Traditional Chinese Medicine College, Shenyang Pharmaceutical University, Shenyang 110016, China.
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.
Molecules. 2021 Mar 23;26(6):1795. doi: 10.3390/molecules26061795.
As the main component of , cedrol has known germinal activity. A range of cedrol formulations have been developed to prevent hair-loss, but compliance remains key issues. In this study, we prepared cedrol nanoemulsion (CE-NE) and determined the particle size and PDI (polydispersion coefficient), investigated the hair growth activity and studied the bioavailability in vitro and in vivo. Results showed that the average particle size of CE-NE is 14.26 ± 0.16 nm, and the PDI value is 0.086 ± 0.019. In vitro drug release investigation and drug release kinetics analysis showed release profile of CE from nanoparticles demonstrates the preferred partition of CE in buffer pH 4.0, the release profile of CE-NE showed a first-order kinetics reaching around 36.7% after 6 h at 37 °C. We artificially depilated the back hair of C57BL/6 mice and compared the efficacy of a designed cedrol nanoemulsion to an existing ointment group. The hair follicles were imaged and quantified using a digital photomicrograph. The results showed that compared with the ointment, CE-NE had positive effects on hair growth, improved drug solubility. Compared with the ointment and 2% minoxidil groups, 50 mg/mL CE-NE led to more robust hair growth. Pharmacokinetics analysis showed that the AUC of CE-NE was 4-fold higher than that of the ointment group, confirming that the bioavailability of the nanoemulsion was greater than that of the ointment. CE-NE also significantly reduced the hair growth time of model mice and significantly increased the growth rate of hair follicles. In conclusion, these data suggest that the nanoemulsion significantly improved the pharmacokinetic properties and hair growth effects cedrol, enhancing its efficacy in vitro and in vivo.
柏木醇作为 的主要成分,具有已知的生发活性。已经开发出多种柏木醇制剂来预防脱发,但合规性仍是关键问题。在本研究中,我们制备了柏木醇纳米乳(CE-NE),并测定了粒径和 PDI(多分散系数),研究了其毛发生长活性,并进行了体外和体内生物利用度研究。结果表明,CE-NE 的平均粒径为 14.26 ± 0.16nm,PDI 值为 0.086 ± 0.019。体外药物释放研究和药物释放动力学分析表明,纳米粒中的 CE 释放呈现出在缓冲液 pH4.0 中优先分配的特征,CE-NE 的释放曲线呈一级动力学,在 37°C 下 6 小时后达到约 36.7%。我们人为地对 C57BL/6 小鼠背部的毛发进行了脱毛,并比较了设计的柏木醇纳米乳与现有软膏组的疗效。使用数字显微照片对毛囊进行成像和定量。结果表明,与软膏相比,CE-NE 对毛发生长有积极作用,提高了药物溶解度。与软膏和 2%米诺地尔组相比,50mg/ml CE-NE 导致更强劲的毛发生长。药代动力学分析表明,CE-NE 的 AUC 是软膏组的 4 倍,证实纳米乳的生物利用度大于软膏。CE-NE 还显著缩短了模型小鼠的毛发生长时间,显著增加了毛囊的生长速度。总之,这些数据表明纳米乳显著改善了柏木醇的药代动力学特性和毛发生长效果,增强了其在体外和体内的疗效。