Enhanced Skin Permeation of Diclofenac by Ion-Pair Formation and Further Enhancement by Microemulsion
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概要
- 論文の詳細を見る
Enhancement of skin permeability of anionic diclofenac from non-aqueous vehicle isopropyl myristate (IPM) by ion-pair formation with either alkylamines or benzylamine as model cationic ions was examined in guinea pig dorsal skin. Diclofenac ion flux increased in the presence of these amines due to an increase in solubility. Maximum flux was observed in the presence of n-hexylamine, which induced 7.3-fold increase accompanied by a 45-fold increase in solubility. Permeability coefficients of the ionic form of diclofenac in the presence of benzylamine, n-hexylamine and iso-octylamine as counter ions in IPM were larger than those of the non-ionic form of diclofenac. Since the solubility of diclofenac was still limited, to obtain further enhancement of skin permeation, the effects of microemulsions as a vehicle consisting of phosphate buffered saline (PBS), isopropyl myristate (IPM), polyoxyethylene sorbitan monooleate (Tween 80) and ethanol were examined for transport of diclofenac-benzylamine ion-pairs. All microemulsion formulations tested increased diclofenac flux 4.9-fold to 10.7-fold over the value without a microemulsion accompanied by a 217-fold to 302-fold improvement in the solubility of diclofenac-benzylamine ion-pairs, but permeability coefficients were decreased 28-44 fold. Maximum enhancement was observed for a microemulsion with a ratio of PBS, IPM, ethanol and Tween 80 of 25 : 8 : 47 : 20 (w/w). The present findings suggest the usefulness of combined use of ion-pairs with microemulsions for enhancement of skin permeation of ionic drugs.
- 公益社団法人日本薬学会の論文
- 2007-03-01
著者
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Kamal Mohammad
Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And Applied Life Sciences
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Kitagawa S
Niigata Univ. Pharmacy And Applied Life Sci. Niigata Jpn
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Kitagawa Shuji
Kobe Pharmaceutical University
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Kitagawa S
Niigata College Of Pharmacy
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NABEKURA Tomohiro
Faculty of Pharmaceutical Sciences Kinki University
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Iimura Nahoko
Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And Applied Life Sciences
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Nabekura Tomohiro
Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And Applied Life Sciences
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