Goto Ryoka, Oaku Yoshihiro, Sasaki Fuka, Kubota Chika, Deguchi Saori, Kadowaki Reita, Abe Akinari, Nagahama Tohru, Nagai Noriaki
Faculty of Pharmacy, Kindai University.
Research & Development Laboratories Self-Medication, Taisho Pharmaceutical Co., Ltd.
Yakugaku Zasshi. 2022;142(9):1015-1020. doi: 10.1248/yakushi.22-00103.
We previously designed the formulation containing minoxidil (MXD) nanoparticles (MXD-NPs), and found that the MXD-NPs can mainly deliver MXD into hair bulbs via hair follicles pathway, and that the therapeutic efficiency for hair growth is higher in comparison with the formulation containing dissolved MXD. In this study, we investigated whether the skin environmental changes by the treatment of steam towel, ethanol, l-menthol and commercially available (CA) carpronium affect the drug behavior in the MXD-NPs-applied mice. The steam towel, ethanol, l-menthol and CA-carpronium were pre-treated 3 min before MXD-NPs application, and the MXD content in the hair bulge, bulb, skin tissue and blood of mice were measured 4 h after MXD-NPs application. No significant difference of MXD levels in the blood was observed by the pre-treatment of steam towel, ethanol, l-menthol and CA-carpronium. On the other hand, the pre-treatment of steam towel and l-menthol enhanced the MXD levels in hair bulge and/or bulb. Although, the MXD levels in hair bulge and bulb were not changed by the pre-treatment of ethanol, the MXD levels in skin tissue was higher than that of saline-pre-treated group (control). The MXD levels in hair bulge, bulb and skin tissue of mice pre-treated with CA-carpronium were remarkably higher in comparison with control. In conclusion, we showed that the changes in skin environment by the steam towel, ethanol, l-menthol and CA-carpronium affected the absorption of MXD-NPs, and these increased MXD levels in the hair bulb and blood by the combination may enhance the therapeutic efficiency without side effects.
我们之前设计了含有米诺地尔(MXD)纳米颗粒(MXD-NPs)的制剂,并发现MXD-NPs可主要通过毛囊途径将MXD递送至毛球,且与含有溶解态MXD的制剂相比,其促进头发生长的治疗效果更高。在本研究中,我们调查了用蒸汽毛巾、乙醇、L-薄荷醇和市售(CA)卡普龙处理后皮肤环境的变化是否会影响应用MXD-NPs的小鼠体内的药物行为。在应用MXD-NPs前3分钟进行蒸汽毛巾、乙醇、L-薄荷醇和CA-卡普龙预处理,并在应用MXD-NPs后4小时测量小鼠毛囊隆突部、毛球、皮肤组织和血液中的MXD含量。蒸汽毛巾、乙醇、L-薄荷醇和CA-卡普龙预处理后,血液中MXD水平未观察到显著差异。另一方面,蒸汽毛巾和L-薄荷醇预处理提高了毛囊隆突部和/或毛球中的MXD水平。虽然乙醇预处理未改变毛囊隆突部和毛球中的MXD水平,但皮肤组织中的MXD水平高于生理盐水预处理组(对照组)。与对照组相比,用CA-卡普龙预处理的小鼠毛囊隆突部、毛球和皮肤组织中的MXD水平显著更高。总之,我们表明蒸汽毛巾、乙醇、L-薄荷醇和CA-卡普龙引起的皮肤环境变化影响了MXD-NPs的吸收,并且这些因素联合作用使毛球和血液中MXD水平升高,可能会提高治疗效果而无副作用。