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一种蛋白质递送系统:可生物降解的藻酸盐-壳聚糖-聚(乳酸-乙醇酸)复合微球。

A protein delivery system: biodegradable alginate-chitosan-poly(lactic-co-glycolic acid) composite microspheres.

作者信息

Zheng Cai-Hong, Gao Jian-Qing, Zhang Ye-Ping, Liang Wen-Quan

机构信息

Department of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310031, China.

出版信息

Biochem Biophys Res Commun. 2004 Oct 29;323(4):1321-7. doi: 10.1016/j.bbrc.2004.09.007.

Abstract

In the present study we developed alginate-chitosan-poly(lactic-co-glycolic acid) (PLGA) composite microspheres to elevate protein entrapment efficiency and decrease its burst release. Bovine serum albumin (BSA), which used as the model protein, was entrapped into the alginate microcapsules by a modified emulsification method in an isopropyl alcohol-washed way. The rapid drug releases were sustained by chitosan coating. To obtain the desired release properties, the alginate-chitosan microcapsules were further incorporated in the PLGA to form the composite microspheres. The average diameter of the composite microcapsules was 31+/-9microm and the encapsulation efficiency was 81-87%, while that of conventional PLGA microspheres was just 61-65%. Furthermore, the burst releases at 1h of BSA entrapped in composite microspheres which containing PLGA (50:50) and PLGA (70:30) decreased to 24% and 8% in PBS, and further decreased to 5% and 2% in saline. On the contrary, the burst releases of conventional PLGA microspheres were 48% and 52% in PBS, respectively. Moreover, the release profiles could be manipulated by regulating the ratios of poly(lactic acid) to poly(glycolic acid) in the composite microspheres.

摘要

在本研究中,我们制备了海藻酸盐-壳聚糖-聚乳酸-羟基乙酸共聚物(PLGA)复合微球,以提高蛋白质包封效率并减少其突释。以牛血清白蛋白(BSA)作为模型蛋白,通过改良乳化法以异丙醇洗涤的方式将其包封于海藻酸盐微囊中。壳聚糖包衣可延缓药物的快速释放。为获得理想的释放特性,将海藻酸盐-壳聚糖微囊进一步与PLGA复合形成复合微球。复合微囊的平均直径为31±9μm,包封率为81%-87%,而传统PLGA微球的包封率仅为61%-65%。此外,含PLGA(50:50)和PLGA(70:30)的复合微球中包封的BSA在PBS中1小时的突释率分别降至24%和8%,在生理盐水中进一步降至5%和2%。相反,传统PLGA微球在PBS中的突释率分别为48%和52%。此外,通过调节复合微球中聚乳酸与聚乙醇酸的比例,可以控制释放曲线。

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