Topical iontophoresis of valaciclovir hydrochloride improves cutaneous aciclovir delivery

To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery. ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro. While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontop...

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Bibliographic Details
Published in:Pharmaceutical research 2006-08, Vol.23 (8), p.1842-1849
Main Authors: ABLA, Nada, NAIK, Aarti, GUY, Richard H, KALIA, Yogeshvar N
Format: Article
Language:English
Subjects:
Acyclovir - administration & dosage
Acyclovir - analogs & derivatives
Acyclovir - pharmacokinetics
Administration, Topical
Algorithms
Animals
Antiviral Agents - administration & dosage
Antiviral Agents - pharmacokinetics
Biological and medical sciences
Chromatography, High Pressure Liquid
Drug Delivery Systems
Drug dosages
Epidermis - metabolism
General pharmacology
Herpes viruses
Humans
Hydrogen-Ion Concentration
In Vitro Techniques
Iontophoresis
Medical sciences
Mice
Mice, Hairless
Pharmaceutical technology. Pharmaceutical industry
Pharmacology
Pharmacology. Drug treatments
Prodrugs
Rabbits
Rodents
Skin
Skin Absorption - physiology
Spectrophotometry, Ultraviolet
Swine
Transdermal medication
Valine - administration & dosage
Valine - analogs & derivatives
Valine - pharmacokinetics
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Summary:To investigate the topical iontophoresis of valaciclovir (VCV) as a means to improve cutaneous aciclovir (ACV) delivery. ACV and VCV electrotransport experiments were conducted using excised porcine skin in vitro. While the charged nature of the prodrug, VCV, enabled it to be more efficiently iontophoresed into the skin than the parent molecule, ACV, only the latter was detectable in the receptor chamber, suggesting that VCV was enzymatically cleaved into the active metabolite during skin transit. Iontophoresis of VCV was significantly more efficient than that of ACV; the cumulative permeation of ACV after 1, 2 and 3 h of VCV iontophoresis at 0.5 mA cm(-2) and using an aqueous 2 mM (approximately 0.06%) formulation was 20+/-10, 104+/-47 and 194+/- 82 microg cm( -2), respectively (cf. non-quantifiable levels, 0.1 and 1.0+/-0.7 microg cm(-2) after ACV iontophoresis). These delivery rates provide ample room to reduce either current density or the duration of current application. Preliminary in vitro data serve to emphasize the potential of VCV iontophoresis to improve the topical therapy of cutaneous herpes simplex infections and merit further investigation to demonstrate clinical efficacy.
ISSN:0724-8741
1573-904X
DOI:10.1007/s11095-006-9017-2