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Lecithin microemulsions for the topical administration of ketoprofen: percutaneous adsorption through human skin and in vivo human skin tolerability

Abstract

The potential application of highly biocompatible o/w microemulsions as topical drug carrier systems for the percutaneous delivery of anti-inflammatory drugs, i.e. ketoprofen, was investigated. Microemulsions were made up of triglycerides as oil phase, a mixt. of lecithin and n-butanol as a surfactant/co-surfactant system and an aq. soln. as the external phase. To evaluate the percutaneous enhancing effect of oleic acid, this compd. was used as a component of some o/w microemulsions. The topical carrier potentialities of lecithin-based o/w microemulsions were compared with respect to conventional formulations, i.e. a w/o emulsion, a o/w emulsion and a gel. Physicochem. characterization of microemulsions was carried out by light scattering and zeta potential analyses. Microemulsions showed mean droplet size <35 nm and a neg. zeta potential, that is -39.5 mV for the oleic acid-lecithin microemulsion and -19.7 mV for the lecithin-based microemulsion. The percutaneous adsorption of the various topical formulations was evaluated through healthy adult human skin, which was obtained from abdominal redn. surgery. Ketoprofen-loaded microemulsions showed an enhanced permeation through human skin with respect to conventional formulations. No significant percutaneous enhancer effect was obsd. for ketoprofen-loaded oleic acid-lecithin microemulsions. The human skin tolerability of various microemulsion formulations was evaluated on human volunteers. Microemulsions showed a good human skin tolerability

Autori

PUGLISI - Giovanni

Altri Autori

Paolino Donatella
Ventura Cinzia Anna
Nistico Steven
Fresta Massimo