羧甲基氧基琥珀酸改性聚乳酸-聚乙二醇共聚物制成的微粒的合成与表征

Synthesis and characterization of microparticles made of carboxymethyloxysuccinic-acid-modified PLA-PEG co-polymer.

作者信息

Zhang Haiyue, Chang Li, Zhang Bin, Li Peng, Wang Min, Yao Kang De, Yang Jun, Yao Fanglian

机构信息

Research Institute of Polymeric Materials, Tianjin University, Tianjin 300072, PR China.

出版信息

J Biomater Sci Polym Ed. 2008;19(1):99-111. doi: 10.1163/156856208783227677.

DOI:10.1163/156856208783227677

PMID:18177557

Abstract

A novel tri-block co-polymer, HO2C-PLA-PEG-PLA-CO2H (co-polymer II), with polybasic carboxylic acids as the end-groups was synthesized and characterized by IR and 1H-NMR. Based on the successful synthesis of co-polymer II, water-soluble sodium salicylate and oil-soluble tetrandrine, used as model drugs, were loaded in the co-polymer microparticles prepared through a modified multiple emulsion method. The encapsulation efficiency and drug-releasing behaviour were also investigated. It is found that the microparticles of about 10 microm in size are porous and can be produced from co-polymer II in better encapsulation efficiency (up to 86.65% and 55.94%) compared to those made from PLA/PEG/PLA (co-polymer I) (77.50% and 44.01%). The drug-release behaviour of co-polymer II exhibits an extended continuous release behaviour and the initial burst was reduced obviously. The results show that such functionalised PLA/PEG/PLA carrier provides higher drug encapsulation efficiency and better profiles.

摘要

合成了一种新型的三嵌段共聚物HO2C-PLA-PEG-PLA-CO2H（共聚物II），其端基为多元羧酸，并通过红外光谱和1H-NMR对其进行了表征。基于共聚物II的成功合成，将水溶性的水杨酸钠和油溶性的粉防己碱作为模型药物，载入通过改进的复乳法制备的共聚物微粒中。还研究了包封率和药物释放行为。结果发现，与由PLA/PEG/PLA（共聚物I）制成的微粒（77.50%和44.01%）相比，由共聚物II制成的尺寸约为10微米的微粒具有多孔性，且包封率更高（高达86.65%和55.94%）。共聚物II的药物释放行为表现出延长的持续释放行为，初始突释明显减少。结果表明，这种功能化的PLA/PEG/PLA载体具有更高的药物包封率和更好的性能。