Ando Kaana, Sugiyama Ikumi, Sadzuka Yasuyuki
Division of Pharmaceutical and Health Sciences, Graduate School of Pharmaceutical Science, Iwate Medical University, Yahaba-cho, Shiwa-gun, Iwate, Japan.
Department of Advanced Pharmaceutics, School of Pharmacy, Iwate Medical University, Yahaba-cho, Shiwa-gun, Iwate, Japan.
Womens Health Rep (New Rochelle). 2024 Feb 29;5(1):193-200. doi: 10.1089/whr.2023.0108. eCollection 2024.
Premenstrual syndrome (PMS) is experienced by many women who suffer from either its psychological or physical symptoms. Current treatment is limited to symptomatic therapy or oral contraceptives. On the other hand, l-theanine, which has a relaxant effect, has been reported to be useful for PMS, but its short half-life when administered orally makes it less effective. Permeability and properties of transdermal gel containing l-theanine were evaluated as a preclinical study of PMS symptoms relief formulation.
Lyogel composed of stearic acid, stearyl alcohol, and propylene glycol was selected. The ratio of these components and the preparation method were investigated. Permeation of Strat-M membranes was evaluated by using Franz cells (). Moreover, lyogel was applied to institute of cancer research mice's backs for 10 days to examine the permeability of l-theanine.
l-Theanine solution did not permeate the Strat-M membrane at all in the permeation study, but lyogel allowed l-theanine to permeate. When the composition of lyogel was 4.4:11.1:296 (mmol) for stearic acid, stearyl alcohol, and propylene glycol, l-theanine absorption through Strat-M membrane was better. In skin permeation study using mice, l-theanine was detected in the serum, that is, it was proven that l-theanine penetrated the skin.
The preparation of transdermal gels contained l-theanine was investigated as a preclinical study. The skin permeability of semisolid formulations of hydrophobic ointments, hydrophilic ointments, oily creams, creams, and lyogel containing theanine was compared and found that lyogel was the best. The composition of lyogel was also studied to obtain a formulation with good application comfort. Although it is suggested that this lyogel could be tested in clinical studies to determine whether it is effective for relief of PMS symptoms, lyogel may be suitable as an easy-to-use l-theanine-containing formulation for women that can relieve PMS symptoms.
许多女性都经历过经前综合征（PMS），会出现心理或身体症状。目前的治疗方法仅限于对症治疗或口服避孕药。另一方面，具有放松作用的L-茶氨酸已被报道对经前综合征有用，但其口服时半衰期短，效果较差。作为经前综合征症状缓解制剂的临床前研究，评估了含L-茶氨酸的透皮凝胶的渗透性和性质。
选择由硬脂酸、硬脂醇和丙二醇组成的冻干凝胶。研究了这些成分的比例和制备方法。使用Franz扩散池评估Strat-M膜的渗透性。此外，将冻干凝胶应用于癌症研究所小鼠的背部10天，以检测L-茶氨酸的渗透性。
在渗透研究中，L-茶氨酸溶液根本不能透过Strat-M膜，但冻干凝胶可使L-茶氨酸透过。当冻干凝胶中硬脂酸、硬脂醇和丙二醇的组成比例为4.4:11.1:296（mmol）时，L-茶氨酸透过Strat-M膜的吸收效果更好。在使用小鼠的皮肤渗透研究中，血清中检测到了L-茶氨酸，即证明L-茶氨酸可穿透皮肤。
作为临床前研究，对含L-茶氨酸的透皮凝胶制剂进行了研究。比较了含茶氨酸的疏水软膏、亲水软膏、油性乳膏、乳膏和冻干凝胶等半固体制剂的皮肤渗透性，发现冻干凝胶效果最佳。还研究了冻干凝胶的组成，以获得应用舒适度良好的制剂。尽管建议可在临床研究中测试这种冻干凝胶，以确定其对缓解经前综合征症状是否有效，但冻干凝胶可能适合作为一种易于使用的含L-茶氨酸制剂，用于缓解女性经前综合征症状。
