Ezati Negin, Roberts Michael Stephen, Zhang Qian, Moghimi Hamid Reza
Department of Pharmaceutics and Pharmaceutical Nanotechnology, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Therapeutics Research Centre, School of Medicine, Translational Research Institute, University of Queensland, Brisbane, QLD, Australia.
Iran J Pharm Res. 2020 Summer;19(3):572-578. doi: 10.22037/ijpr.2019.112435.13755.
Hansen Solubility Parameters (HSP) of human stratum corneum (SC) represent its polarity and are very important for design and optimization of dermatological formulations. However, there is no directly measured data available in the literature for such a crucial property, which is the subject of the present investigation. HSP of the SC was measured by solvent uptake here. 18 solvents/mixtures with different HSP values were selected and their uptake by the SC was measured at 32 °C. The solvents were then divided into good and bad solvents according to their uptake into the SC. The HSP discrete parts of "atomic dispersion forces (δD)", "dipolar intermolecular forces (δP)", and "hydrogen bonding (δH)" were then calculated using uptake data and HSPiP software. Results showed that δD, δP, and δH values of the SC at 32 °C are 16.5, 12, 7.7 respectively. The obtained HSP values, which were measured for the first time here, were then used to interpret enhancement effects of permeation enhancers and the uptake of vehicles by the SC using Relative Energy Difference (RED), with good correlations. SC HSP values can be further used in transdermal drug delivery, cosmetic formulations, safety issues, etc.
人体角质层(SC)的汉森溶解度参数(HSP)体现了其极性,对于皮肤科制剂的设计和优化非常重要。然而,文献中尚无关于这一关键性质的直接测量数据,而这正是本研究的主题。本文通过溶剂吸收法测量了角质层的HSP。选择了18种具有不同HSP值的溶剂/混合物,并在32℃下测量了它们被角质层的吸收情况。然后根据溶剂被角质层的吸收情况将其分为良溶剂和不良溶剂。接着使用吸收数据和HSPiP软件计算了“原子色散力(δD)”、“偶极分子间力(δP)”和“氢键(δH)”的HSP离散部分。结果表明,32℃下角质层的δD、δP和δH值分别为16.5、12、7.7。本文首次测量得到的HSP值随后被用于通过相对能量差(RED)解释渗透促进剂的增强作用以及角质层对载体的吸收情况,相关性良好。角质层HSP值可进一步用于透皮给药、化妆品配方、安全性问题等方面。