Design and development of Cerasomal Gallic acid with controllable sustained release for IBD treatment

Inflammatory bowel disease (IBD) is characterized by chronic relapsing inflammatory disease in the gastrointestinal tract. In spite of great efforts have been made during the past few years, as well as the increasing number of therapeutic agents tested so far, relatively limited compounds are currently available for the management of IBD. Design of a novel biologic therapy by using natural small-molecule drugs with lower side effects than chemicals should be further developed for treating IBD. On the other hand, safely and effectively delivering of drugs via the oral route remains highly challenging for formulation fields. In the present work, we have, for the first time, utilized Gallic acid (GA) as bioactive polyphenols with anti-inflammatory effects capsulated in cerasome forcontrolled drug release. An organic-inorganic hybrid cerasome-forming lipid (CFL) was synthesized via a two-step chemical reaction. Then, the designed thermosensitive liposomal cerasome was prepared by the thin-film hydration method with four ratios at CFL and phospholipids, DPPC (۱۰:۰, ۷:۳, ۵:۵, ۳:۷, ۰:۱۰), respectively. The GA-loaded cerasomes were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), fluorescence spectroscopy, and ultraviolet-visible (UV-vis) spectroscopy, which demonstrated that cerasomes with an average diameter of ۳۳۵ nmand zeta potential -۲۳.۵ mv were uniform. The optimal GA-Cerasomes formulation illustrated high encapsulation (~۵۳%) and controlled release characteristics (gradually released in ۱۴۰h). The structural stability, dispersion stability were systematically investigated by physicochemical characterization methods. We observed that cerasome is more stability than liposome and in the prolonged blood circulation the distribution of them in the perfused tissues were improved. Together these results suggest that cerasomes will be a promising drug delivery system for the long-term storage and controllable sustained release of the antioxidant GA. Consequently, this thermosensitive GA-Cerasomes has considerable prospects as an IBD drug delivery carrier. However, the observation of cellular uptake in vitro and tissue distribution assays in vivo needs to be further determined.

کلیدواژه ها:

Cerasome ، Gallic acid ، Sustained release ، Inflammatory Bowel Disease ، Drug delivery