Burns ( IF 3.2 ) Pub Date : 2021-08-03 , DOI: 10.1016/j.burns.2021.07.017 Maryam Hosseini 1 , Michael S Roberts 2 , Reza Aboofazeli 3 , Hamid R Moghimi 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 (δD), bipolar (δP), and hydrogen bonding (δH) were calculated by HSPiP software.
Results showed δD, δP, and δH 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 δP. Increased temperature decreased them with more changes in δH. 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.
中文翻译:
三度烧伤焦痂汉森溶解度参数的测定
局部药物治疗是三度烧伤创面治疗最有效的方法之一。为了优化和增强药物通过烧伤焦痂的渗透,我们需要表征这一屏障,最重要的是,它对药物的亲和力;本次调查的对象。
汉森溶解度参数 (HSP),作为极性和亲和标度,通过使用 25 °C 和 32 °C 下的 19 种溶剂和两个水合水平的重量分析结合热分析和 Karl 的吸收研究测量人类三度烧伤焦痂费歇尔滴定法。HSP 参数的色散 ( δ D )、双极 ( δ P ) 和氢键 ( δ H ) 由 HSPiP 软件计算。
结果显示,正常水合样品在 25 和 32 °C 时的δ D、δ P和δ H分别为 17.0、12.5、14.6 和 16.8、12.4、14.4。完全水合作用将 HSP 值提高到 17.2、12.9、15.3 (25 °C) 和 17.1、12.8、15.1 (32 °C)。所有参数均观察到溶剂吸收和 HSP 值之间的良好相关性;δ P更高。随着δ H的更多变化,温度升高会降低它们。计算了相对能量差异 (RED),并证明它是预测药物-焦痂亲和力的良好参数。
获得的信息可用于通过烧伤焦痂给药的药物选择和载体设计。