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壳聚糖/有机改性坡缕石微球的制备及药物释放性能。

Preparation and drug release properties of chitosan/organomodified palygorskite microspheres.

机构信息

Key Laboratory for Palygorskite Science and Applied Technology of Jiangsu Province, School of Life Science and Chemical Engineering, Huaiyin Institute of Technology, Huaian 223003, China.

Key Laboratory for Palygorskite Science and Applied Technology of Jiangsu Province, School of Life Science and Chemical Engineering, Huaiyin Institute of Technology, Huaian 223003, China.

出版信息

Int J Biol Macromol. 2014 Jul;68:107-12. doi: 10.1016/j.ijbiomac.2014.04.030. Epub 2014 Apr 24.

DOI:10.1016/j.ijbiomac.2014.04.030
PMID:24769084
Abstract

The novel composite microspheres, based on the hybridization of chitosan (CS) and organomodified palygorskite (OPAL), were prepared by emulsion cross-linking technique and applied as a drug carrier. Palygorskite, a kind of natural one-dimensional clay, was modified with hexadecyl betaine (BS-16) to improve the compatibility and affinity with chitosan matrix, and worked as a perfect micron-filler to enhance drug encapsulation and retard drug migration. The structure of the microspheres was characterized by fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and X-ray diffraction (XRD) techniques. The swelling behavior of the microspheres and the effect of the amount of OPAL and BS-16 on the properties of the drug loading and releasing have been investigated. Compared to the pure chitosan microspheres (CM), the composite one with 20wt% OPAL modified by 20mmol/100g BS-16 possessed the higher encapsulation efficiency and the slower and continuous cumulative release for diclofenac sodium (DS) in phosphate buffer solution (pH 6.8). The study of drug release kinetics in vitro found that the drug release mechanism of the microspheres changed from the simple diffusion-control to diffusion and dissolution-control as the OPAL content in matrix increased from 0 to 20wt%.

摘要

新型复合微球基于壳聚糖(CS)和有机改性凹凸棒石(OPAL)的杂交,通过乳液交联技术制备,并用作药物载体。凹凸棒石是一种天然的一维粘土,用十六烷基甜菜碱(BS-16)改性以提高与壳聚糖基质的相容性和亲和力,并作为完美的微米填料,增强药物包封和延缓药物迁移。微球的结构通过傅里叶变换红外光谱(FT-IR)、扫描电子显微镜(SEM)和 X 射线衍射(XRD)技术进行了表征。研究了微球的溶胀行为以及 OPAL 和 BS-16 的用量对载药和释放性能的影响。与纯壳聚糖微球(CM)相比,用 20mmol/100g BS-16 改性的 20wt%OPAL 的复合微球具有更高的包封效率和更慢且连续的累积释放,用于在磷酸盐缓冲溶液(pH 6.8)中释放双氯芬酸钠(DS)。体外药物释放动力学研究表明,随着基质中 OPAL 含量从 0 增加到 20wt%,药物释放机制从简单的扩散控制转变为扩散和溶解控制。

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