文献类型：期刊文献

中文题名：积雪草苷微乳凝胶的制备与体外透皮研究

英文题名：Preparation of the asiaticoside loaded microemulsion-based gel and its transdermal delivery in vitro

作者：熊慧敏[1];杨响光[2];张琳[1]

第一作者：熊慧敏

机构：[1]北京联合大学特殊教育学院;[2]中国中医科学院广安门医院

第一机构：北京联合大学特殊教育学院

年份：2019

卷号：34

期号：1

起止页码：27-32

中文期刊名：华西药学杂志

外文期刊名：West China Journal of Pharmaceutical Sciences

收录：CSTPCD;;CSCD:【CSCD_E2019_2020】；

语种：中文

中文关键词：积雪草苷;微乳凝胶;卡波姆940;伪三元相图;单纯网格实验设计;Franz扩散池法;透皮吸收;累积透皮量

外文关键词：Asiaticoside;Microemulsion -based gel;Carbomer 940;Pseudo -ternary phase diagram;Simplex lattice experiment design;Franz diffusion cell;Transdermal delivery;Accumulation transdermal amount

摘要：目的制备积雪草苷微乳凝胶,并考察其体外透皮性能。方法考察积雪草苷在不同油、乳化剂、助乳化剂中的平衡溶解度,通过伪三元相图法最终确定积雪草苷微乳的处方组成;分别以玉米油、Smix、水作为考察因素,以形成微乳的平均粒径作为评价指标,利用单纯网格实验设计优化积雪草苷微乳的处方;在透射电镜下观察积雪草苷微乳的微观形态,测定粒径分布、PDI及Zeta电位;以卡波姆940为基质制备积雪草苷微乳凝胶,并采用Franz扩散池法考察了积雪苷霜软膏、微乳及微乳凝胶的体外透皮吸收性能。结果优选积雪草苷微乳的处方组成为:玉米油为15. 2%、Smix为66. 2%、水为18. 6%;透射电镜下观察到积雪草苷微乳呈圆整、规则球形,粒径分布较为均匀,平均粒径为57. 8±3. 6nm,PDI为0. 172±0. 03,Zeta电位为-19. 6±0. 9 m V;积雪草苷微乳和微乳凝胶在12 h时内的药物累积透皮量显著高于积雪苷霜软膏,皮肤内药物滞留量分别是积雪苷霜软膏的3. 3、6. 7倍。结论积雪草苷微乳凝胶可以显著增加药物的累积透皮量,提高药物在皮肤中的滞留量,有望成为积雪草苷的新型局部给药制剂。
OBJECTIVE To prepare the asiaticoside loaded microemulsion -based gel and to investigate its transdermal delivery in vitro.METHODS The solubility of asiaticoside in different oils,emulsifiers and co -emulsifiers was investigated by equilibrium solubility experiments.The formulation composition of asiaticoside microemulsion was determined by Pseudo -ternary phase diagram.By setting the average particle size as dependent variables whilst corn oil,Smix and water as the independent variables,a Simplex Lattice experiment design was used to optimize the asiaticoside loaded microemulsion formulation.The microscopic morphology of asiaticoside loaded microemulsion was observed by transmission electron microscopy,and the particle size distribution,PdI and Zeta potential were determined.The asiaticoside loaded microemulsion -based gel was prepared with Carbomer 940 as a matrix.The in vitro transdermal absorption properties of asiaticoside cream,asiaticoside loaded microemulsion and microemulsion -based gel were investigated by Franz diffusion cell method.RESULTS The composition of the asiaticoside microemulsion was as follows:corn oil was 15.2%;Smix was 66.2% and water was 18.6%.Under the transmission electron microscope,the asiaticoside microemulsion was round and regular spherical,and the particle size distribution was uniform.The average particle size was 57.8±3.6 nm,PDI was 0.172 ±0.013 and Zeta potential was -19.6±0.9 mV.The drug accumulation transdermal amount of asiaticoside microemulsion and the microemulsion -based gel were significantly higher than that of asiaticoside cream after 12 h.The drug retention in the skin were 3.3 and 6.7 fold of asiaticoside cream,respectively. CONCLUSION Asiaticoside loaded microemulsion -based gel can significantly increase the cumulative transdermal delivery of drugs and increase the retention of drugs in the skin.It is expected to be a novel vehicle for the topical use of asiaticoside.