobial properties.

Science.gov (United States)

Haghju, Sara; Beigzadeh, Sara; Almasi, Hadi; Hamishehkar, Hamed

2016-07-17

The objective of this study was to characterise and compare physical, mechanical and antimicrobial properties of chitosan-based films, containing free or nanoencapsulated nettle (Urtica dioica L.) extract (NE) at concentrations of 0, 0.5, 1 and 1.5% w/w. Nanoliposomes were prepared using soy-lecithin by thin-film hydration and sonication method to generate an average size of 107-136 nm with 70% encapsulation efficiency. The information on FT-IR reflected that some new interaction have occurred between chitosan and nanoliposomes. Despite the increasing yellowness and decreasing whiteness indexes, the nanoliposomes incorporation improved the thermal properties and mechanical stiffness and caused to decrease water vapour permeability (WVP), moisture uptake and water solubility. The possible antimicrobial activity of the films containing NE-loaded nanoliposomes against Staphylococcus aureus was decreased in comparison to free NE-incorporated films, which could be due to the inhibition effect of the encapsulation that prevents the release of NE from the matrix.

Flow Cytometry Detection of Bacterial Cell Entrapment within the Chitosan Hydrogel and Antibacterial Property of Extracted Chitosan

Directory of Open Access Journals (Sweden)

Nafise Sadat Majidi

2016-09-01

Full Text Available Background:   Chitosan is unbranched polysaccharide composed of D-glucosamine and N-acetyl-D-glucosamine. Chitosan, derived from shrimp shell, has broad antimicrobial properties against Gram-negative, Gram-positive bacteria and fungi. Methods:  Chitosan was extracted from shrimp shell and studied for cell entrapment and anti-bacterial properties. The hydrogel chitosan was used as the beads for cell entrapment and chitosan beads were designed to deliver cells and nutrients. These data confirmed with flow cytometric analyses.                 Results:   Experimental results exhibited that internal diffusion through the chitosan matrix was the main mechanism for whole gelation by TPP (Tri-polyphosphate. The minimum inhibitory concentration (MIC for chitosan against Staphylococcus aureus and Escherichia coli was 16 and 32 μg/ml respectively. Conclusion:  Despite the antimicrobial properties of chitosan, trapped bacteria in the gel network were alive and were chelated indicating that their access to the outside was limited.

Impact of molecular weight on the formation of electrosprayed chitosan microcapsules as delivery vehicles for bioactive compounds.

Science.gov (United States)

Gómez-Mascaraque, Laura G; Sanchez, Gloria; López-Rubio, Amparo

2016-10-05

The molecular weight of chitosan is one of its most determinant characteristics, which affects its processability and its performance as a biomaterial. However, information about the effect of this parameter on the formation of electrosprayed chitosan microcapsules is scarce. In this work, the impact of chitosan molecular weight on its electrosprayability was studied and correlated with its effect on the viscosity, surface tension and electrical conductivity of solutions. A Discriminant Function Analysis revealed that the morphology of the electrosprayed chitosan materials could be correctly predicted using these three parameters for almost 85% of the samples. The suitability of using electrosprayed chitosan capsules as carriers for bioactive agents was also assessed by loading them with a model active compound, (-)-epigallocatechin gallate (EGCG). This encapsulation, with an estimated efficiency of around 80% in terms of preserved antioxidant activity, showed the potential to prolong the antiviral activity of EGCG against murine norovirus via gradual bioactive release combined with its protection against degradation in simulated physiological conditions. Copyright © 2016 Elsevier Ltd. All rights reserved.

Synthesis of biodegradable plastic from tapioca with N-Isopropylacrylamid and chitosan using glycerol as plasticizer

Science.gov (United States)

Syaubari; Safwani, S.; Riza, M.

2018-04-01

One of natural polymers that can be used as raw material in the manufacture of biodegradable plastic is tapioca and chitosan. The addition of other compounds such as glycerol as plasticizer is to improve the characteristics of the plastic that already produced. N- Isopropylacrylamid (NIPAm) is an organic compound that can be synthesized into a polymer or polymer grafting which also biodegradable too. This research aims tostudy the synthesis of biodegradable plastics from tapioca with the addition of chitosan, NIPAm, poly(NIPAm) and analyze the characteristics of biodegradable plastics that already produced. This research was done in three stages, there are (1) polymerization NIPAm, (2) the grafting of chitosan-poly NIPAm and (3) the synthesis of biodegradable plastics from starch mixture with variation of addition chitosan, NIPAm, poly(NIPAm), chitosan-graft-poly(NIPAm) and also variations of glycerol as plasticizer. The results of this research is a thin sheet of plastic which is will get analyzed for the characteristics of functional groups, mechanical, morphological and its biodegradability. FTIR spectra showed the grafting process with the new group formation of CO single-bond at 850 cm-1. Plastic with the addition of NIPAm and 1 ml glycerol has the highest tensile strength value about 31.1 MPa. Plastic with poly(NIPAm) and 4 ml glycerol produces the highest elongation value about 153.72%. Plastic with Chitosan-graft-poly(NIPAm) with 1 ml glycerol has the longest biodegradation because of the small mass-loss for six weeks which is about 6.6%.

Synthesis and characterization of a stable humic-urease complex: application to barley seed encapsulation for improving N uptake.

Science.gov (United States)

Mvila, Beaufray G; Pilar-Izquierdo, María C; Busto, María D; Perez-Mateos, Manuel; Ortega, Natividad

2016-07-01

Most N fertilizers added to soil are not efficiently used by plants and are lost to the atmosphere or leached from the soil, causing environmental pollution and increasing cost. Barley seed encapsulation in calcium alginate gels containing free or immobilized urease to enhance plant utilization of soil N was investigated. Urease was immobilized with soil humic acids (HA). A central composite face-centered design was applied to optimize the immobilization process, reaching an immobilization yield of 127%. Soil stability of urease was enhanced after the immobilization. Seed encapsulation with free urease (FU) and humic-urease complex (HUC) resulted in a urease activity retention in the coating layer of 46% and 24%, and in germination rates of 87% and 92%, respectively. Under pot culture conditions, the pots planted with seeds encapsulated with FU and HUC showed higher ammonium N (NH4 (+) -N) (26% and 64%, respectively) than the control soil at 28 days after planting (DAP). Moreover, the seed encapsulation with FU and HUC increased the N uptake 83% and 97%, respectively, at 35 DAP. Seed encapsulation with urease could substantially contribute to enhancing plant N nutrition in the early stages of seedling establishment. © 2015 Society of Chemical Industry. © 2015 Society of Chemical Industry.

Preparation and optimization of submicron chitosan capsules by water-based electrospraying for food and bioactive packaging applications.

Science.gov (United States)

Sreekumar, Sruthi; Lemke, Philipp; Moerschbacher, Bruno M; Torres-Giner, Sergio; Lagaron, Jose M

2017-10-01

In the present study, a well-defined set of chitosans, with different degrees of acetylation (DA) and degrees of polymerization (DP), were processed by solution electrospraying from a water-based solvent. The solution properties, in terms of surface tension, conductivity, viscosity, and pH, were characterized and related to the physico-chemical properties of the chitosans. It was observed that both DA and DP values of a given chitosan, in combination with biopolymer concentration, mainly determined solution viscosity. This was, in turn, the major driving factor that defined the electrosprayability of chitosan. In addition, the physico-chemical properties of chitosans highly influenced solution conductivity and results indicated that the chitosan solutions with low or low-to-medium values of conductivity were the most optimal for electrospraying. The results obtained here also demonstrate that a good process control can be achieved by adjusting the working conditions, i.e. applied voltage, flow-rate, and tip-to-collector distance. Finally, it was also shown that electrosprayability of chitosan with inadequate physico-chemical properties can be improved by solution mixing of very different kinds of this polysaccharide. The resultant electrosprayed submicron chitosan capsules can be applied for encapsulation of food additives and to develop bioactive coatings of interest in food packaging, where these particles alone or containing functional ingredients can be released from the package into the food to promote a health benefit.

Chitosan and carboxymethyl-chitosan capping ligands: Effects on the nucleation and growth of hydroxyapatite nanoparticles for producing biocomposite membranes

Energy Technology Data Exchange (ETDEWEB)

Dumont, Vitor C.; Mansur, Alexandra A.P.; Carvalho, Sandhra M.; Medeiros Borsagli, Fernanda G.L.; Pereira, Marivalda M.; Mansur, Herman S., E-mail: hmansur@demet.ufmg.br

2016-02-01

Synthetic biomaterials based on calcium phosphates (CaP) have been widely studied for bone tissue reconstruction therapies, but no definitive solution that fulfills all of the required properties has been identified. Thus, this study reports the synthesis of composite membranes based on nanohydroxyapatite particles (nHA) embedded in chitosan (CHI) and O-carboxymethyl chitosan (CMC) matrices produced using a one-step co-precipitation method in water media. Biopolymers were used as capping ligands for simultaneously controlling the nucleation and growth of the nHA particles during the precipitation process and also to form the polymeric network of the biocomposites. The bionanocomposites were extensively characterized using light microscopy (LM), scanning and transmission electron microscopy (SEM/TEM), energy-dispersive X-ray spectroscopy (EDX), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), atomic force microscopy (AFM), X-ray micro-CT analysis (μCT), and MTT (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide) cell proliferation assays for cell cytotoxicity. The results demonstrated that the ligands used during the synthesis highly affected the composites produced, primarily due the changes in the mechanisms and kinetics of nucleation and growth of the HA particles at the nanoscale level. The SEM images revealed that the use of carboxyl-functionalized chitosan (CMC) ligands significantly reduced the average size of the HA nanoparticles and caused the formation of a narrower size distribution (90 ± 20 nm) compared to the HA nanoparticles produced with chitosan ligands (220 ± 50 nm). The same trend was verified by the AFM analysis, where the nHA particles were formed evenly dispersed in the polymer matrix. However, the CMC-based composites were more homogeneously distributed, which was endorsed by the images collected via X-ray micro-CT. The FTIR spectra and the XRD analysis indicated that nanosized hydroxyapatite was the

Dual drug loaded chitosan nanoparticles-sugar--coated arsenal against pancreatic cancer.

Science.gov (United States)

David, Karolyn Infanta; Jaidev, Leela Raghav; Sethuraman, Swaminathan; Krishnan, Uma Maheswari

2015-11-01

Pancreatic cancer is an aggressive form of cancer with poor survival rates. The increased mortality due to pancreatic cancer arises due to many factors such as development of multidrug resistance, presence of cancer stem cells, development of a stromal barrier and a hypoxic environment due to hypo-perfusion. The present study aims to develop a nanocarrier for a combination of drugs that can address these multiple issues. Quercetin and 5-fluorouracil were loaded in chitosan nanoparticles, individually as well as in combination. The nanoparticles were characterized for morphology, size, zeta potential, percentage encapsulation of drugs as well as their release profiles in different media. The dual drug-loaded carrier exhibited good entrapment efficiency (quercetin 95% and 5-fluorouracil 75%) with chitosan: quercetin: 5-fluorouracil in the ratio 3:1:2. The release profiles suggest that 5-fluorouracil preferentially localized in the periphery while quercetin was located towards the core of chitosan nanoparticles. Both drugs exhibited considerable association with the chitosan matrix. The dual drug-loaded carrier system exhibited significant toxicity towards pancreatic cancer cells both in the 2D as well as in the 3D cultures. We believe that the results from these studies can open up interesting options in the treatment of pancreatic cancer. Copyright © 2015 Elsevier B.V. All rights reserved.

Influence of formulation variables on survival of L. casei loaded in chitosan-Ca-alginate microparticles prepared by spray-drying

OpenAIRE

Petreska Ivanovska, Tanja; Petrusevska Tozi, Lidija; Smilkov, Katarina; Popovski, Emil; Stafilov, Trajče; Grozdanov, Anita; Geskovski, Nikola; Petkovska, Rumenka; Mladenovska, Kristina

2011-01-01

The objective of this work was to evaluate the effect of encapsulating material (chitosan, Ca and alginate)in given ranges of concentrations on viability of the probiotic L. casei in simulated in vivo condititons using polynomial regression model at 2nd level.

Vitamin D-fortified chitosan films from mushroom waste

Science.gov (United States)

Brown mushroom (Agaricus bisporus) stalk bases from mushroom waste were treated with UV-B light to rapidly increase vitamin D2 content. Chitin was also recovered from this waste and converted into chitosan by N-deacetylation. FTIR spectra showed that the mushroom chitosan were similar to chitosan fr...

pH-sensitive chitosan/alginate core-shell nanoparticles for efficient and safe oral insulin delivery.

Science.gov (United States)

Mukhopadhyay, Piyasi; Chakraborty, Souma; Bhattacharya, Sourav; Mishra, Roshnara; Kundu, P P

2015-01-01

Chitosan-alginate (CS/ALG) nanoparticles were prepared by formation of an ionotropic pre-gelation of an alginate (ALG) core entrapping insulin, followed by chitosan (CS) polyelectrolyte complexation, for successful oral insulin administration. Mild preparation process without harsh chemicals is aimed at improving insulin bio-efficiency in in vivo model. The nanoparticles showed an average particle size of 100-200 nm in dynamic light scattering (DLS), with almost spherical or sub-spherical shape and ∼ 85% of insulin encapsulation. Again, retention of almost entire amount of encapsulated insulin in simulated gastric buffer followed by its sustained release in simulated intestinal condition proved its pH sensitivity in in vitro release studies. Significant hypoglycemic effects with improved insulin-relative bioavailability (∼ 8.11%) in in vivo model revealed the efficacy of these core-shell nanoparticles of CS/ALG as an oral insulin carrier. No systemic toxicity was found after its peroral treatment, suggesting these core-shell nanoparticles as a promising device for potential oral insulin delivery. Copyright © 2014 Elsevier B.V. All rights reserved.

Preparation and anti-cancer activity of polymer-encapsulated curcumin nanoparticles

International Nuclear Information System (INIS)

Ha, Phuong Thu; Tran, Dai Lam; Nguyen, Xuan Phuc; Le, Mai Huong; Ha Tran, Thi Hong; Hoang, Thi My Nhung; Huong Le, Thi Thu; Duong, Tuan Quang

2012-01-01

Curcumin (Cur) is a yellow compound isolated from rhizome of the herb curcuma longa. Curcumin possesses antioxidant, anti-inflammatory, anti-carcinogenic and antimicrobial properties, and suppresses proliferation of many tumor cells. However, the clinical application of curcumin in cancer treatment is considerably limited due to its serious poor delivery characteristics. In order to increase the hydrophilicity and drug delivery capability, we encapsulated curcumin into copolymer PLA-TPGS, 1,3-beta-glucan (Glu), O-carboxymethyl chitosan (OCMCs) and folate-conjugated OCMCs (OCMCs-Fol). These polymer-encapsulated curcumin nanoparticles (Cur-PLA-TPGS, Cur-Glu, Cur-OCMCs and Cur-OCMCs-Fol) were characterized by infrared (IR), fluorescence (FL), photoluminescence (PL) spectra, field emission scanning electron microscopy (FE-SEM), and found to be spherical particles with an average size of 50–100 nm, being suitable for drug delivery applications. They were much more soluble in water than not only free curcumin but also other biodegradable polymer-encapsulated curcumin nanoparticles. The anti-tumor promoting assay was carried out, showing the positive effects of Cur-Glu and Cur-PLA-TPGS on tumor promotion of Hep-G2 cell line in vitro. Confocal microscopy revealed that the nano-sized curcumin encapsulated by polymers OCMCs and OCMCs-Fol significantly enhanced the cellular uptake (cancer cell HT29 and HeLa). (paper)

Preparation and anti-cancer activity of polymer-encapsulated curcumin nanoparticles

Science.gov (United States)

Thu Ha, Phuong; Huong Le, Mai; Nhung Hoang, Thi My; Thu Huong Le, Thi; Quang Duong, Tuan; Tran, Thi Hong Ha; Tran, Dai Lam; Phuc Nguyen, Xuan

2012-09-01

Curcumin (Cur) is a yellow compound isolated from rhizome of the herb curcuma longa. Curcumin possesses antioxidant, anti-inflammatory, anti-carcinogenic and antimicrobial properties, and suppresses proliferation of many tumor cells. However, the clinical application of curcumin in cancer treatment is considerably limited due to its serious poor delivery characteristics. In order to increase the hydrophilicity and drug delivery capability, we encapsulated curcumin into copolymer PLA-TPGS, 1,3-beta-glucan (Glu), O-carboxymethyl chitosan (OCMCs) and folate-conjugated OCMCs (OCMCs-Fol). These polymer-encapsulated curcumin nanoparticles (Cur-PLA-TPGS, Cur-Glu, Cur-OCMCs and Cur-OCMCs-Fol) were characterized by infrared (IR), fluorescence (FL), photoluminescence (PL) spectra, field emission scanning electron microscopy (FE-SEM), and found to be spherical particles with an average size of 50-100 nm, being suitable for drug delivery applications. They were much more soluble in water than not only free curcumin but also other biodegradable polymer-encapsulated curcumin nanoparticles. The anti-tumor promoting assay was carried out, showing the positive effects of Cur-Glu and Cur-PLA-TPGS on tumor promotion of Hep-G2 cell line in vitro. Confocal microscopy revealed that the nano-sized curcumin encapsulated by polymers OCMCs and OCMCs-Fol significantly enhanced the cellular uptake (cancer cell HT29 and HeLa).

Two-step preparation of nano-scaled magnetic chitosan particles using Triton X-100 reversed-phase water-in-oil microemulsion system

International Nuclear Information System (INIS)

Zhou, Zhengkun; Jiang, Feihong; Lee, Tung-Ching; Yue, Tianli

2013-01-01

Highlights: •A new two-step route for nano-scaled magnetic chitosan particles preparation. •Triton X-100 reversed-phase microemulsion system was used for chitosan coating. •Narrow size distribution of magnetic chitosan nanoparticles was achieved. •Quantitative evaluation of recoverability for the magnetic chitosan nanoparticles. -- Abstract: A new two-step route for the preparation of nano-scaled magnetic chitosan particles has been developed, different from reported one-step in situ preparation and two-step preparation method of reversed-phase suspension, Triton X-100 reversed-phase water-in-oil microemulsion encapsulation method was employed in coating the pre-prepared Fe 3 O 4 nanoparticles with chitosan. The resultant magnetic chitosan particles owned a narrow size distribution ranging from 50 to 92 nm. X-ray diffraction patterns (XRD) indicated that the chitosan coating procedure did not change the spinal structure of Fe 3 O 4 magnetic nanoparticles. The results of Fourier transform infrared (FTIR) analysis and thermogravimetric analysis (TGA) demonstrated that the chitosan was coated on Fe 3 O 4 nanoparticles and its average mass content was ∼50%. The saturated magnetization of the magnetic Fe 3 O 4 /chitosan nanoparticles reached 18.62 emu/g, meanwhile, the nanoparticles showed the characteristics of superparamagnetism. The magnetic chitosan nanoparticles showed a high recoverability of 99.99% in 10 min when pH exceeded 4. The results suggested that the as-prepared magnetic chitosan particles were nano-scaled with a narrow size distribution and a high recoverability

Characterization of Camptothecin-induced Genomic Changes in the Camptothecin-resistant T-ALL-derived Cell Line CPT-K5

DEFF Research Database (Denmark)

Kjeldsen, Eigil; Nielsen, Christine J F; Roy, Amit

2018-01-01

-K5 and its parental cell line. We identified copy number alterations affecting genes important for maintaining genome integrity and reducing CPT-induced DNA damage. We show for the first time that short tandem repeats are targets for TOP1 cleavage, that can be differentially stimulated by CPT.......Acquisition of resistance to topoisomerase I (TOP1)-targeting camptothecin (CPT) derivatives is a major clinical problem. Little is known about the underlying chromosomal and genomic mechanisms. We characterized the CPT-K5 cell line expressing mutant CPT-resistant TOP1 and its parental T......-cell derived acute lymphoblastic leukemia CPT-sensitive RPMI-8402 cell line by karyotyping and molecular genetic methods, including subtractive oligo-based array comparative genomic hybridization (soaCGH) analysis. Karyotyping revealed that CPT-K5 cells had acquired additional structural aberrations...

Preparation and characterization of chitosan-natural nano hydroxyapatite-fucoidan nanocomposites for bone tissue engineering.

Science.gov (United States)

Lowe, Baboucarr; Venkatesan, Jayachandran; Anil, Sukumaran; Shim, Min Suk; Kim, Se-Kwon

2016-12-01

Solid three dimensional (3D) composite scaffolds for bone tissue engineering were prepared using the freeze-drying method. The scaffolds were composed of chitosan, natural nano-hydroxyapatite (nHA) and fucoidan in the following combinations: chitosan, chitosan-fucoidan, chitosan-nHA, and chitosan-nHA-fucoidan. Fourier transform infrared spectroscopy (FT-IR), thermal gravimetric analysis (TGA), X-ray diffraction analysis (XRD), scanning electron microscopy (SEM), and optical microscopy (OM) were used to determine the physiochemical constituents and the morphology of the scaffolds. The addition of nHA into the chitosan-fucoidan composite scaffold reduced the water uptake and water retention. FT-IR analysis confirmed the presence of a phosphate group in the chitosan-nHA-fucoidan scaffold. This group is present because of the presence of nHA (isolated via alkaline hydrolysis from salmon fish bones). Microscopic results indicated that the dispersion of nHA and fucoidan in the chitosan matrix was uniform with a pore size of 10-400μm. The composite demonstrated a suitable micro architecture for cell growth and nutrient supplementation. This compatibility was further elucidated in vitro using periosteum-derived mesenchymal stem cells (PMSCs). The cells demonstrated high biocompatibility and excellent mineralization for the chitosan-nHA-fucoidan scaffold. We believe that a chitosan-nHA-fucoidan composite is a promising biomaterial for the scaffold that can be used for bone tissue regeneration. Copyright © 2016 Elsevier B.V. All rights reserved.

Effect of Encapsulation on Antimicrobial Activity of Herbal Extracts with Lysozyme

Directory of Open Access Journals (Sweden)

Petra Matouskova

2016-01-01

Full Text Available Resistance of microorganisms to antibiotics has increased. The use of natural components with antimicrobial properties can be of great significance to reduce this problem. The presented work is focused on the study of the effect of encapsulation of selected plant and animal antimicrobial substances (herbs, spices, lysozyme and nisin on their activity and stability. Antimicrobial components were packaged into liposomes and polysaccharide particles (alginate, chitosan and starch. Antimicrobial activity was tested against two Gram-positive (Bacillus subtilis and Micrococcus luteus and two Gram-negative (Escherichia coli and Serratia marcescens bacteria. Encapsulation was successful in all types of polysaccharide particles and liposomes. The prepared particles exhibited very good long-term stability, especially in aqueous conditions. Antimicrobial activity was retained in all types of particles. Liposomes with encapsulated herb and spice extracts exhibited very good inhibitory effect against all tested bacterial strains. Most of herbal extracts had very good antimicrobial effect against the tested Gram-negative bacterial strains, while Gram-positive bacteria were more sensitive to lysozyme particles. Thus, particles with co-encapsulated herbs and lysozyme are more active against different types of bacteria, and more stable and more effective during long-term storage. Particles with encapsulated mixture of selected plant extracts and lysozyme could be used as complex antimicrobial preparation with controlled release in the production of food and food supplements, pharmaceutical and cosmetic industries.

Effect of Green Tea Extract Encapsulated Into Chitosan Nanoparticles on Hepatic Fibrosis Collagen Fibers Assessed by Atomic Force Microscopy in Rat Hepatic Fibrosis Model.

Science.gov (United States)

Safer, Abdel-Majeed A; Hanafy, Nomany A; Bharali, Dhruba J; Cui, Huadong; Mousa, Shaker A

2015-09-01

The present study examined the effect of Green Tea Extract (GTE) encapsulated into Chitosan Nanoparticles (CS-NPs) on hepatic fibrosis in rat model as determined by atomic force microscopy (AFM). The bioactive compounds in GTE encapsulated into CS-NPs were determined using LC-MS/MS method. Additionally, the uptake of GTE-CS NPs in HepG2 cells showed enhanced uptake. In experimental fibrosis model, AFM was used as a high resolution microscopic tool to investigate collagen fibers as an indicator of hepatic fibrosis induced by treatment with CCl4. Paraffin sections of fibrotic liver tissues caused by CC4 treatment of rats and the effect of GTE-CS NPs treatment with or without CCl4 on hepatic fibrosis were examined. Liver tissues from the different groups of animals were de-waxed and processed as for normal H/E staining and Masson's trichrome staining to locate the proper area of ECM collagen in the CCl4 group versus collagen in liver tissues treated with the GTE-CS NPs with or without CCl4. Selected areas of paraffin sections were trimmed off and fixed flat on top of mica and inserted in the AFM stage. H/E staining, Masson's trichrome stained slides, and AFM images revealed that collagen fibers of 250 to 300 nm widths were abundant in the fibrotic liver samples while those of GTE-CS NPs were clear as in the control group. Data confirmed the hypothesis that GTE-CS NPs are effective in removing all the extracellular collagen caused by CCl4 in the hepatic fibrosis rat liver.

Preparation and characterization of chitosan/ZnAl2O4 films

International Nuclear Information System (INIS)

Araujo, P.M.A.G.; Santos, P.T.A.; Rodrigues, P.A.; Costa, A.C.F.M.; Araujo, E.M.

2012-01-01

Chitosan films have been explored for biomedical application, as the chitosan to be, low toxicity, abundant in nature, show affinity for dispersion loads and high mechanical strength. On the other hand, ZnAl 2 O 4 has energy gap of approximately 3.8 eV, which makes it useful for use as photoelectric device ultraviolet. Thus, this work has as objective to prepare films of quitosana/ZnAl 2 O 4 in proportions of 5:1, 5:2, 5:3, 5:4 and evaluate the structural, morphological and thermals characteristics. To this end, ZnAl2O4 first nanoparticles (NPs) was deagglomerated and 325 mesh sieve and added to chitosan diluted in 1% acetic acid, and dried at 60°C. After drying, a solution of 1M sodium hydroxide was added to obtain a film with neutral pH. The films were characterized by XRD, SEM and TG. For all proportions evaluated it was verified the presence of ZnAl 2 O)4 and chitosan phases. By micrographs, it was observed that there was formation of agglomerates of ZnAl 2 O 4 NPs both on the surface of the films, the encapsulated in chitosan. In all samples the ratio 5:4 showed the greatest consistency both in relation to the film surface of the nanoparticles in the chitosan matrix. TG/DTA curves of quitosana/ZnAl 2 O 4 film for all the samples showed that for the concentration of 5:1 to 5:3 occurred three mass loss while for concentration of 5:2 to 5:4 were only two stages decomposition. (author)

Various methods for determination of the degree of N-acetylation of chitin and chitosan: a review.

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Kasaai, Mohammad R

2009-03-11

Chitin, chitosan, and their derivatives have been identified as versatile biopolymers for a broad range of agriculture and food applications. Up to now, several methods have been developed to determine degree of N-acetylation, DA, for chitin and chitosan. In this article, an effort has been made to review the available literature information on the DA determination. These methods are classified into three categories: (1) spectroscopy (IR, (1)H NMR, (13)C NMR, (15)N NMR, and UV); (2) conventional (various types of titration, conductometry, potentiometry, ninhydrin assay, adsorption of free amino groups of chitosan by pictric acid); (3) destructive (elemental analysis, acid or enzymatic hydrolysis of chitin/chitosan and followed by the DA measurement by colorimetry or high performance liquid chromatography, pyrolysis-gas chromatography, and thermal analysis using differential scanning calorimetry) methods. These methods have been compared for their performances and limitations as well as their advantages and disadvantages. The use of IR and NMR spectroscopy methods provides a number of advantages. They do not need long-term procedures to prepare samples, and they provide information on the chemical structure. (1)H NMR and UV techniques are more sensitive than IR, (13)C NMR, and (15)N NMR spectroscopy. The IR technique is mostly used for a qualitative evaluation and comparison studies. Conventional methods are not applicable for highly acetylated chitin. The results of the latter methods are affected by ionic strength of the solvent, pH, and temperature of solution. In destructive methods, longer times are needed for the measurements compared to spectroscopy and conventional methods, but they are applicable for the entire range of the DA.

Kinetic and thermodynamic analysis of 10-hydroxy-camptothecin hydrolysis at physiological pH

Energy Technology Data Exchange (ETDEWEB)

Kunadharaju, Sasank [Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201 (United States); Savva, Michalakis [Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201 (United States)], E-mail: msavva@liu.edu

2008-09-15

To derive accurately the thermodynamic parameters governing the hydrolysis of the lactone ring at physiological pH, a derivative spectrophotometric technique was used for the simultaneous estimation of lactone and carboxylate forms of the 10-hydroxy-camptothecin (10-HC). Validation of the analytical method was done with respect to reproducibility, percent recovery, and level of detection. Hydrolysis of the lactone ring of 10-HC followed a 1st order decay with a rate constant equal to (0.0281 {+-} 0.001) min{sup -1} in PBS at pH 7.4 and at a temperature of 310 K. The activation energy for the hydrolysis reaction as calculated from the Arrhenius equation was (79.41 {+-} 0.92) kJ . mol{sup -1}, whereas the enthalpy and entropy of hydrolysis of 10-hydroxy-camptothecin were on average 12.45 kJ . mol{sup -1} and 52.37 J . K{sup -1} . mol{sup -1}, respectively. The positive enthalpy and entropy values of the 10-HC-lactone hydrolysis indicate that the reaction is endothermic and entropically driven.

Low toxic and high soluble camptothecin derivative 2–47 effectively induces apoptosis of tumor cells in vitro

Energy Technology Data Exchange (ETDEWEB)

Zhou, Yao; Zhao, Hong-Ye; Jiang, Du; Wang, Lu-Yao; Xiang, Cen; Wen, Shao-Peng [Key Laboratory of Industrial Fermentation Microbiology, Tianjin Key Laboratory of Industrial Microbiology, Sino-French Joint Laboratory of Food Nutrition, Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin 300457 (China); Fan, Zhen-Chuan [Key Laboratory of Food Nutrition and Safety, Tianjin University of Science & Technology, Ministry of Education, Tianjin, 300457 (China); Obesita & Algaegen LLC, College Station, TX 77845 (United States); Zhang, Yong-Min [Université Pierre et Marie Curie-Paris 6, Institut Parisien de Chimie Moléculaire UMR CNRS 8232, 4 place Jussieu, 75005, Paris (France); Guo, Na [Key Laboratory of Industrial Fermentation Microbiology, Tianjin Key Laboratory of Industrial Microbiology, Sino-French Joint Laboratory of Food Nutrition, Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin 300457 (China); Teng, Yu-Ou, E-mail: tyo201485@tust.edu.cn [Key Laboratory of Industrial Fermentation Microbiology, Tianjin Key Laboratory of Industrial Microbiology, Sino-French Joint Laboratory of Food Nutrition, Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin 300457 (China); Yu, Peng, E-mail: yupeng@tust.edu.cn [Key Laboratory of Industrial Fermentation Microbiology, Tianjin Key Laboratory of Industrial Microbiology, Sino-French Joint Laboratory of Food Nutrition, Safety and Medicinal Chemistry, Tianjin University of Science and Technology, Tianjin 300457 (China)

2016-04-08

The cytotoxic activity of camptothecin derivatives is so high that these compounds need to be further modified before their successful application as anti-cancer agents clinically. In this study, we reported the synthesis and biological evaluation of a novel camptothecin derivative called compound 2–47. The changes in structure did not reduce its activity to inhibit DNA topoisomerase I. Compound 2–47 induced apoptosis of many tumor cells including leukemia cells K562, Jurkat, HL-60, breast cancer cell BT-549, colon cancer cell HT-29 and liver cancer cell HepG2 with a half maximal inhibitory concentration (IC{sub 50}) of 2- to 3-fold lower than HCPT as a control. In particular, 2–47 inhibited the proliferation of Jurkat cells with an IC{sub 50} of as low as 40 nM. By making use of Jurkat cell as a model, following treatment of Jurkat cells, compound 2–47 activated caspase-3 and PARP, resulting in a decreased Bcl-2/Bax ratio. These data showed that compound 2–47 induces Jurkat cell death through the mitochondrial apoptotic pathway. In addition, compound 2–47 showed a decreased cytotoxic activity against normal cells and an improved solubility in low-polar solvent. For example, compound 2–47 solutes in CHCl{sub 3} 130-fold higher than HCPT. Taken together, our data demonstrated that camptothecin derivative 2–47 notably inhibits the tumor cell proliferation through mitochondrial-mediated apoptosis in vitro. - Highlights: • Compound 2–47 showed a wide inhibitory effect on the tested tumor cell lines with an IC{sub 50} of 3 times lower than that of HCPT in general. • Compound 2–47 inhibited the proliferation of the human leukemia cell Jurkat at an IC{sub 50} of as low as 40 nM. • As compared to HCPT, compound 2–47 showed much reduced cytotoxicity on normal human cells. • As compared to others, compound 2–47 showed a hundreds-fold higher solubility in non-polar organic solution.

Antimicrobial activity of silver nanoparticles encapsulated in poly-N-isopropylacrylamide-based polymeric nanoparticles.

Science.gov (United States)

Qasim, Muhammad; Udomluck, Nopphadol; Chang, Jihyun; Park, Hansoo; Kim, Kyobum

2018-01-01

In this study, we analyzed the antimicrobial activities of poly- N -isopropylacrylamide (pNIPAM)-based polymeric nanoparticles encapsulating silver nanoparticles (AgNPs). Three sizes of AgNP-encapsulating pNIPAM- and pNIPAM-NH 2 -based polymeric nanoparticles were fabricated. Highly stable and uniformly distributed AgNPs were encapsulated within polymeric nanoparticles via in situ reduction of AgNO 3 using NaBH 4 as the reducing agent. The formation and distribution of AgNPs was confirmed by UV-visible spectroscopy, transmission electron microscopy, and inductively coupled plasma optical emission spectrometry, respectively. Both polymeric nanoparticles showed significant bacteriostatic activities against Gram-negative ( Escherichia coli ) and Gram-positive ( Staphylococcus aureus ) bacteria depending on the nanoparticle size and amount of AgNO 3 used during fabrication.

Injectable porous nano-hydroxyapatite/chitosan/tripolyphosphate scaffolds with improved compressive strength for bone regeneration

Energy Technology Data Exchange (ETDEWEB)

Uswatta, Suren P.; Okeke, Israel U. [Department of Bioengineering, The University of Toledo, Toledo, OH 43614 (United States); Jayasuriya, Ambalangodage C., E-mail: a.jayasuriya@utoledo.edu [Department of Bioengineering, The University of Toledo, Toledo, OH 43614 (United States); Department of Orthopaedic Surgery, The University of Toledo, Toledo, OH 43614 (United States)

2016-12-01

In this study we have fabricated porous injectable spherical scaffolds using chitosan biopolymer, sodium tripolyphosphate (TPP) and nano-hydroxyapatite (nHA). TPP was primarily used as an ionic crosslinker to crosslink nHA/chitosan droplets. We hypothesized that incorporating nHA into chitosan could support osteoconduction by emulating the mineralized cortical bone structure, and improve the Ultimate Compressive Strength (UCS) of the scaffolds. We prepared chitosan solutions with 0.5%, 1% and 2% (w/v) nHA concentration and used simple coacervation and lyophilization techniques to obtain spherical scaffolds. Lyophilized spherical scaffolds had a mean diameter of 1.33 mm (n = 25). Further, portion from each group lyophilized scaffolds were soaked and dried to obtain Lyophilized Soaked and Dried (LSD) scaffolds. LSD scaffolds had a mean diameter of 0.93 mm (n = 25) which is promising property for the injectability. Scanning Electron Microscopy images showed porous surface morphology and interconnected pore structures inside the scaffolds. Lyophilized and LSD scaffolds had surface pores < 10 and 2 μm, respectively. 2% nHA/chitosan LSD scaffolds exhibited UCS of 8.59 MPa compared to UCS of 2% nHA/chitosan lyophilized scaffolds at 3.93 MPa. Standardize UCS values were 79.98 MPa and 357 MPa for 2% nHA/chitosan lyophilized and LSD particles respectively. One-way ANOVA results showed a significant increase (p < 0.001) in UCS of 1% and 2% nHA/chitosan lyophilized scaffolds compared to 0% and 0.5% nHA/chitosan lyophilized scaffolds. Moreover, 2% nHA LSD scaffolds had significantly increased (p < 0.005) their mean UCS by 120% compared to 2% nHA lyophilized scaffolds. In a drawback, all scaffolds have lost their mechanical properties by 95% on the 2nd day when fully immersed in phosphate buffered saline. Additionally live and dead cell assay showed no cytotoxicity and excellent osteoblast attachment to both lyophilized and LSD scaffolds at the end of 14th day of in vitro

Injectable porous nano-hydroxyapatite/chitosan/tripolyphosphate scaffolds with improved compressive strength for bone regeneration

International Nuclear Information System (INIS)

Uswatta, Suren P.; Okeke, Israel U.; Jayasuriya, Ambalangodage C.

2016-01-01

In this study we have fabricated porous injectable spherical scaffolds using chitosan biopolymer, sodium tripolyphosphate (TPP) and nano-hydroxyapatite (nHA). TPP was primarily used as an ionic crosslinker to crosslink nHA/chitosan droplets. We hypothesized that incorporating nHA into chitosan could support osteoconduction by emulating the mineralized cortical bone structure, and improve the Ultimate Compressive Strength (UCS) of the scaffolds. We prepared chitosan solutions with 0.5%, 1% and 2% (w/v) nHA concentration and used simple coacervation and lyophilization techniques to obtain spherical scaffolds. Lyophilized spherical scaffolds had a mean diameter of 1.33 mm (n = 25). Further, portion from each group lyophilized scaffolds were soaked and dried to obtain Lyophilized Soaked and Dried (LSD) scaffolds. LSD scaffolds had a mean diameter of 0.93 mm (n = 25) which is promising property for the injectability. Scanning Electron Microscopy images showed porous surface morphology and interconnected pore structures inside the scaffolds. Lyophilized and LSD scaffolds had surface pores < 10 and 2 μm, respectively. 2% nHA/chitosan LSD scaffolds exhibited UCS of 8.59 MPa compared to UCS of 2% nHA/chitosan lyophilized scaffolds at 3.93 MPa. Standardize UCS values were 79.98 MPa and 357 MPa for 2% nHA/chitosan lyophilized and LSD particles respectively. One-way ANOVA results showed a significant increase (p < 0.001) in UCS of 1% and 2% nHA/chitosan lyophilized scaffolds compared to 0% and 0.5% nHA/chitosan lyophilized scaffolds. Moreover, 2% nHA LSD scaffolds had significantly increased (p < 0.005) their mean UCS by 120% compared to 2% nHA lyophilized scaffolds. In a drawback, all scaffolds have lost their mechanical properties by 95% on the 2nd day when fully immersed in phosphate buffered saline. Additionally live and dead cell assay showed no cytotoxicity and excellent osteoblast attachment to both lyophilized and LSD scaffolds at the end of 14th day of in vitro

Nerve transection repair using laser-activated chitosan in a rat model.

Science.gov (United States)

Bhatt, Neel K; Khan, Taleef R; Mejias, Christopher; Paniello, Randal C

2017-08-01

Cranial nerve transection during head and neck surgery is conventionally repaired with microsuture. Previous studies have demonstrated recovery with laser nerve welding (LNW), a novel alternative to microsuture. LNW has been reported to have poorer tensile strength, however. Laser-activated chitosan, an adhesive biopolymer, may promote nerve recovery while enhancing the tensile strength of the repair. Using a rat posterior tibial nerve injury model, we compared four different methods of nerve repair in this pilot study. Animal study. Animals underwent unilateral posterior tibial nerve transection. The injury was repaired by potassium titanyl phosphate (KTP) laser alone (n = 20), KTP + chitosan (n = 12), microsuture + chitosan (n = 12), and chitosan alone (n = 14). Weekly walking tracks were conducted to measure functional recovery (FR). Tensile strength (TS) was measured at 6 weeks. At 6 weeks, KTP laser alone had the best recovery (FR = 93.4% ± 8.3%). Microsuture + chitosan, KTP + chitosan, and chitosan alone all showed good FR (87.4% ± 13.5%, 84.6% ± 13.0%, and 84.1% ± 10.0%, respectively). One-way analysis of variance was performed (F(3,56) = 2.6, P = .061). A TS threshold of 3.8 N was selected as a control mean recovery. Three groups-KTP alone, KTP + chitosan, and microsuture + chitosan-were found to meet threshold 60% (95% confidence interval [CI]: 23.1%-88.3%), 75% (95% CI: 46.8%-91.1%), and 100% (95% CI: 75.8%-100.0%), respectively. In the posterior tibial nerve model, all repair methods promoted nerve recovery. Laser-activated chitosan as a biopolymer anchor provided good TS and appears to be a novel alternative to microsuture. This repair method may have surgical utility following cranial nerve injury during head and neck surgery. NA Laryngoscope, 127:E253-E257, 2017. © 2017 The American Laryngological, Rhinological and Otological Society, Inc.

Microfluidics and BIO-encapsulation for drug- and cell-therapy

Science.gov (United States)

Aloisi, A.; Toma, C. C.; Di Corato, R.; Rinaldi, R.

2017-08-01

We present the construction and the application of biocompatible micro- and nano-structures that can be administered systemically and transport in a targeted and effective way drugs, small molecules, stem cells or immune system cells. These polymeric nano-systems represent a primary goal for the treatment of a wide family of neurological/systemic disorders, as well as tumors and/or acute injuries. As natural, biocompatible, biodegradable and non-immunogenic building blocks, alginate and chitosan are been currently exploited. Ionotropic pre-gelation of the alginate core, followed by chitosan polyelectrolyte complexation, allows to encapsulate selected active molecules by means of physical entrapment and electrostatic interactions within sub-micron sized hydrogel vesicles. Here we present a microfluidicassisted assembly method of nano- and micro-vesicles -under sterile, closed environment and gas exchange adjustable conditions, which is a critical issue, when the cargo to be uploaded is very sensitive. Polymer/polymer and polymer/drug mass ratio relationship are crucial in order to attain the optimum in terms of shuttle size and cargo concentration. By modulating polymer reticulation conditions, it become possible to control drug loading efficiency as well as drug delivery dynamics. Recent results on the application of these vesicles for the encapsulation and delivery of Inhibin-A and Decorin, proteins involved in acute kidney injury (AKI), for Renal tubular cell regeneration will be presented. Finally, the impact of these polysaccharide sub-micron vesicles on Human Immune cells and the metabolic and functional activity of cells embedded in the assembled vesicles will be presented and discussed.

Preparation and characterization of β-cyclodextrin grafted N-maleoyl chitosan nanoparticles for drug delivery

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Xinyu Hou

2017-11-01

Full Text Available β-cyclodextrin (CD grafted N-maleoyl chitosan (CD-g-NMCS with two different degrees of substitution (DS of N-maleoyl (DS = 21.2% and 30.5% were synthesized from maleic anhydride and chitosan bearing pendant cyclodextrin (CD-g-CS. CD-g-NMCS based nanoparticles were prepared via an ionic gelation method together with chitosan and CD-g-CS nanoparticles. The size and zeta potential of prepared CD-g-NMCS nanoparticles were 179.2~274.0 nm and 36.2~42.4 mV, respectively. In vitro stability test indicated that CD-g-NMCS nanoparticles were more stable in phosphate-buffered saline compared with chitosan nanoparticles. Moreover, a poorly water-soluble drug, ketoprofen (KTP, was selected as a model drug to study the obtained nanoparticle's potentials as drug delivery carriers. The drug loading efficiency of CD-g-NMCS20 nanoparticles were 14.8% for KTP. MTT assay showed that KTP loaded CD-g-NMCS nanoparticles were safe drug carriers. Notably, in vitro drug release studies showed that KTP was released in a sustained-release manner for the nanoparticles. The pharmacokinetic of drug loaded CD-g-NMCS20 nanoparticles were evaluated in rats after intravenous administration. The results of studies revealed that, compared with free KTP, KTP loaded CD-g-NMCS20 nanoparticles exhibited a significant increase in AUC0→24h and mean residence time by 6.6-fold and 2.9-fold, respectively. Therefore, CD-g-NMCS nanoparticles could be used as a novel promising nanoparticle-based drug delivery system for sustained release of poorly water-soluble drugs. The carboxylic acid groups of the CD-g-NMCS molecule provide convenient sites for further structural modifications including introduction of tissue- or disease- specific targeting groups.

Two-step preparation of nano-scaled magnetic chitosan particles using Triton X-100 reversed-phase water-in-oil microemulsion system

Energy Technology Data Exchange (ETDEWEB)

Zhou, Zhengkun; Jiang, Feihong [College of Food Science and Engineering, Northwest A and F University, Yangling, Shaanxi 712100 (China); Lee, Tung-Ching, E-mail: lee@aesop.rutgers.edu [Department of Food Science, Rutgers, the State University of New Jersey, 65 Dudley Road, New Brunswick, NJ 08901 (United States); Yue, Tianli, E-mail: yuetl305@nwsuaf.edu.cn [College of Food Science and Engineering, Northwest A and F University, Yangling, Shaanxi 712100 (China)

2013-12-25

Highlights: •A new two-step route for nano-scaled magnetic chitosan particles preparation. •Triton X-100 reversed-phase microemulsion system was used for chitosan coating. •Narrow size distribution of magnetic chitosan nanoparticles was achieved. •Quantitative evaluation of recoverability for the magnetic chitosan nanoparticles. -- Abstract: A new two-step route for the preparation of nano-scaled magnetic chitosan particles has been developed, different from reported one-step in situ preparation and two-step preparation method of reversed-phase suspension, Triton X-100 reversed-phase water-in-oil microemulsion encapsulation method was employed in coating the pre-prepared Fe{sub 3}O{sub 4} nanoparticles with chitosan. The resultant magnetic chitosan particles owned a narrow size distribution ranging from 50 to 92 nm. X-ray diffraction patterns (XRD) indicated that the chitosan coating procedure did not change the spinal structure of Fe{sub 3}O{sub 4} magnetic nanoparticles. The results of Fourier transform infrared (FTIR) analysis and thermogravimetric analysis (TGA) demonstrated that the chitosan was coated on Fe{sub 3}O{sub 4} nanoparticles and its average mass content was ∼50%. The saturated magnetization of the magnetic Fe{sub 3}O{sub 4}/chitosan nanoparticles reached 18.62 emu/g, meanwhile, the nanoparticles showed the characteristics of superparamagnetism. The magnetic chitosan nanoparticles showed a high recoverability of 99.99% in 10 min when pH exceeded 4. The results suggested that the as-prepared magnetic chitosan particles were nano-scaled with a narrow size distribution and a high recoverability.

Facile synthesis of radial-like macroporous superparamagnetic chitosan spheres with in-situ co-precipitation and gelation of ferro-gels.

Directory of Open Access Journals (Sweden)

Chih-Hui Yang

Full Text Available Macroporous chitosan spheres encapsulating superparamagnetic iron oxide nanoparticles were synthesized by a facile and effective one-step fabrication process. Ferro-gels containing ferrous cations, ferric cations and chitosan were dropped into a sodium hydroxide solution through a syringe pump. In addition, a sodium hydroxide solution was employed for both gelation (chitosan and co-precipitation (ferrous cations and ferric cations of the ferro-gels. The results showed that the in-situ co-precipitation of ferro-ions gave rise to a radial morphology with non-spheroid macro pores (large cavities inside the chitosan spheres. The particle size of iron oxide can be adjusted from 2.5 nm to 5.4 nm by tuning the concentration of the sodium hydroxide solution. Using Fourier Transform Infrared Spectroscopy and X-ray diffraction spectra, the synthesized nanoparticles were illustrated as Fe(3O(4 nanoparticles. In addition, the prepared macroporous chitosan spheres presented a super-paramagnetic behaviour at room temperature with a saturation magnetization value as high as ca. 18 emu/g. The cytotoxicity was estimated using cell viability by incubating doses (0∼1000 µg/mL of the macroporous chitosan spheres. The result showed good viability (above 80% with alginate chitosan particles below 1000 µg/mL, indicating that macroporous chitosan spheres were potentially useful for biomedical applications in the future.

Chitosan and Nanohydroxyapatite Roles in Physical and Chemical Characteristics of Gelatin/Chitosan/Nanohydroxyapatite Microspheres

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S. Bagheri-Khoulenjani

2010-12-01

Full Text Available The effects of chitosan/biopolymer (C/P and nanohydroxyapatite/ biopolymer (nHA/P weight ratios on particle size and its uniformity, cross-linking density and NH2 content of nano-hydroxyapatite/chitosan/gelatin (nHA/C/G microspheres were investigated. Microspheres were fabricated using water-in-oil emulsion. Cross-linking of microspheres was performed using water soluble carbodiimide. Particle size and its uniformity were evaluated using an optical microscope. The morphology of microspheres was studied by scanning electron microscopy. The obtained data from particle size measurements revealed that increments in C/P ratio increased the particle size while reducing its uniformity, and increased the NH2 content and cross linking density of the microspheres. It was shown that incremental increase in nHA/P ratio increased the particle size and its uniformity and reduced the NH2 content and cross-linking density of the microspheres.Morphological studies showed that the fabricated microspheres had spherical shape in medium level of C/P ratio and nHA/P ratio. However, increasing in chitosan/biopolymer ratio induced some micro-cracks into the structure of microspheres.

Chitosan-based nanoparticles for rosmarinic acid ocular delivery--In vitro tests.

Science.gov (United States)

da Silva, Sara Baptista; Ferreira, Domingos; Pintado, Manuela; Sarmento, Bruno

2016-03-01

In this study, chitosan nanoparticles were used to encapsulate antioxidant rosmarinic acid, Salvia officinalis (sage) and Satureja montana (savory) extracts as rosmarinic acid natural vehicles. The nanoparticles were prepared by ionic gelation using chitosan and sodium tripolyphosphate (TPP) in a mass ratio of 7:1, at pH 5.8. Particle size distribution analysis and transmission electron microscopy (TEM) confirmed the size ranging from 200 to 300 nm, while surface charge of nanoparticles ranged from 20 to 30 mV. Nanoparticles demonstrate to be safe without relevant cytotoxicity against retina pigment epithelium (ARPE-19) and human cornea cell line (HCE-T). The permeability study in HCE monolayer cell line showed an apparent permeability coefficient Papp of 3.41±0.99×10(-5) and 3.24±0.79×10(-5) cm/s for rosmarinic acid loaded chitosan nanoparticles and free in solution, respectively. In ARPE-19 monolayer cell line the Papp was 3.39±0.18×10(-5) and 3.60±0.05×10(-5) cm/s for rosmarinic acid loaded chitosan nanoparticles and free in solution, respectively. Considering the mucin interaction method, nanoparticles indicate mucoadhesive proprieties suggesting an increased retention time over the ocular mucosa after instillation. These nanoparticles may be promising drug delivery systems for ocular application in oxidative eye conditions. Copyright © 2015 Elsevier B.V. All rights reserved.

Camptothecin and khat (Catha edulis Forsk. induced distinct cell death phenotypes involving modulation of c-FLIPL, Mcl-1, procaspase-8 and mitochondrial function in acute myeloid leukemia cell lines

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Fossan Kjell O

2009-11-01

Full Text Available Abstract Background An organic extract of the recreational herb khat (Catha edulis Forsk. triggers cell death in various leukemia cell lines in vitro. The chemotherapeutics camptothecin, a plant alkaloid topoisomerase I inhibitor, was tested side-by-side with khat in a panel of acute myeloid leukemia cell lines to elucidate mechanisms of toxicity. Results Khat had a profound effect on MOLM-13 cells inducing mitochondrial damage, chromatin margination and morphological features of autophagy. The effects of khat on mitochondrial ultrastructure in MOLM-13 correlated with strongly impaired routine respiration, an effect neither found in the khat-resistant MV-4-11 cells nor in camptothecin treated cells. Enforced expression of anti-apoptotic Bcl-2 protein provided protection against camptothecin-induced cell death and partly against khat toxicity. Khat-induced cell death in MOLM-13 cells included reduced levels of anti-apoptotic Mcl-1 protein, while both khat and camptothecin induced c-FLIPL cleavage and procaspase-8 activation. Conclusion Khat activated a distinct cell death pathway in sensitive leukemic cells as compared to camptothecin, involving mitochondrial damage and morphological features of autophagy. This suggests that khat should be further explored in the search for novel experimental therapeutics.

Cytotoxicity and apoptotic effects of tea polyphenol-loaded chitosan nanoparticles on human hepatoma HepG2 cells.

Science.gov (United States)

Liang, Jin; Li, Feng; Fang, Yong; Yang, Wenjian; An, Xinxin; Zhao, Liyan; Xin, Zhihong; Cao, Lin; Hu, Qiuhui

2014-03-01

Tea polyphenols have strong antioxidant and antitumor activities. However, these health benefits are limited due to their poor in vivo stability and low bioavailability. Chitosan nanoparticles as delivery systems may provide an alternative approach for enhancing bioavailability of poorly absorbed drugs. In this study, tea polyphenol-loaded chitosan nanoparticles have been prepared using two different chitosan biomaterials, and their antitumor effects were evaluated in HepG2 cells, including cell cytotoxicity comparison, cell morphology analysis, cell apoptosis and cell cycle detection. The results indicated that the tea polyphenol-loaded chitosan nanoparticles showed a branch shape and heterogeneous distribution in prepared suspension. MTT assay suggested that tea polyphenol-loaded chitosan nanoparticles could inhibit the proliferation of HepG2 cells, and the cytotoxicity rates were increased gradually and appeared an obvious dose-dependent relationship. Transmission electron microscope images showed that the HepG2 cells treated with tea polyphenol-loaded chitosan nanoparticles exhibited some typical apoptotic features, such as microvilli disappearance, margination of nuclear chromatin, intracytoplasmic vacuoles and the mitochondrial swelling. In addition, the tea polyphenol-loaded chitosan nanoparticles had relatively weak inhibitory effects on HepG2 cancer cells compared with tea polyphenols. Tea polyphenols not only induced cancer cell apoptosis, but also promoted their necrosis. However, tea polyphenol-loaded chitosan nanoparticles exhibited their antitumor effects mainly through inducing cell apoptosis. Our results revealed that the inhibition effects of tea polyphenol-loaded chitosan nanoparticles on tumor cells probably depended on their controlled drug release and effective cell delivery. The chitosan nanoparticles themselves as the delivery carrier showed limited antitumor effects compared with their encapsulated drugs. Copyright © 2013. Published by

Surface functionalization of superparamagnetic nanoparticles encapsulated by chitosan for protein immobilization

International Nuclear Information System (INIS)

Sousa, Jose Silva de

2010-01-01

Nanoscience and nanotechnology have opened up numerous developments of devices and systems on the nanometer scale, with new molecular organization, properties and functions. In this context, the polymeric magnetic nanoparticles are composites formed by magnetic materials with a particle size between 1 and 100 nm combined with functional polymers. They are well-known and have been widely studied because of its applications in various technology areas. Applications on the biological and medical areas include separation and immobilization of enzymes and proteins, improved techniques of magnetic resonance imaging and diagnostic systems for controlled drug delivery. In this work, proteins were immobilized on the surface of a biopolymer combined with superparamagnetic particles of magnetite. The biopolymer chitosan was used, cross-linked and functionalized with glutaraldehyde, applicable to the biological assays. Three types of magnetic composites were obtained, which were called QM1Glu, QM2NaGlu and QM3Glu. They were characterized by X-ray diffraction, scanning electron microscopy, vibrating sample magnetometry, differential scanning calorimetry, thermogravimetry and infrared spectroscopy. They were evaluated concerning the immobilization of the proteins bovine serum albumin (BSA), collagen and trypsin. The study showed that the immobilization of proteins on the biopolymer occurred in 30 min of incubation. The magnetic composite of non functionalized chitosan (QM3) was also evaluated. For trypsin, it was found that the immobilization potential of QM3 was higher than that observed for QM3Glu. After 30 days, the trypsin of the QM3-Trip and QM3Glu-Trip was still with activity. The activity and the enzyme kinetics of the QM3Glu-Trip with the substrate BApNA were demonstrated. (author)

Biomedical Activity of Chitin/Chitosan Based Materials—Influence of Physicochemical Properties Apart from Molecular Weight and Degree of N-Acetylation

Directory of Open Access Journals (Sweden)

Mirko X. Weinhold

2011-11-01

Full Text Available The physicochemical nature of chitin and chitosan, which influences the biomedical activity of these compounds, is strongly related to the source of chitin and the conditions of the chitin/chitosan production process. Apart from widely described key factors such as weight-averaged molecular weight (MW and degree of N-acetylation (DA, other physicochemical parameters like polydispersity (MW/MN, crystallinity or the pattern of acetylation (PA have to be taken into consideration. From the biological point of view, these parameters affect a very important factor—the solubility of chitin and chitosan in water and organic solvents. The physicochemical properties of chitosan solutions can be controlled by manipulating solution conditions (temperature, pH, ionic strength, concentration, solvent. The degree of substitution of the hydroxyl and the amino groups or the degree of quaternization of the amino groups also influence the mechanical and biological properties of chitosan samples. Finally, a considerable research effort has been directed towards developing safe and efficient chitin/chitosan-based products because many factors, like the size of nanoparticles, can determine the biomedical characteristics of medicinal products. The influence of these factors on the biomedical activity of chitin/chitosan-based products is presented in this report in more detail.

Glycol chitosan

DEFF Research Database (Denmark)

Danielsen, E Thomas; Danielsen, E Michael

2017-01-01

Chitosan is a polycationic polysaccharide consisting of β-(1-4)-linked glucosamine units and due to its mucoadhesive properties, chemical derivatives of chitosan are potential candidates as enhancers for transmucosal drug delivery. Recently, glycol chitosan (GC), a soluble derivative of chitosan...

Impact of salt form and molecular weight of chitosan on swelling and drug release from chitosan matrix tablets.

Science.gov (United States)

Huanbutta, Kampanart; Cheewatanakornkool, Kamonrak; Terada, Katsuhide; Nunthanid, Jurairat; Sriamornsak, Pornsak

2013-08-14

Magnetic resonance imaging (MRI) and gravimetric techniques were used to assess swelling and erosion behaviors of hydrophilic matrix tablets made of chitosan. The impact of salt form, molecular weight (MW) and dissolution medium on swelling behavior and drug (theophylline) release was studied. The matrix tablets made of chitosan glycolate (CGY) showed the greatest swelling in both acid and neutral media, compared to chitosan aspartate, chitosan glutamate and chitosan lactate. MRI illustrated that swelling region of CGY in both media was not different in the first 100 min but glassy region (dry core) in 0.1N HCl was less than in pH 6.8 buffer. The tablets prepared from chitosan with high MW swelled greater than those of low MW. Moreover, CGY can delay drug release in the acid condition due to thick swollen gel and low erosion rate. Therefore, CGY may be suitably applied as sustained drug release polymer or enteric coating material. Copyright © 2013 Elsevier Ltd. All rights reserved.

Chitosan-carboxymethylcellulose based microcapsules formulation for controlled release of active ingredients from cosmeto textile

Science.gov (United States)

Roy, J. C.; Ferri, A.; Salaün, F.; Giraud, S.; Chen, G.; Jinping, G.

2017-10-01

Chitosan-based emulsions were prepared at pH from 4.0 to 6.0. The zeta potential and droplet size were monitored at different pH. Double emulsions (wateroil- water) were observed due to the stiff conformation of chitosan at pH 4.0. At pH 5.0, the emulsion droplets were the smallest (2.9 μm) of the experimental pH range. The emulsion droplets were well dispersed due to high surface charge of chitosan (for example, +50 mV at pH 5.5) in entire pH range. The emulsion was treated with carboxymethyl cellulose (CMC) for neutralizing the charged chitosan on the surface of emulsion droplets. Above 10×10-2 mg/ml of CMC, no change in zeta potential was observed indicating no more free chitosan existed after neutralization with CMC. The emulsion was then crosslinked with different amount of glutaraldehyde. Upon increasing the amount of glutaraldehyde, the amount of core content inside the microcapsule and encapsulation efficiency of shell materials decreased gradually. The Dynamic Scanning Calorimetry data confirmed no interaction between core and shell material in the microencapsulation process. The thermal degradation of the microcapsules was examined by thermogravimetric analysis and a gradual decrease in the degradation temperature upon increasing glutaraldehyde concentration was found. The tuning of CMC concentration can provide valuable information regarding stable emulsion and efficient microcapsule formulation via coacervation.

Applying quality by design (QbD) concept for fabrication of chitosan coated nanoliposomes.

Science.gov (United States)

Pandey, Abhijeet P; Karande, Kiran P; Sonawane, Raju O; Deshmukh, Prashant K

2014-03-01

In the present investigation, a quality by design (QbD) strategy was successfully applied to the fabrication of chitosan-coated nanoliposomes (CH-NLPs) encapsulating a hydrophilic drug. The effects of the processing variables on the particle size, encapsulation efficiency (%EE) and coating efficiency (%CE) of CH-NLPs (prepared using a modified ethanol injection method) were investigated. The concentrations of lipid, cholesterol, drug and chitosan; stirring speed, sonication time; organic:aqueous phase ratio; and temperature were identified as the key factors after risk analysis for conducting a screening design study. A separate study was designed to investigate the robustness of the predicted design space. The particle size, %EE and %CE of the optimized CH-NLPs were 111.3 nm, 33.4% and 35.2%, respectively. The observed responses were in accordance with the predicted response, which confirms the suitability and robustness of the design space for CH-NLP formulation. In conclusion, optimization of the selected key variables will help minimize the problems related to size, %EE and %CE that are generally encountered when scaling up processes for NLP formulations. The robustness of the design space will help minimize both intra-batch and inter-batch variations, which are quite common in the pharmaceutical industry.

Formation of nano-hydroxyapatite crystal in situ in chitosan-pectin polyelectrolyte complex network

International Nuclear Information System (INIS)

Li Junjie; Zhu Dunwan; Yin Jianwei; Liu Yuxi; Yao Fanglian; Yao Kangde

2010-01-01

Hydroxyapatite (HA)/polysaccharide composites have been widely used in bone tissue engineering due to their chemical similarity to natural bone. Polymer matrix-mediated synthesis of nano-hydroxyapatite is one of the simplest models for biomimetic. In this article, the nano-hydroxyapatite/chitosan-pectin (nHCP) composites were prepared through in situ mineralization of hydroxyapatite in chitosan-pectin polyelectrolyte complex (PEC) network. The formation processes of nHCP were investigated by X-ray diffraction (XRD) analysis. The interactions between nHA crystal and chitosan-pectin PEC networks were studied using Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). The morphology and structure of nHA crystal were characterized by XRD and Transmission Electron Microscope (TEM). Results suggested that the interfacial interactions between nano-hydroxyapatite crystal and chitosan-pectin PEC network assist the site specific nucleation and growth of nHA nanoparticles. The nHA crystals grow along the c-axis. In this process, pH value is the main factor to control the nucleation and growth of nHA crystal in chitosan-pectin PEC networks, because both the interactions' strength between nHA crystal and chitosan-pectin and diffusion rate of inorganic ions depend on the pH value of the reaction system. Apart from the pH value, the chitosan/pectin ratio and [Ca 2+ ] also take important effects on the formation of nHA crystal. An effective way to control the size of nHA crystal is to adjust the content of pectin and [Ca 2+ ]. It is interesting that the Zeta potential of nHCP composites is about - 30 mV when the chitosan/pectin ratio ≤ 1:1, and the dispersion solution of nHCP composites has higher stability, which provides the possibility to prepare 3D porous scaffolds with nHCP for bone tissue engineering.

Formation of nano-hydroxyapatite crystal in situ in chitosan-pectin polyelectrolyte complex network

Energy Technology Data Exchange (ETDEWEB)

Li Junjie [Department of Polymer Science and Key Laboratory of Systems Bioengineering of Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300072 (China); Research Institute of Polymeric Materials, Tianjin University, Tianjin, 300072 (China); Zhu Dunwan [Institute of Biomedical Engineering, Chinese Academy of Medical Sciences and Peking Union Medical College, Tianjin, 300072 (China); Yin Jianwei; Liu Yuxi [Department of Polymer Science and Key Laboratory of Systems Bioengineering of Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300072 (China); Yao Fanglian, E-mail: yaofanglian@tju.edu.cn [Department of Polymer Science and Key Laboratory of Systems Bioengineering of Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin, 300072 (China); Yao Kangde [Research Institute of Polymeric Materials, Tianjin University, Tianjin, 300072 (China)

2010-07-20

Hydroxyapatite (HA)/polysaccharide composites have been widely used in bone tissue engineering due to their chemical similarity to natural bone. Polymer matrix-mediated synthesis of nano-hydroxyapatite is one of the simplest models for biomimetic. In this article, the nano-hydroxyapatite/chitosan-pectin (nHCP) composites were prepared through in situ mineralization of hydroxyapatite in chitosan-pectin polyelectrolyte complex (PEC) network. The formation processes of nHCP were investigated by X-ray diffraction (XRD) analysis. The interactions between nHA crystal and chitosan-pectin PEC networks were studied using Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC). The morphology and structure of nHA crystal were characterized by XRD and Transmission Electron Microscope (TEM). Results suggested that the interfacial interactions between nano-hydroxyapatite crystal and chitosan-pectin PEC network assist the site specific nucleation and growth of nHA nanoparticles. The nHA crystals grow along the c-axis. In this process, pH value is the main factor to control the nucleation and growth of nHA crystal in chitosan-pectin PEC networks, because both the interactions' strength between nHA crystal and chitosan-pectin and diffusion rate of inorganic ions depend on the pH value of the reaction system. Apart from the pH value, the chitosan/pectin ratio and [Ca{sup 2+}] also take important effects on the formation of nHA crystal. An effective way to control the size of nHA crystal is to adjust the content of pectin and [Ca{sup 2+}]. It is interesting that the Zeta potential of nHCP composites is about - 30 mV when the chitosan/pectin ratio {<=} 1:1, and the dispersion solution of nHCP composites has higher stability, which provides the possibility to prepare 3D porous scaffolds with nHCP for bone tissue engineering.

Comparative Evaluation of Viability of Encapsulated Lactobacillus casei Using Two Different Methods of Microencapsulation

OpenAIRE

Petreska Ivanovska, Tanja; Smilkov, Katarina; Zivikj, Zoran; Petrusevska Tozi, Lidija; Mladenovska, Kristina

2014-01-01

Microencapsulation using two different methods, spray- drying and emulsion technique were applied to preserve the viability of the probiotic Lactobacillus casei during manufacture and refrigerated storage. As coating materials to encapsulate the probiotic by spray-drying method, compatible biopolymers alginate and chitosan were utilized, while as a cross-linking agent, CaCl2 was used. In addition to the probiotic, oligofructose enriched inulin (Synergy 1®) as prebiotic was added to the medium...

Dual responsive PNIPAM–chitosan targeted magnetic nanopolymers for targeted drug delivery

Energy Technology Data Exchange (ETDEWEB)

Yadavalli, Tejabhiram, E-mail: tejabhiram@gmail.com [Nanotechnology Research Centre, SRM University, Chennai 603203 (India); Ramasamy, Shivaraman [Nanotechnology Research Centre, SRM University, Chennai 603203 (India); School of Physics, The University of Western Australia, 35 Stirling Hwy, Crawley, WA 6009 (Australia); Chandrasekaran, Gopalakrishnan; Michael, Isaac; Therese, Helen Annal [Nanotechnology Research Centre, SRM University, Chennai 603203 (India); Chennakesavulu, Ramasamy [Department of Pharmacy practice, SRM College of Pharmacy, Chennai 603203 (India)

2015-04-15

A dual stimuli sensitive magnetic hyperthermia based drug delivery system has been developed for targeted cancer treatment. Thermosensitive amine terminated poly-N-isopropylacrylamide complexed with pH sensitive chitosan nanoparticles was prepared as the drug carrier. Folic acid and fluorescein were tagged to the nanopolymer complex via N-hydroxysuccinimide and ethyl-3-(3-dimethylaminopropyl)carbodiimide reaction to form a fluorescent and cancer targeting magnetic carrier system. The formation of the polymer complex was confirmed using infrared spectroscopy. Gadolinium doped nickel ferrite nanoparticles prepared by a hydrothermal method were encapsulated in the polymer complex to form a magnetic drug carrier system. The proton relaxation studies on the magnetic carrier system revealed a 200% increase in the T1 proton relaxation rate. These magnetic carriers were loaded with curcumin using solvent evaporation method with a drug loading efficiency of 86%. Drug loaded nanoparticles were tested for their targeting and anticancer properties on four cancer cell lines with the help of MTT assay. The results indicated apoptosis of cancer cell lines within 3 h of incubation. - Highlights: • The use of gadolinium doped nickel ferrite with the suggested doping level. • The use of PNIPMA–chitosan polymer with folic acid and fluorescein as a drug carrier complex. • Magnetic hyperthermia studies of gadolinium doped nickel ferrites are being reported for the first time. • Proton relaxivity studies which indicate the MRI contrasting properties on the reported system are new. • Use of curcumin, a hydrophobic Indian spice as a cancer killing agent inside the reported magnetic polymer complex.

pH-responsive self-healing injectable hydrogel based on N-carboxyethyl chitosan for hepatocellular carcinoma therapy.

Science.gov (United States)

Qu, Jin; Zhao, Xin; Ma, Peter X; Guo, Baolin

2017-08-01

Injectable hydrogels with pH-responsiveness and self-healing ability have great potential for anti-cancer drug delivery. Herein, we developed a series of polysaccharide-based self-healing hydrogels with pH-sensitivity as drug delivery vehicles for hepatocellular carcinoma therapy. The hydrogels were prepared by using N-carboxyethyl chitosan (CEC) synthesized via Michael reaction in aqueous solution and dibenzaldehyde-terminated poly(ethylene glycol) (PEGDA). Doxorubicin (Dox), as a model of water-soluble small molecule anti-cancer drug was encapsulated into the hydrogel in situ. Self-healing behavior of the hydrogels was investigated at microscopic and macroscopic levels, and the hydrogels showed rapid self-healing performance without any external stimulus owing to the dynamic covalent Schiff-base linkage between amine groups from CEC and benzaldehyde groups from PEGDA. The chemical structures, rheological property, in vitro gel degradation, morphology, gelation time and in vitro Dox release behavior from the hydrogels were characterized. Injectability was verified by in vitro injection and in vivo subcutaneous injection in a rat. pH-responsive behavior was verified by in vitro Dox release from hydrogels in PBS solutions with different pH values. Furthermore, the activity of Dox released from hydrogel matrix was evaluated by employing human hepatocellular liver carcinoma (HepG2). Cytotoxicity test of the hydrogels using L929 cells confirmed their good cytocompatibility. Together, these pH-responsive self-healing injectable hydrogels are excellent candidates as drug delivery vehicles for liver cancer treatment. STATEMENT OF SIGNIFICANCE: pH-responsive drug delivery system could release drug efficiently in targeted acid environment and minimalize the amount of drug release in normal physiological environment. pH-sensitive injectable hydrogels as smart anti-cancer drug delivery carriers show great potential application for cancer therapy. The hydrogels with self

Chitosan dan Aplikasi Klinisnya Sebagai Biomaterial

Directory of Open Access Journals (Sweden)

Bambang Irawan

2015-10-01

Full Text Available The development of new materials with both organic and inorganic structures is of great interest to obtain special material properties. Chitosan [2-amino-2-deoxy-D-glucan] can be obtained by N-deacetylation of chitin. Chitin is the second most abundant biopolymer in nature and the supporting material of crustaceans, insects, fungi etc. Chitosan is unique polysaccharide and has been widely used in various biomedical application due to its biocompatibility, low toxicity, biodegradability, non-immunogenic and non-carcinogenic character. In the past few years, chitosan and some of its modifications have been reported for use in biomedical applications such as artificial skin, wound dressing, anticoagulant, suture, drug delivery, vaccine carrier and dietary fibers. Recently, the use of chitosan and its derivatives has received much attention as temporary scaffolding to promotie mineralization or stimulate endochodral ossification. This article aims to give a broad overview of chitosan and its clinical applications as biomaterial.

Green synthesis approach: extraction of chitosan from fungus mycelia.

Science.gov (United States)

Dhillon, Gurpreet Singh; Kaur, Surinder; Brar, Satinder Kaur; Verma, Mausam

2013-12-01

Chitosan, copolymer of glucosamine and N-acetyl glucosamine is mainly derived from chitin, which is present in cell walls of crustaceans and some other microorganisms, such as fungi. Chitosan is emerging as an important biopolymer having a broad range of applications in different fields. On a commercial scale, chitosan is mainly obtained from crustacean shells rather than from the fungal sources. The methods used for extraction of chitosan are laden with many disadvantages. Alternative options of producing chitosan from fungal biomass exist, in fact with superior physico-chemical properties. Researchers around the globe are attempting to commercialize chitosan production and extraction from fungal sources. Chitosan extracted from fungal sources has the potential to completely replace crustacean-derived chitosan. In this context, the present review discusses the potential of fungal biomass resulting from various biotechnological industries or grown on negative/low cost agricultural and industrial wastes and their by-products as an inexpensive source of chitosan. Biologically derived fungal chitosan offers promising advantages over the chitosan obtained from crustacean shells with respect to different physico-chemical attributes. The different aspects of fungal chitosan extraction methods and various parameters having an effect on the yield of chitosan are discussed in detail. This review also deals with essential attributes of chitosan for high value-added applications in different fields.

Core–shell hybrid nanocapsules for oral delivery of camptothecin: formulation development, in vitro and in vivo evaluation

Energy Technology Data Exchange (ETDEWEB)

Ünal, Hale, E-mail: unalhale@gmail.com [Hacettepe University, Division of Nanotechnology and Nanomedicine, Institute of Pure and Applied Science (Turkey); D’Angelo, Ivana [Second University of Napoli, Di.S.T.A.Bi.F. (Italy); Pagano, Ester; Borrelli, Francesca; Izzo, Angelo; Ungaro, Francesca; Quaglia, Fabiana [University of Naples Federico II, Department of Pharmacy (Italy); Bilensoy, Erem [Hacettepe University, Division of Nanotechnology and Nanomedicine, Institute of Pure and Applied Science (Turkey)

2015-01-15

The objective of this study was to design and in vitro–in vivo evaluate oral nanocapsules prepared from amphiphilic cyclodextrins (CDs) or poly-ε-caprolactone (PCL) for the effective oral delivery of an anticancer agent, camptothecin (CPT). CPT-loaded anionic and Chitosan (CS)-coated cationic nanocapsules were prepared and characterized in vitro. Morphological analysis was performed by scanning electron microscope (SEM). CPT release profile was evaluated using dialysis method under sink conditions. To determine the protective effect and drug stability provided by nanocapsules, all the formulations were incubated in simulated gastrointestinal media. Measurement of mucoadhesive tendency of CPT-loaded nanocapsules was realized by turbidimetric method. Penetration of nanocapsules was performed through an artificial mucus model. The permeability of CPT in solution form and bound to nanocapsule formulations were demonstrated across Caco-2 cell line. Finally, the intestinal uptake of nanocapsules was evaluated in vivo, in a mouse model. Both anionic and cationic formulations were in the range of 180–220 nm with a narrow size distribution and desired zeta potential values. CPT-loaded nanocapsules were found to be stable in simulated gastrointestinal media. Turbidimetric measurements confirmed the interaction between nanoparticles and mucin. Penetration of CPT through an artificial mucus gel layer was higher with CS-coated nanocapsules in accordance with the results obtained from permeability studies across Caco-2 cell line. In vivo animal studies confirmed that the intestinal uptake of nanocapsules was significantly higher with cationic nanocapsules. CPT-loaded positively charged CD nanocapsules might be an attractive and promising treatment for oral chemotherapy.

Core–shell hybrid nanocapsules for oral delivery of camptothecin: formulation development, in vitro and in vivo evaluation

International Nuclear Information System (INIS)

Ünal, Hale; D’Angelo, Ivana; Pagano, Ester; Borrelli, Francesca; Izzo, Angelo; Ungaro, Francesca; Quaglia, Fabiana; Bilensoy, Erem

2015-01-01

The objective of this study was to design and in vitro–in vivo evaluate oral nanocapsules prepared from amphiphilic cyclodextrins (CDs) or poly-ε-caprolactone (PCL) for the effective oral delivery of an anticancer agent, camptothecin (CPT). CPT-loaded anionic and Chitosan (CS)-coated cationic nanocapsules were prepared and characterized in vitro. Morphological analysis was performed by scanning electron microscope (SEM). CPT release profile was evaluated using dialysis method under sink conditions. To determine the protective effect and drug stability provided by nanocapsules, all the formulations were incubated in simulated gastrointestinal media. Measurement of mucoadhesive tendency of CPT-loaded nanocapsules was realized by turbidimetric method. Penetration of nanocapsules was performed through an artificial mucus model. The permeability of CPT in solution form and bound to nanocapsule formulations were demonstrated across Caco-2 cell line. Finally, the intestinal uptake of nanocapsules was evaluated in vivo, in a mouse model. Both anionic and cationic formulations were in the range of 180–220 nm with a narrow size distribution and desired zeta potential values. CPT-loaded nanocapsules were found to be stable in simulated gastrointestinal media. Turbidimetric measurements confirmed the interaction between nanoparticles and mucin. Penetration of CPT through an artificial mucus gel layer was higher with CS-coated nanocapsules in accordance with the results obtained from permeability studies across Caco-2 cell line. In vivo animal studies confirmed that the intestinal uptake of nanocapsules was significantly higher with cationic nanocapsules. CPT-loaded positively charged CD nanocapsules might be an attractive and promising treatment for oral chemotherapy

Characterization of physicochemical and colloidal properties of hydrogel chitosan-coated iron-oxide nanoparticles for cancer therapy

International Nuclear Information System (INIS)

Catalano, E; Di Benedetto, A

2017-01-01

Superparamagnetic iron oxide nanoparticles have recently been investigated for their potential to kill cancer cells with promising results, owing to their ability to be targeted and heated by magnetic fields. In this study, novel hydrogel, chitosan Fe 3 O 4 magnetic nanoparticles were synthesized to induce magnetic hyperthermia, and targeted delivering of chemotherapeutics in the cancer microenvironment. The characteristic properties of synthesized bare and CS-MNPs were analyzed by various analytical methods: X-ray diffraction, Fourier transformed infrared spectroscopy, Scanning electron microscopy and Thermo-gravimetric analysis/differential thermal analysis. Magnetic nanoparticles were successfully synthesized using the co-precipitation method. This synthesis technique resulted in nanoparticles with an average particle size of 16 nm. The pure obtained nanoparticles were then successfully encapsulated with 4-nm-thick chitosan coating. The formation of chitosan on the surface of nanoparticles was confirmed by physicochemical analyses. Heating experiments at safe magnetic field (f = 100 kHz, H =10-20 kA m -1 ) revealed that the maximum achieved temperature of water stable chitosan-coated nanoparticles (50 mg ml -1 ) is fully in agreement with cancer therapy and biomedical applications. (paper)

Characterization of physicochemical and colloidal properties of hydrogel chitosan-coated iron-oxide nanoparticles for cancer therapy

Science.gov (United States)

Catalano, E.; Di Benedetto, A.

2017-05-01

Superparamagnetic iron oxide nanoparticles have recently been investigated for their potential to kill cancer cells with promising results, owing to their ability to be targeted and heated by magnetic fields. In this study, novel hydrogel, chitosan Fe3O4 magnetic nanoparticles were synthesized to induce magnetic hyperthermia, and targeted delivering of chemotherapeutics in the cancer microenvironment. The characteristic properties of synthesized bare and CS-MNPs were analyzed by various analytical methods: X-ray diffraction, Fourier transformed infrared spectroscopy, Scanning electron microscopy and Thermo-gravimetric analysis/differential thermal analysis. Magnetic nanoparticles were successfully synthesized using the co-precipitation method. This synthesis technique resulted in nanoparticles with an average particle size of 16 nm. The pure obtained nanoparticles were then successfully encapsulated with 4-nm-thick chitosan coating. The formation of chitosan on the surface of nanoparticles was confirmed by physicochemical analyses. Heating experiments at safe magnetic field (f = 100 kHz, H =10-20 kA m-1) revealed that the maximum achieved temperature of water stable chitosan-coated nanoparticles (50 mg ml-1) is fully in agreement with cancer therapy and biomedical applications.

Curcumin and piperine loaded zein-chitosan nanoparticles: Development and in-vitro characterisation

Directory of Open Access Journals (Sweden)

Yücel Baspinar

2018-03-01

It was succeeded to prepare curcumin and piperine loaded zein-chitosan nanoparticles having a mean particle size of approximately 500 nm and high encapsulation efficencies for curcumin (89% and piperine (87%. Using a curcumin concentration of 10–25 µg/ml resulted in reduction of the viability of approximately 50% of the neuroblastoma cells. The here developed nanoparticle formulation consisting of solely natural compounds showed good cytotoxic effects and is a promising approach with appropriate properties for final consumption.

Fragrance material review on β,β,3-trimethyl-benzenepropanol.

Science.gov (United States)

Scognamiglio, J; Jones, L; Letizia, C S; Api, A M

2012-09-01

A toxicologic and dermatologic review of β,β,3-trimethyl-benzenepropanol when used as a fragrance ingredient is presented. β,β,3-Trimethyl-benzenepropanol is a member of the fragrance structural group Aryl Alkyl Alcohols and is a primary alcohol. The AAAs are a structurally diverse class of fragrance ingredients that includes primary, secondary, and tertiary alkyl alcohols covalently bonded to an aryl (Ar) group, which may be either a substituted or unsubstituted benzene ring. The common structural element for the AAA fragrance ingredients is an alcohol group -C-(R1)(R2)OH and generically the AAA fragrances can be represented as an Ar-C-(R1)(R2)OH or Ar-Alkyl-C-(R1)(R2)OH group. This review contains a detailed summary of all available toxicology and dermatology papers that are related to this individual fragrance ingredient and is not intended as a stand-alone document. Available data for β,β,3-trimethyl-benzenepropanol were evaluated then summarized and includes physical properties, acute toxicity, skin irritation, mucous membrane (eye) irritation, skin sensitization, elicitation, phototoxicity, photoallergy, repeated dose, and genotoxicity data. A safety assessment of the entire Aryl Alkyl Alcohols will be published simultaneously with this document; please refer to Belsito et al. (2012) for an overall assessment of the safe use of this material and all Aryl Alkyl Alcohols in fragrances. Copyright © 2012 Elsevier Ltd. All rights reserved.

Chitosan metal-crosslinked beads applied for n-alkylmonoamines removal from aqueous solutions – a thermodynamic study

International Nuclear Information System (INIS)

Oliveira, Margarete; Simoni, Jose A.; Airoldi, Claudio

2014-01-01

Highlights: • Chitosan beads were successfully synthesized with divalent cations. • Well-formed bead structures containing cations act as acceptor electron sites. • n-Alkylmonoamine/bead interactions are favorably sorbed at the solid/liquid interface. • The thermodynamic data were favorably obtained from calorimetric titrations. • Crosslinked metal–chitosan beads can remove amine-like substances from an ecosystem. - Abstract: Chitosan has ability in coordinating divalent cations when immersed in crosslinked beads, after dripping: (i) chitosan gel into a copper solution, (ii) nickel chitosan gel into sodium hydroxide and (iii) chitosan/cobalt gel into sodium tripolyphosphate. The amounts of (1.82; 1.27 and 0.44) mmol · g −1 for copper, nickel and cobalt cations in these well-formed structures were determined, to give nitrogen/metal ratios of 3.52; 2.09 and 8.51, indicating the least effectiveness for cobalt in the coordination. Copper cation is well-adjusted in the coordination model through free amino and hydroxyl electron pairs, while amino and acetamino groups for nickel and cobalt were used. The chitosan–hydrogen bond breaking in bead formation caused decreases in crystallinity to yield amorphous structures for cobalt and nickel. The water mass fraction released during heating depends on the hydration of the cations, with the highest value of 0.20 for cobalt. The quantitative aspects of the interaction among cations on beads and basic n-alkylmonoamines determined via sorption batch methodology adjusted to the Langmuir isothermal model, with maximum sorption quantities to saturate nickel of (2.50; 2.38; 2.03; 1.79) mmol · g −1 and copper of (2.59; 2.29; 2.28; 1.92) mmol · g −1 for ethyl- propyl-, butyl- and pentylamines, respectively. The interaction energies quantitatively determined from isothermal titration calorimetry (ITC) at the solid/liquid interface resulted in exothermic enthalpic values. These negative enthalpy values combined to

Chitosan-sodium lauryl sulfate nanoparticles as a carrier system for the in vivo delivery of oral insulin.

Science.gov (United States)

Elsayed, Amani; Al-Remawi, Mayyas; Qinna, Nidal; Farouk, Asim; Al-Sou'od, Khaldoun A; Badwan, Adnan A

2011-09-01

The present work explores the possibility of formulating an oral insulin delivery system using nanoparticulate complexes made from the interaction between biodegradable, natural polymer called chitosan and anionic surfactant called sodium lauryl sulfate (SLS). The interaction between chitosan and SLS was confirmed by Fourier transform infrared spectroscopy. The nanoparticles were prepared by simple gelation method under aqueous-based conditions. The nanoparticles were stable in simulated gastric fluids and could protect the encapsulated insulin from the GIT enzymes. Additionally, the in vivo results clearly indicated that the insulin-loaded nanoparticles could effectively reduce the blood glucose level in a diabetic rat model. However, additional formulation modifications are required to improve insulin oral bioavailability.

Chitosan Based Self-Assembled Nanoparticles in Drug Delivery

Directory of Open Access Journals (Sweden)

Javier Pérez Quiñones

2018-02-01

Full Text Available Chitosan is a cationic polysaccharide that is usually obtained by alkaline deacetylation of chitin poly(N-acetylglucosamine. It is biocompatible, biodegradable, mucoadhesive, and non-toxic. These excellent biological properties make chitosan a good candidate for a platform in developing drug delivery systems having improved biodistribution, increased specificity and sensitivity, and reduced pharmacological toxicity. In particular, chitosan nanoparticles are found to be appropriate for non-invasive routes of drug administration: oral, nasal, pulmonary and ocular routes. These applications are facilitated by the absorption-enhancing effect of chitosan. Many procedures for obtaining chitosan nanoparticles have been proposed. Particularly, the introduction of hydrophobic moieties into chitosan molecules by grafting to generate a hydrophobic-hydrophilic balance promoting self-assembly is a current and appealing approach. The grafting agent can be a hydrophobic moiety forming micelles that can entrap lipophilic drugs or it can be the drug itself. Another suitable way to generate self-assembled chitosan nanoparticles is through the formation of polyelectrolyte complexes with polyanions. This paper reviews the main approaches for preparing chitosan nanoparticles by self-assembly through both procedures, and illustrates the state of the art of their application in drug delivery.

Comparison of chitosan nanoparticles and chitosan hydrogels for vaccine delivery

DEFF Research Database (Denmark)

Gordon, Sarah; Saupe, Anne; McBurney, Warren

2008-01-01

In this work the potential of chitosan nanoparticles (CNP) and thermosensitive chitosan hydrogels as particulate and sustained release vaccine delivery systems was investigated. CNP and chitosan hydrogels were prepared, loaded with the model protein antigen ovalbumin (OVA) and characterised...... of the release of fluorescently-labelled OVA (FITC-OVA) from CNP and chitosan hydrogels in-vitro showed that approximately 50% of the total protein was released from CNP within a period of ten days; release of antigen from chitosan gel occurred in a more sustained manner, with ... released after 10 days. The slow release from gel formulations may be explained by the strong interactions of the protein with chitosan. While OVA-loaded CNP showed no significant immunogenicity, formulations of OVA in chitosan gel were able to stimulate both cell-mediated and humoral immunity in-vivo....

Functionalization of chitosan by click chemistry

Science.gov (United States)

Cheaburu-Yilmaz, Catalina Natalia; Karavana, Sinem Yaprak; Yilmaz, Onur

2017-12-01

Chitosan modification represents a challenge nowadays. The variety of compounds which can be obtained with various architectures and different functionalities made it attractive to be used in fields like pharmacy and material science. Presents study deals with the chemical modification of chitosan by using click chemistry technique. The study adopted the approach of clicking azidated chitosan with a synthesized alkyne terminated polymer i.e. poly N isopropylacrylamide with thermoresponsive properties. Structures were confirmed by the FT-IR and HNMR spectra. Thermal characterization was performed showing different thermal behaviour with the chemical modification. The final synthesized graft copolymer can play important role within pharmaceutical formulations carrying drugs for topical or oral treatments.

Chitosan and chemically modified chitosan beads for acid dyes sorption

Institute of Scientific and Technical Information of China (English)

AZLAN Kamari; WAN SAIME Wan Ngah; LAI KEN Liew

2009-01-01

The capabilities of chitosan and chitosan-EGDE (ethylene glycol diglycidyl ether) beads for removing Acid Red 37 (AR 37) and Acid Blue 25 (AB 25) from aqueous solution were examined. Chitosan beads were cross-linked with EGDE to enhance its chemical resistance and mechanical strength. Experiments were performed as a function of pH, agitation period and concentration of AR 37 and AB 25. It was shown that the adsorption capacities of chitosan were comparatively higher than chitosan-EGDE for both acid dyes. This is mainly because cross-linking using EGDE reduces the major adsorption sites -NH3+ on chitosan. Langmuir isotherm model showed best conformity compared to Freundlich and BET. The kinetic experimental data agreed very well to the pseudo second-order kinetic model. The desorption study revealed that after three cycles of adsorption and desorption by NaOH and HCl, both adsorbents retained their promising adsorption abilities. FT-IR analysis proved that the adsorption of acid dyes onto chitosan-based adsorbents was a physical adsorption. Results also showed that chitosan and chitosan-EGDE beads were favourable adsorbers and could be employed as low-cost alternatives for the removal of acid dyes in wastewater treatment.

Effects of nickel treatment on H3K4 trimethylation and gene expression.

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Kam-Meng Tchou-Wong

Full Text Available Occupational exposure to nickel compounds has been associated with lung and nasal cancers. We have previously shown that exposure of the human lung adenocarcinoma A549 cells to NiCl(2 for 24 hr significantly increased global levels of trimethylated H3K4 (H3K4me3, a transcriptional activating mark that maps to the promoters of transcribed genes. To further understand the potential epigenetic mechanism(s underlying nickel carcinogenesis, we performed genome-wide mapping of H3K4me3 by chromatin immunoprecipitation and direct genome sequencing (ChIP-seq and correlated with transcriptome genome-wide mapping of RNA transcripts by massive parallel sequencing of cDNA (RNA-seq. The effect of NiCl(2 treatment on H3K4me3 peaks within 5,000 bp of transcription start sites (TSSs on a set of genes highly induced by nickel in both A549 cells and human peripheral blood mononuclear cells were analyzed. Nickel exposure increased the level of H3K4 trimethylation in both the promoters and coding regions of several genes including CA9 and NDRG1 that were increased in expression in A549 cells. We have also compared the extent of the H3K4 trimethylation in the absence and presence of formaldehyde crosslinking and observed that crosslinking of chromatin was required to observe H3K4 trimethylation in the coding regions immediately downstream of TSSs of some nickel-induced genes including ADM and IGFBP3. This is the first genome-wide mapping of trimethylated H3K4 in the promoter and coding regions of genes induced after exposure to NiCl(2. This study may provide insights into the epigenetic mechanism(s underlying the carcinogenicity of nickel compounds.

Sorption of Cu(II) Ions on Chitosan-Zeolite X Composites: Impact of Gelling and Drying Conditions.

Science.gov (United States)

Djelad, Amal; Morsli, Amine; Robitzer, Mike; Bengueddach, Abdelkader; di Renzo, Francesco; Quignard, Françoise

2016-01-19

Chitosan-zeolite Na-X composite beads with open porosity and different zeolite contents were prepared by an encapsulation method. Preparation conditions had to be optimised in order to stabilize the zeolite network during the polysaccharide gelling process. Composites and pure reference components were characterized using X-ray diffraction (XRD); scanning electron microscopy (SEM); N₂ adsorption-desorption; and thermogravimetric analysis (TG). Cu(II) sorption was investigated at pH 6. The choice of drying method used for the storage of the adsorbent severely affects the textural properties of the composite and the copper sorption effectiveness. The copper sorption capacity of chitosan hydrogel is about 190 mg·g(-1). More than 70% of this capacity is retained when the polysaccharide is stored as an aerogel after supercrititcal CO₂ drying, but nearly 90% of the capacity is lost after evaporative drying to a xerogel. Textural data and Cu(II) sorption data indicate that the properties of the zeolite-polysaccharide composites are not just the sum of the properties of the individual components. Whereas a chitosan coating impairs the accessibility of the microporosity of the zeolite; the presence of the zeolite improves the stability of the dispersion of chitosan upon supercritical drying and increases the affinity of the composites for Cu(II) cations. Chitosan-zeolite aerogels present Cu(II) sorption properties.

Heavy Metal Removal by Chitosan and Chitosan Composite

International Nuclear Information System (INIS)

Abdel-Mohdy, F.A.; El-Sawy, S.; Ibrahim, M.S.

2005-01-01

Radiation grafting of diethyl aminoethyl methacrylate (DEAEMA) on chitosan to impart ion exchange properties and to be used for the separation of metal ions from waste water, was carried out. The effect of experimental conditions such as monomer concentration and the radiation dose on grafting were studied. On using chitosan, grafted chitosan and some chitosan composites in metal ion removal they show high up-take capacity for Cu 2+ and lower uptake capacities for the other divalent metal ions used (Zn and Co). Competitive study, performed with solutions containing mixture of metal salts, showed high selectivity for Cu 2+ than the other metal ion. Limited grafting of DEAEMA polymer -containing specific functional groups-onto the chitosan backbone improves the sorption performance

Prediction of the systemic exposure to oral 9-amino-20(S)-camptothecin using single-sample analysis

NARCIS (Netherlands)

Sparreboom, A.; de Jonge, M. J.; Punt, C. J.; Loos, W. J.; Nooter, K.; Stoter, G.; Porro, M. G.; Verweij, J.

1999-01-01

The purpose of this study was to develop and validate limited-sampling strategies for prediction of the area under the plasma-concentration time curves (AUCs) of the lactone and total (i. e., lactone plus carboxylate) forms of the novel topoisomerase-I inhibitor 9-amino-20(S)-camptothecin (9-AC).

Cytotoxicity and apoptotic effects of tea polyphenol-loaded chitosan nanoparticles on human hepatoma HepG2 cells

International Nuclear Information System (INIS)

Liang, Jin; Li, Feng; Fang, Yong; Yang, Wenjian; An, Xinxin; Zhao, Liyan; Xin, Zhihong; Cao, Lin; Hu, Qiuhui

2014-01-01

Tea polyphenols have strong antioxidant and antitumor activities. However, these health benefits are limited due to their poor in vivo stability and low bioavailability. Chitosan nanoparticles as delivery systems may provide an alternative approach for enhancing bioavailability of poorly absorbed drugs. In this study, tea polyphenol-loaded chitosan nanoparticles have been prepared using two different chitosan biomaterials, and their antitumor effects were evaluated in HepG2 cells, including cell cytotoxicity comparison, cell morphology analysis, cell apoptosis and cell cycle detection. The results indicated that the tea polyphenol-loaded chitosan nanoparticles showed a branch shape and heterogeneous distribution in prepared suspension. MTT assay suggested that tea polyphenol-loaded chitosan nanoparticles could inhibit the proliferation of HepG2 cells, and the cytotoxicity rates were increased gradually and appeared an obvious dose-dependent relationship. Transmission electron microscope images showed that the HepG2 cells treated with tea polyphenol-loaded chitosan nanoparticles exhibited some typical apoptotic features, such as microvilli disappearance, margination of nuclear chromatin, intracytoplasmic vacuoles and the mitochondrial swelling. In addition, the tea polyphenol-loaded chitosan nanoparticles had relatively weak inhibitory effects on HepG2 cancer cells compared with tea polyphenols. Tea polyphenols not only induced cancer cell apoptosis, but also promoted their necrosis. However, tea polyphenol-loaded chitosan nanoparticles exhibited their antitumor effects mainly through inducing cell apoptosis. Our results revealed that the inhibition effects of tea polyphenol-loaded chitosan nanoparticles on tumor cells probably depended on their controlled drug release and effective cell delivery. The chitosan nanoparticles themselves as the delivery carrier showed limited antitumor effects compared with their encapsulated drugs. - Highlights: • Tea polyphenol

Cytotoxicity and apoptotic effects of tea polyphenol-loaded chitosan nanoparticles on human hepatoma HepG2 cells

Energy Technology Data Exchange (ETDEWEB)

Liang, Jin [Key Laboratory of Tea Biochemistry and Biotechnology of Ministry of Education and Ministry of Agriculture, Anhui Agricultural University, Hefei 230036 (China); College of Food Science and Technology, Nanjing Agricultural University, Nanjing 210095 (China); Li, Feng [College of Food Science and Technology, Nanjing Agricultural University, Nanjing 210095 (China); Fang, Yong; Yang, Wenjian [College of Food Science and Engineering, Nanjing University of Finance and Economics, Nanjing 210023 (China); An, Xinxin; Zhao, Liyan; Xin, Zhihong; Cao, Lin [College of Food Science and Technology, Nanjing Agricultural University, Nanjing 210095 (China); Hu, Qiuhui, E-mail: qiuhuihu@njau.edu.cn [College of Food Science and Technology, Nanjing Agricultural University, Nanjing 210095 (China); College of Food Science and Engineering, Nanjing University of Finance and Economics, Nanjing 210023 (China)

2014-03-01

Tea polyphenols have strong antioxidant and antitumor activities. However, these health benefits are limited due to their poor in vivo stability and low bioavailability. Chitosan nanoparticles as delivery systems may provide an alternative approach for enhancing bioavailability of poorly absorbed drugs. In this study, tea polyphenol-loaded chitosan nanoparticles have been prepared using two different chitosan biomaterials, and their antitumor effects were evaluated in HepG2 cells, including cell cytotoxicity comparison, cell morphology analysis, cell apoptosis and cell cycle detection. The results indicated that the tea polyphenol-loaded chitosan nanoparticles showed a branch shape and heterogeneous distribution in prepared suspension. MTT assay suggested that tea polyphenol-loaded chitosan nanoparticles could inhibit the proliferation of HepG2 cells, and the cytotoxicity rates were increased gradually and appeared an obvious dose-dependent relationship. Transmission electron microscope images showed that the HepG2 cells treated with tea polyphenol-loaded chitosan nanoparticles exhibited some typical apoptotic features, such as microvilli disappearance, margination of nuclear chromatin, intracytoplasmic vacuoles and the mitochondrial swelling. In addition, the tea polyphenol-loaded chitosan nanoparticles had relatively weak inhibitory effects on HepG2 cancer cells compared with tea polyphenols. Tea polyphenols not only induced cancer cell apoptosis, but also promoted their necrosis. However, tea polyphenol-loaded chitosan nanoparticles exhibited their antitumor effects mainly through inducing cell apoptosis. Our results revealed that the inhibition effects of tea polyphenol-loaded chitosan nanoparticles on tumor cells probably depended on their controlled drug release and effective cell delivery. The chitosan nanoparticles themselves as the delivery carrier showed limited antitumor effects compared with their encapsulated drugs. - Highlights: • Tea polyphenol

Development and evaluation of Desvenlafaxine loaded PLGA-chitosan nanoparticles for brain delivery

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Gui-Feng Tong

2017-09-01

Full Text Available Depression is a debilitating psychiatric condition that remains the second most common cause of disability worldwide. Currently, depression affects more than 4 per cent of the world’s population. Most of the drugs intended for clinical management of depression augment the availability of neurotransmitters at the synapse by inhibiting their neuronal reuptake. However, the therapeutic efficacy of antidepressants is often compromised as they are unable to reach brain by the conventional routes of administration. The purpose of the present study was to reconnoiter the potential of mucoadhesive PLGA-chitosan nanoparticles for the delivery of encapsulated Desvenlafaxine to the brain by nose to brain delivery route for superior pharmacokinetic and pharmacodynamic profile of Desvenlafaxine. Desvenlafaxine loaded PLGA-chitosan nanoparticles were prepared by solvent emulsion evaporation technique and optimized for various physiochemical characteristics. The antidepressant efficacy of optimized Desvenlafaxine was evaluated in various rodent depression models together with the biochemical estimation of monoamines in their brain. Further, the levels of Desvenlafaxine in brain and blood plasma were determined at various time intervals for calculation of different pharmacokinetic parameters. The optimized Desvenlafaxine loaded PLGA-chitosan nanoparticles (∼172 nm/+35 mV on intranasal administration significantly reduced the symptoms of depression and enhanced the level of monoamines in the brain in comparison with orally administered Desvenlafaxine. Nose to brain delivery of Desvenlafaxine PLGA-chitosan nanoparticles also enhanced the pharmacokinetic profile of Desvenlafaxine in brain together with their brain/blood ratio at different time points. Thus, intranasal mucoadhesive Desvenlafaxine PLGA-chitosan nanoparticles could be potentially used for the treatment of depression.

Chitosan and carboxymethyl-chitosan capping ligands: Effects on the nucleation and growth of hydroxyapatite nanoparticles for producing biocomposite membranes.

Science.gov (United States)

Dumont, Vitor C; Mansur, Alexandra A P; Carvalho, Sandhra M; Medeiros Borsagli, Fernanda G L; Pereira, Marivalda M; Mansur, Herman S

2016-02-01

Synthetic biomaterials based on calcium phosphates (CaP) have been widely studied for bone tissue reconstruction therapies, but no definitive solution that fulfills all of the required properties has been identified. Thus, this study reports the synthesis of composite membranes based on nanohydroxyapatite particles (nHA) embedded in chitosan (CHI) and O-carboxymethyl chitosan (CMC) matrices produced using a one-step co-precipitation method in water media. Biopolymers were used as capping ligands for simultaneously controlling the nucleation and growth of the nHA particles during the precipitation process and also to form the polymeric network of the biocomposites. The bionanocomposites were extensively characterized using light microscopy (LM), scanning and transmission electron microscopy (SEM/TEM), energy-dispersive X-ray spectroscopy (EDX), Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), atomic force microscopy (AFM), X-ray micro-CT analysis (μCT), andMTT (3-(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazoliumbromide) cell proliferation assays for cell cytotoxicity. The results demonstrated that the ligands used during the synthesis highly affected the composites produced, primarily due the changes in the mechanisms and kinetics of nucleation and growth of the HA particles at the nanoscale level. The SEMimages revealed that the use of carboxyl-functionalized chitosan (CMC) ligands significantly reduced the average size of theHA nanoparticles and caused the formation of a narrower size distribution (90±20nm) compared to theHAnanoparticles producedwith chitosan ligands (220±50nm). The same trend was verified by the AFM analysis,where the nHA particles were formed evenly dispersed in the polymer matrix. However, the CMC-based composites were more homogeneously distributed, which was endorsed by the images collected via X-ray micro-CT. The FTIR spectra and the XRD analysis indicated that nanosized hydroxyapatite was the predominant calcium

Cytocompatibility of chitosan and collagen-chitosan scaffolds for tissue engineering

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Ligia L. Fernandes

2011-01-01

Full Text Available In this work, chitosan and collagen-chitosan porous scaffolds were produced by the freeze drying method and characterized as potential skin substitutes. Their beneficial effects on soft tissues justify the choice of both collagen and chitosan. Samples were characterized using scanning electron microscope, Fourier Transform InfraRed Spectroscopy (FTIR and thermogravimetry (TG. The in vitro cytocompatibility of chitosan and collagen-chitosan scaffolds was evaluated with three different assays. Phenol and titanium powder were used as positive and negative controls, respectively. Scanning electron microscopy revealed the highly interconnected porous structure of the scaffolds. The addition of collagen to chitosan increased both pore diameter and porosity of the scaffolds. Results of FTIR and TG analysis indicate that the two polymers interact yielding a miscible blend with intermediate thermal degradation properties. The reduction of XTT ((2,3-bis[2-methyloxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide and the uptake of Neutral Red (NR were not affected by the blend or by the chitosan scaffold extracts, but the blend and the titanium powder presented greater incorporation of Crystal Violet (CV than phenol and chitosan alone. In conclusion, collagen-chitosan scaffolds produced by freeze-drying methods were cytocompatible and presented mixed properties of each component with intermediate thermal degradation properties.

Preparation and characterization of PEGylated chitosan nanocapsules as a carrier for pharmaceutical application

Science.gov (United States)

Najafabadi, Alireza Hassani; Abdouss, Majid; Faghihi, Shahab

2014-03-01

A new method to conjugate methoxy polyethylene glycol (mPEG) to C6 position of chitosan under the mild condition is introduced that improves the biocompatibility and water solubility of chitosan. Harsh deprotecting step and several purification cycles are two major disadvantages of the current methods for preparing PEGylated chitosan. In this study, the amine groups at C2 position of chitosan are protected using SDS followed by grafting the PEG. The protecting group of chitosan is simply removed by dialyzing against Tris solution. The chemical structure of the prepared polymer is characterized by FTIR and 1H NMR spectroscopy. Fourier transformed-infrared (FT-IR) and 1H NMR spectra confirmed that the mPEG is successfully grafted to C6 position of chitosan. Prepared methoxy polyethylene glycol (mPEG) is then employed to prepare the nanocapsules for the encapsulation of poor water-soluble drug, propofol. The TEM, AFM, and DLS techniques are used to characterize the prepared nanocapsules size and morphology. The results show a size of about 80 nm with spherical shape for nanocapsules. In vitro drug release is carried out to evaluate the potential of nanocarriers for the intravenous delivery of drugs. The profile of release from formulated nanocapsules is similar to those of commercial lipid emulsion (CLE). In vivo animal sleep-recovery test on rats shows a close similarity between the time of unconsciousness and recovery of righting reflex between nanoparticles and CLE. This study provides an efficient, novel, and easy method for preparing a carrier system that requires less intensive reaction conditions, fewer reaction steps, and less purification steps. In addition, the nanocapsules introduced here could be a promising nano carrier for the delivery of poor water-soluble drugs.

Omics for Investigating Chitosan as an Antifungal and Gene Modulator

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Federico Lopez-Moya

2016-03-01

Full Text Available Chitosan is a biopolymer with a wide range of applications. The use of chitosan in clinical medicine to control infections by fungal pathogens such as Candida spp. is one of its most promising applications in view of the reduced number of antifungals available. Chitosan increases intracellular oxidative stress, then permeabilizes the plasma membrane of sensitive filamentous fungus Neurospora crassa and yeast. Transcriptomics reveals plasma membrane homeostasis and oxidative metabolism genes as key players in the response of fungi to chitosan. A lipase and a monosaccharide transporter, both inner plasma membrane proteins, and a glutathione transferase are main chitosan targets in N. crassa. Biocontrol fungi such as Pochonia chlamydosporia have a low content of polyunsaturated free fatty acids in their plasma membranes and are resistant to chitosan. Genome sequencing of P. chlamydosporia reveals a wide gene machinery to degrade and assimilate chitosan. Chitosan increases P. chlamydosporia sporulation and enhances parasitism of plant parasitic nematodes by the fungus. Omics studies allow understanding the mode of action of chitosan and help its development as an antifungal and gene modulator.

Understanding the properties of chitosan aryl substituted thioureas in their role and potential as antibacterial agents

Science.gov (United States)

Khairul, Wan M.; Daud, Adibah Izzati; Ismail, Noraznawati

2018-02-01

In this study, the effort was to design and synthesize a series of thiourea-chitosan derivatives featuring five aryl substituted members namely N-chitosan-N'-(4-nitrobenzoyl) thiourea (1), N-chitosan-N'-(4-chlorobenzoyl) thiourea (2), N-chitosan-N'-(4-methylbenzoyl) thiourea (3), N-chitosan-N'-(2-iodobenzoyl) thiourea (4), and N-chitosan-N'-(2-methylbenzoyl) thiourea (5) via SN2 reaction pathway having different donating and withdrawing groups. Their molecular structures were then characterised by FT-IR, UV-Vis, and thermogravimetric analysis (TGA). The antimicrobial activities of these derivatives against four species bacteria Bacillus cereus, Staphylococcus aureus, Salmonella typhi, and Escherichia coli of both Gram-positive and Gram-negative type bacteria at minimum concentration 6mg/ml were carried out to investigate their potential as antibacterial agents. Compound 1 exhibited specific activity as it can only inhibit Gram-positive bacteria while other compounds 2-5 showed broad range spectrum activity as they were able to inhibit both Gram-positive and Gram-negative bacteria. Therefore, 1-5 showed good antibacterial activity and have high potential to be further developed as active materials in pharmaceutical interests.

Microwave-Assisted Hydrolysis of Chitosan from Shrimp Shell Waste for Glucosammine Hydrochlorid Production

International Nuclear Information System (INIS)

Zaeni, Ahmad; Safitri, Endang; Fuadah, Badrotul; Sudiana, I Nyoman

2017-01-01

Chitin is the most widespread renewable natural sources following cellulose as the main source of chitosan. Chitin is isolated from crustacean waste and shrimp shells. Chitosan is derived from chitin throuhgt demineralisation, deproteination, decolorisation and deacetylation process using chemicals such as sodium hydroxide, hydrogen chloride and acetone. Glucosamine hydrochloride (GlcN-Cl) can be produced by hydrolysis of chitosan by using hydrogen chloride. During deacetylation and hydrolysis the solution is heated by hotplate or furnace. In this paper we use microwave instead of hotplate for production chitosan and GlcN-Cl. The research investigates effect of microwaves to amount of rendemen and their property. The chitosan was characterized its moisture content, solubility, and degree of deacetylation (DDA). Whereas the glucosammine hydrochloride characterized its functional groups using FTIR and crystallization by using X-Ray Difraction (XRD). The experimental results show that the use of microwave energy on deacetilation of chitosan and hydrolisis processes can decrease time consuming and reactant concentration during production. the DDA value obtained was very high from 70 to 85%. The results also show that microwaves meet chitosan and GlcN-Cl standards. (paper)

Microwave-Assisted Hydrolysis of Chitosan from Shrimp Shell Waste for Glucosammine Hydrochlorid Production

Science.gov (United States)

Zaeni, Ahmad; Safitri, Endang; Fuadah, Badrotul; Nyoman Sudiana, I.

2017-05-01

Chitin is the most widespread renewable natural sources following cellulose as the main source of chitosan. Chitin is isolated from crustacean waste and shrimp shells. Chitosan is derived from chitin throuhgt demineralisation, deproteination, decolorisation and deacetylation process using chemicals such as sodium hydroxide, hydrogen chloride and acetone. Glucosamine hydrochloride (GlcN-Cl) can be produced by hydrolysis of chitosan by using hydrogen chloride. During deacetylation and hydrolysis the solution is heated by hotplate or furnace. In this paper we use microwave instead of hotplate for production chitosan and GlcN-Cl. The research investigates effect of microwaves to amount of rendemen and their property. The chitosan was characterized its moisture content, solubility, and degree of deacetylation (DDA). Whereas the glucosammine hydrochloride characterized its functional groups using FTIR and crystallization by using X-Ray Difraction (XRD). The experimental results show that the use of microwave energy on deacetilation of chitosan and hydrolisis processes can decrease time consuming and reactant concentration during production. the DDA value obtained was very high from 70 to 85%. The results also show that microwaves meet chitosan and GlcN-Cl standards.

Synthesis, physiochemical and optical properties of chitosan based dye containing naphthalimide group.

Science.gov (United States)

Kumar, Santosh; Koh, Joonseok

2013-04-15

A new biopolymer dye containing naphthalimide moiety was synthesized by reaction of N-naphthaloyl chitosan with 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-piperazino-3-quinolinecarboxylic acid. N-naphthaloyl chitosan was synthesized by reaction of chitosan with 4-bromo-1,8-naphthalic anhydride in aqueous media by greener approach. The degree of substitution of chitosan biopolymer dye is 0.55 with a yield of 70%. The synthesized materials were characterized by using UV-vis, (1)H NMR, FTIR, and FT-Raman spectroscopy. Some physical properties and surface morphology were characterized by X-ray diffraction (XRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Optical properties of chitosan biopolymer dye were evaluated by photoluminescence (PL) spectroscopy that showed red shift (λ(em)) peak at 442 nm and 551 nm at excitation wavelength 325 nm in comparison to chitosan. The solubility of chitosan biopolymer dye increased in most of the organic solvents. These results may provide new perspectives in biomedical applications as an optical and sensitive biosensor material. Copyright © 2013 Elsevier Ltd. All rights reserved.

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

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M. J. Barea

2012-01-01

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

Fabrication of antibacterial blend film from poly (vinyl alcohol) and quaternized chitosan for packaging

Energy Technology Data Exchange (ETDEWEB)

Hu, Dongying; Wang, Lijuan, E-mail: donglinwlj@163.com

2016-06-15

Highlights: • HTCC/PVA blend films were prepared through a simple mixing method. • The blend films had greater elongation at break and good optical transmittance. • The blend films had low oxygen permeability and water vapor permeability. • The films had good activity against Escherichia coli and Staphylococcus aureus. - Abstract: Blend films from poly (vinyl alcohol) (PVA) containing N-(2-hydroxy) propyl-3-trimethyl ammonium chloride chitosan (HTCC) were prepared via a simple mixing and casting method. The films were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction measurements (XRD), scanning electron microscopy and ultraviolet-visible measurements (UV–vis). The effects of HTCC amount on mechanical properties, oxygen permeability, water vapor permeation, and antibacterial properties against Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) of the films were investigated. FTIR and XRD analysis show that HTCC and PVA in the blend films interacted by hydrogen bonding. SEM and UV–vis analysis reveal the good compatibility between HTCC and PVA. Compared with pure PVA film, the blend films had greater elongation at break, lower water permeability, and higher antibacterial activity. The HTCC addition decreased the tensile strength and the light transmittance. The results suggest that HTCC/PVA blend films have a potential as packaging materials.

Fabrication of antibacterial blend film from poly (vinyl alcohol) and quaternized chitosan for packaging

International Nuclear Information System (INIS)

Hu, Dongying; Wang, Lijuan

2016-01-01

Highlights: • HTCC/PVA blend films were prepared through a simple mixing method. • The blend films had greater elongation at break and good optical transmittance. • The blend films had low oxygen permeability and water vapor permeability. • The films had good activity against Escherichia coli and Staphylococcus aureus. - Abstract: Blend films from poly (vinyl alcohol) (PVA) containing N-(2-hydroxy) propyl-3-trimethyl ammonium chloride chitosan (HTCC) were prepared via a simple mixing and casting method. The films were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction measurements (XRD), scanning electron microscopy and ultraviolet-visible measurements (UV–vis). The effects of HTCC amount on mechanical properties, oxygen permeability, water vapor permeation, and antibacterial properties against Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureus) of the films were investigated. FTIR and XRD analysis show that HTCC and PVA in the blend films interacted by hydrogen bonding. SEM and UV–vis analysis reveal the good compatibility between HTCC and PVA. Compared with pure PVA film, the blend films had greater elongation at break, lower water permeability, and higher antibacterial activity. The HTCC addition decreased the tensile strength and the light transmittance. The results suggest that HTCC/PVA blend films have a potential as packaging materials.

Production and characterization of nanocapsules encapsulated linalool by ionic gelation method using chitosan as wall material

Directory of Open Access Journals (Sweden)

Zuobing XIAO

Full Text Available Abstract Linalool has been extensively applied in various fields, such as flavoring agent, perfumes, cosmetics and medical science. However, linalool is unstable, volatile and readily oxidizable. A sensitive substance can be encapsulated in a capsule, so encapsulation technology can solve these problems. In this paper, linalool-loaded nanocapsules (Lin-nanocapsules were prepared via the ionic gelation method and Lin-nanocapsules were characterized. The results of Fourier transformation infrared spectroscopy (FTIR showed that linalool was successfully encapsulated in the wall materials. Scanning electron microscopy (SEM results demonstrated that the shapes of Lin-nanocapsules, with smooth surfaces, were nearly spherical. Lin-nanocapsule average particle size was 352 nm and its polydispersity index (PDI was proved to be 0.214 by the results of dynamic light scattering (DLC. Thermogravimetric results indicated that linalool loading capacity (LC was 15.17%, and encapsulation could decrease linalool release and increase linalool retaining time under the high temperature. Oscillatory shear and steady-state shear measurements of Lin-nanocapsule emulsions were systematically investigated. The results of steady-state shear showed that Lin-nanocapsule emulsion, which was Newtonian only for high shear rate, was non-Newtonian. It was proved by oscillatory shear that when oscillation frequency changed from low to high, Lin-nanocapsules emulsion changed from viscous into elastic.

Magnetic chitosan/clay beads: A magsorbent for the removal of cationic dye from water

Energy Technology Data Exchange (ETDEWEB)

Bée, Agnès, E-mail: agnes.bee@upmc.fr [Sorbonne Universités, UPMC Univ Paris 06, CNRS, Laboratoire PHENIX, F-75005 Paris (France); Obeid, Layaly, E-mail: lghannoum@hotmail.fr [Sorbonne Universités, UPMC Univ Paris 06, CNRS, Laboratoire PHENIX, F-75005 Paris (France); CertiNergy Solutions, 33 avenue du Maine, BP 195, 75755 Paris Cedex 15 (France); Mbolantenaina, Rakotomalala, E-mail: mbolantenaina@yahoo.fr [Sorbonne Universités, UPMC Univ Paris 06, CNRS, Laboratoire PHENIX, F-75005 Paris (France); Welschbillig, Mathias, E-mail: welschbillig@certinergysolutions.com [CertiNergy Solutions, 33 avenue du Maine, BP 195, 75755 Paris Cedex 15 (France); Talbot, Delphine, E-mail: delphine.talbot@upmc.fr [Sorbonne Universités, UPMC Univ Paris 06, CNRS, Laboratoire PHENIX, F-75005 Paris (France)

2017-01-01

A magnetic composite material composed of magnetic nanoparticles and clay encapsulated in cross-linked chitosan beads was prepared, characterized and used as a magsorbent for the removal of a cationic dye, methylene blue (MB), from aqueous solutions. The magnetic properties of these beads represent an advantage to recover them at the end of the depollution process. The optimal weight ratio R=clay:chitosan for the removal of MB in a large range of pH was determined. For beads without clay, the maximal adsorption capacity of MB occurs in the pH range [9–12], while for beads with clay, the pH range extends by increasing the amount of clay to reach [3–12] for R>0.5. Adsorption isotherms show that the adsorption capacity of magnetic beads is equal to 82 mg/g. Moreover, the kinetics of dye adsorption is relatively fast since 50% of the dye is removed in the first 13 min for an initial MB concentration equal to 100 mg/L. The estimation of the number of adsorption sites at a given pH shows that the main driving force for adsorption of MB in a large range of pH is the electrostatic interaction between the positively charged dye and the permanent negative charges of clay. - Highlights: • A magsorbent based on magnetic nanoparticles and clay encapsulated in chitosan beads was prepared and characterized. • Clay played significant role for the removal of a cationic dye. • The magnetic beads exhibit a maximum adsorption capacity of 82 mg/g for methylene blue. • The pH range of the maximum adsorption extends from [9–12] to [3–12] by increasing the amount of clay. • The magsorbent could be magnetically removed from solution.

[Effects of cell-mediated immunity induced by intramuscular chitosan-pJME/ GM-CSF nano-DNA vaccine in BAlb/c mice].

Science.gov (United States)

Zhai, Yong-Zhen; Zhou, Yan; Ma, Li; Feng, Guo-He

2014-07-01

This study aimed to investigate the immune adjuvant effect and mechanism induced by chitosan nanoparticles carrying pJME/GM-CSF. In this study, plasmid DNA (pJME/GM-CSF) was encapsulated in chitosan to prepare chitosan-pJME/GM-CSF nanoparticles using a complex coacervation process. Immunohistochemistry was used to detect the type of infiltrating cells at the site of intramuscular injection. The phenotype and functional changes of splenic DCs were measured by flow cytometry after different immunogens were injected intramuscularly. The killing activity of CTLs was assessed using the lactate dehydrogenase (LDH) release assay. The preparation of chitosan-pJME/GM-CSF nanoparticles matched the expected theoretical results. Our results also found that, after pJME/GM-CSF injection, the incoming cells were a mixture of macrophages, neutrophils, and immature DCs. Meanwhile, pJME/GM-CSF increased the expression of MHC class II molecules on splenic DCs, and enhanced their Ag capture and presentation functions. Cell-mediated immunity was induced by the vaccine. Furthermore, chitosan-pJME/GM-CSF nanoparticles outperformed the administration of standard pJME/GM-CSF in terms of DC recruitment, antigen processing and presentation, and vaccine enhancement. These findings reveal that chitosan could be used as delivery vector for DNA vaccine intramuscular immunizations, and enhance pJME/GM-CSF-induced cellular immune responses.

Synthesis and characterization of Cis-5-Norbornene-2, 3-dicarboxylic anhydride-chitosan

International Nuclear Information System (INIS)

Ku Marshilla Ku Ishak; Zulkifli Ahmad; Hazizan Mohd Akil

2009-01-01

Chitosan was chemically modified with bulky structure, cis-5-norbornene-2, 3-dicarboxylic anhydride and the characteristic of this modified chitosan was studied. The resulting material was analyzed by FTIR, TGA, DSC, XRD and SEM to study the effect of N-acylation to the polysaccharide structure. FTIR results show that the anhydride monomer was successfully bound to amine group of chitosan. Thermal analysis of the modified structure provides the chitosan fibers with thermal stability while XRD and SEM show the lost of crystallinity of modified chitosan. XRD of modified chitosan shows broader peak pattern and a considerable increase in a dimension while SEM of chitosan presented the single particle morphology while norbornene-chitosan shows aggromolarate behaviour due to the hydrophobic nature of norbornene pendant group which induced aggromolaration of the particles in modified structure.(author)

Electrical evaluation of crack generation in SiN_x and SiO_xN_y thin-film encapsulation layers for OLED displays

International Nuclear Information System (INIS)

Park, Eun Kil; Kim, Sungmin; Heo, Jaeyeong; Kim, Hyeong Joon

2016-01-01

Highlights: • Crack generation in encapsulation layers were detected by leakage current. • Atomic concentration of SiO_xN_y films affected the bending reliability. • The shapes of the crack tips were affected by the stoichiometry of the SiO_xN_y films. - Abstract: By measuring leakage current density, we detected crack generation in silicon nitride (SiN_x) and silicon oxynitride (SiO_xN_y) thin-film encapsulation layers, and correlated with the films’ water vapor permeability characteristics. After repeated bending cycles, both the changes in water vapor transmission rate and leakage current density were directly proportional to the crack density. Thick SiN_x films had better water vapor barrier characteristics in their pristine state, but cyclic loading led to fast failure. Varying the atomic concentration of the SiO_xN_y films affected their bending reliability. We attribute these differences to changes in the shape of the crack tip as the oxygen content varies.

Chitosan-Coated Collagen Membranes Promote Chondrocyte Adhesion, Growth, and Interleukin-6 Secretion

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Nabila Mighri

2015-11-01

Full Text Available Designing scaffolds made from natural polymers may be highly attractive for tissue engineering strategies. We sought to produce and characterize chitosan-coated collagen membranes and to assess their efficacy in promoting chondrocyte adhesion, growth, and cytokine secretion. Porous collagen membranes were placed in chitosan solutions then crosslinked with glutaraldehyde vapor. Fourier transform infrared (FTIR analyses showed elevated absorption at 1655 cm-1 of the carbon–nitrogen (N=C bonds formed by the reaction between the (NH2 of the chitosan and the (C=O of the glutaraldehyde. A significant peak in the amide II region revealed a significant deacetylation of the chitosan. Scanning electron microscopy (SEM images of the chitosan-coated membranes exhibited surface variations, with pore size ranging from 20 to 50 µm. X-ray photoelectron spectroscopy (XPS revealed a decreased C–C groups and an increased C–N/C–O groups due to the reaction between the carbon from the collagen and the NH2 from the chitosan. Increased rigidity of these membranes was also observed when comparing the chitosan-coated and uncoated membranes at dried conditions. However, under wet conditions, the chitosan coated collagen membranes showed lower rigidity as compared to dried conditions. Of great interest, the glutaraldehyde-crosslinked chitosan-coated collagen membranes promoted chondrocyte adhesion, growth, and interleukin (IL-6 secretion. Overall results confirm the feasibility of using designed chitosan-coated collagen membranes in future applications, such as cartilage repair.

Preparation and Evaluation of Enteric-Coated Chitosan Derivative-Based Microparticles Loaded with Salmon Calcitonin as an Oral Delivery System

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Hiraku Onishi

2016-09-01

Full Text Available Background: The production of protein drugs has recently increased due to advances in biotechnology, but their clinical use is generally limited to parenteral administration due to low absorption in non-parenteral administration. Therefore, non-parenteral delivery systems allowing sufficient absorption draw much attention. Methods: Microparticles (MP were prepared using chitosan-4-thio-butylamidine conjugate (Ch-TBA, trimethyl-chitosan (TMC, and chitosan (Ch. Using salmon calcitonin (sCT as a model protein drug, Ch-TBA-, Ch-TBA/TMC (4/1-, and Ch-based MP were produced, and their Eudragit L100 (Eud-coated MP, named Ch-TBA-MP/Eud, Ch-TBA/TMC-MP/Eud, and Ch-MP/Eud, respectively, were prepared as oral delivery systems. These enteric-coated microparticles were examined in vitro and in vivo. Results: All microparticles before and after enteric coating had a submicron size (600–800 nm and micrometer size (1300–1500 nm, respectively. In vitro release patterns were similar among all microparticles; release occurred gradually, and the release rate was slower at pH 1.2 than at pH 6.8. In oral ingestion, Ch-TBA-MP/Eud suppressed plasma Ca levels most effectively among the microparticles tested. The relative effectiveness of Ch-TBA-MP/Eud to the intramuscular injection was 8.6%, while the sCT solution showed no effectiveness. Conclusion: The results suggest that Eud-coated Ch-TBA-based microparticles should have potential as an oral delivery system of protein drugs.

Antibacterial activity of irradiated and non-irradiated chitosan and chitosan derivatives against Escherichia coli growth

International Nuclear Information System (INIS)

Tg Ahbrizal Farizal Tg Ahmad; Norimah Yusof; Kamarudin Bahari; Kamaruddin Hashim

2006-01-01

Samples of chitosan and four chitosan derivatives [ionic chitosan, chitosan lactate, carboxymethyl chitosan (C) and carboxymethyl chitosan (L)] were studied for their antibacterial activities against Escherichia coli growth. Chitosan and chitosan derivatives were prepared at concentrations 20, 100, 1000, 10000 ppm and 250, 1000, 5000, 10000, 20000 ppm, respectively. Each of the samples was tested before and after irradiation with electron beam at 25 kGy. The turbidity of bacterial growth media was measured periodically at 0, 0.5, 1, 2, 4, 6 and 24 h after inoculation using the optical density method. The results indicated that non- irradiated chitosan inhibited E. coli growth at 20 and 100 ppm. Meanwhile, irradiated chitosan at 100 and 1000 ppm concentration inhibited E. coli growth. Both irradiated and non-irradiated ionic chitosan inhibited E. coli growth at all concentrations used. Chitosan lactate was found to inhibit E. coli at concentration as low as 5000 ppm for both irradiated and non-irradiated samples. E. coli growth was not inhibited by carboxymethyl chitosan (C) and carboxymethyl chitosan (L), before and after irradiation. The findings suggested that chitosan has greater antibacterial activity as compared to the chitosan derivative samples. (Author)

Chitosan from shrimp shell ( Crangon crangon ) and fish scales ...

African Journals Online (AJOL)

Chitosan is a naturally available biopolymer. It has been prepared by alkaline N deacetylation process of shrimp (Crangon crangon) chitin and fish (Labeorohita) chitin. The physico-chemical properties such as the degree of deacetylation (DD), solubility, water binding capacity, fat binding capacity and chitosan yield have ...

Cell Adhesion and Proliferation on Sulfonated and Non-Modified Chitosan Films.

Science.gov (United States)

Martínez-Campos, Enrique; Civantos, Ana; Redondo, Juan Alfonso; Guzmán, Rodrigo; Pérez-Perrino, Mónica; Gallardo, Alberto; Ramos, Viviana; Aranaz, Inmaculada

2017-05-01

Three types of chitosan-based films have been prepared and evaluated: a non-modified chitosan film bearing cationizable aliphatic amines and two films made of N-sulfopropyl chitosan derivatives bearing both aliphatic amines and negative sulfonate groups at different ratios. Cell adhesion and proliferation on chitosan films of C2C12 pre-myoblastic cells and B16 cells as tumoral model have been tested. A differential cell behavior has been observed on chitosan films due to their different surface modification. B16 cells have shown lower vinculin expression when cultured on sulfonated chitosan films. This study shows how the interaction among cells and material surface can be modulated by physicochemical characteristics of the biomaterial surface, altering tumoral cell adhesion and proliferation processes.

Preparation of N,O-carboxymethyl chitosan coated alginate microcapsules and their application to Bifidobacterium longum BIOMA 5920.

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Mi, Yu; Su, Ran; Fan, Dai-Di; Zhu, Xiao-Li; Zhang, Wen-Ni

2013-07-01

In order to greatly improve vitality of probiotic bacteria within the application, a novel biocompatible vehicle, N,O-carboxymethyl chitosan (NOCs) with appropriate degrees of substitution coat alginate (ALg) microparticles, was prepared by electrostatic droplet generation. The amount of chitosan (Cs) and N,O-carboxymethyl chitosan (NOCs) coated on the ALg microparticles was determined by differential scanning calorimetry. The surface morphology of ALg microparticles, Cs coated ALg microparticles and NOCs coated ALg microparticles was determined using scanning electron microscopy. The coating thickness of Cs coated ALg microparticles and that of NOCs coated ALg microparticles was directly observed with confocal laser scanning microscopy. In order to assess pH sensitivity of microparticles, the bovine serum albumin release from the microspheres was tested in acid solution (pH 2.0) for 2 h and subsequently in alkaline solution (pH 7.0) for 2 h. The survival of Bifidobacterium longum BIOMA 5920 loaded in NOCs coated with ALg microparticle was improved in simulated gastric juice (pH 2.0, for 2 h) compared to that of B. longum BIOMA 5920 loaded in ALg microparticles and Cs coated ALg microparticles. After incubation in simulated intestinal juices (pH 7.0, 2 h), the release of microencapsulated B. longum BIOMA 5920 was investigated. Copyright © 2013 Elsevier B.V. All rights reserved.

Synthesis of PVA-Chitosan Hydrogels for Wound Dressing Using Gamma Irradiation. Part I: Radiation Degradation of Chitosan in Solid State and in Solution

International Nuclear Information System (INIS)

Mahlous, M.; Tahtat, D.; Benamer, S.; Nacer Khodja, A.; Larbi Youcef, S.

2010-01-01

Chitosan is a partially deacetylated product of chitin, a very abundant polysaccharide, existing in exoskeleton of crustaceans. It is a polymer consisting of glucosamine and N-acetylglucosamine units linked by β-1-4-glycosidic bonds. Chitosan, like others polysaccharides, such as cellulose derivatives, alginates and carrageenan is widely used in food, medicine and cosmetic fields. Chitosan presents a variety of distinctive properties, such as biocompatibility, biodegradability, nontoxicity and nonantigenicity. Chitosan obtained by the deacetylation of chitin has, generally, a high molecular weight, which limits its solubility in aqueous solvents. The reduction of its molecular weight by degradation is usually used in order to improve its water solubility. Water-soluble chitosan exhibit some specific properties, such as antifungal activity, antimicrobial activity and plant growth promotion. Among the methods that have been tried to produce low molecular weight chitosan, radiation processing is the most promising one, since the process is simple, it is carried out at room temperature and no purification of the product is required after processing

Poly(N-isopropylacrylamide) hydrogel/chitosan scaffold hybrid for three-dimensional stem cell culture and cartilage tissue engineering.

Science.gov (United States)

Mellati, Amir; Kiamahalleh, Meisam Valizadeh; Madani, S Hadi; Dai, Sheng; Bi, Jingxiu; Jin, Bo; Zhang, Hu

2016-11-01

Providing a controllable and definable three-dimensional (3D) microenvironment for chondrogenic differentiation of mesenchymal stem cells (MSCs) remains a great challenge for cartilage tissue engineering. In this work, poly(N-isopropylacrylamide) (PNIPAAm) polymers with the degrees of polymerization of 100 and 400 (NI100 and NI400) were prepared and the polymer solutions were introduced into the preprepared chitosan porous scaffolds (CS) to form hybrids (CSNI100 and CSNI400, respectively). SEM images indicated that the PNIPAAm gel partially occupied chitosan pores while the interconnected porous structure of chitosan was preserved. MSCs were incorporated within the hybrid and cell proliferation and chondrogenic differentiation were monitored. After 7-day incubation of the cell-laden constructs in a growth medium, the cell viability in CSNI100 and CSNI400 were 54 and 108% higher than that in CS alone, respectively. Glycosaminoglycan and total collagen contents increased 2.6- and 2.5-fold after 28-day culture of cell-laden CSNI400 in the chondrogenic medium. These results suggest that the hybrid structure composed of the chitosan porous scaffold and the well-defined PNIPAAm hydrogel, in particular CSNI400, is suitable for 3D stem cell culture and cartilage tissue engineering. © 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 104A: 2764-2774, 2016. © 2016 Wiley Periodicals, Inc.

Evaluation of antioxidant activities and chemical analysis of sulfated chitosan from Sepia prashadi.

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Seedevi, Palaniappan; Moovendhan, Meivelu; Vairamani, Shanmugam; Shanmugam, Annaian

2017-06-01

The chitin and chitosan of S. prashadi was prepared through demineralization, deproteinzation, deacetylation process and sulfation were carried by chlorosulfonic acid in N,N-dimethylformamide. The sulfate content in chitosan was found to be 18.9%. The carbon, hydrogen and nitrogen composition of the sulfated chitosan were recorded 39.09%, 6.95% and 6.58% respectively. The structural analysis was done by using FT-IR and NMR spectroscopy technique. The DSC curves of sulfated chitosan showed a large endothermic peak resolved with T o value of 54.57°C and T P value of 97.46°C. The morphology of sulfated chitin and sulfated chitosan were studied by SEM. The Further in vitro antioxidant activity of sulfated chitosan was screened by scavenging activity of superoxide radical assay, hydroxyl radical scavenging assay, metal-ion chelating effect and reducing power. Its anticoagulant activity was tested for human plasma with respect to Activated Partial Thromboplastin Time (APTT) and Prothrombin Time (PT). Results prove that sulfated chitosan has potent antioxidant and anticoagulant activity. Copyright © 2017 Elsevier B.V. All rights reserved.

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

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Mulia, Kamarza; Andrie; Krisanti, Elsa A.

2018-03-01

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

3D- Printed Poly(ε-caprolactone) Scaffold Integrated with Cell-laden Chitosan Hydrogels for Bone Tissue Engineering.

Science.gov (United States)

Dong, Liang; Wang, Shao-Jie; Zhao, Xin-Rong; Zhu, Yu-Fang; Yu, Jia-Kuo

2017-10-17

Synthetic polymeric scaffolds are commonly used in bone tissue engineering (BTE) due to their biocompatibility and adequate mechanical properties. However, their hydrophobicity and the lack of specific cell recognition sites confined their practical application. In this study, to improve the cell seeding efficiency and osteoinductivity, an injectable thermo-sensitive chitosan hydrogel (CSG) was incorporated into a 3D-printed poly(ε-caprolactone) (PCL) scaffold to form a hybrid scaffold. To demonstrate the feasibility of this hybrid system for BTE application, rabbit bone marrow mesenchymal stem cells (BMMSCs) and bone morphogenetic protein-2 (BMP-2) were encapsulated in CSG. Pure PCL scaffolds were used as controls. Cell proliferation and viability were investigated. Osteogenic gene expressions of BMMSCs in various scaffolds were determined with reverse transcription polymerase chain reaction (RT-PCR). Growth factor releasing profile and mechanical tests were performed. CCK-8 assay confirmed greater cell retention and proliferation in chitosan and hybrid groups. Confocal microscopy showed even distribution of cells in the hybrid system. After 2-week osteogenic culture in vitro, BMMSCs in hybrid and chitosan scaffolds showed stronger osteogenesis and bone-matrix formation. To conclude, chitosan/PCL hybrid scaffolds are a favorable platform for BTE due to its capacity to carry cells and drugs, and excellent mechanical strength.

Microencapsulation of citronella oil by complex coacervation using chitosan-gelatin (b system: operating design, preparation and characterization

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Abdul Aziz Fitrah Rabani

2016-01-01

Full Text Available Citronella oil (CO can be an effective mosquito repellent, but due to its nature which having high volatility, oils rapidly evaporates causing loss of efficacy and shorten the repellent effect. Therefore, microencapsulation technology was implemented to ensure the encapsulated material being protected from immediate contact with environment and offers controlled release. In this study, microencapsulation of CO was done by employing complex coacervation using chitosan-gelatin (B system and utilized proanthocyanidins as the crosslinker. Remarkably, nearly all material involved in this study are from natural sources which are safe to human and environment. In designing operating process condition for CO encapsulation process, we found that wall ratio of 1:35 and pH 5 was the best operating condition based on zeta potential and turbidity analysis. FT-IR analysis found that gelatin-B had coated the CO droplet during emulsification stage, chitosan started to interact with gelatin-B to form a polyelectrolyte complex in adjust pH stage, CO capsules solidified at cooling process and were hardened during crosslinking process. Final product of CO capsules after settling process was identified at the top layer. Surface morphology of CO capsules obtained in this study were described having diameter varies from 81.63 µm to 156.74 µm with almost spherical in shape.

Fabrication, characterization and antimicrobial activities of thymol-loaded zein nanoparticles stabilized by sodium caseinate-chitosan hydrochloride double layers.

Science.gov (United States)

Zhang, Yaqiong; Niu, Yuge; Luo, Yangchao; Ge, Mei; Yang, Tian; Yu, Liangli Lucy; Wang, Qin

2014-01-01

Thymol-loaded zein nanoparticles stabilized with sodium caseinate (SC) and chitosan hydrochloride (CHC) were prepared and characterized. The SC stabilized nanoparticles had well-defined size range and negatively charged surface. Due to the presence of SC, the stabilized zein nanoparticles showed a shift of isoelectric point from 6.18 to 5.05, and had a desirable redispersibility in water at neutral pH after lyophilization. Coating with CHC onto the SC stabilized zein nanoparticles resulted in increased particle size, reversal of zeta potential value from negative to positive, and improved encapsulation efficiency. Both thymol-loaded zein nanoparticles and SC stabilized zein nanoparticles had a spherical shape and smooth surface, while the surfaces of CHC-SC stabilized zein nanoparticles seemed rough and had some clumps. Encapsulated thymol was more effective in suppressing gram-positive bacterium than un-encapsulated thymol for a longer time period. Copyright © 2013 Elsevier Ltd. All rights reserved.

Chitosan films incorporated with nettle (Urtica Dioica L.) extract-loaded nanoliposomes: II. Antioxidant activity and release properties.

Science.gov (United States)

Almasi, Hadi; Zandi, Mohsen; Beigzadeh, Sara; Haghju, Sara; Mehrnow, Nazila

2016-07-14

Chitosan films were loaded with NE nettle (Urtica dioica L.) extract (NE) at concentrations of 0, 0.5, 1 and 1.5%w/w in the free or nanoliposomal form to obtain active and nanoactive films, respectively. The antioxidant potential of the films containing NE-loaded nanoliposomes was decreased in comparison of free NE incorporated films. Diffusion of NE to soybean oil was enough to delay the induction of the oxidation of soybean oil stored for 60 days in contact with chitosan based films. Release studies indicated that the release rate of NE in 95% ethanol simulant significantly decreased by the nanoencapsulation of NE. The diffusion coefficient (D) for chitosan films containing 1.5%w/w of free and encapsulated NE at 25 °C was 18.80 and 3.68 × 10 -7 cm 2  s -1 , respectively. Moreover, the formation of nanoliposomes diminished the increasing effect of temperature on the release rate as when storage temperature increased from 4 °C to 40 °C.

Synthesis of carboxymethylated and quaternized chitosans and their therapeutic effect on nonalcoholic Fatty liver disease.

Science.gov (United States)

Liu, Xiaofei; Yang, Fan; Song, Tao; Zeng, Anrong; Wang, Qi; Sun, Zhong; Shen, Jun

2011-10-12

O-Carboxymethyl chitosan (O-CMCs) and N-((2-hydroxy-3-N,N-dimethylhexadecylammonium)propyl)chitosan chloride (N-CQCs) were synthesized for nonalcoholic fatty liver disease (NAFLD) treatment. The weight-average weight and substitution degree of O-CMCs and N-CQCs were 6.5 × 10(4) and 0.72 and 7.9 × 10(4) and 0.21, respectively. O-CMCs was negatively charged with a zeta-potential value of -31.82 mV, whereas that of N-CQCs was +36.1 mV, and both showed low cytotoxcity. Serum lipid level and liver fat accumulation were reduced with chitosan and its two derivatives. Furthermore, mRNA and protein expression assay of hepatic lipid metabolism enzymes and low-density lipoprotein receptor (LDL-R) were observed by RT-PCR and Western blot. Results showed that N-CQCs exhibited a more evident desired effect than chitosan and O-CMCs, indicating that amphiphilicity, solubility, and surface charge of chitosan and its two derivatives played roles in the expression of hepatic lipid metabolism enzymes and LDL-R. Therefore, dietary supplementation of O-CMCs and N-CQCs can alleviate the high fat diet induced aberrations related to NAFLD by their antilipidemic property.

Thermal degradation kinetics of phycocyanin encapsulation as an antioxidant agent

Science.gov (United States)

Nilamsari, A. M.; Yunanda, A.; Hadiyanto, H.

2018-01-01

Phycocyanin is a blue-light pigment that found in Cyanobacteria and two Eukaryotics algae such as Rhodophyta and Crytophyta. Phycocyanin is soluble in water and has a strong fluorescent properties as an antioxidant and normally used in food industry, cosmetic, biotechnology, and drug. However, Phycocyanin is easily damaged by a heating process. The aim of this study is to obtain the optimal condition of phycocyanin encapsulation with different coating materials, Chitosan and Carrageenan, by the calculation of heat resistance of antioxidant activity (D), range of temperature that increase the rate of degradation (Z), rate constant of degradation (k), and activation energy (Ea). The ratio of phycocyanin and the coating material are 2% (w/v) and 2 % (w/v).

Aryl-NHC-group 13 trimethyl complexes: structural, stability and bonding insights

KAUST Repository

Wu, Melissa M.; Gill, Arran M.; Yunpeng, Lu; Yongxin, Li; Ganguly, Rakesh; Falivene, Laura; Garcí a, Felipe

2016-01-01

Treatment of aromatic N-substituted N-heterocyclic carbenes (NHCs) with trimethyl-gallium and -indium yielded the new Lewis acid-base adducts, IMes·GaMe3 (1), SIMes·GaMe3 (2), IPr·GaMe3 (3), SIPr·GaMe3 (4), IMes·InMe3 (5), SIMes·InMe3 (6), IPr·InMe3 (7), and SIPr·InMe3 (8), with all complexes being identified by X-ray diffraction, IR, and multinuclear NMR analyses. Complex stability was found to be largely dependent on the nature of the constituent NHC ligands. Percent buried volume (%VBur) and topographic steric map analyses were employed to quantify and elucidate the observed trends. Additionally, a detailed bond snapping energy (BSE) decomposition analysis focusing on both steric and orbital interactions of the M-NHC bond (M = Al, Ga and In) has been performed.

Aryl-NHC-group 13 trimethyl complexes: structural, stability and bonding insights

KAUST Repository

Wu, Melissa M.

2016-12-14

Treatment of aromatic N-substituted N-heterocyclic carbenes (NHCs) with trimethyl-gallium and -indium yielded the new Lewis acid-base adducts, IMes·GaMe3 (1), SIMes·GaMe3 (2), IPr·GaMe3 (3), SIPr·GaMe3 (4), IMes·InMe3 (5), SIMes·InMe3 (6), IPr·InMe3 (7), and SIPr·InMe3 (8), with all complexes being identified by X-ray diffraction, IR, and multinuclear NMR analyses. Complex stability was found to be largely dependent on the nature of the constituent NHC ligands. Percent buried volume (%VBur) and topographic steric map analyses were employed to quantify and elucidate the observed trends. Additionally, a detailed bond snapping energy (BSE) decomposition analysis focusing on both steric and orbital interactions of the M-NHC bond (M = Al, Ga and In) has been performed.

Association of Alpha Tocopherol and Ag Sulfadiazine Chitosan Oleate Nanocarriers in Bioactive Dressings Supporting Platelet Lysate Application to Skin Wounds.

Science.gov (United States)

Bonferoni, Maria Cristina; Sandri, Giuseppina; Rossi, Silvia; Dellera, Eleonora; Invernizzi, Alessandro; Boselli, Cinzia; Cornaglia, Antonia Icaro; Del Fante, Claudia; Perotti, Cesare; Vigani, Barbara; Riva, Federica; Caramella, Carla; Ferrari, Franca

2018-02-09

Chitosan oleate was previously proposed to encapsulate in nanocarriers some poorly soluble molecules aimed to wound therapy, such as the anti-infective silver sulfadiazine, and the antioxidant α tocopherol. Because nanocarriers need a suitable formulation to be administered to wounds, in the present paper, these previously developed nanocarriers were loaded into freeze dried dressings based on chitosan glutamate. These were proposed as bioactive dressings aimed to support the application to wounds of platelet lysate, a hemoderivative rich in growth factors. The dressings were characterized for hydration capacity, morphological aspect, and rheological and mechanical behavior. Although chitosan oleate nanocarriers clearly decreased the mechanical properties of dressings, these remained compatible with handling and application to wounds. Preliminary studies in vitro on fibroblast cell cultures demonstrated good compatibility of platelet lysate with nanocarriers and bioactive dressings. An in vivo study on a murine wound model showed an accelerating wound healing effect for the bioactive dressing and its suitability as support of the platelet lysate application to wounds.

Association of Alpha Tocopherol and Ag Sulfadiazine Chitosan Oleate Nanocarriers in Bioactive Dressings Supporting Platelet Lysate Application to Skin Wounds

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Maria Cristina Bonferoni

2018-02-01

Full Text Available Chitosan oleate was previously proposed to encapsulate in nanocarriers some poorly soluble molecules aimed to wound therapy, such as the anti-infective silver sulfadiazine, and the antioxidant α tocopherol. Because nanocarriers need a suitable formulation to be administered to wounds, in the present paper, these previously developed nanocarriers were loaded into freeze dried dressings based on chitosan glutamate. These were proposed as bioactive dressings aimed to support the application to wounds of platelet lysate, a hemoderivative rich in growth factors. The dressings were characterized for hydration capacity, morphological aspect, and rheological and mechanical behavior. Although chitosan oleate nanocarriers clearly decreased the mechanical properties of dressings, these remained compatible with handling and application to wounds. Preliminary studies in vitro on fibroblast cell cultures demonstrated good compatibility of platelet lysate with nanocarriers and bioactive dressings. An in vivo study on a murine wound model showed an accelerating wound healing effect for the bioactive dressing and its suitability as support of the platelet lysate application to wounds.

Peritoneal adhesion prevention with a biodegradable and injectable N,O-carboxymethyl chitosan-aldehyde hyaluronic acid hydrogel in a rat repeated-injury model

Science.gov (United States)

Song, Linjiang; Li, Ling; He, Tao; Wang, Ning; Yang, Suleixin; Yang, Xi; Zeng, Yan; Zhang, Wenli; Yang, Li; Wu, Qinjie; Gong, Changyang

2016-11-01

Postoperative peritoneal adhesion is one of the serious issues because it induces severe clinical disorders. In this study, we prepared biodegradable and injectable hydrogel composed of N,O-carboxymethyl chitosan (NOCC) and aldehyde hyaluronic acid (AHA), and assessed its anti-adhesion effect in a rigorous and severe recurrent adhesion model which is closer to clinical conditions. The flexible hydrogel, which gelated in 66 seconds at 37 °C, was cross-linked by the schiff base derived from the amino groups of NOCC and aldehyde groups in AHA. In vitro cytotoxicity test showed the hydrogel was non-toxic. In vitro and in vivo degradation examinations demonstrated the biodegradable and biocompatibility properties of the hydrogel. The hydrogel discs could prevent the invasion of fibroblasts, whereas fibroblasts encapsulated in the porous 3-dimensional hydrogels could grow and proliferate well. Furthermore, the hydrogel was applied to evaluate the anti-adhesion efficacy in a more rigorous recurrent adhesion model. Compared with normal saline group and commercial hyaluronic acid (HA) hydrogel, the NOCC-AHA hydrogel exhibited significant reduction of peritoneal adhesion. Compared to control group, the blood and abdominal lavage level of tPA was increased in NOCC-AHA hydrogel group. These findings suggested that NOCC-AHA hydrogel had a great potential to serve as an anti-adhesion candidate.

Development of an injectable chitosan/marine collagen composite gel

International Nuclear Information System (INIS)

Wang Wei; Itoh, Soichiro; Aizawa, Tomoyasu; Demura, Makoto; Okawa, Atsushi; Sakai, Katsuyoshi; Ohkuma, Tsuneo

2010-01-01

A chitosan/marine-originated collagen composite has been developed. This composite gel was characterized and its biocompatibility, as well as an inflammatory reaction, was observed. The chitosan gel including N-3-carboxypropanoil-6-O-(carboxymethyl) chitosan of 3 mol%, 6-O-(carboxymethyl) chitosan of 62 mol% and 6-O-(carboxymethyl) chitin of 35 mol% was prepared and compounded with the salmon atelocollagen (SA) gel at different mixture ratios. The composite gels were injected subcutaneously in to the back of rats. The specimens were harvested for a histological survey as well as a tumor necrosis factor-alpha (TNF-α) assay by ELISA. The inflammatory cell infiltration and release of TNF-α were successively controlled low with the ratio of SA to chitosan at 10:90 or 20:80. The SA gel first, within 2 weeks, and then chitosan in the composite gel were slowly absorbed after implantation, followed by soft tissue formation. It is expected that this composite gel will be available as a carrier for tissue filler and drug delivery systems.

Physicochemical Characterization of Biopolymer Chitosan Extracted from Shrimp Shells

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Nezamaddin Mengelizadeh

2015-02-01

Full Text Available Chitosan is a deacetylated derivative of chitin, which is a naturally abundant mucopolysaccharide, supporting the matter of crustaceans, insects, and fungi. Because of its unique properties, such as non-toxicity, biodegradability, and biocompatibility, chitosan has a wide range of applications in various fields. The objective of the present work is to extract the polymer chitosan from Persian Gulf shrimp shells. In order to determine the physicochemical characteristics of the extracted chitosan, degree of deacetylation, molecular weight, water and fat binding capacities extraction rate, and apparent viscosity were measured using a variety of techniques including viscometry, weight measurement method and Fourier transform infrared spectroscopy (FTIR. The results of the study of the physicochemical properties, molecular weight (6.7×105 Da, degree of deacetylation (57%, ash content as well as yield (0.5% of the prepared chitosan indicated that shrimp processing wastes (shrimp shells are a good source of chitosan. The water binding capacity (521% and fat binding capacity (327% of the prepared chitosan are in good agreement with the other studies. The elemental analysis showed the C, H and N contents of 35.92%, 7.02%, and 8.66%, respectively. In this study, the antimicrobial activity of chitosan was evaluated against Staphylococcus aureus and Escherichia coli. The results indicated the high potential of chitosan as an antibacterial agent. Moreover, the results of the study indicated that shrimp shells are a rich source of chitin as 25.21% of the shell’s dry weight.

Drug delivery glucantime in PVP/chitosan membranes

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Oliveira, Maria J.A.; Lugao, Ademar B.; Parra, Duclerc F., E-mail: mariajhho@yahoo.com.br [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil); Amato, Valdir S. [Universidade de Sao Paulo (DMIP/FM/USP), Sao Paulo, SP (Brazil). Faculdade de Medicina. Departamento de Molestias Infecciosas e Parasitarias

2015-07-01

The current study of polymer science considers the area of biomedical application very important to establish developments in new polymeric materials. Examples of that are hydrogels for controlled release of drugs. In this work, hydrogels of poly (N-2-vinil-pyrrolidone) (PVP) containing chitosan and clay nanoparticles were obtained and characterized to investigate chitosan influence on Glucantime drug delivery. The matrixes were crosslinked by gamma irradiation process with doses of 25 kGy. Hydrogels morphologies were observed by X Ray diffraction (DRX). Atomic Force Microscopy (AFM) and swelling kinetic at 22 °C to study the capacity of water retention and, finally, drug delivery tests were performed 'in vitro'. The system showed higher gel fraction for the matrix with 1.0% of clay and 0.5% of chitosan. In this case, besides the interactions of clay ions with PVP, there are interactions of chitosan amine group with PVP amide group. (author)

Drug delivery glucantime in PVP/chitosan membranes

International Nuclear Information System (INIS)

Oliveira, Maria J.A.; Lugao, Ademar B.; Parra, Duclerc F.; Amato, Valdir S.

2015-01-01

The current study of polymer science considers the area of biomedical application very important to establish developments in new polymeric materials. Examples of that are hydrogels for controlled release of drugs. In this work, hydrogels of poly (N-2-vinil-pyrrolidone) (PVP) containing chitosan and clay nanoparticles were obtained and characterized to investigate chitosan influence on Glucantime drug delivery. The matrixes were crosslinked by gamma irradiation process with doses of 25 kGy. Hydrogels morphologies were observed by X Ray diffraction (DRX). Atomic Force Microscopy (AFM) and swelling kinetic at 22 °C to study the capacity of water retention and, finally, drug delivery tests were performed 'in vitro'. The system showed higher gel fraction for the matrix with 1.0% of clay and 0.5% of chitosan. In this case, besides the interactions of clay ions with PVP, there are interactions of chitosan amine group with PVP amide group. (author)

Radiation degradation of chitosan

International Nuclear Information System (INIS)

Norzita Yacob; Maznah Mahmud; Norhashidah Talip; Kamarudin Bahari; Kamaruddin Hashim; Khairul Zaman Dahlan

2010-01-01

In order to obtain an oligo chitosan, degradation of chitosan s were carried out in solid state and liquid state. The effects of an irradiation on the molecular weight and viscosity of the chitosan were investigated using Ubbelohde Capillary Viscometer and Brookfield Viscometer respectively. The molecular weight and viscosity of the chitosan s were decreased with an increase in the irradiation dose. In the presence of hydrogen peroxide, the molecular weight of chitosan can be further decreased. (author)

An integrated buccal delivery system combining chitosan films impregnated with peptide loaded PEG-b-PLA nanoparticles.

Science.gov (United States)

Giovino, Concetta; Ayensu, Isaac; Tetteh, John; Boateng, Joshua S

2013-12-01

Peptide (insulin) loaded nanoparticles (NPs) have been embedded into buccal chitosan films (Ch-films-NPs). These films were produced by solvent casting and involved incorporating in chitosan gel (1.25% w/v), NPs-Insulin suspensions at three different concentrations (1, 3, and 5mg of NPs per film) using glycerol as plasticiser. Film swelling and mucoadhesion were investigated using 0.01M PBS at 37°C and texture analyzer, respectively. Formulations containing 3mg of NPs per film produced optimised films with excellent mucoadhesion and swelling properties. Dynamic laser scattering measurements showed that the erosion of the chitosan backbone controlled the release of NPs from the films, preceding in vitro drug (insulin) release from Ch-films-NPs after 6h. Modulated release was observed with 70% of encapsulated insulin released after 360h. The use of chitosan films yielded a 1.8-fold enhancement of ex vivo insulin permeation via EpiOral™ buccal tissue construct relative to the pure drug. Flux and apparent permeation coefficient of 0.1μg/cm(2)/h and 4×10(-2)cm(2)/h were respectively obtained for insulin released from Ch-films-NPs-3. Circular dichroism and FTIR spectroscopy demonstrated that the conformational structure of the model peptide drug (insulin) released from Ch-films-NPs was preserved during the formulation process. Copyright © 2013 Elsevier B.V. All rights reserved.

Design, characterization and ex vivo evaluation of chitosan film integrating of insulin nanoparticles composed of thiolated chitosan derivative for buccal delivery of insulin.

Science.gov (United States)

Mortazavian, Elaheh; Dorkoosh, Farid Abedin; Rafiee-Tehrani, Morteza

2014-05-01

The purpose of this study is to optimize and characterize of chitosan buccal film for delivery of insulin nanoparticles that were prepared from thiolated dimethyl ethyl chitosan (DMEC-Cys). Insulin nanoparticles composed of chitosan and dimethyl ethyl chitosan (DMEC) were also prepared as control groups. The release of insulin from nanoparticles was studied in vitro in phosphate buffer solution (PBS) pH 7.4. Optimization of chitosan buccal films has been carried out by central composite design (CCD) response surface methodology. Independent variables were different amounts of chitosan and glycerol as mucoadhesive polymer and plasticizer, respectively. Tensile strength and bioadhesion force were considered as dependent variables. Ex vivo study was performed on excised rabbit buccal mucosa. Optimized insulin nanoparticles were obtained with acceptable physicochemical properties. In vitro release profile of insulin nanoparticles revealed that the highest solubility of nanoparticles in aqueous media is related to DMEC-Cys nanoparticles. CCD showed that optimized buccal film containing 4% chitosan and 10% glycerol has 5.81 kg/mm(2) tensile strength and 2.47 N bioadhesion forces. Results of ex vivo study demonstrated that permeation of insulin nanoparticles through rabbit buccal mucosa is 17.1, 67.89 and 97.18% for chitosan, DMEC and DMEC-Cys nanoparticles, respectively. Thus, this study suggests that DMEC-Cys can act as a potential enhancer for buccal delivery of insulin.

Evaluation of cross-linked chitosan microparticles containing acyclovir obtained by spray-drying

International Nuclear Information System (INIS)

Stulzer, Hellen Karine; Tagliari, Monika Piazzon; Parize, Alexandre Luis; Silva, Marcos Antonio Segatto; Laranjeira, Mauro Cesar Marghetti

2009-01-01

The aim of this study was to obtain microparticles containing acyclovir (ACV) and chitosan cross-linked with tripolyphosphate using the spray-drying technique. The resultant system was evaluated through loading efficiency, differential scanning calorimetry (DSC), thermogravimetric analysis (TG), X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), in vitro release and stability studies. The results obtained indicated that the polymer/ACV ratio influenced the final properties of the microparticles, with higher ratios giving the best encapsulation efficiency, dissolution profiles and stability. The DSC and XRPD analyses indicated that the ACV was transformed into amorphous form during the spray-drying process

Comparison of cadmium adsorption onto chitosan and epichlorohydrin crosslinked chitosan/eggshell composite

Science.gov (United States)

Rahmi; Marlina; Nisfayati

2018-05-01

The use of chitosan and epichlorohydrin crosslinked chitosan/eggshell composite for cadmium adsorption from water were investigated. The factors affecting adsorption such as pH and contact time were considered. The results showed that the optimum pH of adsorption was pH = 6.0 and the equilibrium time of adsorption was 40 min. The adsorption isotherm of Cd ions onto chitosan and composite were well fitted to Langmuir equation. The maximum adsorption capacity (fitting by Langmuir model) of chitosan and composite were 1.008 and 11.7647 mg/g, respectively. Adsorption performance of composite after regeneration was better than chitosan.

Photocatalytic enhancement of floating photocatalyst: Layer-by-layer hybrid carbonized chitosan and Fe-N- codoped TiO{sub 2} on fly ash cenospheres

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Song, Jingke; Wang, Xuejiang, E-mail: wangxj@tongji.edu.cn; Bu, Yunjie; Wang, Xin; Zhang, Jing; Huang, Jiayu; Ma, RongRong; Zhao, Jianfu

2017-01-01

Highlights: • Multifunctional TiO{sub 2} was coated on floating fly ash cenospheres. • TiO{sub 2} was integrated with carbonaceous layer from chitosan and Fe-N co-doping. • Carbonized chitosan improved the adsorption of pollutant and photon absorption ability of TiO{sub 2}. • Modified TiO{sub 2} exhibited superior photocatalytic activity and better recyclability. - Abstract: Due to the advantage of floating on water surface, floating photocatalysts show higher rates of radical formation and collection efficiencies. And they were expected to be used for solar remediation of non-stirred and non-oxygenated reservoirs. In this research, floating fly ash cenospheres (FAC) supported layer-by- layer hybrid carbonized chitosan and Fe-N-codoped TiO{sub 2} was prepared by a simple sol-gel method. The catalysts were characterized by X-ray diffraction(XRD), field emission scanning electron microscopy(FESEM), fourier transform infrared spectroscopy(FTIR), X-ray photoelectron spectroscopy (XPS), UV–vis diffuse reflectance spectroscopy(DRS), nitrogen adsorption analyses for Brunauer-Emmett-Teller (BET) specific surface area. It is indicated that Fe-N codoped narrowed the material’s band gap, and the layer of carbonized chitosan (Cts) increased the catalyst’s adsorption capacity and the absorption ability of visible light. Comparing with Fe-N-TiO{sub 2}/FAC and N-TiO{sub 2}/FAC, the composite photocatalyst show excellent performance on the degradation of RhB. Photodegradation rate of RhB by Fe-N-TiO{sub 2}/FAC-Cts was 0.01018 min{sup −1}, which is about 1.5 and 2.09 times higher than Fe-N-TiO{sub 2}/FAC and N-TiO{sub 2}/FAC under visible light irradiation in 240 min, respectively. The dye photosentization, capture of holes and electrons by Fe{sup 3+} ion, and synergistic effect of adsorption and photodegradation were attributed to the results for the improvement of photocatalytic performance. The floating photocatalyst can be reused for at least three consecutive

Preparation and Characterization of Facilitated Transport Membranes Composed of Chitosan-Styrene and Chitosan-Acrylonitrile Copolymers Modified by Methylimidazolium Based Ionic Liquids for CO2 Separation from CH4 and N2

Directory of Open Access Journals (Sweden)

Ksenia V. Otvagina

2016-06-01

Full Text Available CO2 separation was found to be facilitated by transport membranes based on novel chitosan (CS–poly(styrene (PS and chitosan (CS–poly(acrylonitrile (PAN copolymer matrices doped with methylimidazolium based ionic liquids: [bmim][BF4], [bmim][PF6], and [bmim][Tf2N] (IL. CS plays the role of biodegradable film former and selectivity promoter. Copolymers were prepared implementing the latest achievements in radical copolymerization with chosen monomers, which enabled the achievement of outstanding mechanical strength values for the CS-based membranes (75–104 MPa for CS-PAN and 69–75 MPa for CS-PS. Ionic liquid (IL doping affected the surface and mechanical properties of the membranes as well as the gas separation properties. The highest CO2 permeability 400 Barrers belongs to CS-b-PS/[bmim][BF4]. The highest selectivity α (CO2/N2 = 15.5 was achieved for CS-b-PAN/[bmim][BF4]. The operational temperature of the membranes is under 220 °C.

Chitosan-propolis nanoparticle formulation demonstrates anti-bacterial activity against Enterococcus faecalis biofilms.

Directory of Open Access Journals (Sweden)

Teik Hwa Ong

Full Text Available Propolis obtained from bee hives is a natural substance with antimicrobial properties. It is limited by its insolubility in aqueous solutions; hence ethanol and ethyl acetate extracts of Malaysian propolis were prepared. Both the extracts displayed antimicrobial and anti-biofilm properties against Enterococcus faecalis, a common bacterium associated with hospital-acquired infections. High performance liquid chromatography (HPLC analysis of propolis revealed the presence of flavonoids like kaempferol and pinocembrin. This study investigated the role of propolis developed into nanoparticles with chitosan for its antimicrobial and anti-biofilm properties against E. faecalis. Bacteria that grow in a slimy layer of biofilm are resistant to penetration by antibacterial agents. The use of nanoparticles in medicine has received attention recently due to better bioavailability, enhanced penetrative capacity and improved efficacy. A chitosan-propolis nanoformulation was chosen based on ideal physicochemical properties such as particle size, zeta potential, polydispersity index, encapsulation efficiency and the rate of release of the active ingredients. This formulation inhibited E. faecalis biofilm formation and reduced the number of bacteria in the biofilm by ~90% at 200 μg/ml concentration. When tested on pre-formed biofilms, the formulation reduced bacterial number in the biofilm by ~40% and ~75% at 200 and 300 μg/ml, respectively. The formulation not only reduced bacterial numbers, but also physically disrupted the biofilm structure as observed by scanning electron microscopy. Treatment of biofilms with chitosan-propolis nanoparticles altered the expression of biofilm-associated genes in E. faecalis. The results of this study revealed that chitosan-propolis nanoformulation can be deemed as a potential anti-biofilm agent in resisting infections involving biofilm formation like chronic wounds and surgical site infections.

Oxidation-mediated chitosan as additives for creation of chitosan aerogels with diverse three-dimensional interconnected skeletons

International Nuclear Information System (INIS)

Zhang, Sizhao; Feng, Jian; Feng, Junzong; Jiang, Yonggang

2017-01-01

Highlights: • A new synthetic method for controlling morphology of chitosan aerogels is proposed. • Chitosan aerogels with nanoflake-like and nanofiber-like were prepared. • Textures of chitosan aerogels are strongly dependent upon the oxidation pattern. - Abstract: Naturally occurring polymer-based aerogels have myriad practical utilizations due to environmentally benign and fruitful resources. However, engineering morphology-controllable biomass aerogels still represents a great challenge. Here we present a facile solution to synthesize chitosan aerogels having distinguished textures by reacting oxidized chitosan with formaldehyde and chitosan sol. In more detail, chitosan was chemically oxidized using two types of oxidation agents such as ammonium persulphate (SPD) and sodium periodate (APS) to obtain corresponding oxidized chitosan, subsequently cross-linked with chitosan solution containing formaldehyde to harvest SPD-oxidized chitosan aerogels (SCAs) and APS-SPD-oxidized ones (ASCAs) after aging, solvent exchange and supercritical drying processes. We found that the morphologies of as-prepared chitosan aerogels are strongly dependent upon the oxidation pattern towards chitosan. The structural textures of SCAs and ASCAs appear nanoflake-like and nanofiber-like structures, which may be related to spatial freedom of active groups located in chitosan. Selected area electron diffraction analysis reveals that the crystalline properties of chitosan aerogels generally appear the serious deterioration comparing to raw chitosan owing to their interconnected skeletal structure formation. The occurrence of characteristic groups displays cross-linked chain construction by using chemical state measurements such as FT-IR and XPS. Further, a plausible mechanism for controlling morphology of chitosan aerogels is also established. This new family of method for creation of chitosan aerogels may open up a perspective for biomass aerogels with controllable textures.

Oxidation-mediated chitosan as additives for creation of chitosan aerogels with diverse three-dimensional interconnected skeletons

Energy Technology Data Exchange (ETDEWEB)

Zhang, Sizhao, E-mail: bule-soul@hotmail.com; Feng, Jian, E-mail: fengj@nudt.edu.cn; Feng, Junzong; Jiang, Yonggang

2017-02-28

Highlights: • A new synthetic method for controlling morphology of chitosan aerogels is proposed. • Chitosan aerogels with nanoflake-like and nanofiber-like were prepared. • Textures of chitosan aerogels are strongly dependent upon the oxidation pattern. - Abstract: Naturally occurring polymer-based aerogels have myriad practical utilizations due to environmentally benign and fruitful resources. However, engineering morphology-controllable biomass aerogels still represents a great challenge. Here we present a facile solution to synthesize chitosan aerogels having distinguished textures by reacting oxidized chitosan with formaldehyde and chitosan sol. In more detail, chitosan was chemically oxidized using two types of oxidation agents such as ammonium persulphate (SPD) and sodium periodate (APS) to obtain corresponding oxidized chitosan, subsequently cross-linked with chitosan solution containing formaldehyde to harvest SPD-oxidized chitosan aerogels (SCAs) and APS-SPD-oxidized ones (ASCAs) after aging, solvent exchange and supercritical drying processes. We found that the morphologies of as-prepared chitosan aerogels are strongly dependent upon the oxidation pattern towards chitosan. The structural textures of SCAs and ASCAs appear nanoflake-like and nanofiber-like structures, which may be related to spatial freedom of active groups located in chitosan. Selected area electron diffraction analysis reveals that the crystalline properties of chitosan aerogels generally appear the serious deterioration comparing to raw chitosan owing to their interconnected skeletal structure formation. The occurrence of characteristic groups displays cross-linked chain construction by using chemical state measurements such as FT-IR and XPS. Further, a plausible mechanism for controlling morphology of chitosan aerogels is also established. This new family of method for creation of chitosan aerogels may open up a perspective for biomass aerogels with controllable textures.

Chitosan(PEO)/silica hybrid nanofibers as a potential biomaterial for bone regeneration.

Science.gov (United States)

Toskas, Georgios; Cherif, Chokri; Hund, Rolf-Dieter; Laourine, Ezzeddine; Mahltig, Boris; Fahmi, Amir; Heinemann, Christiane; Hanke, Thomas

2013-05-15

New hybrid nanofibers prepared with chitosan (CTS), containing a total amount of polyethylene oxide (PEO) down to 3.6wt.%, and silica precursors were produced by electrospinning. The solution of modified sol-gel particles contained tetraethoxysilane (TEOS) and the organosilane 3-glycidyloxypropyltriethoxysilane (GPTEOS). This is rending stable solution toward gelation and contributing in covalent bonding with chitosan. The fibers encompass advantages of biocompatible polymer template silicate components to form self-assembled core-shell structure of the polymer CTS/PEO encapsulated by the silica. Potential applicability of this hybrid material to bone tissue engineering was studied examining its cellular compatibility and bioactivity. The nanofiber matrices were proved cytocompatible when seeded with bone-forming 7F2-cells, promoting attachment and proliferation over 7 days. These found to enhance a fast apatite formation by incorporation of Ca(2+) ions and subsequent immersion in modified simulated body fluid (m-SBF). The tunable properties of these hybrid nanofibers can find applications as active biomaterials in bone repair and regeneration. Copyright © 2013 Elsevier Ltd. All rights reserved.

2-N, 6-O-sulfated chitosan-assisted BMP-2 immobilization of PCL scaffolds for enhanced osteoinduction

Energy Technology Data Exchange (ETDEWEB)

Cao, Lingyan [Key Laboratory for Ultrafine Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Engineering Research Center for Biomedical Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); CSIRO Manufacturing, Bayview Avenue, Clayton, Victoria 3168 (Australia); Department of Prosthodontics, College of Stomatology, Ninth People' s Hospital, School of Medicine, Shanghai Jiao Tong University, 639 Zhizaoju Road, Shanghai 200011 (China); Yu, Yuanman [Key Laboratory for Ultrafine Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Engineering Research Center for Biomedical Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Wang, Jing, E-mail: biomatwj@163.com [Key Laboratory for Ultrafine Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Engineering Research Center for Biomedical Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Werkmeister, Jerome A [CSIRO Manufacturing, Bayview Avenue, Clayton, Victoria 3168 (Australia); McLean, Keith M, E-mail: Keith.McLean@csiro.au [CSIRO Manufacturing, Bayview Avenue, Clayton, Victoria 3168 (Australia); Liu, Changsheng, E-mail: liucs@ecust.edu.cn [Key Laboratory for Ultrafine Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China); Engineering Research Center for Biomedical Materials of Ministry of Education, East China University of Science and Technology, Shanghai 200237 (China)

2017-05-01

The aim of this study was to develop a 2-N, 6-O-sulfated chitosan (26SCS) modified electrospun fibrous PCL scaffold for bone morphogenetic protein-2 (BMP-2) delivery to improve osteoinduction. The PCL scaffold was modified by an aminolysis reaction using ethylenediamine (ED) and 26SCS was immobilized via electrostatic interactions (PCL-N-S). Scaffolds were characterized by scanning electron microscopy (SEM), atomic force microscopy (AFM), X-ray photoelectron spectroscopy (XPS) and contact angle measurements. In vitro BMP-2 adsorption and release kinetics indicated that modified PCL-N-S scaffolds showed higher levels of binding of BMP-2 (about 30–100 times), moderative burst release (about one third), and prolonged releasing time compared to the unmodified PCL scaffold. The bioactivity of released BMP-2 determined by alkaline phosphatase (ALP) activity assay was maintained and improved 8– 12 times with increasing concentration of immobilized 26SCS on the scaffolds. In vitro studies demonstrated that bone marrow mesenchymal stem cells (BMSCs) attached more readily to the PCL-N-S scaffolds with increased spreading. In conclusion, 26SCS modified PCL scaffolds can be a potent system for the sustained and bioactive delivery of BMP-2. - Graphical abstract: Limited self-regenerating capacity of human body makes the reconstruction of critical size bone defect a significant challenge. Although bone morphogenetic protein-2 (BMP-2) is an important differentiation factor inducing bone regeneration, it's short half-life in vivo and potent side effect at high dosage still show lots of concerns in the clinical use. Herein, modification of electrospun PCL scaffolds was presented through immobilizing of sulfated chitosan (26SCS). The modified scaffolds effectively improve the binding capacity of BMP-2 and exhibited an enhanced bioactivity and sustained release in vitro. Thus, the use of 26SCS modified PCL scaffolds combined with BMP-2 could be a useful scaffold for tissue

Design of a potentially prebiotic and responsive encapsulation material for probiotic bacteria based on chitosan and sulfated β-glucan.

Science.gov (United States)

Yucel Falco, Cigdem; Sotres, Javier; Rascón, Ana; Risbo, Jens; Cárdenas, Marité

2017-02-01

Chitosan and sulfated oat β-glucan are materials suitable to create a prebiotic coating for targeted delivery to gastrointestinal system, using the layer by layer technology. Quartz crystal microbalance with dissipation (QCM-D), spectroscopic ellipsometry (SE) and atomic force microscopy (AFM) were used to assess the multilayer formation capacity and characterize the resulting coatings in terms of morphology and material properties such as structure and rigidity. The coating of colloidal materials was proven, specifically on L. acidophilus bacteria as measured by changes in the bacterial suspension zeta potential. Viability of coated cells was shown using plate counting method. The coatings on solid surfaces were examined after exposure to mimics of gastrointestinal fluids and a commercially available β-glucanase. Successful build-up of multilayers was confirmed with QCM-D and SE. Zeta potential values proved the coating of cells. There was 2 log CFU/mL decrease after coating cells with four alternating layers of chitosan and sulfated β-glucan when compared to viability of uncoated cells. The coatings were partially degraded after exposure to simulated intestinal fluid and restructured as a result of β-glucanase treatment, mimicking enzymes present in the microflora of the human gut, but seemed to resist acidic gastric conditions. Therefore, coatings of chitosan and sulfated β-glucan can potentially be exploited as carriers for probiotics and delicate nutraceuticals. Copyright © 2016 Elsevier Inc. All rights reserved.

Chitosan coated carbon fiber microelectrode for selective in vivo detection of neurotransmitters in live zebrafish embryos

International Nuclear Information System (INIS)

Ozel, Rifat Emrah; Wallace, Kenneth N.; Andreescu, Silvana

2011-01-01

Graphical abstract: Chitosan coated fiber electrodes are sensitive to serotonin detection while rejecting physiological levels of ascorbic acid interferences. - Abstract: We report the development of a chitosan modified carbon fiber microelectrode for in vivo detection of serotonin. We find that chitosan has the ability to reject physiological levels of ascorbic acid interferences and facilitate selective and sensitive detection of in vivo levels of serotonin, a common catecholamine neurotransmitter. Presence of chitosan on the microelectrode surface was investigated using scanning electron microscopy (SEM) and cyclic voltammetry (CV). The electrode was characterized using differential pulse voltammetry (DPV). A detection limit of 1.6 nM serotonin with a sensitivity of 5.12 nA/μM, a linear range from 2 to 100 nM and a reproducibility of 6.5% for n = 6 electrodes were obtained. Chitosan modified microelectrodes selectively measure serotonin in presence of physiological levels of ascorbic acid. In vivo measurements were performed to measure concentration of serotonin in the live embryonic zebrafish intestine. The sensor quantifies in vivo intestinal levels of serotonin while successfully rejecting ascorbic acid interferences. We demonstrate that chitosan can be used as an effective coating to reject ascorbic acid interferences at carbon fiber microelectrodes, as an alternative to Nafion, and that chitosan modified microelectrodes are reliable tools for in vivo monitoring of changes in neurotransmitter levels.

Chitosan coated carbon fiber microelectrode for selective in vivo detection of neurotransmitters in live zebrafish embryos

Energy Technology Data Exchange (ETDEWEB)

Ozel, Rifat Emrah [Department of Chemistry and Biomolecular Science, 8 Clarkson Ave, Potsdam, NY 136995810 (United States); Wallace, Kenneth N. [Department of Biology, Clarkson University, Potsdam, NY 136995810 (United States); Andreescu, Silvana, E-mail: eandrees@clarkson.edu [Department of Chemistry and Biomolecular Science, 8 Clarkson Ave, Potsdam, NY 136995810 (United States)

2011-06-10

Graphical abstract: Chitosan coated fiber electrodes are sensitive to serotonin detection while rejecting physiological levels of ascorbic acid interferences. - Abstract: We report the development of a chitosan modified carbon fiber microelectrode for in vivo detection of serotonin. We find that chitosan has the ability to reject physiological levels of ascorbic acid interferences and facilitate selective and sensitive detection of in vivo levels of serotonin, a common catecholamine neurotransmitter. Presence of chitosan on the microelectrode surface was investigated using scanning electron microscopy (SEM) and cyclic voltammetry (CV). The electrode was characterized using differential pulse voltammetry (DPV). A detection limit of 1.6 nM serotonin with a sensitivity of 5.12 nA/{mu}M, a linear range from 2 to 100 nM and a reproducibility of 6.5% for n = 6 electrodes were obtained. Chitosan modified microelectrodes selectively measure serotonin in presence of physiological levels of ascorbic acid. In vivo measurements were performed to measure concentration of serotonin in the live embryonic zebrafish intestine. The sensor quantifies in vivo intestinal levels of serotonin while successfully rejecting ascorbic acid interferences. We demonstrate that chitosan can be used as an effective coating to reject ascorbic acid interferences at carbon fiber microelectrodes, as an alternative to Nafion, and that chitosan modified microelectrodes are reliable tools for in vivo monitoring of changes in neurotransmitter levels.

Impedance spectroscopy study of dehydrated chitosan and chitosan containing LiClO4

International Nuclear Information System (INIS)

Costa, M.M.; Terezo, A.J.; Matos, A.L.; Moura, W.A.; Giacometti, Jose A.; Sombra, A.S.B.

2010-01-01

Cast films of chitosan and chitosan containing LiClO 4 were characterized using Fourier transform infrared spectroscopy and the thermogravimetric technique. The electric properties of hydrated and dehydrated films were investigated with impedance spectroscopy in the frequency range from 0.1 Hz to 1 MHz, at temperatures varying from 30 to 110 o C. The frequency dependence of the impedance for dehydrated chitosan and chitosan containing LiClO 4 films indicated ionic conduction. Two relaxation peaks were evident on the imaginary curve of the electric modulus, which were assigned to ionic conduction. The peak at higher frequency was found for chitosan and chitosan containing LiClO 4 films. The peak at lower frequency was attributed to Li + conduction since it appeared only for the chitosan containing LiClO 4 . The peak frequency varied with the temperature according to an Arrhenius process with activation energies of circa of 0.6 and 0.45 eV, for H + and Li + conduction, respectively.

Preliminary evaluation of the encapsulation of new antidiabetic sulphonylhydrazone and antitumor N-acylhydrazone derivatives using PLGA nanoparticles

International Nuclear Information System (INIS)

Costa, F N; Ibiapino, A L; De Figueiredo, L P; De Castro, C E; Giacomelli, F C; Ferreira, F F; Barreiro, E J; Lima, L M; Do Amaral, D N

2015-01-01

It has been demonstrated the feasibly of using PLGA nanoparticles to promote the encapsulation of novel anti-diabetic sulphonylhydrazone and antitumor N-acylhydrazone derivatives. The motivation is to further demonstrate the possibility of long-term release of anti-diabetic as well as higher accumulation of the antitumor derivative by using the nanotechnology-based production. The produced nanoparticles were obtained by the nanoprecipitation method, which revealed to be effective in the encapsulation of the bioactive compounds. The determined sizes were in the range of ∼100 nm, which are supposed to be suitable for both potential applications. The preliminary experimental data demonstrated the formation of stable nanosystems and further experiments are underway in order to determine the loading content, encapsulation efficiency and release profile of the hydrophobic bioactive compounds. (paper)

Matrix Effect on the Spray Drying Nanoencapsulation of Lippia sidoides Essential Oil in Chitosan-Native Gum Blends.

Science.gov (United States)

Paula, Haroldo C B; Oliveira, Erick F; Carneiro, Maria J M; de Paula, Regina C M

2017-03-01

Essential oils have many applications in the pharmaceutical, chemical, and food fields, however, their use is limited to the fact that they are very labile, requiring their a priori encapsulation, aiming to preserve their properties.This work reports on the preparation of chitosan-gum nanoparticles loaded with thymol containing Lippia sidoides essential oil, using exudates of Anacardium Occidentale (cashew gum), Sterculia striata (chichá gum), and Anadenanthera macrocarpa trees (angico gum). Nanoparticles were produced by spray drying an emulsion of L. sidoides essential oil and aqueous solution of gums with different chitosan : gum ratios. Samples were characterized by FTIR and UV/VIS spectroscopy, particle size, volume distribution, and zeta potential. The FTIR spectrum showed the main signals of chitosan and the gums. Data obtained revealed that the samples had sizes in the nano range, varying from 17 nm to 800 nm. The zeta potential varied from + 30 mV to - 40 mV. Nanoparticle loading values varied from 6.7 % to 15.6 %, with an average encapsulating efficiency of 62 %, where the samples with high ratios of cashew gum and chichá gum presented high oil loading values. The data revealed that both the chitosan : gum ratio and polysaccharide characteristics play major roles in nanoencapsulation processes. Georg Thieme Verlag KG Stuttgart · New York.

Experimental evaluation of photocrosslinkable chitosan as a biologic adhesive with surgical applications.

Science.gov (United States)

Ono, K; Ishihara, M; Ozeki, Y; Deguchi, H; Sato, M; Saito, Y; Yura, H; Sato, M; Kikuchi, M; Kurita, A; Maehara, T

2001-11-01

In various surgical cases, effective tissue adhesives are required for both hemostasis (eg, intraoperative bleeding) and air sealing (eg, thoracic surgery). We have designed a chitosan molecule (Az-CH-LA) that can be photocrosslinked by ultraviolet (UV) light irradiation, thereby forming a hydrogel. The purpose of this work was to evaluate the effectiveness and safety of the photocrosslinkable chitosan hydrogel as an adhesive with surgical applications. The sealing ability of the chitosan hydrogel, determined as a bursting pressure, was assessed with removed thoracic aorta, trachea, and lung of farm pigs and in a rabbit model. The carotid artery and lung of rabbits were punctured with a needle, and the chitosan hydrogel was applied to, respectively, stop the bleeding and the air leakage. In vivo chitosan degradability and biologic responses were histologically assessed in animal models. The bursting pressure of chitosan hydrogel (30 mg/mL) and fibrin glue, respectively, was 225 +/- 25 mm Hg (mean +/- SD) and 80 +/- 20 mm Hg in the thoracic aorta; 77 +/- 29 mm Hg and 48 +/- 21 mm Hg in the trachea; and in the lung, 51 +/- 11 mm Hg (chitosan hydrogel), 62 +/- 4 mm Hg (fibrin glue, rubbing method), and 12 +/- 2 mm Hg (fibrin glue, layer method). The sealing ability of the chitosan hydrogel was stronger than that of fibrin glue. All rabbits with a carotid artery (n = 8) or lung (n = 8) that was punctured with a needle and then sealed with chitosan hydrogel survived the 1-month observation period without any bleeding or air leakage from the puncture sites. Histologic examinations demonstrated that 30 days after application, a fraction of the chitosan hydrogel was phagocytosed by macrophages, had partially degraded, and had induced the formation of fibrous tissues around the hydrogel. A newly developed photocrosslinkable chitosan has demonstrated strong sealing ability and a great potential for use as an adhesive in surgical operations.

Development of silver/titanium dioxide/chitosan adipate nanocomposite as an antibacterial coating for fruit storage

Science.gov (United States)

A novel nanocomposite of silver/titanium dioxide/chitosan adipate (Ag/TiO2/CS) was developed through photochemical reduction using a chitosan adipate template. Chitosan served as a reducing agent for the metal ions, and anchored metal ions by forming Ag–N coordination bonds and electrostatic attract...

Rheological and structural studies of carboxymethyl derivatives of chitosan

Science.gov (United States)

Winstead, Cherese; Katagumpola, Pushpika

2014-05-01

The degrees of substitution of chitosan derivatives were varied and the viscoelastic behavior of these biopolymer solutions was studied using rheology. Chitosan is a cationic copolymer of glucosamine and N-acetylglucosamine obtained by alkaline deacetylation of chitin. Due to its inherent non-toxicity, biocompatibility, and biodegradability, chitosan has gained much interest. However, the poor solubility of the biopolymer in water and most common organic solvents limits its applications. Therefore, the focus of this work is the chemical modification of chitosan via carboxymethylation as well as studying the viscoelastic behavior of these polymer solutions. Varying degrees of substitution (DS) of carboxymethyl chitosan derivatives were synthesized by treating chitosan with monochloroacetic acid under alkylated medium varying the reaction time and temperature. The effect of degree of substitution on the rheology of these polymer solutions was studied as a function of concentration. The viscosity of chitosan derivatives sharply increased with increase in degree of substitution. G' and G" dependence on strain and angular frequency were studied and were found to exhibit predominantly viscous behavior. Additional characterization of the derivatized products were further studied using Fourier transform infrared (FT-IR), 1H Nuclear Magnetic Resonance (1H NMR) spectroscopy, X-ray diffraction (XRD), and thermal gravimetric analysis as well as differential scanning calorimetry (DSC). Degree of substitution (DS) was calculated by titrimetric method.

Rheological and structural studies of carboxymethyl derivatives of chitosan

International Nuclear Information System (INIS)

Winstead, Cherese; Katagumpola, Pushpika

2014-01-01

The degrees of substitution of chitosan derivatives were varied and the viscoelastic behavior of these biopolymer solutions was studied using rheology. Chitosan is a cationic copolymer of glucosamine and N-acetylglucosamine obtained by alkaline deacetylation of chitin. Due to its inherent non-toxicity, biocompatibility, and biodegradability, chitosan has gained much interest. However, the poor solubility of the biopolymer in water and most common organic solvents limits its applications. Therefore, the focus of this work is the chemical modification of chitosan via carboxymethylation as well as studying the viscoelastic behavior of these polymer solutions. Varying degrees of substitution (DS) of carboxymethyl chitosan derivatives were synthesized by treating chitosan with monochloroacetic acid under alkylated medium varying the reaction time and temperature. The effect of degree of substitution on the rheology of these polymer solutions was studied as a function of concentration. The viscosity of chitosan derivatives sharply increased with increase in degree of substitution. G' and G' dependence on strain and angular frequency were studied and were found to exhibit predominantly viscous behavior. Additional characterization of the derivatized products were further studied using Fourier transform infrared (FT-IR), 1 H Nuclear Magnetic Resonance ( 1 H NMR) spectroscopy, X-ray diffraction (XRD), and thermal gravimetric analysis as well as differential scanning calorimetry (DSC). Degree of substitution (DS) was calculated by titrimetric method

Trichloro(1,4,7-trimethyl-1,4,7-triazacyclononane)chromium(III)

DEFF Research Database (Denmark)

Klitgaard, Søren Kegnaes; Schau-Magnussen, Magnus

2005-01-01

The 1,4,7-trimethyl-1,4,7-triazacyclononane (tmtacn) ligand has become one of the classic ligands in coordination chemistry (Wieghardt et al., 1982 [Wieghardt, K., Chaudhuri, P., Nuber, B. & Weiss, J. (1982). Inorg. Chem. 21, 3086-3090.] ). In recent years, tmtacn-metal complexes ...

Irradiation gamma on chitosan films

Energy Technology Data Exchange (ETDEWEB)

Mello, Luana Miranda Lopes de; Souza, Adriana Regia Marques de; Arthur, Valter, E-mail: lumilopes@hotmail.com, E-mail: drilavras@yahoo.com.br, E-mail: arthur@cena.usp.br [Universidade Federal do Tocantins (UFT), Palmas,TO (Brazil). Departmento de Ciencia e Tecnologia de Alimentos; Universidade Federal de Goias (UFGO), Goiania (Brazil). Departmento de Ciencia e Tecnologia de Alimentos; Centro de Energia Nuclear na Agricultura (CENA/USP), Piracicaba, SP (Brazil)

2017-11-01

Films are preformed structures, independent, that are used to wrap food after processing, increasing their shelf life and enhancing its bright and attractive appearance. They are prepared from biological materials as an alternative to the plastic synthetic containers to improve the quality of the environment. Chitosan is a biodegradable polymer composed of β-(1-4) linked D-glucosamine (deacetylated unit) and N-acetyl-D- glucosamine (acetylated unit). It is produced commercially by deacetylation of chitin, which is a structural component of the exoskeleton of crustaceans. She is able to form films and edible and/or biodegradable coatings. With the objective to evaluate the effect of different doses of gamma radiation (0, 5, 10 and 15 kGy) and chitosan concentrations (1 and 2%) in film properties, it was evaluated its optical, mechanical and morphological properties. The films were produced by casting. Irradiation did not affect the thickness of the films, but influenced its colors, increasing the tone of the film for a stronger yellowish color. This fact can be attributed to the increased concentration of C = O bonds of chitosan due to the breakdown of the chain reaction and the Maillard reaction. Irradiated films showed smoother surface and less rough, due to the degradation of the chitosan molecule and poor mechanical properties, not showing good flexibility and stretching. (author)

Irradiation gamma on chitosan films

International Nuclear Information System (INIS)

Mello, Luana Miranda Lopes de; Souza, Adriana Regia Marques de; Arthur, Valter

2017-01-01

Films are preformed structures, independent, that are used to wrap food after processing, increasing their shelf life and enhancing its bright and attractive appearance. They are prepared from biological materials as an alternative to the plastic synthetic containers to improve the quality of the environment. Chitosan is a biodegradable polymer composed of β-(1-4) linked D-glucosamine (deacetylated unit) and N-acetyl-D- glucosamine (acetylated unit). It is produced commercially by deacetylation of chitin, which is a structural component of the exoskeleton of crustaceans. She is able to form films and edible and/or biodegradable coatings. With the objective to evaluate the effect of different doses of gamma radiation (0, 5, 10 and 15 kGy) and chitosan concentrations (1 and 2%) in film properties, it was evaluated its optical, mechanical and morphological properties. The films were produced by casting. Irradiation did not affect the thickness of the films, but influenced its colors, increasing the tone of the film for a stronger yellowish color. This fact can be attributed to the increased concentration of C = O bonds of chitosan due to the breakdown of the chain reaction and the Maillard reaction. Irradiated films showed smoother surface and less rough, due to the degradation of the chitosan molecule and poor mechanical properties, not showing good flexibility and stretching. (author)

SU-8 doped and encapsulated n-type graphene nanomesh with high air stability

Energy Technology Data Exchange (ETDEWEB)

Al-Mumen, Haider [Department of Electrical and Computer Engineering, Michigan State University, East Lansing, Michigan 48824 (United States); Department of Electrical Engineering, University of Babylon, Babylon (Iraq); Dong, Lixin; Li, Wen, E-mail: wenli@egr.msu.edu [Department of Electrical and Computer Engineering, Michigan State University, East Lansing, Michigan 48824 (United States)

2013-12-02

N-type doping of graphene with long-term chemical stability in air represents a significant challenge for practical application of graphene electronics. This paper reports a reversible doping method to achieve highly stable n-type graphene nanomeshes, in which the SU-8 photoresist simultaneously serves as an effective electron dopant and an excellent encapsulating layer. The chemically stable n-type characteristics of the SU-8 doped graphene were evaluated in air using their Raman spectra, electrical transport properties, and electronic band structures. The SU-8 doping does minimum damage to the hexagonal carbon lattice of graphene and is completely reversible by removing the uncrosslinked SU-8 resist.

Suitability of Different Food Grade Materials for the Encapsulation of Some Functional Foods Well Reported for Their Advantages and Susceptibility.

Science.gov (United States)

Wani, Touseef Ahmed; Shah, Adil Gani; Wani, Sajad Mohd; Wani, Idrees Ahmed; Masoodi, Farooq Ahmad; Nissar, Nazia; Shagoo, Mudasir Ahmad

2016-11-17

Functional foods find a very important place in the modern era, where different types of cancer, diabetes, cardiovascular diseases, etc. are on a high. Irrespective of the abundance of bioactive components in different fruits and vegetables, their low solubility in aqueous solution, vulnerability to destruction in different environmental and gastrointestinal conditions and a low intestinal absorption becomes a concern. Because it is quite difficult to commercialize non food materials for the food encapsulation purposes due to their safety concerns in the human body, scientists in the recent times have come up with the idea of encapsulating the different bioactive components in different food grade materials that are able to safeguard these bioactive components against the different environmental and gastrointestinal conditions and ensure their safe and targeted delivery at their absorption sites. Different food grade encapsulation materials including various oligosaccharides, polysaccharides (starch, cyclodextrins, alginates, chitosan, gum arabic, and carboxymethyl cellulose) and proteins and their suitability for encapsulating various bioactive components like flavonoids (catechins, rutin, curcumin, hesperetin, and vanillin), nonflavonoids (resveratrol), carotenoids (β-carotene, lycopene, and lutein), and fatty acids (fish oil, flaxseed oil, and olive oil) of high medical and nutritional value are reviewed here.

Evaluation of Hemagglutination Activity of Chitosan Nanoparticles Using Human Erythrocytes

Directory of Open Access Journals (Sweden)

Jefferson Muniz de Lima

2015-01-01

Full Text Available Chitosan is a polysaccharide composed of randomly distributed chains of β-(1-4 D-glucosamine and N-acetyl-D-glucosamine. This compound is obtained by partial or total deacetylation of chitin in acidic solution. The chitosan-based hemostatic agents have been gaining much attention in the management of bleeding. The aim of this study was to evaluate in vitro hemagglutination activity of chitosan nanoparticles using human erythrocytes. The preparation of nanoparticles was achieved by ionotropic gelification technique followed by neutralization with NaOH 1 mol/L−1. The hemagglutination activity was performed on a solution of 2% erythrocytes (pH 7.4 on PBS collected from five healthy volunteers. The hemolysis determination was made by spectrophotometric analysis. Chitosan nanoparticle solutions without NaOH addition changed the reddish colour of the wells into brown, suggesting an oxidative reaction of hemoglobin and possible cell lysis. All neutralized solutions of chitosan nanoparticles presented positive haemagglutination, without any change in reaction color. Chitosan nanoparticles presented hemolytic activity ranging from 186.20 to 223.12%, while neutralized solutions ranged from 2.56 to 72.54%, comparing to distilled water. Results highlight the need for development of new routes of synthesis of chitosan nanoparticles within human physiologic pH.

Influence of Chitosan Treatment on Surrogate Serum Markers of Cholesterol Metabolism in Obese Subjects

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Dieter Lütjohann

2018-01-01

Full Text Available Chitosan treatment results in significantly lower serum low density lipoprotein (LDL cholesterol concentrations. To assess the working mechanisms of chitosan, we measured serum surrogate markers of cholesterol absorption (campesterol, sitosterol, cholestanol, synthesis (lathosterol, lanosterol, desmosterol, and degradation to bile acids (7α-hydroxy-cholesterol, 27-hydroxy-cholesterol, corrected for cholesterol concentration (R_sterols. Over 12 weeks, 116 obese subjects (Body Mass Index, BMI 31.7, range 28.1–38.9 kg/m2 were studied under chitosan (n = 61 and placebo treatments (n = 55. The participants were briefly educated regarding improvement of nutrition quality and energy expenditure. Daily chitosan intake was 3200 mg. Serum LDL cholesterol concentration decreased significantly more (p = 0.0252 under chitosan (−8.67 ± 18.18 mg/dL, 5.6% than under placebo treatment (−1.00 ± 24.22 mg/dL, 0.9%. This reduction was not associated with the expected greater decreases in markers of cholesterol absorption under chitosan treatment. Also, increases in markers of cholesterol synthesis and bile acid synthesis under chitosan treatment were not any greater than under placebo treatment. In conclusion, a significant selective reduction of serum LDL cholesterol under chitosan treatment is neither associated with a reduction of serum surrogate markers of cholesterol absorption, nor with increases of markers for cholesterol and bile acid synthesis.

Influence of chitosan concentration on mechanical and barrier properties of corn starch/chitosan films.

Science.gov (United States)

Ren, Lili; Yan, Xiaoxia; Zhou, Jiang; Tong, Jin; Su, Xingguang

2017-12-01

The active packaging films based on corn starch and chitosan were prepared through mixing the starch solution and the chitosan solution (1:1) by casting. The aim of this work was to characterize and analyze the effects of the chitosan concentrations (0, 21, 41, 61 and 81wt% of starch) on physicochemical, mechanical and water vapor barrier properties as well as morphological characteristics of the corn starch/chitosan (CS/CH) films. Starch molecules and chitosan could interact through hydrogen bonding as confirmed from the shift of the main peaks to higher wavenumbers in FTIR and the reduction of crystallinity in XRD. Results showed that the incorporation of chitosan resulted in an increase in film solubility, total color differences, tensile strength and elongation at break and a decrease in Young's modulus and water vapor permeability (WVP). Elongation at break of the CS/CH films increased with increasing of chitosan concentration, and reached a maximum at 41 wt%, then declined at higher chitosan concentration. The WVP of CS/CH films increased with an increase of chitosan concentration and the same tendency observed for the moisture content. The results suggest that this biodegradable CS/CH films could potentially be used as active packaging films for food and pharmaceutical applications. Copyright © 2017 Elsevier B.V. All rights reserved.

Immunization with Recombinant TcdB-Encapsulated Nanocomplex Induces Protection against Clostridium difficile Challenge in a Mouse Model

Directory of Open Access Journals (Sweden)

Yi-Wen Liu

2017-07-01

Full Text Available Clostridium difficile is considered to be one of the major cause of infectious diarrhea in healthcare systems worldwide. Symptoms of C. difficile infection are caused largely by the production of two cytotoxins: toxin A (TcdA and toxin B (TcdB. Vaccine development is considered desirable as it would decrease the mounting medical costs and mortality associated with C. difficile infections. Biodegradable nanoparticles composed of poly-γ-glutamic acid (γ-PGA and chitosan have proven to be a safe and effective antigen delivery system for many viral vaccines. However, few studies have used this efficient antigen carrier for bacterial vaccine development. In this study, we eliminated the toxin activity domain of toxin B by constructing a recombinant protein rTcdB consists of residues 1852-2363 of TcdB receptor binding domain. The rTcdB was encapsulated in nanoparticles composed of γ-PGA and chitosan. Three rounds of intraperitoneal vaccination led to high anti-TcdB antibody responses and afforded mice full protection mice from lethal dose of C. difficile spore challenge. Protection was associated with high levels of toxin-neutralizing antibodies, and the rTcdB-encapsulated NPs elicited a longer-lasting antibody titers than antigen with the conventional adjuvant, aluminum hydroxide. Significant reductions in the level of proinflammatory cytokines and chemokines were observed in vaccinated mouse. These results suggested that polymeric nanocomplex-based vaccine design can be useful in developing vaccine against C. difficile infections.

Coupling Deep Transcriptome Analysis with Untargeted Metabolic Profiling in Ophiorrhiza pumila to Further the Understanding of the Biosynthesis of the Anti-Cancer Alkaloid Camptothecin and Anthraquinones

Science.gov (United States)

Yamazaki, Mami; Mochida, Keiichi; Asano, Takashi; Nakabayashi, Ryo; Chiba, Motoaki; Udomson, Nirin; Yamazaki, Yasuyo; Goodenowe, Dayan B.; Sankawa, Ushio; Yoshida, Takuhiro; Toyoda, Atsushi; Totoki, Yasushi; Sakaki, Yoshiyuki; Góngora-Castillo, Elsa; Buell, C. Robin; Sakurai, Tetsuya; Saito, Kazuki

2013-01-01

The Rubiaceae species, Ophiorrhiza pumila, accumulates camptothecin, an anti-cancer alkaloid with a potent DNA topoisomerase I inhibitory activity, as well as anthraquinones that are derived from the combination of the isochorismate and hemiterpenoid pathways. The biosynthesis of these secondary products is active in O. pumila hairy roots yet very low in cell suspension culture. Deep transcriptome analysis was conducted in O. pumila hairy roots and cell suspension cultures using the Illumina platform, yielding a total of 2 Gb of sequence for each sample. We generated a hybrid transcriptome assembly of O. pumila using the Illumina-derived short read sequences and conventional Sanger-derived expressed sequence tag clones derived from a full-length cDNA library constructed using RNA from hairy roots. Among 35,608 non-redundant unigenes, 3,649 were preferentially expressed in hairy roots compared with cell suspension culture. Candidate genes involved in the biosynthetic pathway for the monoterpenoid indole alkaloid camptothecin were identified; specifically, genes involved in post-strictosamide biosynthetic events and genes involved in the biosynthesis of anthraquinones and chlorogenic acid. Untargeted metabolomic analysis by Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR-MS) indicated that most of the proposed intermediates in the camptothecin biosynthetic pathway accumulated in hairy roots in a preferential manner compared with cell suspension culture. In addition, a number of anthraquinones and chlorogenic acid preferentially accumulated in hairy roots compared with cell suspension culture. These results suggest that deep transcriptome and metabolome data sets can facilitate the identification of genes and intermediates involved in the biosynthesis of secondary products including camptothecin in O. pumila. PMID:23503598

Model for the mechanism and regulation of chitosan synthesis in Mucor rouxii

International Nuclear Information System (INIS)

Davis, L.L.; Bartnicki-Garcia, S.

1984-01-01

The cell walls of mucoraceous fungi are characterized by the joint occurrence of chitosan and chitin, the β-1,4-linked polysaccharides of G1cN and G1cNAc, respectively. It has been proposed that chitosan is made from chitin by enzymatic deacetylation, but the evidence is inconclusive since the deacetylase isolated from Mucor rouxii is effective against glycol chitin, but not against genuine chitin; consequently, chitosan synthesis in vitro was not achieved. The authors discovered that the same deacetylase can deacetylate chitin efficiently if it is allowed to act on chitin chains as they are being formed; i.e. the simultaneous presence and operation of chitin synthetase and chitin deacetylase is required for chitosan synthesis. Subsequent studies on the effect of digitonin on chitosan synthesis were the basis for a model the authors have developed for the regulation of chitosan and chitin syntheses in vivo

Scanning electron microscopy and swelling test of shrimp shell chitosan and chitosan-RGD scaffolds

Science.gov (United States)

Mandacan, M. C.; Yuniastuti, M.; Amir, L. R.; Idrus, E.; Suniarti, D. F.

2017-08-01

Shrimp shell chitosan and chitosan-RGD scaffold membranes are produced to be biocompatible with tissue engineering. Nonetheless, their architectural properties have not yet been studied. Analyze the architectural properties of chitosan and chitosan-RGD scaffolds. Analyze pore count and size, interpore distance, and porosity (using SEM testing and ImageJ analysis) and water absorption (using a swelling test). The properties of the chitosan and chitosan-RGD scaffolds were as follows, respectively. The pore counts were 225 and 153; pore size, 171.4 μam and 180.2 μam interpore distance, 105.7 μam and 101.4 μam porosity, 22% and 10.2%; and water absorption, 9.1 mgH2O/mgScaffold and 19.3 mgH2O/mgScaffold. The shrimp shell chitosan-RGD membrane scaffold was found to have architectural properties that make it more conducive to use in tissue engineering.

Transfection efficiency of chitosan and thiolated chitosan in retinal pigment epithelium cells: A comparative study

Directory of Open Access Journals (Sweden)

Ana V Oliveira

2013-01-01

Full Text Available Objective: Gene therapy relies on efficient vector for a therapeutic effect. Efficient non-viral vectors are sought as an alternative to viral vectors. Chitosan, a cationic polymer, has been studied for its gene delivery potential. In this work, disulfide bond containing groups were covalently added to chitosan to improve the transfection efficiency. These bonds can be cleaved by cytoplasmic glutathione, thus, releasing the DNA load more efficiently. Materials and Methods: Chitosan and thiolated chitosan nanoparticles (NPs were prepared in order to obtain a NH3 + :PO4− ratio of 5:1 and characterized for plasmid DNA complexation and release efficiency. Cytotoxicity and gene delivery studies were carried out on retinal pigment epithelial cells. Results: In this work, we show that chitosan was effectively modified to incorporate a disulfide bond. The transfection efficiency of chitosan and thiolated chitosan varied according to the cell line used, however, thiolation did not seem to significantly improve transfection efficiency. Conclusion: The apparent lack of improvement in transfection efficiency of the thiolated chitosan NPs is most likely due to its size increase and charge inversion relatively to chitosan. Therefore, for retinal cells, thiolated chitosan does not seem to constitute an efficient strategy for gene delivery.

Effect of layer-by-layer polyelectrolyte method on encapsulation of vanillin.

Science.gov (United States)

Noshad, Mohammad; Mohebbi, Mohebbat; Shahidi, Fakhri; Koocheki, Arash

2015-11-01

The objective of this work was to microencapsulate vanillin by multilayer emulsion followed by spray drying, aiming to protect it and control its release. An electrostatic layer-by-layer deposition method was used to create the multilayered interfacial membranes around microcapsules with different compositions: (i) one-layer (soy protein isolate); (ii) two-layer (soy protein isolate - OSA starch); (iii) three-layer (soy protein isolate - OSA starch - Chitosan). The morphology of the microcapsules was analyzed by scanning electronic microscopy. The hygroscopicity, solubility, particle size, encapsulation efficiency, Fourier transform infrared spectroscopy and release into water (37°C and 80°C) were also examined. FTIR confirmed the interaction between the wall materials. All microcapsules were not very water-soluble or hygroscopic while three-layer microcapsules compared to one and two layer microcapsules have lower moisture content and predominantly shriveled surfaces. The results indicated it was possible to encapsulate vanillin with the techniques employed and that these protected the vanillin even at 80°C. The reduced solubility and low release rates indicated the enormous potential of the vehicle developed in controlling the release of the vanillin into the food and pharmaceuticals. Copyright © 2015 Elsevier B.V. All rights reserved.

Cobalt-boron amorphous alloy prepared in water/cetyl-trimethyl-ammonium bromide/n-hexanol microemulsion as anode for alkaline secondary batteries

International Nuclear Information System (INIS)

Tong, D.G.; Wang, D.; Chu, W.; Sun, J.H.; Wu, P.

2010-01-01

Amorphous cobalt-boron (Co-B) with uniform nanoparticles was prepared for the first time via reduction of cobalt acetate by potassium borohydride in the water/cetyl-trimethyl-ammonium bromide/n-hexanol microemulsion system. The sample was characterized by X-ray diffraction, transmission electron microscopy, nitrogen adsorption-desorption, X-ray photoelectron spectroscopy, inductively coupled plasma, cyclic voltammetry, differential scanning calorimetry, temperature-programmed desorption, scanning electron microscopy, charge-discharge test and electrochemical impedance spectra. The results demonstrate that electrochemical activity of the as-synthesized Co-B was higher than that of the regular Co-B prepared in aqueous solution. It indicates that the homogeneous distribution and large specific surface area helped the electrochemical hydrogen storage of the as-synthesized Co-B. Furthermore, the as-synthesized Co-B even had 347 mAh g -1 after 50 cycles, while the regular Co-B prepared in aqueous solution only had 254 mAh g -1 after 30 cycles at a current of 100 mA g -1 . The better cycling performance can be ascribed to its smaller interfacial impedance between electrode and electrolyte.

Kaempferol loaded lecithin/chitosan nanoparticles: preparation, characterization, and their potential applications as a sustainable antifungal agent.

Science.gov (United States)

Ilk, Sedef; Saglam, Necdet; Özgen, Mustafa

2017-08-01

Flavonoid compounds are strong antioxidant and antifungal agents but their applications are limited due to their poor dissolution and bioavailability. The use of nanotechnology in agriculture has received increasing attention, with the development of new formulations containing active compounds. In this study, kaempferol (KAE) was loaded into lecithin/chitosan nanoparticles (LC NPs) to determine antifungal activity compared to pure KAE against the phytopathogenic fungus Fusarium oxysporium to resolve the bioavailability problem. The influence of formulation parameters on the physicochemical properties of KAE loaded lecithin chitosan nanoparticles (KAE-LC NPs) were studied by using the electrostatic self-assembly technique. KAE-LC NPs were characterized in terms of physicochemical properties. KAE has been successfully encapsulated in LC NPs with an efficiency of 93.8 ± 4.28% and KAE-LC NPs showed good physicochemical stability. Moreover, in vitro evaluation of the KAE-LC NP system was made by the release kinetics, antioxidant and antifungal activity in a time-dependent manner against free KAE. Encapsulated KAE exhibited a significantly inhibition efficacy (67%) against Fusarium oxysporium at the end of the 60 day storage period. The results indicated that KAE-LC NP formulation could solve the problems related to the solubility and loss of KAE during use and storage. The new nanoparticle system enables the use of smaller quantities of fungicide and therefore, offers a more environmentally friendly method of controlling fungal pathogens in agriculture.

Development of Poly(lactic acid)/Chitosan Fibers Loaded with Essential Oil for Antimicrobial Applications

Science.gov (United States)

Liu, Yaowen; Wang, Shuyao; Zhang, Rong; Lan, Wenting; Qin, Wen

2017-01-01

Cinnamon essential oil (CEO) was successfully encapsulated into chitosan (CS) nanoparticles at different loading amounts (1%, 1.5%, 2%, and 2.5% v/v) using oil-in-water (o/w) emulsion and ionic-gelation methods. In order to form active packaging, poly(lactic acid) (PLA) was used to fabricate PLA/CS-CEO composite fibers using a simple electrospinning method. The shape, size, zeta potential, and encapsulation efficacy of the CS-CEO nanoparticles were investigated. The composition, morphology, and release behavior of the composite fibers were investigated. PLA/CS-CEO-1.5 showed good stability and favorable sustained release of CEO, resulting in improved antimicrobial activity compared to the other blends. The PLA/CS-CEO fibers showed high long-term inactivation rates against Escherichia coli and Staphylococcus aureus due to the sustained release of CEO, indicating that the developed PLA/CS-CEO fibers have great potential for active food packaging applications. PMID:28737719

The dispersion of fine chitosan particles by beads-milling

Science.gov (United States)

Rochima, Emma; Utami, Safira; Hamdani, Herman; Azhary, Sundoro Yoga; Praseptiangga, Danar; Joni, I. Made; Panatarani, Camellia

2018-02-01

This research aimed to produce fine chitosan particles from a crab shell waste by beads-milling method by two different concentration of PEG as dispersing agent (150 and 300 wt. %). The characterization was performed to obtain the size and size distribution, the characteristics of functional groups and the degree of deacetylation. The results showed that the chitosan fine particles was obtained with a milling time 120 minutes with the best concentration of PEG 400 150 wt. %. The average particle size of the as-prepared suspension is 584 nm after addition of acetic acid solution (1%, v/v). Beads milling process did not change the glucosamine and N-acetylglucosamine content on chitosan structure which is indicated by degree of deacetylation higher than 70%. It was concluded that beads milling process can be applied to prepare chitosan fineparticles by proper adjustment in the milling time, pH and dosage of dispersing agent.

Thermoresponsive behavior of chitosan-g-N-isopropylacrylamide copolymer solutions.

Science.gov (United States)

Recillas, Maricarmen; Silva, Luisa L; Peniche, Carlos; Goycoolea, Francisco M; Rinaudo, Marguerite; Argüelles-Monal, Waldo M

2009-06-08

Chitosan-g-N-isopropylacrylamide (NIPAm) water-soluble copolymers were synthesized and characterized by FTIR and (1)H NMR spectroscopies combined with conductometric and potentiometric titrations. Their thermoresponsive, fully reversible, behavior in aqueous solutions was characterized by means of microcalorimetry and rheology. During heating of copolymer solutions there is a well-known endothermic effect, which coincides with a marked increase in G' and a moderate decrement in G'' due to the formation of a hydrophobic network at the expense of the net amount of sol fraction. It was also found that a straight dependence between the values of G' above the LCST and the enthalpies associated with the transition reflecting that the connectivity in the gel network is governed by the net number of formed enthalpic-hydrophobic driven-junctions. Both the LCST and the enthalpy change vary with the ionic strength of copolymer solutions, but no dependence was found with the neutralization of the polyelectrolyte chain.

Preparation and characterisation of irradiated crab chitosan and New Zealand Arrow squid pen chitosan

International Nuclear Information System (INIS)

Shavandi, Amin; Bekhit, Adnan A.; Bekhit, Alaa El-Din A.; Sun, Zhifa; Ali, M. Azam

2015-01-01

The properties of chitosan from Arrow squid (Nototodarus sloanii) pen (CHS) and commercial crab shell (CHC) were investigated using FTIR, DSC, SEM and XRD before and after irradiation at the dose of 28 kGy in the presence or absence of 5% water. Also, the viscosity, deacetylation degree, water and oil holding capacities, colour and antimicrobial activities of the chitosan samples were determined. Irradiation decreased (P < 0.05) the viscosity of CHC from 0.21 to 0.03 Pa s and of CHS from 1.71 to 0.23 Pa s. The inclusion of water had no effect on the viscosity of irradiated chitosan. Irradiation did not affect the degree of deacetylation of CHC, but increased the deacetylation degree of CHS from 72.78 to 82.29% in samples with 5% water. Water and oil holding capacities of CHS (1197.30% and 873.3%, respectively) were higher (P < 0.05) than those found in CHC (340.70% and 264.40%, respectively). The water and oil holding capacities were decreased for both types of chitosan irradiation, but were not affected by the addition of water. Squid pen chitosan was whiter in colour (White Index = 90.06%) compared to CHC (White Index = 83.70%). Generally, the CHC samples (control and irradiated) exhibited better antibacterial activity compared to CHS, but the opposite was observed with antifungal activity. - Highlights: • Chitosan prepared from Arrow squid pens (Nototodarus sloanii). • Chitosan samples were gamma irradiated at 28 kGy. • Squid pen chitosan showed high fat and water uptake capacities compared to crab shell chitosan. • Gamma irradiation enhanced the DDA of squid pen chitosan but not crab shell chitosan.

N-PEG´ylation of chitosan via "click chemistry" reactions

Czech Academy of Sciences Publication Activity Database

Kulbokaite, R.; Ciuta, G.; Netopilík, Miloš; Makuška, R.

2009-01-01

Roč. 69, č. 10 (2009), s. 771-778 ISSN 1381-5148 R&D Projects: GA ČR GA203/07/0659 Institutional research plan: CEZ:AV0Z40500505 Keywords : chitosan * poly(ethylene glycol) * click chemistry Subject RIV: CD - Macromolecular Chemistry Impact factor: 2.461, year: 2009

Two-Ply Composite Membranes with Separation Layers from Chitosan and Sulfoethylcellulose on a Microporous Support Based on Poly(diphenylsulfone-N-phenylphthalimide

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Svetlana V. Kononova

2017-12-01

Full Text Available Two-ply composite membranes with separation layers from chitosan and sulfoethylcellulose were developed on a microporous support based on poly(diphenylsulfone-N-phenylphthalimide and investigated by use of X-ray diffraction and scanning electron microscopy methods. The pervaporation properties of the membranes were studied for the separation of aqueous alcohol (ethanol, propan-2-ol mixtures of different compositions. When the mixtures to be separated consist of less than 15 wt % water in propan-2-ol, the membranes composed of polyelectrolytes with the same molar fraction of ionogenic groups (-NH3+ for chitosan and -SO3− for sulfoethylcellulose show high permselectivity (the water content in the permeate was 100%. Factors affecting the structure of a non-porous layer of the polyelectrolyte complex formed on the substrate surface and the contribution of that complex to changes in the transport properties of membranes are discussed. The results indicate significant prospects for the use of chitosan and sulfoethylcellulose for the formation of highly selective pervaporation membranes.

Multilayer encapsulated mesoporous silica nanospheres as an oral sustained drug delivery system for the poorly water-soluble drug felodipine

Energy Technology Data Exchange (ETDEWEB)

Hu, Liang [Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 32, Liaoning Province, Shenyang 110016 (China); Sun, Hongrui [English Teaching Department, School of Basic Courses, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016 (China); Zhao, Qinfu; Han, Ning; Bai, Ling; Wang, Ying; Jiang, Tongying [Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 32, Liaoning Province, Shenyang 110016 (China); Wang, Siling, E-mail: silingwang@syphu.edu.cn [Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 32, Liaoning Province, Shenyang 110016 (China)

2015-02-01

We used a combination of mesoporous silica nanospheres (MSN) and layer-by-layer (LBL) self-assembly technology to establish a new oral sustained drug delivery system for the poorly water-soluble drug felodipine. Firstly, the model drug was loaded into MSN, and then the loaded MSN were repeatedly encapsulated by chitosan (CHI) and acacia (ACA) via LBL self-assembly method. The structural features of the samples were studied using scanning electron microscopy (SEM), transmission electron microscopy (TEM) and nitrogen adsorption. The encapsulating process was monitored by zeta-potential and surface tension measurements. The physical state of the drug in the samples was characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). The influence of the multilayer with different number of layers on the drug release rate was studied using thermal gravimetric analysis (TGA) and surface tension measurement. The swelling effect and the structure changes of the multilayer were investigated to explore the relationship between the drug release behavior and the state of the multilayer under different pH conditions. The stability and mucosa adhesive ability of the prepared nanoparticles were also explored. After multilayer coating, the drug release rate was effectively controlled. The differences in drug release behavior under different pH conditions could be attributed to the different states of the multilayer. And the nanoparticles possessed good stability and strong mucosa adhesive ability. We believe that this combination offers a simple strategy for regulating the release rate of poorly water-soluble drugs and extends the pharmaceutical applications of inorganic materials and polymers. - Highlights: • A combination of inorganic and organic materials was applied. • Mesoporous silica nanospheres (MSN) were used as drug carriers. • Chitosan and acacia were encapsulated through layer-by-layer self-assembly. • The release rate of the poorly

Multilayer encapsulated mesoporous silica nanospheres as an oral sustained drug delivery system for the poorly water-soluble drug felodipine

International Nuclear Information System (INIS)

Hu, Liang; Sun, Hongrui; Zhao, Qinfu; Han, Ning; Bai, Ling; Wang, Ying; Jiang, Tongying; Wang, Siling

2015-01-01

We used a combination of mesoporous silica nanospheres (MSN) and layer-by-layer (LBL) self-assembly technology to establish a new oral sustained drug delivery system for the poorly water-soluble drug felodipine. Firstly, the model drug was loaded into MSN, and then the loaded MSN were repeatedly encapsulated by chitosan (CHI) and acacia (ACA) via LBL self-assembly method. The structural features of the samples were studied using scanning electron microscopy (SEM), transmission electron microscopy (TEM) and nitrogen adsorption. The encapsulating process was monitored by zeta-potential and surface tension measurements. The physical state of the drug in the samples was characterized by differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). The influence of the multilayer with different number of layers on the drug release rate was studied using thermal gravimetric analysis (TGA) and surface tension measurement. The swelling effect and the structure changes of the multilayer were investigated to explore the relationship between the drug release behavior and the state of the multilayer under different pH conditions. The stability and mucosa adhesive ability of the prepared nanoparticles were also explored. After multilayer coating, the drug release rate was effectively controlled. The differences in drug release behavior under different pH conditions could be attributed to the different states of the multilayer. And the nanoparticles possessed good stability and strong mucosa adhesive ability. We believe that this combination offers a simple strategy for regulating the release rate of poorly water-soluble drugs and extends the pharmaceutical applications of inorganic materials and polymers. - Highlights: • A combination of inorganic and organic materials was applied. • Mesoporous silica nanospheres (MSN) were used as drug carriers. • Chitosan and acacia were encapsulated through layer-by-layer self-assembly. • The release rate of the poorly

MLL2 conveys transcription-independent H3K4 trimethylation in oocytes

Czech Academy of Sciences Publication Activity Database

Hanna, C. W.; Taudt, A.; Huang, J.; Gahurová, Lenka; Kranz, A.; Andrews, S.; Dean, W.; Francis Stewart, A.; Colomé-Tatché, M.; Kelsey, G.

2018-01-01

Roč. 25, č. 1 (2018), s. 73-82 ISSN 1545-9993 Institutional support: RVO:67985904 Keywords : H3K4 trimethylation Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Biochemistry and molecular biology Impact factor: 12.595, year: 2016

Development of Novel Protocol for Preclinical Monitoring the Release of Adjuvants Encapsulated Mucosal Delivery Carriers

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Mohamed Ibrahim-Saeed

2015-12-01

Full Text Available This work contributes in vaccines down-stream process by introducing a novel platform for in-vitro monitoring of vaccine-adjuvant delivery profile as a crucial preclinical optimizing step in mucosal vaccines. Nano and micro particles of Calcium phosphate (Cap vaccine-adjuvant were encapsulated in Chitosan and Alginate polymeric carriers. Adjuvants release profiles monitored in a permeable bag at 37°C, pH 2, incubated in isotonic buffer for 96 hours. The released Calcium in the outer buffer was monitored and compared in-addition to the carrier’s swelling and biophysical properties. The adjuvants and carriers did not interfere with the proliferation of cultured hepatocytes an indicator of their safe use; Chitosan’s viscosity and swelling were higher than Alginate. Chitosan’s Zeta-potential was significantly high positive, while Cap and Alginate were negative. The prepared CaP and Chitosan particles were in nano-size, while the ready-made CaP adjuvant and Alginate were in micro-size using zeta-seizer and scanning electron-micrograph. The release of nano-size particle was in ascending, extended and controlled manner compared to micro-size adjuvant. Moreover, nano-adjuvant release profile from Chitosan was superior compared to Alginate. The core controlling factors in vaccine-adjuvant sustained release includes; smaller adjuvant particles (nano-size, carrier’s low swelling, high viscosity and importantly carrier-adjuvant entrapment reversibility. Chitosan offers sustained ascending superior capacity in releasing Nano-Cap adjuvant. This novel in-vitro pre-clinical study answer a crucial downstream preparative step for optimizing mucosal vaccines before their direct routine in-vivo trial on animal regardless of adjuvant’s particle size or delivery kinetics.

Ni0 encapsulated in N-doped carbon nanotubes for catalytic reduction of highly toxic hexavalent chromium

Science.gov (United States)

Yao, Yunjin; Zhang, Jie; Chen, Hao; Yu, Maojing; Gao, Mengxue; Hu, Yi; Wang, Shaobin

2018-05-01

N-doped carbon nanotubes encapsulating Ni0 nanoparticles (Ni@N-C) were fabricated via thermal reduction of dicyandiamide and NiCl2·6H2O, and used to remove CrVI in polluted water. The resultant products present an excellent catalytic activity for CrVI reduction using formic acid under relatively mild conditions. The CrVI reduction efficiency of Ni@N-C was significantly affected by the preparation conditions including the mass of nickel salt and synthesis temperatures. The impacts of several reaction parameters, such as initial concentrations of CrVI and formic acid, solution pH and temperatures, as well as inorganic anions in solution on CrVI reduction efficiency were also evaluated in view of scalable industrial applications. Owing to the synergistic effects amongst tubes-coated Ni0, doped nitrogen, oxygen containing groups, and the configuration of carbon nanotubes, Ni@N-C catalysts exhibit excellent catalytic activity and recyclable capability for CrVI reduction. Carbon shell can efficiently protect inner Ni0 core and N species from corrosion and subsequent leaching, while Ni0 endows the Ni@N-C catalysts with ferromagnetism, so that the composites can be easily separated via a permanent magnet. This study opens up an avenue for design of N-doped carbon nanotubes encapsulating Ni0 nanoparticles with high CrVI removal efficiency and magnetic recyclability as low-cost catalysts for industrial applications.

Hybrid Nanostructures Containing Sulfadiazine Modified Chitosan as Antimicrobial Drug Carriers

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Bogdanel Silvestru Munteanu

2016-11-01

Full Text Available Chitosan (CH nanofibrous structures containing sulfadiazine (SDZ or sulfadiazine modified chitosan (SCH in the form of functional nanoparticles attached to nanofibers (hybrid nanostructures were obtained by mono-axial and coaxial electrospinning. The mono-axial design consisted of a SDZ/CH mixture solution fed through a single nozzle while the coaxial design consisted of SCH and CH solutions separately supplied to the inner and outer nozzle (or in reverse order. The CH ability to form nanofibers assured the formation of a nanofiber mesh, while SDZ and SCH, both in form of suspensions in the electrospun solution, assured the formation of active nanoparticles which remained attached to the CH nanofiber mesh after the electrospinning process. The obtained nanostructures were morphologically characterized by scanning electron microscopy (SEM and atomic force microscopy (AFM. The SDZ release profiles and kinetics were analyzed. The SDZ or SCH nanoparticles loosely attached at the surface of the nanofibers, provide a burst release in the first 20 min, which is important to stop the possible initial infection in a wound, while the SDZ and SCH from the nanoparticles which are better confined (or even encapsulated into the CH nanofibers would be slowly released with the erosion/disruption of the CH nanofiber mesh.

Gelatin/chitosan biofilm: preparation and characterization

International Nuclear Information System (INIS)

Trindade, Luciane da C.; Nunes, Raquel A.; Diniz, Nadie K.S.; Braga, Carla R.C.; Silva, Suedina M. de Lima

2011-01-01

In this study, gelatin, chitosan and gelatin/chitosan bio films using the ratio of gelatin/chitosan (50/50) were prepared by casting method. The bio films prepared were characterized by X-ray diffraction, scanning electron microscopy and dissolution ratio. According to the results, the incorporation of chitosan into gelatin indicate the decrease of crystallinity of chitosan, a compact structure without large pores and that the dissolution of gelatin/chitosan film is little influenced by hot water than gelatin films. (author)

Fabrication of chitosan microparticles loaded in chitosan and poly

Indian Academy of Sciences (India)

In recent decades, the use of microparticle-mediated drug delivery is widely applied in the field of biomedicalapplication. Here, we report the new dressing material with ciprofloxacin-loaded chitosan microparticle (CMP) impregnatedin chitosan (CH) and poly(vinyl alcohol) (PVA) scaffold for effective delivery of drug in a ...

Non-isothermal kinetics of thermal degradation of chitosan

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Georgieva Velyana

2012-08-01

Full Text Available Abstract Background Chitosan is the second most abundant nitrogen containing biopolymer in nature, obtained from the shells of crustaceans, particularly crabs, shrimp and lobsters, which are waste products of seafood processing industries. It has great potential application in the areas of biotechnology, biomedicine, food industries, and cosmetics. Chitosan is also capable of adsorbing a number of metal ions as its amino groups can serve as chelation sites. Grafted functional groups such as hydroxyl, carboxyl, sulfate, phosphate, and amino groups on the chitosan have been reported to be responsible for metal binding and sorption of dyes and pigments. The knowledge of their thermal stability and pyrolysis may help to better understand and plan their industrial processing. Results Thermogravimetric studies of chitosan in air atmosphere were carried out at six rates of linear increasing of the temperature. The kinetics and mechanism of the thermal decomposition reaction were evaluated from the TG data using recommended from ICTAC kinetics committee iso-conversional calculation procedure of Kissinger-Akahira-Sunose, as well as 27 mechanism functions. The comparison of the obtained results showed that they strongly depend on the selection of proper mechanism function for the process. Therefore, it is very important to determine the most probable mechanism function. In this respect the iso-conversional calculation procedure turned out to be the most appropriate. Conclusion Chitosan have excellent properties such as hydrophilicity, biocompatibility, biodegradability, antibacterial, non-toxicity, adsorption application. The thermal degradation of chitosan occurs in two stages. The most probable mechanism function for both stages is determined and it was best described by kinetic equations of n-th order (Fn mechanism. For the first stage, it was established that n is equal to 3.0 and for the second stage – to 1.0 respectively. The values of the

Development of coated liposomes loaded with ghrelin for nose-to-brain delivery for the treatment of cachexia.

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Salade, Laurent; Wauthoz, Nathalie; Deleu, Magali; Vermeersch, Marjorie; De Vriese, Carine; Amighi, Karim; Goole, Jonathan

2017-01-01

The aim of the present study was to develop a ghrelin-containing formulation based on liposomes coated with chitosan intended for nose-brain delivery for the treatment of cachexia. Among the three types of liposomes developed, anionic liposomes provided the best results in terms of encapsulation efficiency (56%) and enzymatic protection against trypsin (20.6% vs 0% for ghrelin alone) and carboxylesterase (81.6% vs 17.2% for ghrelin alone). Ghrelin presented both electrostatic and hydrophobic interactions with the anionic lipid bilayer, as demonstrated by isothermal titration calorimetry. Then, anionic liposomes were coated with N -(2-hydroxy) propyl-3-trimethyl ammonium chitosan chloride. The coating involved a size increment from 146.9±2.7 to 194±6.1 nm, for uncoated and coated liposomes, respectively. The ζ-potential was similarly increased from -0.3±1.2 mV to 6±0.4 mV before and after coating, respectively. Chitosan provided mucoadhesion, with an increase in mucin adsorption of 22.9%. Enhancement of permeation through the Calu3 epithelial monolayer was also observed with 10.8% of ghrelin recovered in the basal compartment in comparison to 0% for ghrelin alone. Finally, aerosols generated from two nasal devices (VP3 and SP270) intended for aqueous dispersion were characterized with either coated or uncoated liposomes. Contrarily to the SP270 device, VP3 device showed minor changes between coated and uncoated liposome aerosols, as shown by their median volume diameters of 38.4±5.76 and 37.6±5.74 µm, respectively. Overall, the results obtained in this study show that the developed formulation delivered by the VP3 device can be considered as a potential candidate for nose-brain delivery of ghrelin.

Electrical evaluation of crack generation in SiN{sub x} and SiO{sub x}N{sub y} thin-film encapsulation layers for OLED displays

Energy Technology Data Exchange (ETDEWEB)

Park, Eun Kil [Department of Materials Science and Engineering, Seoul National University, Seoul 151-744 (Korea, Republic of); Display Research Center, Samsung Display Co., Ltd., Yongin-City, Gyeonggi-Do 446-711 (Korea, Republic of); Kim, Sungmin [Department of Materials Science and Engineering, Seoul National University, Seoul 151-744 (Korea, Republic of); Heo, Jaeyeong, E-mail: jheo@jnu.ac.kr [Department of Materials Science and Engineering, and the Optoelectronics Convergence Research Center, Chonnam National University, Gwangju 500-757 (Korea, Republic of); Kim, Hyeong Joon, E-mail: thinfilm@snu.ac.kr [Department of Materials Science and Engineering, Seoul National University, Seoul 151-744 (Korea, Republic of)

2016-05-01

Highlights: • Crack generation in encapsulation layers were detected by leakage current. • Atomic concentration of SiO{sub x}N{sub y} films affected the bending reliability. • The shapes of the crack tips were affected by the stoichiometry of the SiO{sub x}N{sub y} films. - Abstract: By measuring leakage current density, we detected crack generation in silicon nitride (SiN{sub x}) and silicon oxynitride (SiO{sub x}N{sub y}) thin-film encapsulation layers, and correlated with the films’ water vapor permeability characteristics. After repeated bending cycles, both the changes in water vapor transmission rate and leakage current density were directly proportional to the crack density. Thick SiN{sub x} films had better water vapor barrier characteristics in their pristine state, but cyclic loading led to fast failure. Varying the atomic concentration of the SiO{sub x}N{sub y} films affected their bending reliability. We attribute these differences to changes in the shape of the crack tip as the oxygen content varies.

Antimicrobial activity of chitosan coatings and films against Listeria monocytogenes on black radish.

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Jovanović, Gordana D; Klaus, Anita S; Nikšić, Miomir P

2016-01-01

The antibacterial activity of chitosan coatings prepared with acetic or lactic acid, as well as of composite chitosan-gelatin films prepared with essential oils, was evaluated in fresh shredded black radish samples inoculated with Listeria monocytogenes ATCC 19115 and L. monocytogenes ATCC 19112 during seven days of storage at 4°C. The chitosan coating prepared with acetic acid showed the most effective antibacterial activity. All tested formulations of chitosan films exhibited strong antimicrobial activity on the growth of L. monocytogenes on black radish, although a higher inhibition of pathogens was achieved at higher concentrations of chitosan. The antimicrobial effect of chitosan films was even more pronounced with the addition of essential oils. Chitosan-gelatin films with thyme essential oils showed the most effective antimicrobial activity. A reduction of 2.4log10CFU/g for L. monocytogenes ATCC 19115 and 2.1log10CFU/g for L. monocytogenes ATCC 19112 was achieved in the presence of 1% chitosan film containing 0.2% of thyme essential oil after 24h of storage. Copyright © 2016 Asociación Argentina de Microbiología. Publicado por Elsevier España, S.L.U. All rights reserved.

Physicochemical properties and drug release behavior of biguanidino and O-carboxymethyl chitosan microcapsules.

Science.gov (United States)

Huo, Weiqiang; Zhang, Weixin; Wang, Wei; Zhou, Xiaohua

2014-09-01

Two types of microcapsules (MCs) were prepared by the emulsion cross-linking method, where biguanidino chitosan (BGCS)and O-carboxymethyl chitosan (O-CMCS) served as the wall materials, and the antibacterial agent 2,4-diamino-6-(2-pyridyl)-1,3,5-triazine (PyTNH) served as a model water-soluble drug. The physicochemical performance of the MCs and their drug release behavior were investigated by Fourier transform infrared spectroscopy, thermogravimetric analysis/derivative thermogravimetric analysis, scanning electron microscopy, and swelling and in vitro drug release studies of the two MCs with unmodified chitosan-MCs (CS-MCs) used as the control. The results indicated that the degree of cross-linking, encapsulation efficiency, and thermal stability of the shell wall of the BGCS-microcapsules (BGCS-MCs) were much higher than those of the control and the O-CMCS-microcapsules (CMCS-MCs), owing to the reduction of steric hindrance and development of the conjugation effect in the cross-linking process. Studies on the swelling and in vitro drug-release behavior revealed a sustained release effect of the BGCS-MCs. Moreover, the CMCS-MCs were found to exhibit a pH-dependent drug release behavior, which can be attributed to the successive formation of H-bonds and repulsive forces with the change in the pH of the medium. Based on these results, the swelling-release models and the drug release kinetics of BGCS-MCs and CMCS-MCs are proposed. Copyright © 2014 Elsevier B.V. All rights reserved.

Isolation and Identification of an Indigenous Probiotic Lactobacillus Strain: Its Encapsulation with Natural Branched Polysaccharids to Improve Bacterial Viability

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Nafiseh Sadat Foroutan

2017-06-01

Full Text Available Background and Objective: Probiotics have to reach their site of action in certain numbers in order to exhibit positive health effects. Encapsulation has shown remarkable enhancing effects on probiotic survival in simulated gastric conditions compared to free bacteria. The purpose of this study was identification and evaluation of a potential probiotic strain using encapsulation process by new carriers in order to improve probiotic viability during in vitro simulated conditions.Material and Methods: A native Lactobacillus was isolated from yogurt, identified as Lactobacillus casei PM01 (NCBI registered and analyzed for probiotic properties alongside established probiotic strains of Lactobacillus acidophilus ATCC 43556, and Lactobacillus rhamnosus ATCC 7469. Acid and bile resistance, adhesion to Caco-2 cells and antibiotic resistance were evaluated. Lactobacillus casei PM01 was encapsulated with alginate, chitosan and natural branched polysaccharides (pectin, tragacanth gum and gum Arabic by using extrusion technique. Encapsulation efficiency, acidification activity and viability of entrapped Lactobacillus casei PM01 in simulated gastric pH were determined. Results and Conclusion: Based on the results, all the three strains could be considered as potential probiotics, and are good candidates for further in vitro and in vivo evaluation. The results showed that the survival of encapsulated Lactobacillus casei PM01 was significantly (p≤0.05 increased when it was incubated in simulated gastric pH. It can be concluded that indigenous Lactobacillus casei PM01 in encapsulated form is introduced as an efficient probiotic strain for using in dairy products.Conflict of interest: The authors declare no conflict of interest.

Synthesis of a novel amphiphilic quaternized chitosan and its distribution in rats.

Science.gov (United States)

Liu, Xiaofei; Zeng, Anrong; Li, Lin; Yang, Fan; Wang, Qi; Sun, Zhong; Shen, Jun

2011-01-01

A novel amphiphilic chitosan derivative, N-[(2-hydroxy-3-N,N-dimethylhexadecyl ammonium)propyl]chitosan chloride (N-CQCs), was prepared with a degree of substitution (DS) of 15.58%. N-CQCs was positively charged and its zeta potential was +28.4 mV. The introduction of a long carbon chain with a quaternary ammonium salt group into the chitosan backbone enabled N-CQCs to be lipotropic and hydrophilic. According to the hypothesis of the hypocholesterolemic effect of N-CQCs, its organ distribution in rats was investigated 48 h after administration via gavage using fluorescein isothiocyanate labeling. N-CQCs showed lower cytotoxicity. The plasma half-life of N-CQCs in rats was 48 h and the plasma AUC0-48 h (P) was 371.70 μg/ml per h, suggesting that N-CQCs remained in body for a long time. The results also showed that the accumulation in adipose tissue and gastrointestinal tract was higher than in thymus, kidney, liver and spleen at 48 h after administration. It could be presumed that N-CQCs play an important part in the metabolic process of body fat. Adipose tissue and gastrointestinal tract were the probable interaction sites of N-CQCs and body fat.

Functionalized and graft copolymers of chitosan and its pharmaceutical applications.

Science.gov (United States)

Bhavsar, Chintan; Momin, Munira; Gharat, Sankalp; Omri, Abdelwahab

2017-10-01

Chitosan is the second most abundant natural polysaccharide. It belongs a family of polycationic polymers comprised of repetitive units of glucosamine and N-acetylglucosamine. Its biodegradability, nontoxicity, non-immunogenicity and biocompatibility along with properties like mucoadhesion, fungistatic and bacteriogenic have made chitosan an appreciated polymer with numerous applications in the pharmaceutical, comestics and food industry. However, the limited solubility of chitosan at alkaline and neutral pH limits its widespread commercial use. This can be circumvented by fabrication of chitosan by graft copolymerization with acyl, alkyl, monomeric and polymeric moieties. Areas covered: Modifications like quarterization, thiolation, acylation and grafting result in copolymers with higher mucoadhesion strength, increased hydrophobic interactions (advantageous in hydrophobic drug entrapment), and increased solubility in alkaline pH, the ability for adsorption of metal ions, protein and peptide delivery and nutrient delivery. Insights on methods of polymerization, including atomic transfer radical polymerization and click chemistry are discussed. Applications of such modified chitosan copolymers in medical and surgical, and drug delivery, including nasal, oral and buccal delivery have also been covered. Expert opinion: Despite a number of successful investigations, commercialization of chitosan copolymers still remains a challenge. Further advancements in polymerization techniques may address the unmet needs of the healthcare industry.

Chitosan-Coated Magnetic Nanoparticles with Low Chitosan Content Prepared in One-Step

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Yolanda Osuna

2012-01-01

Full Text Available Chitosan-coated magnetic nanoparticles (CMNP were obtained at 50°C in a one-step method comprising coprecipitation in the presence of low chitosan content. CMNP showed high magnetization and superparamagnetism. They were composed of a core of 9.5 nm in average diameter and a very thin chitosan layer in accordance with electron microscopy measurements. The results from Fourier transform infrared spectrometry demonstrated that CMNP were obtained and those from thermogravimetric analysis allowed to determine that they were composed of 95 wt% of magnetic nanoparticles and 5 wt% of chitosan. 67% efficacy in the Pb+2 removal test indicated that only 60% of amino groups on CMNP surface bound to Pb, probably due to some degree of nanoparticle flocculation during the redispersion. The very low weight ratio chitosan to magnetic nanoparticles obtained in this study, 0.053, and the high yield of the precipitation reactions (≈97% are noticeable.

Structure and properties of microcrystalline chitosan

International Nuclear Information System (INIS)

Pighinelli, Luciano; Guimaraes, Fernando Machado; Paz, Luan Rios; Zanin, Gabrielle Brehm; Kmiec, Marzena; Tedesco, Felipe Melleu; Reis, Victoria Oliva dos; Silva, Matheus Machado; Becker, Cristiane Miotto; Zehetmeyer, Gislene; Rasia, Gisele

2016-01-01

Full text: The microcrystalline chitosan is a modified form of chitosan; it has been elaborated from obtaining method of chitosan salts. It is characterized by special properties of the initial chitosan such as biocompatibility, bioactivity, non-toxic, biodegradability [1]. The objective of this study is to develop a different method to obtain the microcrystalline chitosan and the following characterization of the initial chitosan and MCCh. The material was characterized by FTIR, scanning of electron microscopy, SEM, nuclear magnetic resonance, NMR, and x-ray diffraction. The results indicate that the process to obtain MCCh, did not change the structure of the initial chitosan. The MCCh shows the same functional groups of the initial chitosan. The NMR results shows the acetylated and deacetylated groups. The morphology shows a homogeneous structure of surface. The X-ray diffraction shows the reduction of the crystallinity in the MCCh, indicating a bigger amorphous structure of the MCCh. The chitosan and its derivatives are polymers with excellent properties to be used in regenerative medicine because of ensure efficiency in healing process. This polysaccharide has a great potential to develop a new generation of biomaterials that can be used in regenerative medicine and tissue engineering [2]. References: [1]. LI, Q. et al. Applications and properties of chitosan. In: GOOSEN, M. F. A. (Ed.). Applications of chitin and chitosan. Basel: Technomic, 1997. p. 3-29; [2]. Luciano Pighinelli, Magdalena Kucharska, Dariuz Wawro. Preparation of Microcrystalline chitosan: (MCCh0/tricalcium phosphate complex with Hydroxyapatite in sponge and fibre from for hard tissue regeneration. (author)

Structure and properties of microcrystalline chitosan

Energy Technology Data Exchange (ETDEWEB)

Pighinelli, Luciano; Guimaraes, Fernando Machado; Paz, Luan Rios; Zanin, Gabrielle Brehm; Kmiec, Marzena; Tedesco, Felipe Melleu; Reis, Victoria Oliva dos; Silva, Matheus Machado, E-mail: lpighinelli@hotmail.com [Universidade Luterana, Sao Paulo, SP (Brazil); Becker, Cristiane Miotto; Zehetmeyer, Gislene; Rasia, Gisele [Centro Universitario SENAI CIMATEC, Salvador, BA (Brazil). Instituto de Engenharia de Materiais Polimericos

2016-07-01

Full text: The microcrystalline chitosan is a modified form of chitosan; it has been elaborated from obtaining method of chitosan salts. It is characterized by special properties of the initial chitosan such as biocompatibility, bioactivity, non-toxic, biodegradability [1]. The objective of this study is to develop a different method to obtain the microcrystalline chitosan and the following characterization of the initial chitosan and MCCh. The material was characterized by FTIR, scanning of electron microscopy, SEM, nuclear magnetic resonance, NMR, and x-ray diffraction. The results indicate that the process to obtain MCCh, did not change the structure of the initial chitosan. The MCCh shows the same functional groups of the initial chitosan. The NMR results shows the acetylated and deacetylated groups. The morphology shows a homogeneous structure of surface. The X-ray diffraction shows the reduction of the crystallinity in the MCCh, indicating a bigger amorphous structure of the MCCh. The chitosan and its derivatives are polymers with excellent properties to be used in regenerative medicine because of ensure efficiency in healing process. This polysaccharide has a great potential to develop a new generation of biomaterials that can be used in regenerative medicine and tissue engineering [2]. References: [1]. LI, Q. et al. Applications and properties of chitosan. In: GOOSEN, M. F. A. (Ed.). Applications of chitin and chitosan. Basel: Technomic, 1997. p. 3-29; [2]. Luciano Pighinelli, Magdalena Kucharska, Dariuz Wawro. Preparation of Microcrystalline chitosan: (MCCh0/tricalcium phosphate complex with Hydroxyapatite in sponge and fibre from for hard tissue regeneration. (author)

The effect of hydroxylation on CNT to form Chitosan-CNT composites: A DFT study

International Nuclear Information System (INIS)

Yu, Rui; Ran, Maofei; Wen, Jie; Sun, Wenjing; Chu, Wei; Jiang, Chengfa; He, Zhiwei

2015-01-01

Graphical abstract: - Highlights: • The effect of hydroxylation on CNT to form Chitosan-CNT composites was studied. • The adsorption of Chitosan on CNTs is very weak by electrostatic interactions. • Chitosan loads onto CNT-OH_n via hydrogen-bond interactions. • Chitosan transfers electron to CNT-OH_n and thus improves the reactivity of CNT. - Abstract: The effect of types of CNTs (pristine and hydroxylated) on the synthesis of Chitosan-CNT (CS-CNT) composites was investigated theoretically. The adsorption energy (E_a_d_s) of CS on the pristine CNT and hydroxylated CNTs (CNT-OH_n, n = 1–6) as well as the structural and electronic properties of said composites have been investigated. Results show that the adsorption of CS on CNT and CNT-OH_n is thermodynamically favored. The E_a_d_s of CS on CNTs was calculated to be −20.387 kcal/mol from electrostatic interactions. For CS adsorbed into CNT-OH_n, E_a_d_s ranges from −20.612 to −37.567 kcal/mol. Hydroxyl groups on CNT are the main adsorption sites for CS loading onto CNT-OH_n via hydrogen-bond interactions. The CS-CNT-OH_3 is the most sable composite among tested complexes. The energy gap (ΔE_g_a_p) of CS-CNT-OH_3 was calculated less than pristine CNT and CNT-OH_3, indicative of the composites being more reactive than that of pristine CNTs and CNT-OH_3. It was proved that CS can transfer electron to the hydroxylated CNTs, thus overcoming the drawbacks of CNTs being chemically inert.

The effect of hydroxylation on CNT to form Chitosan-CNT composites: A DFT study

Energy Technology Data Exchange (ETDEWEB)

Yu, Rui [China-America Cancer Research Institute, Key Laboratory for Medical Molecular Diagnostics of Guangdong Province, Guangdong Medical University, Dongguan, Guangdong 523808 (China); Department of Chemical Engineering, Sichuan University, Chengdu 610065 (China); Ran, Maofei [College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Chengdu 610041, Sichuan (China); Wen, Jie [College of Chemistry and Chemical Engineering, Southwest Petroleum University, Chengdu 610500, Sichuan (China); Sun, Wenjing, E-mail: swj_gdmc@163.com [China-America Cancer Research Institute, Key Laboratory for Medical Molecular Diagnostics of Guangdong Province, Guangdong Medical University, Dongguan, Guangdong 523808 (China); Chu, Wei; Jiang, Chengfa [Department of Chemical Engineering, Sichuan University, Chengdu 610065 (China); He, Zhiwei, E-mail: zhiweihe688@yahoo.com [China-America Cancer Research Institute, Key Laboratory for Medical Molecular Diagnostics of Guangdong Province, Guangdong Medical University, Dongguan, Guangdong 523808 (China)

2015-12-30

Graphical abstract: - Highlights: • The effect of hydroxylation on CNT to form Chitosan-CNT composites was studied. • The adsorption of Chitosan on CNTs is very weak by electrostatic interactions. • Chitosan loads onto CNT-OH{sub n} via hydrogen-bond interactions. • Chitosan transfers electron to CNT-OH{sub n} and thus improves the reactivity of CNT. - Abstract: The effect of types of CNTs (pristine and hydroxylated) on the synthesis of Chitosan-CNT (CS-CNT) composites was investigated theoretically. The adsorption energy (E{sub ads}) of CS on the pristine CNT and hydroxylated CNTs (CNT-OH{sub n}, n = 1–6) as well as the structural and electronic properties of said composites have been investigated. Results show that the adsorption of CS on CNT and CNT-OH{sub n} is thermodynamically favored. The E{sub ads} of CS on CNTs was calculated to be −20.387 kcal/mol from electrostatic interactions. For CS adsorbed into CNT-OH{sub n}, E{sub ads} ranges from −20.612 to −37.567 kcal/mol. Hydroxyl groups on CNT are the main adsorption sites for CS loading onto CNT-OH{sub n} via hydrogen-bond interactions. The CS-CNT-OH{sub 3} is the most sable composite among tested complexes. The energy gap (ΔE{sub gap}) of CS-CNT-OH{sub 3} was calculated less than pristine CNT and CNT-OH{sub 3}, indicative of the composites being more reactive than that of pristine CNTs and CNT-OH{sub 3}. It was proved that CS can transfer electron to the hydroxylated CNTs, thus overcoming the drawbacks of CNTs being chemically inert.

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

Science.gov (United States)

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

2013-04-01

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

Pseudo-thermosetting chitosan hydrogels for biomedical application.

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Berger, J; Reist, M; Chenite, A; Felt-Baeyens, O; Mayer, J M; Gurny, R

2005-01-06

To prepare transparent chitosan/beta-glycerophosphate (betaGP) pseudo-thermosetting hydrogels, the deacetylation degree (DD) of chitosan has been modified by reacetylation with acetic anhydride. Two methods (I and II) of reacetylation have been compared and have shown that the use of previously filtered chitosan, dilution of acetic anhydride and reduction of temperature in method II improves efficiency and reproducibility. Chitosans with DD ranging from 35.0 to 83.2% have been prepared according to method II under homogeneous and non-homogeneous reacetylation conditions and the turbidity of chitosan/betaGP hydrogels containing homogeneously or non-homogeneously reacetylated chitosan has been investigated. Turbidity is shown to be modulated by the DD of chitosan and by the homogeneity of the medium during reacetylation, which influences the distribution mode of the chitosan monomers. The preparation of transparent chitosan/betaGP hydrogels requires a homogeneously reacetylated chitosan with a DD between 35 and 50%.

Preparation of curcumin-loaded pluronic F127/chitosan nanoparticles for cancer therapy

International Nuclear Information System (INIS)

Phuc Le, Thi Minh; Pham, Van Phuc; Lua Dang, Thi Minh; Huyen La, Thi; Le, Thi Hanh; Le, Quang Huan

2013-01-01

Nanoparticles (NPs) have been proven to be an effective delivery system with few side effects for anticancer drugs. In this study, curcumin-loaded NPs have been prepared by an ionic gelation method using chitosan (Chi) and pluronic ® F-127 (PF) as carriers to deliver curcumin to the target cancer cells. Prepared NPs were characterized using Zetasizer, fluorescence microscopy, scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Our results showed that the encapsulation efficiency of curcumin was approximately 50%. The average size of curcumin-loaded PF/Chi NPs was 150.9 nm, while the zeta potential was 5.09 mV. Cellular uptake of curcumin-loaded NPs into HEK293 cells was confirmed by fluorescence microscopy. (paper)

Folate-decorated chitosan/doxorubicin poly(butyl)cyanoacrylate nanoparticles for tumor-targeted drug delivery

Energy Technology Data Exchange (ETDEWEB)

Duan Jinghua [Xiangya Hospital, Central South University, Hepatobiliary and Enteric Surgery Research Center (China); Liu Mujun [Central South University, School of Biological Science and Technology (China); Zhang Yangde; Zhao Jinfeng; Pan Yifeng [Xiangya Hospital, Central South University, Hepatobiliary and Enteric Surgery Research Center (China); Yang Xiyun, E-mail: bax_2007@126.com [Central South University, School of Metallurgical Science and Engineering (China)

2012-03-15

A novel chitosan coated poly(butyl cyanoacrylate) (PBCA) nanoparticles loaded doxorubicin (DOX) were synthesized and then conjugated with folic acid to produce a folate-targeted drug carrier for tumor-specific drug delivery. Prepared nanoparticles were surface modified by folate for targeting cancer cells, which is confirmed by FTIR spectroscopy and characterized for shape, size, and zeta potential measurements. The size and zeta potential of prepared DOX-PBCA nanoparticles (DOX-PBCA NPs) were almost 174 {+-} 8.23 nm and +23.14 {+-} 4.25 mV, respectively with 46.8 {+-} 3.32% encapsulation capacity. The transmission electron microscopy study revealed that preparation allowed the formation of spherical nanometric and homogeneous. Fluorescent microscopy imaging and flow cytometry analysis revealed that DOX-PBCA NPs were endocytosed into MCF-7 cells through the interaction with overexpressed folate receptors on the surface of the cancer cells. The results demonstrate that folate-conjugated DOX-PBCA NPs drug delivery system could provide increased therapeutic benefit by delivering the encapsulated drug to the folate receptor positive cancer cells.

Halloysite and chitosan oligosaccharide nanocomposite for wound healing.

Science.gov (United States)

Sandri, Giuseppina; Aguzzi, Carola; Rossi, Silvia; Bonferoni, Maria Cristina; Bruni, Giovanna; Boselli, Cinzia; Cornaglia, Antonia Icaro; Riva, Federica; Viseras, Cesar; Caramella, Carla; Ferrari, Franca

2017-07-15

Halloysite is a natural nanotubular clay mineral (HNTs, Halloysite Nano Tubes) chemically identical to kaolinite and, due to its good biocompatibility, is an attractive nanomaterial for a vast range of biological applications. Chitosan oligosaccharides are homo- or heterooligomers of N-acetylglucosamine and D-glucosamine, that accelerate wound healing by enhancing the functions of inflammatory and repairing cells. The aim of the work was the development of a nanocomposite based on HNTs and chitosan oligosaccharides, to be used as pour powder to enhance healing in the treatment of chronic wounds. A 1:0.05 wt ratio HTNs/chitosan oligosaccharide nanocomposite was obtained by simply stirring the HTNs powder in a 1% w/w aqueous chitosan oligosaccharide solution and was formed by spontaneous ionic interaction resulting in 98.6% w/w HTNs and 1.4% w/w chitosan oligosaccharide composition. Advanced electron microscopy techniques were considered to confirm the structure of the hybrid nanotubes. Both HTNs and HTNs/chitosan oligosaccharide nanocomposite showed good in vitro biocompatibility with normal human dermal fibroblasts up to 300μg/ml concentration and enhanced in vitro fibroblast motility, promoting both proliferation and migration. The HTNs/chitosan oligosaccharide nanocomposite and the two components separately were tested for healing capacity in a murine (rat) model. HTNs/chitosan oligosaccharide allowed better skin reepithelization and reorganization than HNTs or chitosan oligosaccharide separately. The results suggest to develop the nanocomposite as a medical device for wound healing. The present work is focused on the development of halloysite and chitosan oligosaccharide nanocomposite for wound healing. It considers a therapeutic option for difficult to heal skin lesions and burns. The significance of the research considers two fundamental aspects: the first one is related to the development of a self-assembled nanocomposite, formed by spontaneous ionic

Oxygen and nitrogen plasma etching of three-dimensional hydroxyapatite/chitosan scaffolds fabricated by additive manufacturing

Science.gov (United States)

Myung, Sung-Woon; Kim, Byung-Hoon

2016-01-01

Three-dimensional (3D) chitosan and hydroxyapatite (HAp)/chitosan (CH) scaffolds were fabricated by additive manufacturing, then their surfaces were etched with oxygen (O2) and nitrogen (N2) plasma. O2 and N2 plasma etching was performed to increase surface properties such as hydrophilicity, roughness, and surface chemistry on the scaffolds. After etching, hydroxyapatite was exposed on the surface of 3D HAp/CH scaffolds. The surface morphology and chemical properties were characterized by contact angle measurement, scanning electron microscopy, X-ray diffraction, and attenuated total reflection Fourier infrared spectroscopy. The cell viability of 3D chitosan scaffolds was examined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The differentiation of preosteoblast cells was evaluated by alkaline phosphatase assay. The cell viability was improved by O2 and N2 plasma etching of 3D chitosan scaffolds. The present fabrication process for 3D scaffolds might be applied to a potential tool for preparing biocompatible scaffolds.

Synthesis and Optimization of Chitosan Nanoparticles of Shrimp shell as Adsorbent of Pb2+ Ions

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Sulistyani Sulistyani

2017-11-01

Full Text Available Synthesis and optimization of chitosan nanoparticles from shrimp shell as an adsorbent of Pb2+ ions has been done. Chitosan is obtained through several stages, namely deproteinase, demineralization and deacetylation. Deproteinase by using 2 N NaOH solution (a ratio of 1:6 w/v while stirring at 90 °C for 1 hour. Demineralization by using 1 N HCl solution (a ratio of 1:12 w/v while stirring at room temperature for 1 hour. Deacetylation by using 50% NaOH solution (a ratio of 1:10 w/v at 120 °C for 3 hours. Chitosan nanoparticles are obtained by adding a solution of 1% CH3COOH and a few drops of NH3 concentrated at 90 °C to form a white gel is then washed to pH neutral and dried. Characterization of chitosan include analysis of degree of deacetylation by using FTIR and analysis of particle size by using Particle Size Analyzer (PSA. Chitosan nanoparticles was then applied as an adsorbent of lead. Optimization of chitosan as an adsorbent include contact time and pH. Concentration of lead is determined using Atomic Absorption Spectroscopy (AAS. The results showed chitosan synthesis product has a size of ~600 nm, so that it can be expressed as nanoparticles with a degree of deacetylation of 62.69%. Chitosan nanoparticles as adsorbent optimum at pH 3 and a contact time of 2 hours with an adsorption capacity of 13,25 mg/g .

The effect of chitosan and whey proteins-chitosan films on the growth of Penicillium expansum in apples.

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Simonaitiene, Dovile; Brink, Ieva; Sipailiene, Ausra; Leskauskaite, Daiva

2015-05-01

Penicillium expansum causes a major post-harvest disease of apples. The aim of this study was to investigate the inhibition effect of chitosan and whey proteins-chitosan films containing different amounts of quince and cranberry juice against P. expansum on the simulation medium and on apples. The mechanical properties of films were also evaluated. The presence of cranberry and quince juice in the composition of chitosan and whey proteins-chitosan films caused a significant (P ≤ 0.05) increase in elasticity and decrease in tensile strength of films. Chitosan and whey proteins-chitosan films with quince and cranberry juice demonstrated a significant (P ≤ 0.05) inhibition effect against P. expansum growth on the simulated medium and apples. The presence of cranberry juice in the composition of chitosan and whey proteins-chitosan films resulted in a longer lag phase and a lower P. expansum growth rate on the simulation medium in comparison with films made with the addition of quince juice. These differences were not evident when experiment was conducted with apples. Addition of quince and cranberry juice to the chitosan and whey proteins-chitosan films as natural antifungal agents has some potential for prolonging the shelf life of apples. © 2014 Society of Chemical Industry.

Alginate-hydroxypropylcellulose hydrogel microbeads for alkaline phosphatase encapsulation.

Science.gov (United States)

Karewicz, A; Zasada, K; Bielska, D; Douglas, T E L; Jansen, J A; Leeuwenburgh, S C G; Nowakowska, M

2014-01-01

There is a growing interest in using proteins as therapeutics agents. Unfortunately, they suffer from limited stability and bioavailability. We aimed to develop a new delivery system for proteins. ALP, a model protein, was successfully encapsulated in the physically cross-linked sodium alginate/hydroxypropylcellulose (ALG-HPC) hydrogel microparticles. The obtained objects had regular, spherical shape and a diameter of ∼4 µm, as confirmed by optical microscopy and SEM analysis. The properties of the obtained microbeads could be controlled by temperature and additional coating or crosslinking procedures. The slow, sustained release of ALP in its active form with no initial burst effect was observed for chitosan-coated microspheres at pH = 7.4 and 37 °C. Activity of ALP released from ALG/HPC microspheres was confirmed by the occurance of effectively induced mineralization. SEM and AFM images revealed formation of the interpenetrated three-dimensional network of mineral, originating from the microbeads' surfaces. FTIR and XRD analyses confirmed formation of hydroxyapatite.

Development of highly durable deep-ultraviolet AlGaN-based LED multichip array with hemispherical encapsulated structures using a selected resin through a detailed feasibility study

Science.gov (United States)

Nagai, Shoko; Yamada, Kiho; Hirano, Akira; Ippommatsu, Masamichi; Ito, Masahiro; Morishima, Naoki; Aosaki, Ko; Honda, Yoshio; Amano, Hiroshi; Akasaki, Isamu

2016-08-01

To replace mercury lamps with AlGaN-based deep-ultraviolet (DUV) LEDs, a simple and low-cost package with increased light extraction efficiency (LEE) is indispensable. Therefore, resin encapsulation is considered to be a key technology. However, the photochemical reactions induced by DUV light cause serious problems, and conventional resins cannot be used. In the former part of this study, a comparison of a silicone resin and fluorine polymers was carried out in terms of their suitability for encapsulation, and we concluded that only one of the fluorine polymers can be used for encapsulation. In the latter part, the endurance of encapsulation using the selected fluorine polymer was investigated, and we confirmed that the selected fluorine polymer can guarantee a lifetime of over 6,000 h at a wavelength of 265 nm. Furthermore, a 3 × 4 array module of encapsulated dies on a simple AlN submount was fabricated, demonstrating the possibility of W/cm2-class lighting.

Development and characterisation of chitosan films impregnated with insulin loaded PEG-b-PLA nanoparticles (NPs): a potential approach for buccal delivery of macromolecules.

Science.gov (United States)

Giovino, Concetta; Ayensu, Isaac; Tetteh, John; Boateng, Joshua S

2012-05-30

Mucoadhesive chitosan based films, incorporated with insulin loaded nanoparticles (NPs) made of poly(ethylene glycol)methyl ether-block-polylactide (PEG-b-PLA) have been developed and characterised. Blank-NPs were prepared by double emulsion solvent evaporation technique with varying concentrations of the copolymer (5 and 10%, w/v). The optimised formulation was loaded with insulin (model protein) at initial loadings of 2, 5 and 10% with respect to copolymer weight. The developed NPs were analysed for size, size distribution, surface charge, morphology, encapsulation efficiency and drug release. NPs showing negative (ζ)-potential ( 300 nm and a polydispersity index (P.I.) of ≈ 0.2, irrespective of formulation process, were achieved. Insulin encapsulation efficiencies of 70% and 30% for NPs-Insulin-2 and NPs-Insulin-5 were obtained, respectively. The in vitro release behaviour of both formulations showed a classic biphasic sustained release of protein over 5 weeks which was influenced by pH of the release medium. Optimised chitosan films embedded with 3mg of insulin loaded NPs were produced by solvent casting with homogeneous distribution of NPs in the mucoadhesive matrix, which displayed excellent physico-mechanical properties. The drug delivery system has been designed as a novel platform for potential buccal delivery of macromolecules. Copyright © 2012 Elsevier B.V. All rights reserved.

Application of chitosan and its N-heterocyclic derivatives for preconcentration of noble metal ions and their determination using atomic absorption spectrometry.

Science.gov (United States)

Azarova, Yu A; Pestov, A V; Ustinov, A Yu; Bratskaya, S Yu

2015-12-10

Chitosan and its N-heterocyclic derivatives N-2-(2-pyridyl)ethylchitosan (2-PEC), N-2-(4-pyridyl) ethylchitosan (4-PEC), and N-(5-methyl-4-imidazolyl) methylchitosan (IMC) have been applied in group preconcentration of gold, platinum, and palladium for subsequent determination by atomic absorption spectroscopy (AAS) in solutions with high background concentrations of iron and sodium ions. It has been shown that the sorption mechanism, which was elucidated by XPS, significantly influences the sorption capacity of materials, the efficiency of metal ions elution after preconcentration, and, as a result, the accuracy of metal determination by AAS. We have shown that native chitosan was not suitable for preconcentration of Au(III), if the elution step was used as a part of the analysis scheme. The group preconcentration of Au(III), Pd(II), and Pt(IV) with subsequent quantitative elution using 0.1M HCl/1M thiourea solution was possible only on IMC and 4-PEC. Application of IMC for analysis of the national standard quartz ore sample proved that gold could be accurately determined after preconcentration/elution with the recovery above 80%. Copyright © 2015 Elsevier Ltd. All rights reserved.

Improved mucoadhesion and cell uptake of chitosan and chitosan oligosaccharide surface-modified polymer nanoparticles for mucosal delivery of proteins.

Science.gov (United States)

Dyawanapelly, Sathish; Koli, Uday; Dharamdasani, Vimisha; Jain, Ratnesh; Dandekar, Prajakta

2016-08-01

The main aim of the present study was to compare mucoadhesion and cellular uptake efficiency of chitosan (CS) and chitosan oligosaccharide (COS) surface-modified polymer nanoparticles (NPs) for mucosal delivery of proteins. We have developed poly (D, L-lactide-co-glycolide) (PLGA) NPs, surface-modified COS-PLGA NPs and CS-PLGA NPs, by using double emulsion solvent evaporation method, for encapsulating bovine serum albumin (BSA) as a model protein. Surface modification of NPs was confirmed using physicochemical characterization methods such as particle size and zeta potential, SEM, TEM and FTIR analysis. Both surface-modified PLGA NPs displayed a slow release of protein compared to PLGA NPs. Furthermore, we have explored the mucoadhesive property of COS as a material for modifying the surface of polymeric NPs. During in vitro mucoadhesion test, positively charged COS-PLGA NPs and CS-PLGA NPs exhibited enhanced mucoadhesion, compared to negatively charged PLGA NPs. This interaction was anticipated to improve the cell interaction and uptake of NPs, which is an important requirement for mucosal delivery of proteins. All nanoformulations were found to be safe for cellular delivery when evaluated in A549 cells. Moreover, intracellular uptake behaviour of FITC-BSA loaded NPs was extensively investigated by confocal laser scanning microscopy and flow cytometry. As we hypothesized, positively charged COS-PLGA NPs and CS-PLGA NPs displayed enhanced intracellular uptake compared to negatively charged PLGA NPs. Our results demonstrated that CS- and COS-modified polymer NPs could be promising carriers for proteins, drugs and nucleic acids via nasal, oral, buccal, ocular and vaginal mucosal routes.

Preparation and characterization of chitosan/genipin/poly(N-vinyl-2-pyrrolidone) films for controlled release drugs

Energy Technology Data Exchange (ETDEWEB)

Aldana, Ana Agustina, E-mail: aaldana@fcq.unc.edu.ar [Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba (UNC), Edificio de Ciencias II, Medina Allende y Haya de la Torre, Ciudad Universitaria, Cordoba 5000 (Argentina); Gonzalez, Agustin, E-mail: agustingonzalez@fcq.unc.edu.ar [Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba (UNC), Edificio de Ciencias II, Medina Allende y Haya de la Torre, Ciudad Universitaria, Cordoba 5000 (Argentina); Strumia, Miriam C., E-mail: mcs@fcq.unc.edu.ar [Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba (UNC), Edificio de Ciencias II, Medina Allende y Haya de la Torre, Ciudad Universitaria, Cordoba 5000 (Argentina); Martinelli, Marisa, E-mail: mmartinelli@fcq.unc.edu.ar [Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba (UNC), Edificio de Ciencias II, Medina Allende y Haya de la Torre, Ciudad Universitaria, Cordoba 5000 (Argentina)

2012-05-15

Highlights: Black-Right-Pointing-Pointer Cross-linked chitosan films using genipin and/or PVP. Black-Right-Pointing-Pointer Propranolol hydrochloride was used like a model drug to release studies. Black-Right-Pointing-Pointer Incorporating PVP improves mechanical and diffusion properties. Black-Right-Pointing-Pointer Ch-Gen 0.10% and Ch-Gen 0.10%-PVP have optimal behavior. - Abstract: The study of the physicochemical and functional properties of chitosan films cross-linked with genipin and poly(N-vinyl-2-pyrrolidone) (PVP) was performed in this work. Cross-linked films were prepared by casting method from acetic acid solutions. The structure and physical properties of the films were analyzed by infrared spectroscopy (FT-IR), nuclear magnetic resonance spectroscopy ({sup 13}C NMR), differential scanning calorimetry (DSC) and mechanical testings. Propranolol hydrochloride was used like a model drug to determine the behavior of drug release from films. The drug release capacity was measured and compared with the degree of cross-linking, mechanical properties and swelling index. There was an appropriate balance of hydrophilicity, mechanical properties and diffusion by the incorporation of PVP into the networks cross-linked with genipin. The combination of both cross-linkers allows obtaining a soft and tough material potentially applicable as a controlled release. This research represents the first report where both cross-linkers, chemical and ionic agents, are used for obtaining films. These studies suggest that the chitosan films prepared here are promising drug delivery systems for buccal application, with thermal stability and acceptable mechanical properties. Buccal films may be preferred in terms of flexibility and comfort.

Preparation and characterization of chitosan/genipin/poly(N-vinyl-2-pyrrolidone) films for controlled release drugs

International Nuclear Information System (INIS)

Aldana, Ana Agustina; González, Agustín; Strumia, Miriam C.; Martinelli, Marisa

2012-01-01

Highlights: ► Cross-linked chitosan films using genipin and/or PVP. ► Propranolol hydrochloride was used like a model drug to release studies. ► Incorporating PVP improves mechanical and diffusion properties. ► Ch–Gen 0.10% and Ch–Gen 0.10%–PVP have optimal behavior. - Abstract: The study of the physicochemical and functional properties of chitosan films cross-linked with genipin and poly(N-vinyl-2-pyrrolidone) (PVP) was performed in this work. Cross-linked films were prepared by casting method from acetic acid solutions. The structure and physical properties of the films were analyzed by infrared spectroscopy (FT-IR), nuclear magnetic resonance spectroscopy ( 13 C NMR), differential scanning calorimetry (DSC) and mechanical testings. Propranolol hydrochloride was used like a model drug to determine the behavior of drug release from films. The drug release capacity was measured and compared with the degree of cross-linking, mechanical properties and swelling index. There was an appropriate balance of hydrophilicity, mechanical properties and diffusion by the incorporation of PVP into the networks cross-linked with genipin. The combination of both cross-linkers allows obtaining a soft and tough material potentially applicable as a controlled release. This research represents the first report where both cross-linkers, chemical and ionic agents, are used for obtaining films. These studies suggest that the chitosan films prepared here are promising drug delivery systems for buccal application, with thermal stability and acceptable mechanical properties. Buccal films may be preferred in terms of flexibility and comfort.

Development and evaluation of N-naphthyl-N,O-succinyl chitosan micelles containing clotrimazole for oral candidiasis treatment.

Science.gov (United States)

Tonglairoum, Prasopchai; Woraphatphadung, Thisirak; Ngawhirunpat, Tanasait; Rojanarata, Theerasak; Akkaramongkolporn, Prasert; Sajomsang, Warayuth; Opanasopit, Praneet

2017-03-01

Clotrimazole (CZ)-loaded N-naphthyl-N,O-succinyl chitosan (NSCS) micelles have been developed as an alternative for oral candidiasis treatment. NSCS was synthesized by reductive N-amination and N,O-succinylation. CZ was incorporated into the micelles using various methods, including the dropping method, the dialysis method, and the O/W emulsion method. The size and morphology of the CZ-loaded micelles were characterized using dynamic light scattering measurements (DLS) and a transmission electron microscope (TEM), respectively. The drug entrapment efficiency, loading capacity, release characteristics, and antifungal activity against Candida albicans were also evaluated. The CZ-loaded micelles prepared using different methods differed in the size of micelles. The micelles ranged in size from 120 nm to 173 nm. The micelles prepared via the O/W emulsion method offered the highest percentage entrapment efficiency and loading capacity. The CZ released from the CZ-loaded micelles at much faster rate compared to CZ powder. The CZ-loaded NSCS micelles can significantly hinder the growth of Candida cells after contact. These CZ-loaded NSCS micelles offer great antifungal activity and might be further developed to be a promising candidate for oral candidiasis treatment.

Preparation, characterization and application of N-methylene phosphonic acid chitosan grafted magnesia–zirconia stationary phase

Energy Technology Data Exchange (ETDEWEB)

Wang, Qing; Chen, Jie; Huang, Kun; Zhang, Xin; Xu, Li [Tongji School of Pharmacy, Huazhong University of Science and Technology, Wuhan 430030 (China); Shi, Zhi-guo, E-mail: shizg@whu.edu.cn [Department of Chemistry, Wuhan University, Wuhan 430072 (China)

2015-01-07

Highlights: • N-methylene phosphonic acid chitosan grafted MgO–ZrO{sub 2} was prepared. • It exhibited superior HILIC chromatographic performance to the bare MgO–ZrO{sub 2}. • Monosaccharides, phospholipids and peptides were successfully separated. • It was a promising HILIC stationary phase. - Abstract: A hydrophilic stationary phase (SP) was prepared through grafting N-methylene phosphonic acid chitosan on magnesia–zirconia particles (P-CTS-MgO–ZrO{sub 2}) via Lewis acid–base interaction. The resulting material was characterized by thermogravimetric analysis, Fourier transform infrared spectroscopy, scanning electron microscope and nitrogen adsorption analysis. The chromatographic performance of P-CTS-MgO–ZrO{sub 2} was systemically evaluated by studying effect of acetonitrile content, pH and buffer concentration in the mobile phase. The results demonstrated that the novel SP provided hydrophilic, electrostatic-repulsion and ion-exchange interactions. Compared to the bare MgO–ZrO{sub 2}, P-CTS-MgO–ZrO{sub 2} exhibited superior peak shape, reasonable resolution and reduced analysis time in separation of basic analytes. Besides, remarkable resolving power of acids, i.e. six non-steroidal anti-inflammatory drugs which failed to be eluted from the bare MgO–ZrO{sub 2}, was obtained with the theoretical plate number (N/m) of 4653–31313, asymmetry factor <1.21 and the resolution of 1.6–3.4. Finally, P-CTS-MgO–ZrO{sub 2} SP was applied to separate monosaccharides, phospholipids and peptides. P-CTS-MgO–ZrO{sub 2} was a promising hydrophilic SP for wide applications.

A sulfuric-lactic acid process for efficient purification of fungal chitosan with intact molecular weight.

Science.gov (United States)

Naghdi, Mitra; Zamani, Akram; Karimi, Keikhosro

2014-02-01

The most recent method of fungal chitosan purification, i.e., two steps of dilute sulfuric acid treatment, pretreatment of cell wall at room temperature for phosphate removal and extraction of chitosan from the phosphate free cell wall at high temperature, significantly reduces the chitosan molecular weight. This study was aimed at improvement of this method. In the pretreatment step, to choose the best conditions, cell wall of Rhizopus oryzae, containing 9% phosphate, 10% glucosamine, and 21% N-acetyl glucosamine, was treated with sulfuric, lactic, acetic, nitric, or hydrochloric acid, at room temperature. Sulfuric acid showed the best performance in phosphate removal (90%) and cell wall recovery (89%). To avoid depolymerisation of chitosan, hot sulfuric acid extraction was replaced with lactic acid treatment at room temperature, and a pure fungal chitosan was obtained (0.12 g/g cell wall). Similar pretreatment and extraction processes were conducted on pure shrimp chitosan and resulted in a chitosan recovery of higher than 87% while the reduction of chitosan viscosity was less than 15%. Therefore, the sulfuric-lactic acid method purified the fungal chitosan without significant molecular weight manipulation. Copyright © 2013 Elsevier B.V. All rights reserved.

Radiation processing of chitosan derivative and its characteristics

International Nuclear Information System (INIS)

Kamarudin Bahari; Kamarolzaman Hussein; Kamaruddin Hashim; Khairul Zaman Mohd Dahlan

2002-01-01

Chitosan is natural polymer derived from chitin, a polysaccharide found in the exoskeleton of shrimps, crabs, fungi and others. Chitosan is a naturally occurring substance that is chemically similar to cellulose. Chitosan possesses a positive ionic charge give ability to chemically bond with negatively charged fats. Chitosan is soluble in organic acid but insoluble in water. Carboxymethyl-chitosan (cm-chitosan) is a derivative of chitosan which is water-soluble was then prepared by a carboxymethylation process of chitosan produced from local shrimp shell. A simple method for synthesis of cm-chitosan has been developed at 55 degree C in aqueous sodium hydroxide / propanol with chloroacetic acid (CAA) or sodium chloroacetate salt (SCA). The modification of chitosan to water-soluble chitosan can be used in hydrogel as anti-bacterial agent and it overcome the problem of bad smell using acetic acid. (Author)

Synthesis, characterization and radiation processing of carboxymethyl-chitosan

International Nuclear Information System (INIS)

Kamarudin Bahari; Kamarolzaman Hussein; Kamaruddin Hashim; Khairul Zaman Mohd Dahlan

2002-01-01

Chitosan is natural polymer derived from chitin, a polysaccharide found in the exoskeleton of shrimps, crabs, fungi and others. Chitosan is a naturally occurring substance that is chemically similar to cellulose. Chitosan possesses a positive ionic charge give ability to chemically bond with negatively charged fats. Chitosan is soluble in organic acid but insoluble in water. Carboxymethyl-chitosan (cm-chitosan) is a derivative of chitosan which is water-soluble was then prepared by carboxymethylation process of chitosan produced from local shrimp shell. A simple method for synthesis of cm-chitosan has been developed at 55 degree C in aqueous sodium hydroxide / propanol with chloroacetic acid (CAA) or sodium chloroacetate salt (SCA). The modification of chitosan to water-soluble chitosan can be used in hydrogel as anti-bacterial and anti-fungal agent, and it overcome the problem of bad smell using organic acid. (Author)

Encapsulation of gold nanoparticles into self-assembling protein nanoparticles

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Yang Yongkun

2012-10-01

Full Text Available 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 to encapsulate gold nanoparticles. The protein nanoparticles are formed upon self-assembly of a protein chain that is composed of a pentameric coiled-coil domain at the N-terminus and trimeric coiled-coil domain at the C-terminus. The self-assembling protein nanoparticles form a central cavity of about 10 nm in size, which is ideal for the encapsulation of gold nanoparticles with similar sizes. Results We have used SAPNs to encapsulate several commercially available gold nanoparticles. The hydrodynamic size and the surface coating of gold nanoparticles are two important factors influencing successful encapsulation by the SAPNs. Gold nanoparticles with a hydrodynamic size of less than 15 nm can successfully be encapsulated. Gold nanoparticles with citrate coating appear to have stronger interactions with the proteins, which can interfere with the formation of regular protein nanoparticles. Upon encapsulation gold nanoparticles with polymer coating interfere less strongly with the ability of the SAPNs to assemble into nanoparticles. Although the central cavity of the SAPNs carries an overall charge, the electrostatic interaction appears to be less critical for the efficient encapsulation of gold nanoparticles into the protein nanoparticles. Conclusions The SAPNs can be used to encapsulate gold nanoparticles. The SAPNs can be further functionalized by engineering functional peptides or proteins to either their N- or C-termini. Therefore encapsulation of gold

Radiation Synthesis and Application of Carboxymethylated Chitosan Hydrogels

Energy Technology Data Exchange (ETDEWEB)

Noh, Young Chang

2007-08-15

This research proposal is to investigate radiation effect of carboxymethylated chitosan in order to obtain the crosslinked carboxymethylated chitosan. The application studies on CM-chitosan- based intelligent hydrogels will be tried too. Chitin is the most abundant natural amino polysaccharide and estimated to be produced annually almost as much as cellulose. Chitosan is the deacetylated product of chitin showing the enhanced solubility in dilute acids, further, carboxymethylated chitosan (CM-chitosan) can solve in both acidic and basic physiological media, which might be good candidates as a kind of biomedical materials. Radiation technique is an important method for modification of chitin derivatives. It includes radiation-induced degradation, grafting, and crosslinking. It was found that CM-chitosan degraded in solid state or dilute aqueous solution under irradiation, but crosslinked at paste-like sate when the concentration of CM-chitosan is more than 10%. Both degraded and crosslinked CM-chitosan have antibacterial activity, so it is essential to investigate in detail the radiation effect of CM-chitosan. Study on radiation effect of CM-chitosan in different condition is beneficial to modification of CM-chitosan by irradiation technique. However, little study was reported on radiation crosslinking and application of CM-chitosan. The radiation-closslinked CM-chitosan synthesized from chitosan was characterized by a Fourier transform infrared spectroscopy (FT-IR) analysis. A kinetic swelling in water and the mechanical properties such as a gelation, water absorptivity, and gel strength were also investigated. For the preparation of crosslinked CM-chitosan by using gamma irradiation, the concentration of an aqueous CM-chitosan is above 10wt%. We confirmed that the gel contents was in the range of 15-63%, and when the irradiation dose was increased, the degree of gelation was decreased by disintegration of the CM-chitosan. In conclusion, we developed a new

Radiation Synthesis and Application of Carboxymethylated Chitosan Hydrogels

International Nuclear Information System (INIS)

Noh, Young Chang

2007-08-01

This research proposal is to investigate radiation effect of carboxymethylated chitosan in order to obtain the crosslinked carboxymethylated chitosan. The application studies on CM-chitosan- based intelligent hydrogels will be tried too. Chitin is the most abundant natural amino polysaccharide and estimated to be produced annually almost as much as cellulose. Chitosan is the deacetylated product of chitin showing the enhanced solubility in dilute acids, further, carboxymethylated chitosan (CM-chitosan) can solve in both acidic and basic physiological media, which might be good candidates as a kind of biomedical materials. Radiation technique is an important method for modification of chitin derivatives. It includes radiation-induced degradation, grafting, and crosslinking. It was found that CM-chitosan degraded in solid state or dilute aqueous solution under irradiation, but crosslinked at paste-like sate when the concentration of CM-chitosan is more than 10%. Both degraded and crosslinked CM-chitosan have antibacterial activity, so it is essential to investigate in detail the radiation effect of CM-chitosan. Study on radiation effect of CM-chitosan in different condition is beneficial to modification of CM-chitosan by irradiation technique. However, little study was reported on radiation crosslinking and application of CM-chitosan. The radiation-closslinked CM-chitosan synthesized from chitosan was characterized by a Fourier transform infrared spectroscopy (FT-IR) analysis. A kinetic swelling in water and the mechanical properties such as a gelation, water absorptivity, and gel strength were also investigated. For the preparation of crosslinked CM-chitosan by using gamma irradiation, the concentration of an aqueous CM-chitosan is above 10wt%. We confirmed that the gel contents was in the range of 15-63%, and when the irradiation dose was increased, the degree of gelation was decreased by disintegration of the CM-chitosan. In conclusion, we developed a new