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Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
Published on: October 10, 2016
Pickering emulsions stabilized by biodegradable block copolymer micelles for controlled topical drug delivery
Faiza Laredj-Bourezg1, Marie-Alexandrine Bolzinger1, Jocelyne Pelletier1
1Université de Lyon, Université Claude Bernard Lyon 1, CNRS UMR 5007, Laboratoire d'Automatique et de Génie des Procédés (LAGEP), 43 bd 11 Novembre, 69622 Villeurbanne, France; Université Claude Bernard Lyon 1, Institut des Sciences Pharmaceutiques et Biologiques, Laboratoire de Dermopharmacie et Cosmétologie, 8 av Rockefeller, 69373 Lyon, France.
Abstract:
Surfactant-free biocompatible and biodegradable Pickering emulsions were investigated as vehicles for skin delivery of hydrophobic drugs. O/w emulsions of medium-chain triglyceride (MCT) oil droplets loaded with all-trans retinol as a model hydrophobic drug were stabilized by block copolymer nanoparticles: either poly(lactide)-block-poly(ethylene glycol) (PLA-b-PEG) or poly(caprolactone)-block-poly(ethylene glycol) (PCL-b-PEG). Those innovative emulsions were prepared using two different processes allowing drug loading either inside oil droplets or inside both oil droplets and non-adsorbed block copolymer nanoparticles. Skin absorption of retinol was investigated in vitro on pig skin biopsies using the Franz cell method. Supplementary experiments by confocal fluorescence microscopy allowed the visualization of skin absorption of the Nile Red dye on histological sections. Retinol and Nile Red absorption experiments showed the large accumulation of hydrophobic drugs in the stratum corneum for the Pickering emulsions compared to the surfactant-based emulsion and an oil solution. Loading drug inside both oil droplets and block copolymer nanoparticles enhanced again skin absorption of drugs, which was ascribed to the supplementary contribution of free block copolymer nanoparticles loaded with drug. Such effect allowed tuning drug delivery to skin over a wide range by means of a suitable selection of either the formulation or the drug loading process.
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