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
何黎黎 1王恩龙 1张鑫 1田生乾 1胡明慧1
作者信息
- 1. 西南民族大学药学院,四川成都 610041
- 折叠
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)％.
Abstract
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Key words
hydroxypropyl tetrahydropyrantriol/liposome/encapsulation efficiency/Box-Behnken response surface methodology引用本文复制引用
出版年
2024
NETL
NSTL
万方数据