The Graduate School of Nanoscience and Technology, Korea Advanced Institute of Science and Technology (KAIST), 291 University Rd, Daejeon, 305-701, South Korea.
Biotechnol Prog. 2014 Jan-Feb;30(1):215-23. doi: 10.1002/btpr.1835. Epub 2013 Nov 27.
The effective controlled release of small hydrophilic drugs from poly(d,l-lactic-co-glycolic acid) (PLGA) microspheres has remained a challenge, largely due to the difficulty of loading a large amount of the drug inside the microspheres, owing to the hydrophilicity of the drugs. This study provides a new strategy for increasing encapsulation of small hydrophilic drugs inside PLGA microspheres by utilizing noncovalent, physical adsorption between hydrophilic drugs and emulsifying polymers of poly(vinyl alcohol) and pluronic. An order of magnitude increase in drug loading efficiency from 2.7 to 18.6% for dopamine, a model small hydrophilic drug, was achieved. The large amount of dopamine-loaded PLGA formulation herein could be useful for the treatment of Parkinson's disease.
从聚(丙交酯-乙交酯)(PLGA)微球中有效控制释放小亲水性药物一直是一个挑战,主要是由于药物的亲水性,使得大量药物载入微球内部具有一定难度。本研究提供了一种新的策略,通过利用亲水性药物与聚乙烯醇和泊洛沙姆的乳化聚合物之间的非共价、物理吸附,来增加小亲水性药物在 PLGA 微球中的包封率。以多巴胺(一种模型小亲水性药物)为例,药物载药效率从 2.7%提高到 18.6%,提高了一个数量级。本文中大量载多巴胺的 PLGA 制剂可用于治疗帕金森病。