Frelichowska Justyna, Bolzinger Marie-Alexandrine, Valour Jean-Pierre, Mouaziz Hanna, Pelletier Jocelyne, Chevalier Yves
Université Lyon 1, Laboratoire de Dermopharmacie et Cosmétologie, Institut des Sciences Pharmaceutiques et Biologiques, Lyon F-69003, France.
Int J Pharm. 2009 Feb 23;368(1-2):7-15. doi: 10.1016/j.ijpharm.2008.09.057. Epub 2008 Oct 17.
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 25 microg cm(-2)h(-1), threefold higher than from a classical emulsion (9.7 microg cm(-2)h(-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.
首次对作为一种新型剂型的皮克林乳液的皮肤吸收进行了研究。皮克林乳液是由吸附的固体颗粒而非乳化剂分子来稳定的。它们是很有前景的剂型,在几个特性方面与传统乳液有显著不同。研究了一种亲水性模型渗透剂(咖啡因)从水包油型皮克林乳液中的皮肤渗透情况,并与用乳化剂稳定的水包油型传统乳液进行了比较。为了聚焦界面层对药物释放和皮肤吸收过程的影响,两种乳液具有相同的组成和物理化学性质。从皮克林乳液获得了最高的渗透速率,其伪稳态通量为25微克·厘米⁻²·小时⁻¹,比传统乳液(9.7微克·厘米⁻²·小时⁻¹)高三倍。暴露24小时后,咖啡因大多存在于接受液和真皮中;皮克林乳液中咖啡因的累积量更高。研究了几种物理化学现象以阐明皮克林乳液增强渗透的机制。其中,揭示了皮克林乳液液滴对皮肤表面的更高附着力。吸附在二氧化硅颗粒上的咖啡因的转运也被认为是相关的,因为皮肤剥离显示二氧化硅颗粒聚集体深入角质层。