Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand.
Center for Research and Development of Herbal Health Products (CRD-HHP), Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen, Thailand.
Drug Dev Ind Pharm. 2021 Nov;47(11):1824-1834. doi: 10.1080/03639045.2022.2064486. Epub 2022 Apr 21.
Diarylheptanoids, extracted from the (CC) rhizome, have been reported to exhibit estrogenic activity. However, oral administration of the extract showed a short half-life.
This study aimed to formulate and to investigate the potential of transfersomal gels for the transport of phytoestrogenic diarylheptanoids across the skin into the blood circulation.
The transfersomes were developed and optimized for their compositions including sources of phospholipid (egg yolk and soybean), types of edge activators (polysorbate 80, sorbitan oleate 80, and sodium cholate), and concentrations of CC extract (10-60 mg). The optimal formulation was further incorporated into Carbopol® Ultrez 21 gel and evaluated for in vitro release, permeation, and in vivo absorption.
The optimal transfersomes containing 10% of polysorbate 80 were selected due to high drug entrapment efficiency and a small diameter. The release kinetic of transfersomal gels followed a zero model. The maximum permeation flux through porcine ear skin was 1.38 ± 0.25 µg/cm/h for (4E, 6E)-1, 7-diphenylhepta-4, 6-dien-3-ol, and 0.40 ± 0.11 µg/cm/h for (6E)-1, 7-diphenylhept-6-en-3-ol. Results of the in vivo pharmacokinetics study in rats showed that transfersomal gel provided a maximum concentration of 219.71 ± 4.05 ng/ml and prolonged plasma concentration of diarylheptanoids for over 12 h. There was no significant variation found in the physical characteristics including viscosity, pH, and size after six months of storage at room temperature (30 ± 1 °C) and high temperature (40 ± 1 °C).
The obtained data suggested that the developed transfersomal gel of CC extract should be beneficial for improving the delivery of phytoestrogenic diarylheptanoids.
从 （CC） 根茎中提取的二芳庚烷类化合物已被报道具有雌激素活性。然而，该提取物的口服给药半衰期较短。
本研究旨在制备并研究传递体凝胶在将植物雌激素二芳庚烷类化合物通过皮肤输送到血液循环中的潜力。
开发并优化了传递体，包括磷脂来源（蛋黄和大豆）、边缘活性剂类型（聚山梨酯 80、山梨坦油酸酯 80 和胆酸钠）和 CC 提取物浓度（10-60mg）。进一步将最佳配方纳入 Carbopol®Ultrez 21 凝胶中，并评估其体外释放、渗透和体内吸收。
由于高药物包封效率和小粒径，选择含有 10%聚山梨酯 80 的最佳传递体。传递体凝胶的释放动力学遵循零级模型。通过猪耳皮的最大渗透通量分别为（4E，6E）-1,7-二苯基庚-4,6-二烯-3-醇 1.38±0.25μg/cm/h 和（6E）-1,7-二苯基庚-6-烯-3-醇 0.40±0.11μg/cm/h。大鼠体内药代动力学研究结果表明，传递体凝胶提供了 219.71±4.05ng/ml 的最大浓度，并将二芳庚烷类植物雌激素的血浆浓度延长超过 12 小时。在室温（30±1°C）和高温（40±1°C）下储存六个月后，粘度、pH 值和粒径等物理特性没有发现明显变化。
获得的数据表明，CC 提取物的开发传递体凝胶应该有利于改善植物雌激素二芳庚烷类化合物的递送。
