获取途径

作者

Yaping Wang Xihui Wang Xiangyu Wang Yilei Song Xiaodan Wang Jifu Hao

作者单位

College of Pharmacy,Taishan Medical University,Taian,People’s Republic of China

刊名

AAPS PharmSciTech

年份

2019

卷号

Vol.20 No.2

ISSN

1530-9932

关键词

lidocaine microemulsions eutectic mixture transdermal delivery tail-flick test

分类号

615.1

摘要

Topical administration is a preferable choice for local anesthetic delivery. Microemulsions have shown great effectiveness for transdermal transport of lidocaine. However, fabrication of microemulsions containing highly concentrated lidocaine to provide an extended local anesthetic effect is still a challenge. This study investigated the feasibility of using microemulsions for transdermal delivery of a high dosage of lidocaine . At first, eutectic mixtures by kneading lidocaine with thymol were...更多

Topical administration is a preferable choice for local anesthetic delivery. Microemulsions have shown great effectiveness for transdermal transport of lidocaine. However, fabrication of microemulsions containing highly concentrated lidocaine to provide an extended local anesthetic effect is still a challenge. This study investigated the feasibility of using microemulsions for transdermal delivery of a high dosage of lidocaine . At first, eutectic mixtures by kneading lidocaine with thymol were tailored to form a lipophilic solution, then the mixtures were readily incorporated into the oil phase of microemulsions after addition of proper surfactants and cosurfactants. The physicochemical properties, the skin permeation, local anesthetic efficacy, and the irritation experiment of the developed microemulsions were evaluated. The optimum composition was as follows: 12% of ethyl oleate as oil phase, 28% of the mixed surfactant, and cosurfactant and 60% of the aqueous phase. The average particle size was about 13 nm. The transmission electron microscope studies revealed almost homogeneous spherical globules without aggregation. The Fourier-transform infrared spectroscopy results highlighted the drugs homogeneously dispersed in the microemulsions. In vitro skin permeation and in vivo anesthesia effect evaluation indicated that microemulsions can enhance and extend the anesthetic effect of lidocaine. The irritable results indicated that the microemulsions had the better biocompatibility and the negligible influence on the dermal. Therefore, incorporating the eutectic mixtures into microemulsions could be proposed as an attractive choice and a promising transdermal delivery strategy for the future topical anesthetic therapy.收起

学科

【SCI学科】PHARMACOLOGY & PHARMACY 【ESI学科】PHARMACOLOGY & TOXICOLOGY

影响因子

2016年:2.451;2015年:1.954;2014年:1.641;2013年:1.776;2012年:1.584

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期刊

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