In vitro transdermal iontophoretic delivery of leuprolide under constant current application

Journal of Controlled Release : Official Journal of the Controlled Release Society
Charu Kochhar, Georgios Imanidis

Abstract

Transdermal delivery of Leuprolide, a nonapeptide LHRH agonist, was studied using constant current iontophoresis to explore methods for improving iontophoretic efficiency and determine the feasibility of delivery of therapeutic doses of the drug. Universal buffer consisting of citrate, phosphate and borate was used to carry out in vitro permeation experiments with heat separated human epidermis at pH 4.5 and 7.2. In addition, the effect of substituting this buffer with a macromolecular electrolyte, polymaleic acid, on the drug flux and the transference number was studied. Current densities from 0.5 to 2.3 microA/cm2 were used requiring moderate potential differences between 60 and 420 mV to be applied thus limiting irreversible epidermal membrane alterations. The rather high electrical resistance of the epidermis of the order of 200 kohms cm2 was related to the sub-physiological electrolyte concentration. Resistance was continuously monitored to guarantee barrier integrity of the membrane. The permeation rate increased linearly with the current density for the universal buffer and was at pH 7.2 almost double that at pH 4.5 despite the greater ionic valence of the drug at pH 4.5 compared to pH 7.2; this being because of the oppo...Continue Reading

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Dec 18, 2002·Journal of Pharmaceutical Sciences·Charu Kochhar, Georgios Imanidis

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Citations

Mar 8, 2012·Scientia pharmaceutica·Vinod DhoteDinesh K Mishra
Feb 18, 2012·Expert Opinion on Drug Delivery·Donato TeutonicoGilles Ponchel
Mar 6, 2007·Expert Opinion on Drug Delivery·Lingxin ChenBing Yan
Feb 2, 2008·Journal of Pharmaceutical Sciences·Guilherme Martins GelfusoRenata Fonseca Vianna Lopez
Sep 1, 2014·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Kristina MalinovskajaJouni Hirvonen

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