盐酸青藤碱-聚乳酸/羟基乙酸共聚物缓释微球制备工艺的研究

Study on the preparation of poly( lactic-co-glycolic acid) microspheres containing sinomenine hydrochloride

目的制备盐酸青藤碱(SM)-PLGA缓释微球。方法以PLGA为骨架材料,采用油包油乳化-溶剂挥发法制备盐酸青藤碱-PLGA缓释微球,以粒径、载药量为评价指标经正交试验筛选最优工艺;应用显微镜、扫描电镜、差示扫描量热分析等手段对微球进行表征,用高效液相色谱法测定微球载药量。结果正交试验最优工艺条件:Span80的质量分数为1%、溶剂挥发时间为6 h、PLGA摩尔质量为20 000 g/mol、SM与PLGA质量比为1∶5、转速为700 r/min、PLGA质量浓度为80 mg/m L;按最优工艺制备所得微球圆整,平均粒径为7.90μm,载药量为4.54%。结论采用油包油乳化-溶剂挥发法制备盐酸青藤碱-聚乳酸/羟基乙酸共聚物微球有较高载药量,具有较大的应用前景。

Objective To prepare poly（ lactic-co-glycolic acid）（ PLGA） microspheres containing sinomenine hydrochloride（ SM）. Methods Microspheres were prepared from PLGA using an oil-in-oil（ O / O） solvent evaporation method. An orthogonal test was designed to optimize the process with particle size and drug loading as indices. Microspheres were characterized with a microscope,scanning electron microscopy and differential scanning calorimetry analysis,and the drug loading was measured by HPLC. Results The optimum method was as follows： 1% Span80,6 hours of solvent evaporation,20 000 g / mol of PLGA molecular weight,1∶ 5 weight ratio of SM to PLGA,700 r / min emulsification speed and 80 mg / m L PLGA concentration. Microspheres were round with an average particle size of 7. 90 μm and 4. 54% drug loading. Conclusion The PLGA microspheres containing sinomenine hydrochloride prepared using this O /O solvent evaporation method had an advantage of higher drug loading and good application prospect.