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Transdermal delivery of ionic drugs by using ion-pair formation and microemulsion

利用离子对形成和微乳剂透皮递送离子药物

基本信息

批准号：
18590041
负责人：
KITAGAWA Shuji
金额：
$ 1.98万
依托单位：
Kobe Pharmaceutical University
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (C)
财政年份：
2006
资助国家：
日本
起止时间：
2006 至 2007
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-18590041/
关键词：
skin permeation skin ion-pair microemulsion abosorption enhancement ionic drugs ketotifen polyphenols ジクロフェナク

项目摘要

We first examined the enhancement of skin permeation of anionic diclofenac from non-aqueous vehicle isopropyl myristate (IPM) by ion-pair formation with either alkylamine or benzylamine as model counter ions. Permeation of diclofenac through excised guinea pig dorsal skin increased in the presence of these amines as well as solubility. Since the solubility of diclofenac was still limited, to obtain further enhancement of skin permeation, the effects of microemulsions as a vehicle for solubilizing the diclefonac-amine ion-pairs consisting of phosphate buffered saline, IPM, polyoxyethylene sorbitan monooleate and ethanol were examined. The microemulsions significantly increased diclofenac flux as well as its solubility. These findings indicated the usefulness of the combined use of ion-pair formation and microemulsion for the enhancement of skin permeation of ionic drugs. We also confirmed the enhancement of skin permeation of cationic ketotifen by ion-par formation by using alkylsulfonates such as 1-octanesulfonate as counter ions.We furthermore examined the usefulness of microemulsions for the improvement of the efficiency of intradermal delivery of polyphenols. The findings indicate the potential use of microemulsions for the intradermal delivery of polyphenols, especially for those such as quercetin and rutin which have relatively large molecular weights.The obtained results indicated the usefulness of ion-pair formation and microemulsion for transdermal snd intradermal drug delivery.

我们首先研究了增强皮肤渗透的阴离子双氯芬酸从非水介质肉豆蔻酸异丙酯（IPM）的离子对形成与烷基胺或苄胺作为模型抗衡离子。双氯芬酸通过离体豚鼠背部皮肤的渗透增加，在这些胺的存在下，以及溶解度。由于双氯芬酸的溶解度仍然有限，为了进一步增强皮肤渗透，检查了微乳剂作为增溶双氯芬酸-胺离子对（由磷酸盐缓冲盐水、IPM、聚氧乙烯脱水山梨糖醇单油酸酯和乙醇组成）的载体的作用。微乳显着增加双氯芬酸通量以及其溶解度。这些结果表明，离子对形成和微乳液的组合使用，以促进离子型药物的皮肤渗透的有用性。我们还证实了通过使用烷基磺酸盐如1-辛烷磺酸盐作为反离子形成离子PAR来增强阳离子酮替芬的皮肤渗透，我们进一步研究了微乳液对改善多酚皮内递送效率的有用性。结果表明，微乳可用于多酚类物质的皮内给药，尤其是分子量较大的槲皮素和芦丁，表明离子对形成和微乳可用于经皮给药和皮内给药。