McGinity JW, O'Donnell PB
Drug Dynamics Institute, College of Pharmacy, The University of Texas at Austin, Austin, TX, 78712-1074, USA
Adv Drug Deliv Rev. 1997 Oct 13;28(1):25-42. doi: 10.1016/s0169-409x(97)00049-5.
The microencapsulation process in which the removal of the hydrophobic polymer solvent is achieved by evaporation has been widely reported in recent years for the preparation of microspheres and microcapsules based on biodegradable polymers and copolymers of hydroxy acids. The properties of biodegradable microspheres of poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) have been extensively investigated. The encapsulation of highly water soluble compounds including proteins and peptides presents formidable challenges to the researcher. The successful encapsulation of such entities requires high drug loading in the microspheres, prevention of protein degradation by the encapsulation method, and predictable release of the drug compound from the microspheres. To achieve these goals, multiple emulsion techniques and other innovative modifications have been made to the conventional solvent evaporation process.
近年来,通过蒸发去除疏水性聚合物溶剂的微囊化工艺已被广泛报道,用于制备基于可生物降解聚合物和羟基酸共聚物的微球和微囊。聚乳酸(PLA)和聚乳酸-乙醇酸共聚物(PLGA)的可生物降解微球的性质已得到广泛研究。对包括蛋白质和肽在内的高水溶性化合物进行包封,给研究人员带来了巨大挑战。成功包封此类物质需要微球具有高载药量,包封方法能防止蛋白质降解,以及药物化合物能从微球中实现可预测的释放。为实现这些目标,对传统溶剂蒸发工艺进行了多重乳液技术及其他创新性改进。