影响蛋白质药物在聚乳酸-羟基乙酸微球制备过程中稳定性与增加累积释放的方法

Formulation Aspects of Protein Stability and Complete Release in Poly (Lactic-co-glycolic acid) Microspheres

目的介绍增加乳酸-羟基乙酸聚合物(PLGA)蛋白微球中药物稳定性与蛋白累积释放量的方法。方法根据国内外文献,较全面地总结了PLGA微球中稳定蛋白,解决不完全释放的策略。结果与结论虽然PLGA微球制备与药物释放过程中存在不利于蛋白稳定的因素,但通过选用不同添加剂、优化体外释放介质及装置、改进制备工艺、开发复合材料及复合微球等方法可以有效保存其活性,增加累积释放量。

OBJECTIVE To give a brief introduction of methods which can stabilize encapsulated protein and increase the cumulative release of protein from PLGA microspheres. METHODS On the base of literatures at home and abroad, strategies to improve the stability of protein and facilitate its complete release were generally summarized here. RESULTS AND CONCLUSION Although proteins are unstable in PLGA, by choosing proper additives, optimizing release device and medium in vitro＇, improving the technique of microspheres fabrication, employing composite polymers, we can preserve their activities and solve the problem of incomplete release.