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目的:制备槲皮素-(聚乳酸-羟基乙酸共聚物)嵌段共聚物(QC-PLGA)纳米粒冻干粉并考察其体外释放规律。方法:采用乳化溶剂挥发法制备QC-PLGA纳米粒,通过正交试验确定最优处方工艺,通过单因素试验筛选冻干保护剂,通过动态透析技术考察QC-PLGA纳米粒冻干粉的体外释药规律。结果:最佳制备工艺为0.2%聚乙烯醇,PLGA质量浓度10 g·L~(-1),油/水相体积比1∶35,槲皮素用量5 mg,冻干保护剂为2%乳糖。QC-PLGA纳米粒冻干粉的外表光滑,形态无皱缩塌陷、结构致密且加入注射用水振摇后再分散性良好,体外释放规律基本符合Weibull方程的释药模型,释药动力学方程ln[ln(1/1-Q)]=0.399lnt-1.503(R~2=0.973)。结论:QC-PLGA纳米粒冻干粉制备工艺简单可行、性质稳定、易储存,相比槲皮素原料药具有明显的缓释作用。
OBJECTIVE: To prepare the freeze-dried powder of quercetin-poly (lactic-co-glycolic acid) block copolymer (QC-PLGA) nanoparticles and investigate their in vitro release patterns. Methods: QC-PLGA nanoparticles were prepared by emulsion solvent evaporation method. The optimal prescription was determined by orthogonal test. The lyoprotectant was screened by single factor test and the release of QC-PLGA nanoparticle freeze-dried powder in vitro by dynamic dialysis Drug law. Results: The optimum preparation conditions were as follows: 0.2% polyvinyl alcohol, PLGA 10 g · L -1, volume ratio of oil to water 1:35, dosage of quercetin 5 mg, lyoprotectant 2% lactose. QC-PLGA nanoparticle freeze-dried powder has a smooth appearance and no collapsing collapse in morphology, and has a compact structure and good dispersibility after being shaken by water for injection. The in vitro release pattern basically meets the Weibull equation release model, and the release kinetic equation ln [ln (1/1-Q)] = 0.399lnt-1.503 (R-2 = 0.973). Conclusion: The preparation process of QC-PLGA nanoparticle freeze-dried powder is simple and feasible, stable in nature, easy to store, and has a significant slow-release effect compared to quercetin API.