多肽及蛋白类药物微球的载体材料、制备以及突释现象

Carrier materials, preparation and fast release of polypeptide and protein microspheres

多肽及蛋白类药物微球在提高药物的利用度的同时,存在的主要要问题是微球制备过程中药物失活及药物突释而产生的毒副作用。微球进入体内后的突释现象已成为微球控释系统研究者面临的一个急待解决的问题。聚合物的相对分子质量、浓度、结构及载药量/药物含量对药物突释产生重要的影响。采用结构修饰、聚合物联用、选用添加剂、控制微球粒径、降低微球载药量等方法控制突释程度取得一定效果。

Polypeptide and protein microspheres can elevate drug availability, but drug devitalization and drug fast release can result in side effects during microsphere preparation. Fast release in the body is a burning question facting investigators who studying microsphere controlled release system. Relative molecular mass, concentration, structure and drug content of the polymer can greatly affect drug fast release. Fast release can be controlled by structural modification, using additives, controlling particle diameter of microspheres and decreasing drug content.