Department of Chemical Science and Technologies, University of Rome 'Tor Vergata', Via della Ricerca Scientifica, 00133 Rome, Italy.
Department of Pharmacy, University of Naples 'Federico II', Via Domenico Montesano 49, 80131 Naples, Italy.
Molecules. 2020 Feb 16;25(4):866. doi: 10.3390/molecules25040866.
Thymol and the corresponding brominated derivatives constitute important biological active molecules as antibacterial, antioxidant, antifungal, and antiparasitic agents. However, their application is often limited, because their pronounced fragrance, their poor solubility in water, and their high volatility. The encapsulation of different thymol derivatives into biocompatible lignin-microcapsules is presented as a synergy-delivering remedy. The adoption of lignosulfonate as an encapsulating material possessing relevant antioxidant activity, as well as general biocompatibility allows for the development of new materials that are suitable for the application in various fields, especially cosmesis. To this purpose, lignin microcapsules containing thymol, 4-bromothymol, 2,4-dibromothymol, and the corresponding -methylated derivatives have been efficiently prepared through a sustainable ultrasonication procedure. Actives could be efficiently encapsulated with efficiencies of up to 50%. To evaluate the applicability of such systems for topical purposes, controlled release experiments have been performed in acetate buffer at pH 5.4, to simulate skin pH: all of the capsules show a slow release of actives, which is strongly determined by their inherent lipophilicity.
百里酚和相应的溴代衍生物作为抗菌、抗氧化、抗真菌和抗寄生虫药物，构成了重要的生物活性分子。然而，它们的应用往往受到限制，因为它们的香气浓郁、在水中的溶解度低、挥发性高。将不同的百里酚衍生物包封到生物相容性的木质素微胶囊中，被认为是一种协同传递的治疗方法。采用木质素磺酸盐作为一种具有相关抗氧化活性和一般生物相容性的包封材料，允许开发适合各种领域应用的新材料，特别是化妆品。为此，通过可持续的超声处理程序，有效地制备了含有百里酚、4-溴百里酚、2,4-二溴百里酚和相应的 - 甲基化衍生物的木质素微胶囊。活性成分的封装效率高达 50%。为了评估这些系统在局部应用方面的适用性，在 pH 值为 5.4 的醋酸缓冲液中进行了控制释放实验，以模拟皮肤 pH 值：所有的胶囊都显示出活性成分的缓慢释放，这主要取决于其内在的亲脂性。
