BSA-PLGA缓释微球制备工艺的优化

Optimization of preparation of BSA-PLGA controlled-release microspheres

目的:以牛血清白蛋白(BSA)为模型蛋白,乳酸/羟乙酸共聚物(PLGA)为载体,优化微球的制备工艺。方法:采用复乳溶剂挥发法制备BSA-PLGA微球,以包封率、载药量、粒径及24h释放率等为观察指标,通过正交设计法优化显著影响微球制备工艺条件的7种因素。结果:优化后的工艺条件是BSA用量为5mg、PEG用量为0.2mL、PLGA用量为200mg、PVA浓度为1%、NaCl浓度为10%、超声功率为40W、复乳搅拌速度为1000r/min。结论:该制备工艺简单、稳定,可以得到包封率高、粒径适宜、突释较少的BSA-PLGA微球。

Objective To optimize the preparation technique for microspheres using BSA as model protein and PLGA as controlled-release carrier. Methods BSA-PLGA microspheres were prepared using （water-in-oil） in water emulsion solvent evaporation technique. Using entrapment effciency, loading effciency , particle size, and 24 h-release amount as the evaluating indicators, we optimized the 7 factors that markedly influenced the preparation technique for microspheres by orthogonal factorization method. Results The optimized parameters were BSA of 5 rag, PEG of 0.2 mL, PLGA of 200 rag, 1% PVA, 10% NaCl, ultrasonic power of 40 W, and stirring rate of secondary emulsion of 1 000 r·min^-1. Conclusions The preparation technique for BSA-PLGA microspheres is simple and stable, by which we can acquire the microspheres with high entrapment efficiency, low burst release amount, and proper particle size.