Influence of the poly(lactide-co-glycolide) type on the leuprolide release from in situ forming microparticle systems
Influence of the poly(lactide-co-glycolide) type on the leuprolide release from in situ forming microparticle systems
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DOI：
10.1016/j.jconrel.2005.10.005
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发表时间：
2006-01-10
影响因子：
10.8
通讯作者：
Bodmeier, R
中科院分区：
文献类型：
--
作者：
Luan, XS;Bodmeier, R
目的是研究聚（丙交酯-共-乙交酯）（PLGA）类型（分子量和端基官能度）对亮丙瑞林从原位形成微粒（ISM）系统中释放的影响。ISM系统基于PLGA溶液分散在油相中的乳液。聚合物液滴在与水性流体接触后固化并原位形成微粒。与通过经典溶剂蒸发方法制备的微粒相反，使用较低分子量的PLGA导致ISM具有比用较高分子量的PLGA制备的ISM更低的初始释放。用PLGA组合制备的ISM显示出随着低分子量PLGA含量的增加而降低的初始释放。从低分子量PLGA溶液液滴到释放介质中的较慢溶剂扩散导致所得微粒的多孔结构较少，从而解释了较低的初始释放。与具有酯化端基的PLGA相比，具有游离羧酸端基的PLGA导致较低的药物释放。6-将不同相对分子质量的聚乳酸共混，可得到月控释亮丙瑞林ISM。(c)2005 Elsevier B. V.保留所有权利。
The objective was to investigate the influence of poly(lactide-co-glycolide)(PLGA) type (molecular weight and end-group functionality) on the leuprolide release from in situ forming microparticle (ISM) systems. ISM systems are based on an emulsion of the PLGA solution dispersed in an oil phase. The polymer droplets solidify after contact with aqueous fluids and form microparticles in situ. In contrast to microparticles prepared by the classical solvent evaporation method, the use of the lower molecular weight PLGA resulted in ISM with a lower initial release than ISM prepared with the higher molecular weight PLGA. ISM prepared with PLGA combinations showed a decreasing initial release with increasing low-molecular-weight PLGA content. A slower solvent diffusion from the low-molecular-weight PLGA solution droplets into the release medium led to a less porous structure of the resulting microparticles, thus explaining the lower initial release. PLGA with free carboxylic acid end groups led to a lower drug release compared to PLGA with esterified end groups. 6-month controlled release leuprolide ISM could be obtained by blending poly(lactides) (PLA) with different molecular weights. (c) 2005 Elsevier B.V. All rights reserved.