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用于眼科药物输送的聚(丙烯酸)-聚(乙二醇)纳米粒子。

Poly(acrylic acid)-poly(ethylene glycol) nanoparticles designed for ophthalmic drug delivery.

机构信息

Faculty of Chemical Engineering and Environmental Protection, Gheorghe Asachi Technical University, Iasi, 700050, Romania.

出版信息

J Pharm Sci. 2014 Feb;103(2):676-86. doi: 10.1002/jps.23793. Epub 2013 Dec 19.

Abstract

Poly(acrylic acid) (PAA) and poly(ethylene glycol) (PEG), four-arm, amine-terminated particles with nanometer size and spherical shape were obtained by the polymers cross-linking, via activation with 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide hydrochloride, in a w/o emulsion. The morphology and surface charge of the final particles are strongly dependent on the molar ratio of PAA-PEG and the PAA concentration. The physicochemical characteristics correlated with the drug-loading capacity, in vitro and ex vivo release kinetics of pilocarpine hydrochloride and biocompatibility results indicate that these nanoparticles exhibit the prerequisite behavior for use as carriers of ophthalmic drugs.

摘要

聚(丙烯酸)(PAA)和聚(乙二醇)(PEG),四臂,胺封端的纳米级球形颗粒是通过聚合物交联,用 1-乙基-3-(3-二甲基氨基丙基)碳二亚胺盐酸盐活化得到的,在 w/o 乳液中。最终颗粒的形态和表面电荷强烈依赖于 PAA-PEG 的摩尔比和 PAA 的浓度。与载药能力相关的物理化学特性、盐酸毛果芸香碱的体外和体内释放动力学以及生物相容性结果表明,这些纳米粒子表现出作为眼科药物载体的必要行为。

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