Anti-ulcerogenic and anti-inflammatory potential of ethyl ascorbic acid protected quercetin-pantoprazole pellets and its polyphenolic binding with bovine serum albumin; in-vitro, in vivo, and in-silico analysis

The objective of the recent study was to improve the potency of proton pump inhibitors (PPI) by antagonistic binding of quercetin (Quer) with bovine serum albumin (BSA) previously protected by newly synthesized ethyl ascorbic acid (EAA). Dually coated pellets (CPQ-P4a-d) of Pantoprazole (Pantop) and Quer were prepared by using EAA and Eudragit RL-100 (ERL-100) as inner and outer coats, respectively. Alkaline sensitivity, permeation properties, and DPPH scavenging activity of Quer and EAA were observed. Changes from the negative charge on the surface of uncoated pellets (UPQP4) to the positive charge in CPQ-P4a-d were observed and may be due to the presence of quaternary ammonium in ERL-100, which ultimately favored mucoadhesive behavior. Content uniformity and confirmation of the binding interaction in the form of hydrogen bonding of Pantop and Quer at site I and site III of BSA were observed by the newly developed High-performance Liquid Chromatography (HPLC) method and computational studies. Binding plots Stern-Volmer, Direct, Scatchard, Klotz, and Hitchcock provide complimentary information about the ligand-BSA interaction's nature, stoichiometry, and binding strength. Maximum absorbable dose (MAD) was 42 ± 0.01 %, paw edema inhibition was 83.1 ± 1.12 %, ulcer index rate was 82.12 ± 1.42 % and ulcer score turned to 0 and 1 ± 0.04 % with CPQP4d proved its anti-ulcerant effect which were calculated by the histopathological scoring model. Reduction in severity of ulcers and restoration of stomach pH, proved CPQP4d as an alternative of conventional treatment of gastric ulcers (GU) and atrophic gastritis (AG).