Chinembiri Tawona N, Gerber Minja, du Plessis Lissinda, du Preez Jan, du Plessis Jeanetta
Centre of Excellence for Pharmaceutical Sciences, North-West University, Private Bag X6001, Potchefstroom, 2520, South Africa.
AAPS PharmSciTech. 2015 Dec;16(6):1390-9. doi: 10.1208/s12249-015-0328-7. Epub 2015 May 9.
Drug delivery vehicles can influence the topical delivery and the efficacy of an active pharmaceutical ingredient (API). In this study, the influence of Pheroid™ technology, which is a unique colloidal drug delivery system, on the skin permeation and antimelanoma efficacy of 5-fluorouracil were investigated. Lotions containing Pheroid™ with different concentrations of 5-fluorouracil were formulated then used in Franz cell skin diffusion studies and tape stripping. The in vitro efficacy of 5-fluorouracil against human melanoma cells (A375) was investigated using a flow cytometric apoptosis assay. Statistically significant concentrations of 5-fluorouracil diffused into and through the skin with Pheroid™ formulations resulting in an enhanced in vitro skin permeation from the 4.0% 5-fluorouracil lotion (p < 0.05). The stratum corneum-epidermis and epidermis-dermis retained 5-fluorouracil concentrations of 2.31 and 6.69 μg/ml, respectively, after a diffusion study with the 4.0% Pheroid™ lotion. Subsequent to the apoptosis assay, significant differences were observed between the effect of 13.33 μg/ml 5-fluorouracil in Pheroid™ lotion and the effects of the controls. The results obtained suggest that the Pheroid™ drug delivery system possibly enhances the flux and delivery of 5-fluorouracil into the skin. Therefore, using Pheroid™ could possibly be advantageous with respect to topical delivery of 5-fluorouracil.
药物递送载体可影响活性药物成分（API）的局部递送及疗效。在本研究中，对一种独特的胶体药物递送系统——Pheroid™技术，对5-氟尿嘧啶的皮肤渗透及抗黑色素瘤疗效的影响进行了研究。配制了含有不同浓度5-氟尿嘧啶的Pheroid™洗剂，然后用于Franz细胞皮肤扩散研究和胶带剥离实验。使用流式细胞术凋亡检测法研究了5-氟尿嘧啶对人黑色素瘤细胞（A375）的体外疗效。使用Pheroid™制剂时，有统计学意义浓度的5-氟尿嘧啶扩散进入并透过皮肤，使得4.0% 5-氟尿嘧啶洗剂的体外皮肤渗透增强（p < 0.05）。在用4.0% Pheroid™洗剂进行扩散研究后，角质层-表皮和表皮-真皮中5-氟尿嘧啶的浓度分别为2.31和6.69 μg/ml。在凋亡检测后，观察到Pheroid™洗剂中13.33 μg/ml 5-氟尿嘧啶的效果与对照的效果之间存在显著差异。所得结果表明，Pheroid™药物递送系统可能增强了5-氟尿嘧啶向皮肤中的通量和递送。因此，对于5-氟尿嘧啶的局部递送而言，使用Pheroid™可能具有优势。
