Design of Hydrogel for the Drug Delivery of Less Permeable Ursolic Acid Isolated from Rhododendron arboreum Flower in Animal Skin Membrane

Bigyan Joshi, N. L. Bhandari, S. Shyaula, Uttam Budathoki, R. Gyawali, Panna Thapa
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Abstract

Ursolic acid (UA) is a pentacyclic triterpene that has antioxidant, anticancer, and anti-inflammatory properties. As it belongs to the biopharmaceutical classification system IV due to its poor water solubility and permeability restricts its use in clinical application. So, the research is focused on the development of hydrogel containing encapsulated liposomes of ursolic acid to increase its permeability. The ursolic acid liposomal gel was prepared with a 0.5%, 1%, and 1.5% mixture of carbopol 934P and HPMC K4M as gelling agents. The pH and spreadability of liposomal gel were found to be in the range of (6.93±0.035 to 7.12±0.03) and (15.41±0.36 to 24.47±0.90) g.cm/sec respectively. The drug content was found to be in (19.77±0.02 to 20.11±0.02)%. The study of drug release kinetics showed Higuchi release followed by a non-Fickian diffusion mechanism. The result of the permeation study by Franz diffusion cell showed 1.55 times higher compared to the plain gel at the 5th hour of the study with a flux value of 0.455(mg/cm2/hr). It resolved the fast and enhanced delivery of liposomal ursolic acid through the skin membrane.
从杜鹃花中提取的渗透性较低的熊果酸在动物皮膜中的给药水凝胶设计
熊果酸(UA)是一种五环三萜类化合物,具有抗氧化、抗癌和抗炎特性。由于其水溶性和渗透性较差,属于生物制药分类系统 IV,限制了其在临床上的应用。因此,研究重点是开发含有熊果酸封装脂质体的水凝胶,以增加其渗透性。以 0.5%、1% 和 1.5% 的 carbopol 934P 和 HPMC K4M 混合物为胶凝剂,制备了熊果酸脂质体凝胶。脂质体凝胶的 pH 值和铺展性分别为(6.93±0.035 至 7.12±0.03)克/厘米和(15.41±0.36 至 24.47±0.90)克/秒。药物含量为(19.77±0.02 至 20.11±0.02)%。药物释放动力学研究表明,Higuchi 释放遵循非 Fickian 扩散机制。弗朗兹扩散池的渗透研究结果表明,在研究的第 5 个小时,通量值为 0.455(mg/cm2/hr),是普通凝胶的 1.55 倍。这说明熊果酸脂质体能快速、高效地透过皮肤膜。
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