Formulation, optimization and characterization of allantoin-loaded chitosan nanoparticles to alleviate ethanol-induced gastric ulcer: in-vitro and in-vivo studies

Abstract

Allantoin (ALL) is a phytochemical possessing an impressive array of biological activities. Nonetheless, developing a nanostructured delivery system targeted to augment the gastric antiulcerogenic activity of ALL has not been so far investigated. Consequently, in this survey, ALL-loaded chitosan/sodium tripolyphosphate nanoparticles (ALL-loaded CS/STPP NPs) were prepared by ionotropic gelation technique and thoroughly characterized. A full 24 factorial design was adopted using four independently controlled parameters (ICPs). Comprehensive characterization, in vitro evaluations as well as antiulcerogenic activity study against ethanol-induced gastric ulcer in rats of the optimized NPs formula were conducted. The optimized NPs formula, (CS (1.5% w/v), STPP (0.3% w/v), CS:STPP volume ratio (5:1), ALL amount (13 mg)), was the most convenient one with drug content of 6.26 mg, drug entrapment efficiency % of 48.12%, particle size of 508.3 nm, polydispersity index 0.29 and ζ-potential of + 35.70 mV. It displayed a sustained in vitro release profile and mucoadhesive strength of 45.55%. ALL-loaded CS/STPP NPs (F-9) provoked remarkable antiulcerogenic activity against ethanol-induced gastric ulceration in rats, which was accentuated by histopathological, immunohistochemical (IHC) and biochemical studies. In conclusion, the prepared ALL-loaded CS/STPP NPs could be presented to the phytomedicine field as an auspicious oral delivery system for gastric ulceration management.

Impairment of electron transport chain and induction of apoptosis by chrysin nanoparticles targeting succinate-ubiquinone oxidoreductase in pancreatic and lung cancer cells

“…The IC 50 values for CCNPs and CNPs were 14, 20, and 155.6 µg/mL and 394, 285, and 311 µg/mL in A549, PANC-1, and normal broblast cells, respectively, which agreed with results from previous studies (40,41). These results indicated that CCNPs could improve the e ciency of chrysin on cell growth inhibition (40).…”

Gastro protecting influence of Topiramate in ethanol produced gastric ulcers in rats

“…Ethanol is used for inducing experimental gastric ulcers in rats either alone [ 19 , 20 ] or in combination with hydrochloric acid (HCL) [ 21 , 22 ]. Ethanol was used for the induction of gastric ulcers as we observed it to be highly effective in producing gastric ulcers in fasted rats [ 7 ], the ulceration was observed in all the animals administered ethanol.…”

Mucoadhesive and Antimicrobial Allantoin/β Cyclodextrins-Loaded Carbopol Gels as Scaffolds for Regenerative Medicine

“…For polymers with enhanced hydrophilicity, the diffusion coefficient is low [ 50 ]. The decrease in diffusion coefficient has been explained byenhanced cluster size of the diffuse species, which become less movable [ 51 ].…”