Enhanced transdermal delivery of AZT (Zidovudine) using iontophoresis and penetration enhancer

The effect of current, its magnitude and penetration enhancers (propylene glycol/oleic acid) on the transdermal flux of AZT (Zidovudine) across hairless mouse skin was studied and the results were compared. The in vitro iontophoretic flux from AZT solution increased to about 5–40 fold that obtained...

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Bibliographic Details
Published in:Journal of controlled release 1998-02, Vol.51 (2), p.161-168
Main Authors: Oh, S.Y, Jeong, S.Y, Park, T.G, Lee, J.H
Format: Article
Language:English
Subjects:
Administration, Cutaneous
AIDS/HIV
Animals
Anti-HIV Agents - administration & dosage
Anti-HIV Agents - metabolism
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
AZT
Biological and medical sciences
Buffers
Drug Delivery Systems
Female
General pharmacology
Glycerol
Iontophoresis
Iontophoresis - methods
Karaya Gum
Medical sciences
Mice
Mice, Hairless
Oleic Acid
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Propylene Glycol
Resistance
Reverse Transcriptase Inhibitors - administration & dosage
Reverse Transcriptase Inhibitors - metabolism
Skin Absorption - drug effects
Skin Absorption - physiology
Synergistic effect
Zidovudine - administration & dosage
Zidovudine - metabolism
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Summary:The effect of current, its magnitude and penetration enhancers (propylene glycol/oleic acid) on the transdermal flux of AZT (Zidovudine) across hairless mouse skin was studied and the results were compared. The in vitro iontophoretic flux from AZT solution increased to about 5–40 fold that obtained by passive diffusion, depending on the magnitude of current density. When the donor side was karaya gum matrix, instead of solution, the flux enhancement effect by iontophoresis was much smaller. Incorporation of penetration enhancers into the matrix increased the passive flux 2–50 fold, depending on the amount of penetration enhancers in the matrix. These enhancers worked synergistically with iontophoresis in the transdermal transport: a much larger flux than that expected from a simple additive effect was observed. Electrical resistance data from our previous work is utilized to further discuss this synergistic effect.
ISSN:0168-3659
1873-4995
DOI:10.1016/S0168-3659(97)00162-4