Iannuccelli V, Coppi G, Sergi S, Mezzena M, Scalia S
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Modena, Italy.
Skin Pharmacol Physiol. 2008;21(1):30-8. doi: 10.1159/000109656. Epub 2007 Oct 11.
Lipid microparticles (lipospheres) loaded with butyl methoxydibenzoylmethane (BMDBM), a widely used UV-A sunscreen agent, were prepared by melt technique and evaluated for skin permeation both in vivo, by tape stripping method, and in vitro, by a flow-through diffusion chamber. Following in vivo human skin application of an O/W emulsion containing 2% of BMDBM loaded in lipospheres, 15% of the applied sunscreen accumulated in the uppermost layers of the stratum corneum without remarkably modifying the skin permeation of the unencapsulated sunscreen. These results were found to be predicted by an in vitro methodology involving the diffusion of BMDBM through a lipophilized synthetic membrane into a hydrophilic receptor phase, simulating the viable epidermis better than an ethanolic receptor phase.
通过熔融技术制备了负载有丁基甲氧基二苯甲酰甲烷(BMDBM,一种广泛使用的UV - A防晒剂)的脂质微粒(脂质球),并通过胶带剥离法在体内以及通过流通扩散室在体外评估其皮肤渗透性。在对含2%负载于脂质球中的BMDBM的水包油乳液进行人体皮肤体内应用后,15%的施用防晒剂积聚在角质层的最上层,而未显著改变未包封防晒剂的皮肤渗透情况。这些结果通过一种体外方法得以预测,该方法涉及BMDBM通过亲脂化合成膜扩散到亲水性受体相中,相较于乙醇受体相,能更好地模拟活表皮。