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.

我们首先检查了通过离子对以烷基胺或苄胺作为模型抗衡离子的离子生成形成，从非水媒介物异丙基肉豆蔻酸酯（IPM）研究了皮肤渗透的皮肤渗透。在这些胺的存在以及溶解度的情况下，通过切除的豚鼠背皮渗透到豚鼠的背皮增加。由于双氯芬酸的溶解度仍然受到限制，以进一步增强皮肤渗透，因此微乳剂作为溶解dile-fonac-氨基离子对的载体，由磷酸盐缓冲盐水，IPM，多氧乙二基sorbitan monooleate和乙醇研究。微乳液显着增加了双氯芬酸通量及其溶解度。这些发现表明，离子对形成和微乳液的联合使用对增强离子药物渗透的有用性。我们还通过使用烷基磺酸盐（例如1-辛烷磺酸盐）作为反离子来证实通过离子-PAR形成阳离子酮to的皮肤渗透。研究结果表明，微乳液在多酚的皮内输送中的潜在用途，特别是对于槲皮素和鲁丁蛋白等分子量相对较大的结果。获得的结果表明离子对形成和微乳液对经dranddermal SND SND的有用性。