Kumar Pawan, Singh Shailendra Kumar, Handa Vandana, Kathuria Himanshu
Department of Pharmaceutical sciences, Guru Jambheshwar University of science & Technology, Hisar 125001, India.
School of Pharmacy, Krishna Institute of Engineering and Technology, Ghaziabad 201206, India.
Medicines (Basel). 2018 Sep 14;5(3):103. doi: 10.3390/medicines5030103.
Current topical minoxidil (MXD) formulations involve an unpleasant organic solvent which causes patient incompliance in addition to side effects in some cases. Therefore, the objective of this work was to develop an MXD formulation providing enhanced follicular delivery and reduced side effects. Oleic acid, being a safer material, was utilized to prepare the nanovesicles, which were characterized for size, entrapment efficiency, polydispersity index (PDI), zeta potential, and morphology. The nanovesicles were incorporated into the emugel Sepineo P 600 (2% /) to provide better longer contact time with the scalp and improve physical stability. The formulation was evaluated for in vitro drug release, ex vivo drug permeation, and drug deposition studies. Follicular deposition of the vesicles was also evaluated using a differential tape stripping technique and elucidated using confocal microscopy. The optimum oleic acid vesicles measured particle size was 317 ± 4 nm, with high entrapment efficiency (69.08 ± 3.07%), narrow PDI (0.203 ± 0.01), and a negative zeta potential of -13.97 ± 0.451. The in vitro drug release showed the sustained release of MXD from vesicular gel. The skin permeation and deposition studies revealed superiority of the prepared MXD vesicular gel (0.2%) in terms of MXD deposition in the stratum corneum (SC) and remaining skin over MXD lotion (2%), with enhancement ratios of 3.0 and 4.0, respectively. The follicular deposition of MXD was 10-fold higher for vesicular gel than the control. Confocal microscopy also confirmed the higher absorption of rhodamine via vesicular gel into hair follicles as compared to the control. Overall, the current findings demonstrate the potential of oleic acid vesicles for effective targeted skin and follicular delivery of MXD.
目前局部用米诺地尔（MXD）制剂含有一种令人不适的有机溶剂，这不仅会导致患者依从性差，在某些情况下还会产生副作用。因此，本研究的目的是开发一种能增强毛囊递送并减少副作用的MXD制剂。油酸作为一种更安全的材料，被用于制备纳米囊泡，并对其尺寸、包封率、多分散指数（PDI）、zeta电位和形态进行了表征。纳米囊泡被掺入乳化凝胶Sepineo P 600（2%/）中，以提供与头皮更好的更长接触时间并提高物理稳定性。对该制剂进行了体外药物释放、离体药物渗透和药物沉积研究。还使用差分胶带剥离技术评估了囊泡的毛囊沉积情况，并通过共聚焦显微镜进行了阐明。最佳油酸囊泡的测量粒径为317±4 nm，具有高包封率（69.08±3.07%）、窄PDI（0.203±0.01）和-13.97±0.451的负zeta电位。体外药物释放显示MXD从囊泡凝胶中持续释放。皮肤渗透和沉积研究表明，制备的MXD囊泡凝胶（0.2%）在角质层（SC）和其余皮肤中的MXD沉积方面优于MXD洗剂（2%），增强率分别为3.0和4.0。MXD在囊泡凝胶中的毛囊沉积比对照高10倍。共聚焦显微镜也证实，与对照相比，若丹明通过囊泡凝胶进入毛囊的吸收更高。总体而言，目前的研究结果证明了油酸囊泡在有效靶向皮肤和毛囊递送MXD方面的潜力。
