Jacobs Gerda A, Gerber Minja, Malan Maides M, du Preez Jan L, Fox Lizelle T, du Plessis Jeanetta
a Faculty of Health Sciences , Centre of Excellence for Pharmaceutical Sciences, North-West University , Potchefstroom , South Africa.
Drug Deliv. 2016;23(2):631-41. doi: 10.3109/10717544.2014.933283. Epub 2014 Jul 9.
Viral and fungal cutaneous manifestations are regularly encountered in immunocompromised human immunodeficiency virus/acquired immunodeficiency syndrome individuals and can be treated by drugs such as acyclovir and ketoconazole, respectively.
The aim of this study was to determine whether the novel Pheroid delivery system improved the transdermal delivery and/or dermal delivery of acyclovir and ketoconazole when incorporated into semi-solid formulations.
Semi-solid products (creams and emulgels) containing these drug compounds were formulated, either with or without (control) the Pheroid delivery system. The stability of the formulated semi-solid products was examined over a period of six months and included the assay of the actives, pH, viscosity, mass loss and particle size observation. Vertical Franz cell diffusion studies and tape stripping methods were used to determine the in vitro, stratum corneum (SC)-epidermis and epidermis-dermis delivery of these formulations.
Stability tests showed that none of the formulations were completely stable. Acyclovir showed a biphasic character during the in vitro skin diffusion studies for all the tested formulations. The Pheroid™ cream enhanced the transdermal, SC-epidermis and epidermis-dermis delivery of acyclovir the most. The average amount of ketoconazole diffused over 12 h showed improved delivery of ketoconazole, with the Pheroid™ emulgel exhibiting the best transdermal and epidermis-dermis delivery.
The Pheroid formulae increased transdermal penetration as well as delivery to the dermal and epidermal skin layers. The Pheroid emulgel and the Pheroid cream increased the topical delivery of ketoconazole and acyclovir, respectively.
病毒和真菌性皮肤表现常见于免疫功能低下的人类免疫缺陷病毒/获得性免疫缺陷综合征患者，分别可用阿昔洛韦和酮康唑等药物治疗。
本研究旨在确定新型Pheroid递送系统在掺入半固体制剂时是否能改善阿昔洛韦和酮康唑的透皮递送和/或真皮递送。
配制含有这些药物化合物的半固体产品（乳膏和乳胶），有或没有（对照）Pheroid递送系统。对配制的半固体产品进行为期六个月的稳定性检查，包括活性成分测定、pH值、粘度、质量损失和粒度观察。采用垂直Franz细胞扩散研究和胶带剥离法测定这些制剂在体外角质层（SC）-表皮和表皮-真皮的递送情况。
稳定性测试表明，所有制剂均未完全稳定。在所有测试制剂的体外皮肤扩散研究中，阿昔洛韦表现出双相特征。Pheroid™乳膏对阿昔洛韦的透皮、SC-表皮和表皮-真皮递送增强作用最大。酮康唑在12小时内的平均扩散量表明其递送有所改善，Pheroid™乳胶的透皮和表皮-真皮递送效果最佳。
Pheroid配方增加了透皮渗透以及向真皮和表皮层的递送。Pheroid乳胶和Pheroid乳膏分别增加了酮康唑和阿昔洛韦的局部递送。
