Enhanced Transdermal Delivery of Zidovudine in Rats and Human Skin

概要

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Zidovudine (azidothymidine, AZT), a potent antiviral agent acting on acquired immunodeficiency syndrome virus, was examined with regard to permeation through rat and human skin. A steady state plasma concentration of AZT after transdermal application in rats estimated from both pharmacokinetics data after i.v. administration and penetration rate through excised rat skin from 10% oleic acid (OA) aqueous solution shows penetration about 85 tims higher compared to that from 10% OA would be needed for therapeutic efficacy. A mixed-solvent system consisted of 5% Sefsol-318^<[○!R]> (S-318), 10% OA, 10% N-methyl-2-pyrrolidone (MP), 20% propylene glycol (PG) and water showed promising characteristics as a vehicle in terms of permeability of AZT through excised rat skin. The maximum flux of 0.41 μmol/cm^2/h was observed in excised human skin after application of a gel formulation including S-318,OA, MP and PG. The result suggests a possible use of the gel formulation to gain an effective plasma concentration in humans.
公益社団法人日本薬学会の論文
1990-11-25