Advanced bioactive lipid nanocarriers loaded with natural and synthetic anti-inflammatory actives

Abstract

Abstract Current research is focused toward the development of a new approach based on efficient bioactive lipid nanocarriers (BLN) in order to obtain enhanced benefit to risk ratios of natural and synthetic actives. For this purpose, the bioactivities of several BLN (prepared with raspberry oil, Rso, and rice bran oil, Rbo) containing a natural extract (willow bark extract, Wbe) or a blend of Wbe and the synthetic anti-inflammatory drug indomethacin (Ind) have been comparatively analysed. BLN exhibited homogeneity regarding the particle size (diameters less than 140\u202fnm), excellent physical stability (negative surface charge of −40 and −48\u202fmV) and high encapsulation efficiency (89 to 91% for salicin from Wbe and 65 to 72.5% for Ind). The association of Wbe together with Ind co-loaded BLN resulted in a noticeable amplification of the antioxidant activity (the scavenging of free oxygen radicals exceeds 90%), a protective effect on L929 cells (low apoptosis values of 11.6 and 15.9%) and a significant ability to reduce the TNF-α and IL-6 inflammatory marker levels. The in vitro release, achieved on BLN-Wbe-Ind based-hydrogels, has revealed a gradual release of both kinds of actives. BLN may represent a valuable strategy for overcoming the side effects of synthetic drugs while treating inflammation-related skin disorders.