Pickering emulsions stabilized by biodegradable block copolymer micelles for controlled topical drug delivery

[Display omitted] 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...

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Bibliographic Details
Published in:International journal of pharmaceutics 2017-10, Vol.531 (1), p.134-142
Main Authors: Laredj-Bourezg, Faiza, Bolzinger, Marie-Alexandrine, Pelletier, Jocelyne, Chevalier, Yves
Format: Article
Language:English
Subjects:
Animals
Block copolymer nanoparticles
Chemical and Process Engineering
Chemical Sciences
Cutaneous absorption
Drug Carriers - chemistry
Emulsions - chemistry
Engineering Sciences
Ethylene Glycols
Galenic pharmacology
Lactates
Life Sciences
Material chemistry
Micelles
or physical chemistry
Pharmaceutical sciences
Pickering emulsion
Polyesters
Polyethylene Glycols
Polymers
Retinol
Skin Absorption
Skin delivery
Swine
Theoretical and
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Summary:[Display omitted] 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.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2017.08.065