Effect of lipopeptides and iontophoresis on aciclovir skin delivery

Swine; Surface-Active Agents; Skin Absorption; Skin; Permeability; Peptides, Cyclic; Lipopeptides; Excipients; Drug Synergism; Calorimetry, Differential Scanning; Antiviral Agents; Animals; Transdermal penetration; Lipopeptide; Acyclovir; Iontophoresis; Epidermis; Biosurfactant

Abstract :

[en] Objectives Lipopeptides are compounds derived from microorganisms that exhibit pronounced surface and emulsifying activity. The ability of lipopeptides to interact with stratum corneum lipids makes them candidates as transdermal penetration enhancers. We have investigated the potential of two lipopeptides, fengycin and surfactin, to act as enhancers for the transdermal penetration and skin accumulation of aciclovir. Methods To investigate a possible synergistic effect, surfactin and fengycin were associated with anodal iontophoresis. Permeation experiments were performed using vertical diffusion cells and pig ear skin as barrier. Differential scanning calorimetry was used to study the interaction between fengycin and stratum corneum lipids. Key findings The results obtained indicated that surfactin and fengycin were not suitable to enhance aciclovir flux across the skin, not even when associated with iontophoresis. Aciclovir flux was slightly decreased in passive conditions and unchanged (fengycin) or decreased (surfactin) in anodal iontophoretic conditions. When applied in passive conditions, fengycin and surfactin increased aciclovir concentration in the epidermis by a factor of 2. Conclusions Surfactin and fengycin did not enhance aciclovir transport across the skin (not even when associated with iontophoresis) although they increased aciclovir concentration in the epidermis by a factor of 2. © 2010 Royal Pharmaceutical Society of Great Britain.

Disciplines :

Dermatology
Chemistry

Author, co-author :

Nicoli, S.; Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43100 Parma, Italy

Eeman, M.; Department of Industrial Biological Chemistry, Gembloux Agro-Bio Tech, Liege University, Gembloux, Belgium

Deleu, Magali ; Université de Liège - ULiège > Chimie et bio-industries > Chimie biologique industrielle

Bresciani, E.; Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43100 Parma, Italy

Padula, C.; Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43100 Parma, Italy

Santi, P.; Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, 43100 Parma, Italy

Language :

English

Title :

Effect of lipopeptides and iontophoresis on aciclovir skin delivery

Publication date :

2010

Journal title :

Journal of Pharmacy and Pharmacology

ISSN :

0022-3573

eISSN :

2042-7158

Publisher :

Wiley, London, United Kingdom

Volume :

Issue :

Pages :

702-708

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 14 January 2011

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