Abstract

Numerous skin disorders and diseases are related to oxidative stress. The application of an antioxidant, serving as a strong defense agent against oxidation, is of great interest in dermatology yet remains challenging for delivery. This paper aimed to develop a niosome carrier system to deliver the antioxidant (+) Catechin into the skin. (+) Catechin-loaded niosomes were prepared using film hydration technique and the physicochemical properties of drug-loaded niosomes were characterised and investigated by a series of in vitro and ex vivo studies. The optimised formulation displayed an acceptable size in nanoscale (204 nm), high drug entrapment efficiency (49%) and amorphous state of drug in niosomes. It was found that (+) Catechin-loaded niosomes could effectively prolong the drug release. Drug deposition in the viable layers of human skin was significantly enhanced when niosomal carriers were applied (p < 0.05). Compared to the pure drug, the niosomal formulation had a greater protective effect on the human skin fibroblasts (Fbs). This is consistent with the observation of internalisation of niosomes by Fbs which was concentration-, time- and temperature-dependent, via an energy-dependent process of endocytosis. The research highlighted that niosomes are potential topical carriers for dermal delivery of antioxidants in skin-care and pharmaceutical products.

摘要

许多皮肤病和疾病都与氧化应激有关。作为一种强大的抗氧化防御剂的抗氧化剂的应用在皮肤病学中引起了极大的兴趣，但在交付方面仍然具有挑战性。本文旨在开发一种 niosome 载体系统，将抗氧化剂 (+) 儿茶素输送到皮肤中。(+) 使用薄膜水合技术制备了装载儿茶素的 niosomes，并通过一系列体外和离体的表征和研究了装载药物的 niosomes 的理化性质学习。优化的配方显示出可接受的纳米级尺寸 (204 nm)、高药物包封率 (49%) 和药物在 niosome 中的无定形状态。发现(+) 儿茶素负载的niosomes 可以有效地延长药物释放。当应用 niosomal 载体时，药物在人体皮肤活层中的沉积显着增强 ( p  < 0.05)。与纯药物相比，niosomal 制剂对人皮肤成纤维细胞 (Fbs) 具有更大的保护作用。这与观察到的 Fbs 对 niosomes 的内化作用是一致的，Fbs 是浓度、时间和温度依赖性的，通过一种依赖能量的内吞过程。该研究强调，niosomes 是皮肤护理和医药产品中抗氧化剂经皮递送的潜在局部载体。