改良溶剂挥发法制备姜黄素衍生物mPEG_(5000)-PLGA纳米粒的研究

Preparation of curcumin-(oleic acid)_2 loaded mPEG_(5000)-PLGA nanoparticles by modified solvent evaporation method

目的 对改良溶剂挥发法制备姜黄素衍生物Cur（OA）2的聚乙二醇单甲醚-聚乳酸-乙醇酸共聚物[poly-1actide-co- glycolide-co-poly-（ethylene-glycol），mPEG5000-PLGA]纳米粒[Cur（OA）2-NPs]的工艺进行优化，并对Cur（OA）2-NPs加以表征。方法 以包封率、形态、粒径为指标，采用正交设计筛选优化制备工艺。以激光粒度仪和透射电子显微镜分别对Cur（OA）2-NPs的粒径、Zeta电位和形貌进行表征。结果 优化的制备方案：药物Cur（OA）2与载体mPEG5000-PLGA的用量（质量）比为1∶4，有机相与水相溶剂体积比为1∶2；搅拌速率为1 200 r/min，泊洛沙姆188（F68）的用量为0.3%。所得Cur（OA）2-NPs为球形粒子，分布较均匀，平均粒径86.23 nm（粒径范围80～100 nm），Zeta电位为？23.8 mV。结论 改良溶剂挥发法适于载姜黄素衍生物的mPEG5000-PLGA纳米粒子的制备。

Objective To optimize the technological process for the preparation of curcumin-（oleic acid）2 [Cur（OA）2] loaded by mPEG5000-PLGA with modified solvent evaporation method and to characterize the nanoparticles [Cur（OA）2-NPs]. Methods Using entrapment efficiency （EE）, appearance, and particle size as indexes, orthogonal test design was used to optimize the preparation technology. Laser particle size analyzer and transmission electron microscopy （TEM） were carried out to evaluate the Cur（OA）2-NPs size, Zeta potential, and morphological characteristics. Results The optimal preparation conditions for Cur（OA）2-NPs were as follows： Cur（OA）2- mPEG5000-PLGA （1∶4）; organic solvent-aqueous solvent （1∶2）; the stirring speed was 1 200 r/min; Poloxamer 188 （F68） concentration was 0.3%. The Cur（OA）2-NPs were spherical and uniformly distributed, with average particle size 86.23 nm （range of particle size： 80-100 nm） and Zeta potential -23.8 mV. Conclusion The modified solvent evaporation method is suitable to prepare the curcumin derivatives loaded mPEG5000-PLGA NPs.