Pickering w/o emulsions: Drug release and topical delivery

• Published in: International journal of pharmaceutics Vol. 368; no. 1-2; pp. 7 - 15
• Main Authors: Frelichowska, Justyna, Bolzinger, Marie-Alexandrine, Valour, Jean-Pierre, Mouaziz, Hanna, Pelletier, Jocelyne, Chevalier, Yves
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 23.02.2009; Elsevier
• Subjects: Administration, Topical; Adsorption; Animals; Caffeine - chemistry; Caffeine - metabolism; Caffeine - pharmacology; Chemical and Process Engineering; Chemical Sciences; Chemistry, Pharmaceutical; Dosage Forms; Drug Carriers - metabolism; Drug Carriers - pharmacology; Drug release; Drug Stability; Emulsions - chemistry; Emulsions - metabolism; Emulsions - pharmacology; Engineering Sciences; Galenic pharmacology; Hydrogen-Ion Concentration; In Vitro Techniques; Kinetics; Life Sciences; Material chemistry; Oils - chemistry; or physical chemistry; Particle Size; Permeability; Pharmaceutical sciences; Pickering emulsion; Polymers; Silicon Dioxide - metabolism; Silicon Dioxide - pharmacology; Skin absorption; Skin Absorption - drug effects; Surface-Active Agents - metabolism; Surface-Active Agents - pharmacology; Swine; Theoretical and; Water - chemistry; Drug release; Skin absorption; Pickering emulsion; ACL
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2008.09.057

The skin absorption from Pickering emulsions as a new dosage form was investigated for the first time. Pickering emulsions are stabilized by adsorbed solid particles instead of emulsifier molecules. They are promising dosage forms that significantly differ from classical emulsions within several features. The skin permeation of a hydrophilic model penetrant (caffeine) was investigated from a w/o Pickering emulsion and compared to a w/o classical emulsion stabilized with an emulsifier. Both emulsions had the same composition and physicochemical properties in order to focus on the effect of the interfacial layer on the drug release and skin absorption processes. The highest permeation rates were obtained from the Pickering emulsion with a pseudo-steady state flux of 25μgcm−2h−1, threefold higher than from a classical emulsion (9.7μgcm−2h−1). After 24h exposure, caffeine was mostly in the receptor fluid and in the dermis; cumulated amounts of caffeine were higher for the Pickering emulsion. Several physicochemical phenomena were investigated for clearing up the mechanisms of enhanced permeation from the Pickering emulsion. Among them, higher adhesion of Pickering emulsion droplets to skin surface was disclosed. The transport of caffeine adsorbed on silica particles was also considered relevant since skin stripping showed that aggregates of silica particles entered deeply the stratum corneum.