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新型泊洛沙姆-壳聚糖胶束作为眼部给药系统。

Novel pluronic-chitosan micelle as an ocular delivery system.

机构信息

Department of Chemical and Materials Engineering, Southern Taiwan University of Science and Technology, Tainan 710, Taiwan.

出版信息

J Biomed Mater Res B Appl Biomater. 2013 Jul;101(5):689-99. doi: 10.1002/jbm.b.32871. Epub 2013 Jan 29.

Abstract

Pluronic micelles were prepared for ophthalmic delivery by incorporation of ethyl acetate as a dispersion agent and their surfaces were modified by chitosan to improve their bioavailability. The micelles disperse well in the solution and have a core-shell like structure with a particle size ranging from 93 to 181 nm for drug unloaded, 123-232 nm for drug-loaded, and a zeta potential between 6.1 and 9.2 mV, indicating very suitable use as ophthalmic carrier. The in vitro serum stability tests indicate the particle size of the micelles was very stable during the serum absorption. The turbidity test reveals that the prepared micelles were very stable under phosphate buffered saline environment, which can prevent the blurred vision. The loading efficiency of metipranolol in micelles can be as high as 83%. Finally, the in vitro and in vivo studies indicate the pluronic micelles modified by chitosan have sustained release behavior and good pharmacological response. As the results, the pluroic-chitosan micelles system provides a potential opportunity in decreasing frequency of administration and improving patient compliance for ocular drug delivery.

摘要

Pluronic 胶束通过加入乙酸乙酯作为分散剂来制备用于眼部给药,并用壳聚糖对其表面进行修饰以提高其生物利用度。胶束在溶液中分散良好,具有核壳结构,载药胶束的粒径为 93 至 181nm,未载药胶束的粒径为 123 至 232nm,zeta 电位在 6.1 至 9.2mV 之间,表明非常适合用作眼部载体。体外血清稳定性试验表明,胶束的粒径在血清吸收过程中非常稳定。浊度试验表明,所制备的胶束在磷酸盐缓冲盐环境下非常稳定,可防止视力模糊。米替泼龙在胶束中的载药量可高达 83%。最后,体外和体内研究表明,壳聚糖修饰的 Pluronic 胶束具有持续释放行为和良好的药理反应。结果表明,pluroic-壳聚糖胶束系统为减少眼部药物给药的给药频率和提高患者依从性提供了潜在机会。

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