A novel cerasomal gallic acid as a non-ulcerogenic agent with an improved anti-inflammatory potential

Abstract

In order to treat inflammatory bowel disease (IBD), there is an attempt to develop local drug delivery systems. The use of bioactive compounds such as gallic acid (GA) in a precise colon-targeting drug delivery platform is expected to enhance its bioavailability and increase local therapeutic responses. In this study, a novel cerasome-forming lipid (CFL) containing organosilane-based oleic acid was mixed with 1, 2-dipalmitoyl-sn-glycero-3-phosphocholine via one-step construction to prepare composite cerasomes by varying mole ratios. The physicochemical properties, drug-loading capacity, long-term storage stability, and release rates of (GA) from cerasomes have been investigated. The size of cerasomal gallic acid (CG) was about 319 nm with −23 mV surface charge and 77% drug sustained released after 140 h in the simulated gastrointestinal fluids. Composite vesicles consisting of DPPC and CFL with a 1:1 M ratio exhibited good cytocompatibility and cellular uptake, also, the released gallic acid effectively inhibit the reactive species in LPS-induced inflammation of Caco-2 cells, compared to free (GA). Our results indicate that this novel CG has great potential to be applied as a non-ulcerogenic agent due to the prolonging duration of action in IBD therapy.