Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil.
Photochem Photobiol. 2012 Jul-Aug;88(4):913-21. doi: 10.1111/j.1751-1097.2012.01147.x. Epub 2012 Apr 24.
It is desirable and challenging to prevent E-resveratrol (E-RSV) from photoisomerizing to its Z-configuration to preserve its biological and pharmacological activities. The aim of this research was to evaluate the photostability of E-RSV-loaded supramolecular structures and the skin penetration profile of chemically and physically stable nanoestructured formulations. Different supramolecular structures were developed to act as carriers for E-RSV, that is, liposomes, polymeric lipid-core nanocapsules and nanospheres and solid lipid nanoparticles. The degrees of photostability of these formulations were compared with that of an ethanolic solution of E-RSV. The skin penetration profiles of the stable formulations were obtained using vertical diffusion cells (protected from light and under UVA radiation) with porcine skin as the membrane, followed by tape stripping and separation of the viable epidermis and dermis in a heated water bath. Photoisomerization was significantly delayed by the association of resveratrol with the nanocarriers independently of the supramolecular structure. Liposomes were the particles capable of maintaining E-RSV concentration for the longest time. On the other hand, E-RSV-loaded liposomes reduced in size showing low physical stability under UVA radiation. In the dark, the skin penetration profiles were very similar, but under UVA radiation the E-RSV-loaded nanocarriers showed increasing amounts in the total epidermis.
防止 E-白藜芦醇(E-RSV)光异构化为 Z-构型以保持其生物和药理活性是理想且具有挑战性的。本研究旨在评估负载 E-RSV 的超分子结构的光稳定性和化学及物理稳定的纳米结构制剂的皮肤渗透特性。开发了不同的超分子结构作为 E-RSV 的载体,即脂质体、聚合物脂质核纳米胶囊和纳米球以及固体脂质纳米粒。将这些制剂的光稳定性程度与 E-RSV 的乙醇溶液进行了比较。通过垂直扩散细胞(避光并在 UVA 辐射下)获得稳定制剂的皮肤渗透特性,使用猪皮作为膜,然后在热水浴中通过胶带剥离和分离可存活的表皮和真皮。白藜芦醇与纳米载体结合可显著延迟光异构化,而与超分子结构无关。脂质体是能够维持 E-RSV 浓度最长时间的颗粒。另一方面,负载 E-RSV 的脂质体在 UVA 辐射下会减小,表现出低物理稳定性。在黑暗中,皮肤渗透特性非常相似,但在 UVA 辐射下,负载 E-RSV 的纳米载体在整个表皮中显示出越来越多的含量。