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半固态功能化纳米结构化脂质载体负载百里香酚用于皮肤疾病。

Semi-solid functionalized nanostructured lipid carriers loading thymol for skin disorders.

机构信息

Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain.

Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028, Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028, Barcelona, Spain.

出版信息

Int J Pharm. 2024 Feb 15;651:123732. doi: 10.1016/j.ijpharm.2023.123732. Epub 2023 Dec 22.

Abstract

Acne constitutes one of the most prevalent skin disorder affecting both skin and mental health of patients. However, no cure has been developed so far. In this area, Thymol constitutes a potential candidate since it is able to restore the healthy microbiota of the skin. However, its permeation properties cause its fast elimination and, to avoid this problem, thymol has been loaded into nanostructured lipid carriers (TH-NLCs). Moreover, to increase the suitability of these systems for skin applications, several surface functionalization strategies of TH-NLCs had been assessed. Among the different molecules, phosphatidylcholine-TH-NLCs demonstrated to be safe as well as to provide high antioxidant activity in cellular studies. Therefore, to administer these systems to the skin, functionalized TH-NLCs were dispersed into a carbomer gel developing semi-solid formulations. Rheological properties, porosity and extensibility of TH dispersed in carbomer as well as phosphatidylcholine-TH-NLCs were assessed demonstrating suitable properties for dermal applications. Moreover, both formulations were applied in healthy volunteers demonstrating that gel-phosphatidylcholine-TH-NLCs were able to increase in skin hydration, decrease water loss and reduce skin sebum. Therefore, gel-phosphatidylcholine-TH-NLCs proved to be a suitable system for skin pathologies linked with high sebum generation, loss of hydration and high oxidation, such as acne vulgaris.

摘要

痤疮是一种最常见的皮肤疾病,影响着患者的皮肤和心理健康。然而,到目前为止还没有治愈的方法。在这一领域,百里酚是一种有潜力的候选药物,因为它能够恢复皮肤的健康微生物群。然而,其渗透性能导致其快速消除,为了避免这个问题,百里酚已被负载到纳米结构化脂质载体(TH-NLCs)中。此外,为了提高这些系统在皮肤应用中的适用性,已经评估了几种 TH-NLCs 的表面功能化策略。在不同的分子中,磷脂酰胆碱-TH-NLCs 被证明是安全的,并且在细胞研究中具有高抗氧化活性。因此,为了将这些系统施用于皮肤,将功能化的 TH-NLCs 分散到卡波姆凝胶中,开发出半固态制剂。评估了 TH 分散在卡波姆中的流变性质、孔隙率和可扩展性以及磷脂酰胆碱-TH-NLCs,证明它们具有适合皮肤应用的性质。此外,两种制剂都在健康志愿者中进行了应用,结果表明凝胶-磷脂酰胆碱-TH-NLCs 能够增加皮肤的水分含量,减少水分流失,并减少皮肤皮脂。因此,凝胶-磷脂酰胆碱-TH-NLCs 被证明是一种适合治疗与皮脂生成过多、水分流失和氧化过高相关的皮肤疾病的系统,如寻常痤疮。

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