Vehicle effects on in vitro release and skin permeation of octylmethoxycinnamate from microemulsions.
The high content of surfactants is one of the major limits to microemulsions (MEs) use in pharmaceutical and cosmetic field. In this work MEs with low surfactant content were prepared by the phase inversion temperature (PIT) method using different oil phases and emulsifiers. The effects of vehicle composition on in vitro release and skin permeation of octylmethoxycinnamte (OMC), one of the most used UVB filter, was evaluated. These MEs showed droplet sizes in the range 32-77nm and a single peak in size distribution. MEs prepared using the most lipophilic lipids (decyl oleate or cetyl stearyl isononanoate) showed the lowest stability. In vitro release and skin permeation profiles were affected by both lipophilicty and structure of the lipid used as internal phase and the formulation that released the lowest amount of OMC provided the lowest active compound skin permeation. It is noteworthy that no OMC release and skin permeation were observed using oleth-20/glyceryl oleate as emulsifiers. Furthermore, a skin permeation enhancement effect was observed depending on the vehicle components. The results of this work suggest that PIT MEs could provide controlled skin drug delivery by choosing proper associations of oil phase lipids and emulsifiers.
Department of Pharmaceutical Sciences, University of Catania, V.le A. Doria 6, 95125 Catania, Italy. lmontene@unict.it
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Montenegro
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Carbone
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Puglisi
D000328:Adult; D002934:Cinnamates / Q000737:chemistry* / Q000493:pharmacokinetics*; D003358:Cosmetics; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry; D004655:Emulsions; D005079:Excipients; D006801:Humans; D008055:Lipids / Q000737:chemistry; D014677:Pharmaceutical Vehicles; D044367:Phase Transition; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption; D012995:Solubility; D013473:Sunscreening Agents / Q000737:chemistry* / Q000493:pharmacokinetics*; D013501:Surface-Active Agents / Q000737:chemistry*; D013696:Temperature
D002934:Cinnamates; D003358:Cosmetics; D045703:Emulsifying Agents; D004655:Emulsions; D005079:Excipients; D008055:Lipids; D014677:Pharmaceutical Vehicles; D013473:Sunscreening Agents; D013501:Surface-Active Agents; C118580:octylmethoxycinnamate