Nastiti Christofori M R R, Ponto Thellie, Mohammed Yousuf, Roberts Michael S, Benson Heather A E
School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth, WA 6845, Australia.
Faculty of Pharmacy, Sanata Dharma University, Yogyakarta 55282, Indonesia.
Pharmaceutics. 2020 Jan 29;12(2):108. doi: 10.3390/pharmaceutics12020108.
Resveratrol (RSV) is a potent lipophilic antioxidant with a low aqueous solubility. Novel nanoformulations have been successfully developed and evaluated to increase the potential of resveratrol as a skin targeting antioxidant. Nanoformulations were prepared using a spontaneous emulsification method, and characterized and evaluated for their capabilities to penetrate/permeate the skin. In nanoformulations, the thermodynamic activity of the RSV penetration into/permeation through the skin was correlated with the thermodynamic activity of the RSV in the formulations. When terpenes were incorporated into the nanoformulations, the permeation of RSV through the skin increased and correlated with an increasing lipophilicity of the terpene. The nanoemulsion containing eugenol showed the highest RSV penetration into the stratum corneum (SC) and the epidermis-dermis-follicle region, whereas the limonene containing nanoemulsion had the highest RSV permeation through the skin (the enhancement ratios, compared to a saturated solution of RSV, were (i) 9.55 and (ii) 12.61, respectively, based on the average RSV amount (i) in each skin region and (ii) permeation through skin).
白藜芦醇(RSV)是一种具有低水溶性的强效亲脂性抗氧化剂。已成功开发并评估了新型纳米制剂,以提高白藜芦醇作为皮肤靶向抗氧化剂的潜力。采用自发乳化法制备纳米制剂,并对其穿透/渗透皮肤的能力进行表征和评估。在纳米制剂中,RSV渗透进入皮肤的热力学活性与制剂中RSV的热力学活性相关。当将萜类化合物加入纳米制剂中时,RSV通过皮肤的渗透率增加,且与萜类化合物亲脂性的增加相关。含丁香酚的纳米乳剂显示出RSV穿透角质层(SC)以及表皮-真皮-毛囊区域的能力最强,而含柠檬烯的纳米乳剂则具有RSV通过皮肤的最高渗透率(与RSV饱和溶液相比,基于(i)每个皮肤区域的平均RSV量和(ii)通过皮肤的渗透率,增强率分别为(i)9.55和(ii)12.61)。