聚唾液酸修饰的白藜芦醇亚微乳的制备与优化  

Preparation and optimization of polisialic acid modified resveratrol submicroemulsion

作　　者：沈琳暄 熊婷婷 鲁丹丹 敖莎 俞燕娜 朱柯武 骆翔 SHEN Linxuan;XIONG Tingting;LU Dandan;AO Sha;YU Yanna;ZHU Kewu;LUO Xiang(Shaoxing University,Shaoxing 312000,China;Affiliated Hospital of Shaoxing University,Shaoxing 312000,China)

机构地区：[1]绍兴文理学院,浙江绍兴312000 [2]绍兴文理学院附属医院,浙江绍兴312000

出　　处：《中国药剂学杂志（网络版）》2023年第2期57-70,共14页Chinese Journal of Pharmaceutics：Online Edition

基　　金：浙江省大学生科技创新活动计划暨新苗人才计划(2021R432011);绍兴文理学院校级重点科研项目(2020LG1002,2020LG1008)。

摘　　要：目的制备白藜芦醇亚微乳制剂并采用星点设计效应面法对处方进行优化,获得最优处方。方法以中链甘油三酸酯(MCT)为油相,聚唾液酸-十八胺(PSA-C18)为乳化剂,大豆卵磷脂(SPC-98A)为助乳化剂,采用超声法制备白藜芦醇亚微乳。并采用星点设计效应面法,以离心稳定常数(Ke)与药物总含量(Con)为考察指标作响应面,通过粒径、Zeta电位和透射电子显微镜的测定,筛选出最佳处方和制备工艺。结果制备的白藜芦醇亚微乳制剂离心稳定常数相对较小,药物总含量相对较高,且制备的白藜芦醇乳剂具有较高稳定性。确定最优处方为:1%白藜芦醇、5%MCT、0.5%PSA-C18、0.1%SPC-98A。白藜芦醇亚微乳的平均粒径为(93.7±3.5)nm,多分散指数(PDI)为0.295,Zeta电位为(-36.7±2.7)mV。Objective Resveratrol sub-microemulsion formulations were prepared and the prescriptions were optimized using the central composite design response surface method to obtain optim al prescriptions.Methods The resveratrol sub-microemulsions were prepared by ultrasonication using medium chain triglyceride(MCT)as the oil phase,Polysialic acid-octadecylamine(PSA-C18)as the emulsifier,Soy lecithin(SPC-98A)as the co-emulsifier,and the response surface was determined by centrifugal stability constant(Ke)and total drug content(Con)using the central composite design response surface method.The optimum prescription and preparation process were determined by particle size,Zeta potential and transmission electron microscopy.Results Based on the relatively small centrifugal stability constant,the relatively high total drug content and the high stability of the resveratrol emulsions were prepared.The optimal prescription included:1%resveratrol,5%MCT,0.5%PSA-C18,0.1%Soy lecithin(SPC-98A).Under these conditions,the average particle size of the resveratrol sub-microemulsion was(93.7±3.5)nm,the polydispersity index(PDI)was 0.295 and the Z eta potential was(-36.7±2.7)mV.

关 键 词：白藜芦醇 聚唾液酸-十八胺 亚微乳 星点设计效应面法 中心复合试验 

分 类 号：R94[医药卫生—药剂学]