Evaluation of the in vitro skin permeation of antiviral drugs from ...

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Herpes simplex virus infection (HSV) is a common and ubiquitous infection of the skin which causes mucocutaneous lesions called cold sores (herpes labialis) or fever blisters. It is estimated that approximately 80% of the population worldwide are carriers of the Herpes simplex virus, approximately 40% suffer from recurrent recurrent infections.

This study evaluates the in vitro skin permeation and penetration of penciclovir and acyclovir from commercialized creams for the treatment of herpes labialis (cold sores), using non viable excised human abdominal skin samples, which were exposed to 5 mg/cm2 of acyclovir 5% cream or penciclovir 1% cream.

Methods: After 24 h of cream application, excess cream was washed off and layers of stratum corneum were removed by successive tape stripping.

Amounts of active ingredients having penetrated through the skin were measured, as well as the amounts in the washed-off cream, in skin strips and creams remaining in the skin. Molecular modelling was used to evaluate physico-chemical differences between the drugs.

Western blot analysis enabled to determine whether the marker of basal cells keratin 5 could be detected in the various tape strips.

Results: Application of penciclovir 1% cream yielded higher concentration of drug in the deeper layers of the epidermis as well as a higher drug flux through the skin. Molecular modelling showed two higher hydrophobic moieties for acyclovir.

Presence of the basal cell marker keratin 5 was underscored in the deeper tape strips from the skin, giving evidence that both drugs can reach their target cells.

Conclusion: Penciclovir 1% cream has the tendency to facilitate the diffusion of the drug through the stratum corneum into the deeper epidermis layers, in which it could reach the target basal cells at effective therapeutical concentration. The small difference in the surface properties between both molecules might also contribute to favour the passage of penciclovir through the epidermis into the deeper basal cells.

Author: Nathalie Hasler-Nguyen, Donald Shelton, Gilbert Ponard, Marlene Bader, Martina Schaffrik and Pascal Mallefet
Credits/Source: BMC Dermatology 2009, 9:3

Published on: 2009-04-02

Additional information:

Treatment of Recurrent Herpes Simplex Labialis with Levamisole
Herpes Labialis (Oral Herpes Simplex ) - Symptoms, Diagnosis
BiomedExperts: Herpes simplex labialis in children with acute
Epidermodysplasia verruciformis with Hansen's disease, herpes
Buy Herpes Simplex Labialis Medications Online Now!
Acta Tropica : Herpes simplex labialis in children with acute
References - Herpes labialis - Skin disorders - Clinical Evidence
Identification of a Herpes Simplex Labialis Susceptibility Region
Pathogenesis of herpes simplex labialis : excretion of virus in the
Herpes labialis (Lippenherpes) , NetDoktor.de

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