PMID: 8961162Nov 1, 1996Paper

Evaluation of in-vivo transdermal absorption of cyclosporin with absorption enhancer using intradermal microdialysis in rats

The Journal of Pharmacy and Pharmacology
M NakashimaM Ichikawa

Abstract

The purpose of this study was to evaluate the effect of absorption enhancer on in-vivo transdermal absorption of cyclosporin using intradermal microdialysis in rats. Cyclosporin oily solutions (0.5, 2, 8% w/v) were prepared from Sandimmun (10% w/v oily oral preparation of cyclosporin) by diluting with olive oil. 1-[2-(Decylthio)ethyl] azacyclopentan-2-one (HPE-101) and glycerin were added to the cyclosporin formulation as an absorption enhancer at various concentrations between 1 and 20%. These formulations were applied to the shaved abdomen of rats treated with intradermal microdialysis at a flow rate of 2.5 microL min-1 for 6 h. Cyclosporin was immediately detected and attained a plateau in the dermal dialysate after topical application of cyclosporin oily solution alone. Cyclosporin levels in the dialysate increased with increasing cyclosporin concentrations in the formulation from 0.5 to 8% (w/v). HPE-101 did not influence cyclosporin absorption at concentrations less than 6% (w/v). Addition of 10% (w/v) HPE-101 significantly enhanced an apparent absorption rate of cyclosporin by 4.9 times. However, 20% (w/v) HPE-101 did not show the enhancing activity. On the other hand, addition of glycerin at concentrations of 6, 10, and...Continue Reading

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Citations

Nov 7, 2007·Pharmaceutical Research·Christophe HerkenneRichard H Guy
Apr 10, 2004·International Journal of Pharmaceutics·Ramesh R BoinpallyBhaskara R Jasti
Dec 4, 2002·Advanced Drug Delivery Reviews·Mads Kreilgaard
Dec 13, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·E Schnetz, M Fartasch
Aug 27, 2005·Clinical Pharmacokinetics·Christian Joukhadar, Markus Müller
Jun 13, 2014·Drug Development and Industrial Pharmacy·Dipal R PatelGrazia Stagni
Aug 9, 2007·Expert Opinion on Drug Delivery·Hongzhuo LiuSanming Li
Jul 2, 2005·Expert Opinion on Investigational Drugs·G Cevc
Oct 19, 2004·International Journal of Pharmaceutics·Kyoung-Jin LeeChi-Ho Lee
May 8, 2016·International Journal of Pharmaceutics·Feng XieDong-Hai Zhang
Nov 30, 2007·Photochemical & Photobiological Sciences : Official Journal of the European Photochemistry Association and the European Society for Photobiology·Asta JuzenieneJohan Moan
Jan 6, 1999·Journal of Pharmaceutical Sciences·D K HansenC E Lunte

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