Rungseevijitprapa Wandee, Wichayapreechar Panikchar, Sivamaruthi Bhagavathi Sundaram, Jinarat Damrongsak, Chaiyasut Chaiyavat
Department of Pharmaceutical Chemistry and Technology, Faculty of Pharmaceutical Sciences, Ubon Ratchathani University, Ubon Ratchathani 34190, Thailand.
Department of Cosmetic Science, School of Pharmaceutical Sciences, University of Phayao, Phayao 56000, Thailand.
Pharmaceutics. 2021 Dec 17;13(12):2177. doi: 10.3390/pharmaceutics13122177.
The study aimed to develop the finasteride-loaded proniosome (FLP) to enhance the transfollicular delivery of finasteride (FN). The response surface methodology (RSM) combined with central composite design (CCD) with three independent variables (FN concentrations, total lipid content, and cholesterol content) was used to optimize the FLP preparation. The particles size, zeta potential, entrapment efficiency, and drug loading capacity of the FLP were analyzed. The transfollicular delivery of the optimum formulation was investigated in vitro. In vivo hair growth stimulation study was performed on C57BL/6Mlac mice dorsal areas. The Draize primary skin irritation test for erythema and edema was performed in the New Zealand white rabbit skin. The optimum FLP consists of 5.0 mM of FN, 10.1 mM of total lipid content, and 50.0% of the cholesterol in the total lipid. The prepared proniosome delivered the FN significantly ( < 0.05), compared to the naked finasteride solution in a dose- and time-dependent manner. The FLP treatment significantly increases the number and size of hair follicles in a dose-dependent manner. The efficiency of 1% FLP was comparable to the 2% minoxidil solution. The FLP exhibited no skin irritation after 72 h. Therefore, the results demonstrated that the FLP could stimulate hair growth via a transfollicular delivery system.
该研究旨在开发载有非那雄胺的前体脂质体（FLP），以增强非那雄胺（FN）的经毛囊递送。采用响应面法（RSM）结合中心复合设计（CCD），以三个自变量（FN浓度、总脂质含量和胆固醇含量）优化FLP制剂。分析了FLP的粒径、ζ电位、包封率和载药量。在体外研究了最佳制剂的经毛囊递送情况。在C57BL/6Mlac小鼠背部区域进行了体内毛发生长刺激研究。在新西兰白兔皮肤上进行了Draize原发性皮肤红斑和水肿刺激性试验。最佳FLP由5.0 mM的FN、10.1 mM的总脂质含量和总脂质中50.0%的胆固醇组成。与裸非那雄胺溶液相比，制备的前体脂质体以剂量和时间依赖性方式显著递送FN（<0.05）。FLP治疗以剂量依赖性方式显著增加毛囊的数量和大小。1%FLP的效果与2%米诺地尔溶液相当。72小时后FLP未表现出皮肤刺激性。因此，结果表明FLP可通过经毛囊递送系统刺激毛发生长。
