Ionic liquids as tools to improve gel formulations containing sparingly soluble phenolic acids

Ana Júlio, Nádia Remtula, M. Nicolai, Tânia Santos de Almeida
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Abstract

Hydroxycinnamic acids, namely caffeic and p-coumaric acids, have several pharmaceutical and cosmetic applications, but due to their low aqueous solubility, their applicability can be limited. Ionic liquids (ILs) have been shown to be a valuable tool to improve the solubility and assist in the incorporation of various phenolic compounds into delivery systems. Thus, this work aims to evaluate the impact of incorporating three choline-based ILs, namely (2-hydroxyethyl)-trimethylammonium-L-phenylalanine [Cho][Phe], (2-hydroxyethyl)-trimethylammonium-L-glutamate [Cho][Glu] and (2-hydroxyethyl)-trimethylammonium-glycinate [Cho][Gly], into an aqueous gel formulation containing the poorly soluble caffeic and p-coumaric acids. The results obtained confirm that the ILs not only increase the drug solubility, but also allow higher amounts of both studied drugs to be incorporated into the gels, without interfering with the stability of the aqueous gels. Moreover, the ILs altered the fluidity of the gels, both in the absence and presence of both phenolic acids, as they increase the viscosity of the formulations, contributing to higher flow resistance of the gel, which may be better accepted by the consumer. Keywords: Ionic liquids; Hydroxycinnamic acids; Poorly soluble drugs; Gels; Increased Viscosity
离子液体作为工具,以改善凝胶配方含有少量可溶性酚酸
羟基肉桂酸,即咖啡酸和对香豆酸,有几种制药和化妆品应用,但由于其水溶性低,其适用性受到限制。离子液体(ILs)已被证明是一种有价值的工具,以提高溶解度和协助纳入各种酚类化合物进入输送系统。因此,本研究旨在评估将三种基于胆碱的il,即(2-羟乙基)-三甲胺- l -苯丙氨酸[Cho][Phe],(2-羟乙基)-三甲胺- l -谷氨酸[Cho][Glu]和(2-羟乙基)-三甲胺-甘氨酸[Cho][Gly]加入含有难溶性咖啡酸和对香豆酸的水凝胶配方中的影响。得到的结果证实,il不仅增加了药物的溶解度,而且允许更多的研究药物被纳入凝胶,而不影响水凝胶的稳定性。此外,在两种酚酸存在和不存在的情况下,il改变了凝胶的流动性,因为它们增加了配方的粘度,有助于提高凝胶的流动阻力,这可能更容易被消费者接受。关键词:离子液体;Hydroxycinnamic酸;难溶性药物;凝胶;粘度增加
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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