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通过优化和比较评价依托度酸囊泡凝胶的经皮给药设计。

Design by optimization and comparative evaluation of vesicular gels of etodolac for transdermal delivery.

机构信息

a Department of Pharmaceutical Technology , AU College of Pharmaceutical Sciences, Andhra University , Visakhapatnam , India.

b Department of Chemistry , GITAM Institute of Technology, GITAM (Deemed to be University) , Visakhapatnam , India.

出版信息

Drug Dev Ind Pharm. 2019 Apr;45(4):611-628. doi: 10.1080/03639045.2019.1569030. Epub 2019 Feb 4.

DOI:10.1080/03639045.2019.1569030
PMID:30712433
Abstract

Aim of the present study was to design vesicular gels of etodolac loaded liposomes and ethosomes for effective transdermal delivery. The physicochemical properties of vesicular gels were compared with 45% v/v ethanolic etodolac solution and commercial product (PROXYM®). The liposomes were prepared by film hydration technique whereas ethosomes were prepared by cold method respectively. Both the systems were characterized for various physicochemical properties. The size range of liposomes shows 186 nm-363 nm whereas for ethosomes 170 nm-261 nm respectively. The zeta potential of optimized liposomes and ethosomes was found to be -36.5 mV and -48.3 mV, respectively. The highest %EE of liposomes and ethosomes shows 71.5% and 78.5%, respectively. The permeation of liposomes shows in the range of 67.50%-86.06% whereas ethosomes shows 52.30%-99.49%, respectively. The optimization was done by 3 experimental design. The optimized vesicular dispersions were subjected to gel preparation using carbopol 940 NF. The prepared liposomal gel (ETO-LG) and ethosomal gel (ETO-EG) were optimized and characterized. The vesicular gels showed desirable results compared to other test formulations.

摘要

本研究旨在设计载有依托度酸的囊泡凝胶,包括脂质体囊泡凝胶和醇质体囊泡凝胶,以实现有效的经皮给药。将囊泡凝胶的理化性质与 45%v/v 乙醇依托度酸溶液和市售产品(PROXYM®)进行比较。脂质体通过薄膜水化技术制备,而醇质体通过冷法制备。分别对两种系统进行各种理化性质的表征。脂质体的粒径范围为 186nm-363nm,而醇质体的粒径范围为 170nm-261nm。优化后的脂质体和醇质体的 zeta 电位分别为-36.5mV 和-48.3mV。脂质体和醇质体的最高载药量分别为 71.5%和 78.5%。脂质体的渗透范围为 67.50%-86.06%,而醇质体的渗透范围为 52.30%-99.49%。通过 3 次实验设计进行优化。将优化后的囊泡分散体用卡波姆 940 NF 制备成凝胶。制备的脂质体凝胶(ETO-LG)和醇质体凝胶(ETO-EG)进行优化和表征。与其他测试配方相比,囊泡凝胶显示出良好的效果。

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