Nanoparticle Coated Submicron Emulsions: Sustained In-vitro Release and Improved Dermal Delivery of All-trans-retinol
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The aim of this research is to investigate the dermal delivery of all-trans-retinol from nanoparticle-coated submicron oil-in-water emulsions as a function of the initial emulsifier type, the loading phase of nanoparticles, and the interfacial structure of nanoparticle layers.
The interfacial structure of emulsions was characterized using freeze-fracture-SEM. In-vitro release and skin penetration of all-trans-retinol were studied using Franz diffusion cells with cellulose acetate membrane, and excised porcine skin. The distribution profile was obtained by horizontal sectioning of the skin using microtome-cryostat and HPLC assay.
The steady-state flux of all-trans-retinol from silica-coated lecithin emulsions was decreased (up to 90%) and was highly dependent on the initial loading phase of nanoparticles; incorporation from the aqueous phase provided more pronounced sustained release. For oleylamine emulsions, sustained release effect was not affected by initial location of nanoparticles. The skin retention significantly (p ≤ 0.05) increased and was higher for positive oleylamine-stabilised droplets. All-trans-retinol was mainly localized in the epidermis with deeper distribution to viable skin layers in the presence of nanoparticles, yet negligible permeation (∼1% of topically applied dose) through full-thickness skin.
Sustained release and targeted dermal delivery of all-trans-retinol from oil-in-water emulsions by inclusion of silica nanoparticles is demonstrated.
KEY WORDSall-trans-retinol in-vitro release silica nanoparticles skin penetration/permeation submicron emulsion
The Australian Research Council’s Discovery grant scheme (DP0558920), Itek Pty. Ltd., and BioInnovation SA are acknowledged for the funding. The authors thank Dr. Peter Self for the assistance with the Freeze-Fracture SEM.
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