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Cutaneous iontophoretic delivery of CGP69669A, a sialyl Lewis x mimetic, in vitro
Author(s) -
Gratieri Taís,
Wagner Beatrice,
Kalaria Dhaval,
Ernst Beat,
Kalia Yogeshvar N.
Publication year - 2012
Publication title -
experimental dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.108
H-Index - 96
eISSN - 1600-0625
pISSN - 0906-6705
DOI - 10.1111/j.1600-0625.2011.01429.x
Subject(s) - iontophoresis , transdermal , permeation , chemistry , chromatography , pharmacology , in vitro , medicine , membrane , biochemistry , radiology
The aim was to investigate the feasibility of using iontophoresis for the cutaneous delivery of the E‐selectin antagonist CGP69669A, a sialyl Lewis x ‐glycomimetic with potential activity against inflammatory skin diseases. The effects of current density and formulation on iontophoretic transport were evaluated in porcine and human skin in vitro . Cumulative permeation of CGP69669A increased with current density (69.73 ± 9.51, 113.97 ± 26.80 and 160.44 ± 13.79 μg/cm 2 at 0.1, 0.3 and 0.5 mA/cm 2 , respectively) and drug concentration (37.42 ± 13.13, 78.96 ± 23.13 and 160.44 ± 13.79 μg/cm 2 , at 1, 3 and 5 mg/ml, respectively). In contrast, passive delivery was negligible. Although permeation from a 2% hydroxyethyl cellulose gel was lower than that from aqueous solution, skin deposition – more relevant for the local treatment of dermatological conditions – was 3‐fold higher. The results demonstrated that although CGP69669A cannot be delivered passively into the skin it is an excellent candidate for transdermal iontophoresis, a technique that is ideally suited to the delivery of glycomimetics.