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雪松醇乳膏的促毛发生长作用及其皮肤药代动力学

Hair growth promotion effect of cedrol cream and its dermatopharmacokinetics.

作者信息

Zhang Yan, Wang Jie-Wen, Qu Fan-Zhi, Zhang Yu-Meng, Su Guang-Yue, Zhao Yu-Qing

机构信息

Shenyang Pharmaceutical University No. 103, Wenhua Road Shenyang 110016 People's Republic of China

Key Laboratory of Structure-based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University Shenyang 110016 China.

出版信息

RSC Adv. 2018 Dec 18;8(73):42170-42178. doi: 10.1039/c8ra08667b. eCollection 2018 Dec 12.

Abstract

Topical use of cedrol ethanol has been reported to have a beneficial effect on hair loss. However, the use of cedrol has been limited by application-related issues, such as poor water solubility and volatile features. Therefore, the present study developed a cream formulation of cedrol and evaluated various physicochemical parameters of the prepared cream. The optimized cedrol cream was selected after orthogonal tests and determined further. The dermatopharmacokinetics were studied to investigate the absorption difference between cedrol cream and cedrol ethanol after dermal application, and the concentrations of cedrol in skin were analysed by the gas chromatography-mass spectrometry (GC-MS) method. By comparison, the area under the curve (AUC) of cedrol cream was almost three times higher than that of cedrol ethanol. Moreover, this study was undertaken to evaluate the hair growth promoting efficacy of cedrol cream in C57BL/6 mice and Wistar rats. Macroscopic assessment and alopecia score showed that C57BL/6 mice treated with cedrol cream showed a faster production of pigmentation and a higher score at different growth stages than other groups. The hair length of the cedrol cream-treated group was much longer than those of the cedrol ethanol and minoxidil groups. Histological analyses indicated that in the cedrol ethanol group, most follicles of the C57BL/6 mice were in the catagen phase, whereas nearly 83% of hair follicles in the cedrol cream group remained in the anagen phase. Taken together, our data strongly suggest that the cream formulation of cedrol has a stronger hair growth promotion effect, gave no irritation and was safe for topical administration.

摘要

据报道,外用柏木醇乙醇对脱发有有益作用。然而,柏木醇的使用受到与应用相关问题的限制,如水溶性差和挥发性强等特点。因此,本研究开发了一种柏木醇乳膏制剂,并评估了所制备乳膏的各种理化参数。通过正交试验筛选出优化后的柏木醇乳膏,并进一步确定其性质。研究了皮肤药代动力学,以探讨经皮应用后柏木醇乳膏和柏木醇乙醇之间的吸收差异,并采用气相色谱 - 质谱联用(GC-MS)法分析皮肤中柏木醇的浓度。相比之下,柏木醇乳膏的曲线下面积(AUC)几乎是柏木醇乙醇的三倍。此外,本研究旨在评估柏木醇乳膏对C57BL/6小鼠和Wistar大鼠的促毛发生长功效。宏观评估和脱发评分显示,与其他组相比,用柏木醇乳膏治疗的C57BL/6小鼠在不同生长阶段色素沉着产生更快,评分更高。柏木醇乳膏治疗组的毛发长度比柏木醇乙醇组和米诺地尔组长得多。组织学分析表明,在柏木醇乙醇组中,C57BL/6小鼠的大多数毛囊处于退行期,而在柏木醇乳膏组中,近83%的毛囊仍处于生长期。综上所述,我们的数据强烈表明,柏木醇乳膏制剂具有更强的促毛发生长作用,无刺激性,局部给药安全。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/de50/9092075/f1841103c20f/c8ra08667b-f1.jpg

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