Insumrong Kamonlak, Waranuch Neti, Ingkaninan Kornkanok, Tanuphol Nutchaninad, Mishra Abhay Prakash, Wisuitiprot Wudtichai, Wongwad Eakkaluk, Ngamdokmai Ngamrayu, Suphrom Nungruthai
Department of Chemistry, Faculty of Science, Naresuan University, Phitsanulok 65000, Thailand.
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Center of Excellence for Innovation in Chemistry, Naresuan University, Phitsanulok 65000, Thailand.
Molecules. 2025 Mar 4;30(5):1151. doi: 10.3390/molecules30051151.
The leaf extract of L.f. has shown potential as a 5α-reductase inhibitor, with two bioactive markers, namely (+)-eperua-8,13-dien-15-oic acid () and (+)-eperua-7,13-dien-15-oic acid (), used for extract standardization. The purpose of this research was to investigate the in vitro skin penetration behavior of and in leaf ethanolic extract solution and ready-to-use extract in propylene glycol (PG), and secondly, to determine their physicochemical properties, including partition coefficients and solubility. The appropriate vehicle for the in vitro skin penetration study was evaluated using the shake-flask method. The in vitro skin penetration study was conducted using the Franz diffusion cell model, and the amounts of the two active compounds in the extracts were analyzed using the HPLC method. Compounds and showed poor solubility in distilled water, whereas their solubility in HEPES buffer with 2% / of Tween 20 was significantly greater. The partition coefficient (log P) value for was 5.77 ± 0.07, and for , it was 5.66 ± 0.02, indicating that both compounds are hydrophobic. After 24 h of an in vitro skin penetration study, in both extracts showed significantly higher cumulative amounts (%) compared to . These findings suggest that is more hydrophobic and readily penetrates the stratum corneum. When a PG enhancer was added, high cumulative amount trends of and in the ethanolic extract and extract in PG in the receiver compartment were detected after 24 h. These studies provide important insights that will guide the further development of products with extracts for treating hair loss.
L.f. 的叶提取物已显示出作为 5α-还原酶抑制剂的潜力，有两种生物活性标记物，即(+)-埃佩鲁阿-8,13-二烯-15-酸（）和(+)-埃佩鲁阿-7,13-二烯-15-酸（），用于提取物标准化。本研究的目的是研究和在L.f. 叶乙醇提取物溶液以及丙二醇（PG）即用型提取物中的体外皮肤渗透行为，其次，确定它们的物理化学性质，包括分配系数和溶解度。使用摇瓶法评估用于体外皮肤渗透研究的合适载体。使用Franz扩散池模型进行体外皮肤渗透研究，并使用HPLC法分析提取物中两种活性化合物的含量。化合物和在蒸馏水中溶解度较差，而它们在含有2%吐温20的HEPES缓冲液中的溶解度显著更高。的分配系数（log P）值为5.77±0.07，的为5.66±0.02，表明这两种化合物都是疏水性的。体外皮肤渗透研究24小时后，两种提取物中的与相比，累积量（%）显著更高。这些发现表明更疏水且更容易穿透角质层。当添加PG增强剂时，24小时后在接受室中检测到乙醇提取物和PG提取物中的和有较高的累积量趋势。这些研究提供了重要的见解，将指导含L.f. 提取物的脱发治疗产品的进一步开发。
