Department of Pharmaceutics and 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 4102, Australia; School of Pharmacy and Medical Sciences, University of South Australia, Adelaide 5000, Australia.
Burns. 2022 Jun;48(4):860-871. doi: 10.1016/j.burns.2021.07.017. Epub 2021 Aug 3.
Topical drug therapy is one of the most effective approaches in third-degree burn wound treatments. To optimize and enhance drug permeation through burn eschar, we need to characterize this barrier, most importantly, its affinity to drugs; the subject of this investigation. Hansen Solubility Parameters (HSP), as polarity and affinity scale, were measured here for human third-degree burn eschar through uptake studies using 19 solvents at 25 °C and 32 °C and two hydration levels by gravimetric method combined with thermal analysis and Karl Fischer titration. HSP parameters of dispersion (δ), bipolar (δ), and hydrogen bonding (δ) were calculated by HSPiP software. Results showed δ, δ and δ of 17.0, 12.5, 14.6 and 16.8, 12.4, 14.4 at 25 and 32 °C respectively for normally-hydrated samples. Full hydration increased HSP values to 17.2, 12.9, 15.3 (25 °C) and 17.1, 12.8, 15.1 (32 °C). Good correlations between solvents uptakes and HSP values were observed for all parameters; higher for δ. Increased temperature decreased them with more changes in δ. Relative Energy Differences (RED) were calculated and shown to be a good parameter for predicting drug-eschar affinity. The obtained information is useful for drug selection and carrier design in drug delivery through burn eschar.
局部药物治疗是治疗三度烧伤创面最有效的方法之一。为了优化和增强药物通过烧伤焦痂的渗透,我们需要对这种屏障进行特征描述,最重要的是其对药物的亲和力;这是本研究的主题。Hansen 溶解度参数(HSP)作为极性和亲和力的尺度,通过在 25°C 和 32°C 下使用 19 种溶剂和两种水合水平的吸收研究,用重量法结合热分析和卡尔费休滴定法对人体三度烧伤焦痂进行了测量。HSPiP 软件计算了色散(δ)、双极(δ)和氢键(δ)的 HSP 参数。结果表明,正常水合样品在 25°C 和 32°C 时的 δ、δ 和 δ 值分别为 17.0、12.5、14.6 和 16.8、12.4、14.4。完全水合将 HSP 值提高到 17.2、12.9、15.3(25°C)和 17.1、12.8、15.1(32°C)。所有参数都观察到溶剂吸收与 HSP 值之间存在良好的相关性,其中 δ 的相关性更高。温度升高会降低它们,而 δ 的变化更大。计算了相对能量差异(RED),并证明它是预测药物-焦痂亲和力的一个很好的参数。获得的信息对于通过烧伤焦痂输送药物时的药物选择和载体设计很有用。