向日葵根乙醇提取物的自微乳化体系,以提高其溶解度和释放亲和蛋白

Dailenys Marrero-Morfa, César Ibarra-Alvarado, Francisco J. Luna-Vázquez, Miriam Estévez, Eremy Miranda Ledesma, Alejandra Rojas-Molina, Carlos T. Quirino-Barreda
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引用次数: 0

摘要

自微乳化或自纳米乳化给药系统(SMEDDS/SNEDDS)以改善疏水药物(包括草药提取物)的溶出度和提高口服生物利用度而闻名。向日葵根有机提取物及其主要成分亲和蛋白具有血管舒张作用;然而,它们的水溶性很差,因此很难通过口服给药和给药。本研究旨在通过拟三元相图,建立一种以龙骨根乙醇提取物(HL-SMDS)为原料制备的自微乳化体系。此外,还对优化后的脂基配方进行了表征,并测定了其体外胃肠模拟溶出度。该配方由trancutol, 55%(增溶剂)组成;吐温80/PG, 10%(表面活性剂/助溶剂);Labrasol, 35%(表面活性剂);优选的药材提取物为SMEDDS,与水接触后形成微乳液,液滴尺寸小于100 nm。稳定性测试表明,HL-SMDS在极端条件下保持稳定。此外,在pH为1和6.8的条件下,HL-SMDS的亲和蛋白释放量高于根乙醇提取物。这些结果表明,HL-SMDS是一种新的替代方法,可以提高龙参根乙醇提取物的水溶性,从而提高其口服生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Self-microemulsifying system of an ethanolic extract of Heliopsis longipes root for enhanced solubility and release of affinin
Abstract Self-microemulsifying or self-nanoemulsifying drug delivery systems (SMEDDS/SNEDDS) are well known to improve the dissolution and increase the oral bioavailability of hydrophobic drugs, including herbal extracts. Organic extracts of Heliopsis longipes root and affinin, its main component, induce a vasodilator effect; however, they are poorly water soluble and therefore are difficult to administer and dose by the oral route. This research aimed to develop, through pseudo-ternary phase diagrams, a self-microemulsifying system prepared from an ethanolic extract of H. longipes root (HL-SMDS). In addition, the optimized lipid-based formulation was characterized and its in vitro gastrointestinal simulated dissolution was determined. The formulation composed of Transcutol, 55% (solubilizer); Tween80/PG, 10% (surfactant/co-solvent); Labrasol, 35% (surfactant); and the herbal extract was selected as optimal and identified as a SMEDDS, since when coming into contact with water, it forms a micro-emulsion with droplet sizes less than 100 nm. The stability tests showed that HL-SMDS remained stable over time under extreme conditions. Furthermore, the amount of affinin released from HL-SMDS at pH 1 and 6.8 was higher than that of the ethanolic extract from H. longipes root. These results indicate that HL-SMDS is a novel alternative to improve the aqueous solubility and therefore the oral bioavailability of the ethanolic extract of H. longipes root.
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