Box-Behnken效应面法优化羟丙基四氢吡喃三醇脂质体的处方工艺  

Optimization of formulation and preparation for hydroxypropyl tetrahydropyrantriol liposomes using Box-Behnken response surface method

作　　者：何黎黎 王恩龙 张鑫 田生乾 胡明慧 HE Li-li;WANG En-long;ZHANG Xin;TIAN Sheng-qian;HU Ming-hui(School of pharmacy,Southwest Minzu University,Chengdu 610041,China)

机构地区：[1]西南民族大学药学院,四川成都610041

出　　处：《西南民族大学学报(自然科学版)》2024年第6期644-652,共9页Journal of Southwest Minzu University(Natural Science Edition)

基　　金：四川省科技厅青年科学基金项目(2022NSFSC1437);四川省中医药管理局科学技术研究专项课题(2021MS121);西南民族大学中央高校基本科研业务费专项资金项目(ZYN2022040)。

摘　　要：为了提高羟丙基四氢吡喃三醇的皮肤透过性,将羟丙基四氢吡喃三醇制成脂质体,并优化其制备处方及工艺.以脂质体的粒径和包封率作为指标,筛选出了羟丙基四氢吡喃三醇脂质体的制备方法,确定了采用逆向蒸发法制备羟丙基四氢吡喃三醇脂质体;在前期单因素考察的基础上,选取对评价指标影响较显著的磷脂与胆固醇的比例、药脂比和超声时间作为考察对象,以脂质体的粒径和包封率作为指标,通过Box-Behnken效应面法优化处方,得到羟丙基四氢吡喃三醇脂质体的最优处方,所得最佳处方是磷脂与胆固醇比例为4.49∶1,药脂比为0.23∶1,超声时间为7.2 min;制得的脂质体外观良好,平均粒径(93.46±11.81)nm,包封率(67.10±1.83)%,载药量(11.15±0.30)%.In order to improve the skin permeability of hydroxypropyl tetrahydropyrantriol,liposomes were made,and the formu-lation and preparation process were optimized.Using the size and encapsulation rate of the liposomes as indicator,reverse evapo-ration method was used as the preparation method of hydroxypropyl tetrahydropyrantriol liposomes.Based on data of previous single-factor investigation,the ratio of phospholipid to cholesterol,drug-lipid ratio and ultrasound time,which had a significant impact on the evaluation indexes,were selected as the objects of investigation,and the size and encapsulation rate of liposome were taken as the indexes.The Box-Behnken response surface method was used to optimize the formulation.The following opti-mal formula was obtained:phospholipid to cholesterol ratio of 4.49∶1,drug to lipid ratio of 0.23∶1,and ultrasound time of 7.2 minutes.The prepared liposomes had good appearance,with average particle size(93.46±11.81)nm,encapsulation rate(67.10±1.83)%,and drug loading(11.15±0.30)%.

关 键 词：羟丙基四氢吡喃三醇 脂质体 包封率 BOX-BEHNKEN效应面法 

分 类 号：TQ658[化学工程—精细化工] R943[医药卫生—药剂学]