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用于控释给药的壳聚糖微粒的制备与表征

Preparation and characterization of chitosan microparticles intended for controlled drug delivery.

作者信息

Ko J A, Park H J, Hwang S J, Park J B, Lee J S

机构信息

Graduate School of Biotechnology, Korea University, Seoul 136-701, South Korea.

出版信息

Int J Pharm. 2002 Dec 5;249(1-2):165-74. doi: 10.1016/s0378-5173(02)00487-8.

Abstract

Chitosan microparticles were prepared with tripolyphosphate (TPP) by ionic crosslinking. The particle sizes of TPP-chitosan microparticles were in range from 500 to 710 microm and encapsulation efficiencies of drug were more than 90%. The morphologies of TPP-chitosan microparticles were examined with scanning electron microscopy. As pH of TPP solution decreased and molecular weight (MW) of chitosan increased, microparticles had more spherical shape and smooth surface. Release behaviors of felodipine as a model drug were affected by various preparation processes. Chitosan microparticles prepared with lower pH or higher concentration of TPP solution resulted in slower felodipine release from microparticles. With decreasing MW and concentration of chitosan solution, release behavior was increased. The release of drug from TPP-chitosan microparticles decreased when cross-linking time increased. These results indicate that TPP-chitosan microparticles may become a potential delivery system to control the release of drug.

摘要

采用离子交联法,用三聚磷酸钠(TPP)制备了壳聚糖微粒。TPP-壳聚糖微粒的粒径范围为500至710微米,药物包封率超过90%。用扫描电子显微镜检查了TPP-壳聚糖微粒的形态。随着TPP溶液pH值降低和壳聚糖分子量(MW)增加,微粒形状更接近球形,表面更光滑。作为模型药物的非洛地平的释放行为受各种制备工艺的影响。用较低pH值或较高浓度的TPP溶液制备的壳聚糖微粒导致非洛地平从微粒中的释放较慢。随着壳聚糖溶液分子量和浓度的降低,释放行为增强。交联时间增加时,药物从TPP-壳聚糖微粒中的释放减少。这些结果表明,TPP-壳聚糖微粒可能成为一种控制药物释放的潜在给药系统。

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