[关键词]
[摘要]
目的 优化丁香苦苷聚乳酸(Syr)-羟基乙酸共聚物[poly(lactic-co-glycolic acid),PLGA] 纳米粒(Syr-NPs)的处方。方法 采用纳米沉淀法制备Syr-NPs,以包封率、载药量、平均粒径以及总评"归一值"为评价指标,采用星点设计-效应面法考察PLGA质量浓度(A)、丁香苦苷质量浓度(B)、水相与有机相比例(C)3因素考察对包封率、载药量、平均粒径以及总评归一值的影响,以星点设计-效应面法选取最佳处方条件进行预测分析。结果 最优处方工艺为PLGA质量浓度为9.63 mg/mL,Syr质量浓度为12.88 mg/mL,有机相与水相的比例为1:9.46,制得的Syr-NPs的包封率、载药量、平均粒径分别为(27.86±0.87)%、(7.02±0.15)%、(110.0±1.20)nm。结论 该方法稳定可行,可用于优化包载Syr的PLGA纳米粒处方与制备工艺。
[Key word]
[Abstract]
Objective To optimize the formulation of syringopicrosides poly (lactic-co-glycolic acid, PLGA) nanoparticles (Syr-NPs). Methods Syr-NPs were prepared by nanoprecipitation method. The encapsulation efficiency (EE), drug loading (DL), average particle size and general evaluation "normalized value" were used as evaluation indexes. The central composite design was used to inspect the effects of the concentration of PLGA (A), the concentration of syringopicrosides (B), the ratio of aqueous phase to organic phase (C) on three evaluation indexes mentioned above and the "normalized value" ofgeneral evaluation. Prediction and analysis for selecting the best prescription condition were carried out by using the central composite design-response surface method. Results The concentration of PLGA, the concentration of syringopicrosides and the ratio of aqueous phase to organic phase according to the optimized prescription were 9.63 mg/mL, 12.88 mg/mL and 1:9.46, respectively; And the EE, drug loading and average particle diameter of Syr-NPs prepared according to the optimized prescription were (27.86 ±0.87)%, (7.02 ±0.15)%, and (110.0 ±1.20) nm, respectively. Conclusion This method is stable and feasible and can be used to optimize the formulation and preparation process of syringopicrosides wrapped inside with PLGA nanoparticles.
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[基金项目]
国家自然科学基金面上项目(81703719);中国博士后项目(2018W631);黑龙江省自然科学基金项目(H2018050);黑龙江省自然科学基金项目(LH2019H102)