黄芩素PLGA纳米粒的制备及制剂学性质研究

Preparation and character in pharmacy of Scutellarein loaded PLGA nanoparticles

[目的]优化影响黄芩素聚乳酸/羟基乙酸共聚物(PLGA)纳米粒成型工艺参数,并评价优化工艺后所制纳米粒的制剂学性质。[方法]采用乳化-溶剂挥发法制备黄芩素PLGA纳米粒,以粒径、包封率为评价指标,单因素实验考察了聚乙烯醇(PVA)浓度、PLGA型号、PLGA分子量、PLGA浓度、水相与有机相体积比、丙酮与无水乙醇体积比、药物与PLGA的比例共7个参数对纳米粒成型工艺的作用规律。[结果]优化处方工艺制备的纳米粒包封率为(95.03±1.33)%、平均粒径为(126.80±4.50)nm、Zeta电位(-21.30±0.23)mV。[结论]乳化-溶剂挥发法制备的黄芩素PLGA纳米粒圆整,粒径均一。

[Objective] To optimize the processing parameters of Scutellarein loaded PLGA nanoparticles （PLGANP） and study the character in pharmacy of the optimal Seutellarein-PLGANP. [Methods] Seven processing parameters were assessed systematically to enhance the Scutellarein incorporation into PLGA nanoparticles and to minimize the panicle size,including PVA concentration in the aqueous phase, PLGA models, PLGA molecular mass, PLGA concentration in the organic phase, aqueous phase/organic phase volume ratio, acetone/ethanol volume ratio, Scutellarein/ PLGA mass ratio. [Results] The Seutellarein-PLGANP produced by the optimal formulation were submicron size of （126.80±4.50） nm and the zeta potential was （-21.30±0.23） mV, with the entrapment efficiency of （95.03± 1.33）%. [Conclusion] Scutellarein drug loaded PLGANP can be prepared by O/W emulsion solvent evaporation.