JOURNAL OF APPLIED POLYMER SCIENCE
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2015
·Vol. 132
·期 22
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IF 1.768
Yong Liu,Jieyi Liang,Shoulian Wei,Ling Liu,Miaochan Liao
The purpose of this study was to fabricate and evaluate nanoparticles based on β-conglycinin (7S) and chitosan (CS) to deliver 5-fluorouracil (5-FU). The nanoparticles were prepared with a self-assembly method. Turbidity measurements performed at 600 nm were used to investigate the formation of the nanoparticles as a function of the pH, 7S-to-CS mass ratio, and total concentration of 7S and CS. The optimum conditions for the preparation of the nanoparticles were a pH of 5.5, a 7S-to-CS mass ratio of 4 : 1, and total concentration of 7S and CS of 9 mg/mL. Under these conditions, the nanoparticles in solution had a high turbidity and good stability. Fourier transform infrared spectroscopy revealed that the nanoparticles were formed mainly through electrostatic interactions between the amine groups ( NH 3 + ) of CS and the carboxyl groups ( COO − ) of 7S. Scanning electron microscopy micrographs and dynamic light scattering analysis showed that the nanoparticles had an approximately spherical morphology with a smooth surface, and the mean particle size was about 120 nm with a narrow size distribution. The release of 5-FU showed an initial burst release followed by a sustained release, and the release was pH-dependent. The release mechanism of 5-FU was Fickian diffusion according to the Ritger–Peppas model. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015 , 132 , 41963.
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JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
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2013
·Vol. 24
·期 9
·2093-2100
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IF 2.141
Guo Rui,Chen Lili,Cai Shushan,Liu Zonghua,Zhu Yi,Xue Wei,Zhang Yuanming
Polysaccharides based polyelectrolyte complex nanoparticles (PCNs) intended for use in the delivery of macromolecules were prepared by the self-assembly of deoxycholic acid hydrophobically modified chitosan (CS-DCA) core and then coated with sodium alginate (ALG) shell. The CS-DCA capable of forming nano-sized self-aggregates in medium was prepared by the grafting of DCA to CS. In order to increase the stability of nanoparticles and prevent burst release of drug in bloodstream, polyanionic ALG was coated on the surface of positively charged CS-DCA nanoparticles to form PCNs. Dynamic light scattering results revealed that the mean diameter of the PCNs was about 330 nm, larger than that of uncoated nanoparticles (~150 nm). The zeta potential was big enough to keep the stability of PCNs (−28 mV); no size change was found even upon 1 month storage. Bovine serum albumin could be easily incorporated into the PCNs with encapsulation efficiency (>44 %) and keep a sustained manner without burst release when exposed to PBS (pH 7.4) at 37 °C. These results suggested that PCNs may be a promising drug carrier for a prolonged and sustained delivery in the bloodstream.
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CARBOHYDRATE POLYMERS
·
2013
·
IF 3.479
Bo Lu,Dan Huang,Hua Zheng,Zhijun Huang,Peihu Xu,Haixing Xu,Yihua Yin,Xia Liu,Dan Li,Xueqiong Zhang
A series of melphalan-O-carboxymethyl chitosan (Mel-OCM-chitosan) conjugates with different spacers were prepared and structurally characterized. All conjugates showed satisfactory water-solubility (160-217 times of Mel solubility). In vitro drug release behaviors by both chemical and enzymatic hydrolysis were investigated. The prodrugs released Mel rapidly within papain and lysosomal enzymes of about 40–75%, while released only about 4–5% in buffer and plasma, which suggested that the conjugates have good plasma stability and the hydrolysis in both papain and lysosomes occurs mostly via enzymolysis. It was found that the spacers have important effect on the drug content, water solubility, drug release properties and cytotoxicity of Mel-OCM-chitosan conjugates. Cytotoxicity studies by MTT assay demonstrated that these conjugates had 52–70% of cytotoxicity against RPMI8226 cells in vitro as compared with free Mel, indicating the conjugates did not lose anti-cancer activity of Mel. Overall these studies indicated Mel-OCM-chitosan conjugates as potential prodrugs for cancer treatment.
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RSC Advances
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2015
·Vol. 5
·期 128
·105901-105907
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IF 3.84
Guan-Hai Wang,Hui-Kang Yang,Yi Zhao,Da-Wei Zhang,Li-Ming Zhang,Jian-Tao Lin
In this work, novel biodegradable cationic micelles were prepared based on poly-(N-ε-carbobenzyloxy-L-lysine) (PZLL) and chitosan (CS) by click reaction, and applied for co-delivery of doxorubicin (DOX) and p53 plasmid. The structure of the copolymer was characterized by 1H NMR and FTIR. The loading amount of DOX in the micelles was 12.8%. Fluorescence spectra confirmed that DOX interacted via π–π stacking with micelles when DOX was encapsulated into the micelles. In particular, its complexation with plasmid DNA was investigated using agarose gel electrophoresis, flow cytometry, zeta potential, and particle size analyses as well as transmission electron microscopy observations. The results showed that the copolymers have a strong pDNA condensation ability and provide protection of pDNA against deoxyribonuclease I degradation. CS-g-PZLL/DOX/p53 nanoparticles showed good gene transfection efficiency in vitro. Fluorescence images and flow cytometry tests revealed that p53 and DOX could be efficiently transported into Hela tumor cells simultaneously, and the optimum N/P ratio for p53 transfection was 20/1. For co-delivery analysis, the obtained CS-g-PZLL/DOX/p53 complexes showed a better inhibitory effect on Hela tumor cells than DOX or p53 used singly.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2014
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IF 3.096
Weiqiang Huo,Weixin Zhang,Wei Wang,Xiaohua Zhou
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.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
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2016
·
IF 3.994
Juntao Yin,Cuiyu Xiang,Xiaoyong Song
Psoralidin (PL) has recently been attracting more attention as a new anticancer agent candidate. Nevertheless, peroral administration of PL is largely challenged by its insoluble nature and intestinal efflux. This article aimed to develop a nanoencapsulation formulation of PL using water-soluble chitosan and Eudragit S100 and to evaluate its potential for bioavailability enhancement. PL-loaded nanocapsules (PL-NCs) were prepared by a solvent diffusion and high-pressure homogenization technique with Poloxamer 188 as a stabilizer. The resultant PL-NCs were approximately 132.5 nm in particle size and possessed a high entrapment efficiency (98.1%). In vitro release showed that PL was released less from the nanocapsules due to electrostatic complexation. A lipolytic experiment demonstrated that our prepared PL-NCs were not degraded by lipase , in contrast with the most commonly used lipid nanoparticles. Furthermore, PL-NCs appeared to have less affinity for intestinal mucins. Following oral administration, the bioavailability of PL was significantly enhanced via the PL-NCs, with a value of 339.02% relative to the reference (suspensions). Excellent intestinal adhesion and transepithelial permeability accounted for the enhancement of oral bioavailability. Taken together, these results indicate that nanoencapsulation of PL with chitosan and Eudragit S100 is a promising strategy for improved PL oral delivery.
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JOURNAL OF BIOMATERIALS APPLICATIONS
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2017
·
IF 2.31
Jianzhou Cai,Wu Zhang,Jiake Xu,Wei Xue,Zonghua Liu
Chitosan, as a potential vaccine delivery material, has obtained much attention for immunization prevention and therapy. However, its poor water solubility brings inconvenience for the practical applications. To address this issue, researchers have carried out many chemical modifications to prepare water-soluble chitosan derivatives for vaccine delivery. In this work, we prepared a chitosan derivative N-phosphonium chitosan with excellent water solubility and explored its potential as an intramuscular vaccine delivery system by using ovalbumin as a model antigen. Different vaccine formulations were intramuscularly injected into test mice. Through an immunohistochemistry assay, N-phosphonium chitosan-based antigen formulation could promote antigen arrival from injection site to the secondary lymph organ spleen. Further immunization results showed that 1 mg/ml N-phosphonium chitosan-based vaccine formulation could contribute to significantly higher level of antigen-specific immune responses, including higher antigen-specific IgG antibody titer, splenocyte proliferation, and cytokines secretion (interferon-γ, interleukin-10, and interleukin-4) by the splenocytes of the immunized mice. From the results, the water-soluble chitosan derivative N-phosphonium chitosan could be developed as a potential antigen carrier for immunization prevention and therapy.
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ACS Applied Materials & Interfaces
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2016
·
IF 7.145
Donghui Liang,Zhong Lu,Hao Yang,Jingting Gao,Rong Chen
A novel silver nanoparticles (AgNPs)/chitosan composite dressing with asymmetric wettability surfaces was successfully prepared via a simple two-step method for biomedical applications as wound healing materials. First, AgNPs were assembled into the chitosan sponge which was prepared by lyophilization process. Then one side of the sponge was modified by a thin layer of stearic acid. The incorporation of AgNPs into chitosan dressing could enhance the antibacterial activity against drug-sensitive and drug-resistant pathogenic bacteria. The asymmetric surface modification endows the dressing with both highly hydrophobic property and inherent hydrophilic nature of chitosan. The hydrophobic surface of the dressing shows waterproof and antiadhesion for contaminant properties, whereas the hydrophilic surface preserves its water-absorbing capability and efficiently inhibits the growth of bacteria. Furthermore, the AgNPs/chitosan composite dressing displays improved moisture retention and blood clotting ability compared to the unmodified dressings. Cytocompatibility test evaluated in vitro and in a wound infection model illustrates the nontoxic nature of the composite dressing. More importantly, the in vivo wound healing model evaluation in mice reveals that the asymmetric AgNPs/chitosan dressing promotes the wound healing and accelerates the reepithelialization and collagen deposition. The silver accumulation in mice body treated by the composite dressing is far lower than that of the clinically used Acasin nanosilver dressing treated mice. This work indicates the huge potential of the novel AgNPs/chitosan wound dressing with asymmetrical wettability for clinical use.
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SEPARATION AND PURIFICATION TECHNOLOGY
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2016
·
IF 3.299
Qinqin Liu,Yan Zhao,Jiefeng Pan,Bart Van der Bruggen,Jiangnan Shen
Using molecularly imprinted technology and the phase inversion method, a chlorogenic acid molecularly imprinted chitosan membrane was prepared. Chlorogenic acid was used as the template molecule and chitosan as the film-forming material. Sulfuric acid was chosen as the cross-linking agent, in order to inhibit the swelling of chitosan membranes. The selectivity of these imprinted membranes in terms of permeability and adsorption capacity was studied. Furthermore, the chemical composition and surface structure of the membranes as well as their thermo-stability were characterized. Scatchard results show that there are two kinds of adsorption sites present on the molecularly imprinted membranes, one with high affinity sites and one with low affinity sites. For the high affinity sites, the maximum adsorption capacity was 139.57 μmol g −1 and that for the low affinity sites was 287.86 μmol g −1 . In contrast, for the non-imprinted membranes, only one kind of sites was found, with a maximum adsorption capacity of 83.84 μmol g −1 . The adsorption isotherms indicate that the adsorption isotherm curve of chlorogenic acid binding onto the imprinted membrane agrees with the Freundlich model while that of the non-imprinted membrane conforms to the Langmuir model. The permeation experiments proved that the imprinted membrane has a selective adsorption capacity for chlorogenic acid.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2016
·
IF 3.138
Ying Ren,Hongguo Xie,Xiaocen Liu,Fan Yang,Weiting Yu,Xiaojun Ma
The goal of this work is to tune the formation and stability of the alginate-chitosan (AC) polyelectrolyte complexes (PECs) and microcapsules. Particularly, we explore the role of the conformation of chitosan on its interaction with alginate to understand the mechanism underpinning their interactions at the molecular level. Reducing the charge density by increasing pH will increase the compactness of chitosan, the values of the enthalpy (H) and stoichiometry (N) of binding between chitosan and alginate. Consequently, chitosan has advantage in being adsorbed on alginate beads to form microcapsules, including the binding rate and binding amount. Though the total heat release remain similar in the range of ionic strength , chitosan diffuses much easier into alginate hydrogels when in higher ionic strength. Increasing pH and ionic strength both help AC microcapsules to have higher stability. The results indicate that the formation and stability of AC microcapsules are related to the rigidity and conformations of chitosan molecules. After increasing acetylation degree (DA) of chitosan, the binding rate of chitosan and mechanical strength of AC microcapsules are both reduced. This work demonstrates the versatility and feasibility of tuning the formation and stability of polysaccharide microcapsules by physical factors and chitosan chemical structures.
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EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
·
2016
·
IF 3.773
Yashu Yao,Mengxin Xia,Huizhen Wang,Guowen Li,Hongyi Shen,Guang Ji,Qianchao Meng,Yan Xie
A novel nanogel/gel based on chitosan (CS) for the oral delivery of myricetin (Myr) was developed and evaluated comprehensively. The particle size of the obtained Myr-loaded CS/β-glycerol phosphate (β-GP) nanogels was in the range of 100–300 nm. The rheological tests showed that the sol-gel transition happened when the nanogels were exposed to physiological temperatures, and 3D network structures of the gelatinized nanogels (gels) were confirmed by Scanning Electron Microscopy. Myr was released from CS/β-GP nanogel/gel in acidic buffers via a Fickian mechanism, and this release was simultaneously accompanied by swelling and erosion. Moreover, the nanogel/gel exhibited no cytotoxicity by MTT assay, and the oral bioavailability of Myr in rats was improved with an accelerated absorption rate after Myr was loaded into CS/β-GP nanogel/gel. In summary, all of the above showed that CS/β-GP nanogel/gel was an excellent system for orally delivering Myr.
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CHEMICAL ENGINEERING JOURNAL
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2016
·
IF 5.31
Shaopeng Zhang,Yayi Dong,Zhen Yang,Weiben Yang,Jiaqing Wu,Chang Dong
A series of magnetic composite adsorbents with core-brush topology were prepared through grafting co-polymerization on the surface of chitosan/Fe 3 O 4 composite particles (CS-MCP), and then applied for the removal of two pharmaceuticals (diclofenac sodium (DCF) and tetracycline hydrochloride) from water. Adsorption performance evaluation, including adsorption capacities from single- and binary-solute solutions at different pHs, influences of coexisting salts, desorption and reusability, demonstrated CD-MCP with polycationic brushes was a cost-effective adsorbent for DCF removal: Compared to CS-MCP, all the modified MCPs exhibited higher removal efficiencies, due to the enhanced surface areas resulting from core-brush topology; Among the modified MCPs with different surface charges, CD-MCP displayed the highest adsorption capacities, attributed to the electrostatic attraction between the positively charged brushes and the anionic contaminant’s species. Adsorption mechanism was investigated from both the macroscopic (thermodynamics and kinetics) and microscopic (changes of solution pH and spectral analyses of the adsorbent after adsorption) viewpoints: Charge attraction was the intrinsic driving force; A monolayer coverage of pharmaceuticals were adsorbed onto the brushes of CD-MCP; OH − exerted competitive adsorption effect; After adsorption, the originally extended polycationic brushes turned collapsed. The current study provided a strategy for the design of adsorbents from both topological and chemical structures.
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