Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

Abstract

Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility of the flavonoid. The formulations also contained sodium alginate as a gel forming agent, calcium carbonate as a calcium source and carbon dioxide producer and hydroxypropyl methylcellulose K100M as a drug release retarding polymer. The chewable tablets incorporated mannitol as a diluent. Both liquid and chewable tablet formulations exhibited rapid floating behaviour (lag time < 1 min) and long floating duration (>24 h) in 0.1 N HCl. The optimized liquid formulation showed superior characteristics based on high raft strength (10.4 g) and sustained release of quercetin (93 % over 8 h) whereas the optimized chewable tablet formulation exhibited lower raft strength (7.2 g) and lower drug release (79 % in 8 h). The optimized liquid and chewable tablet formulations were found to induce anti-inflammatory activity in cell culture using RAW 264.7 cells macrophages and enhance the migration of human gastric adenocarcinoma (AGS) epithelial cells in vitro , indicating wound healing potential for treatment of gastric ulcers.

Development of Gastroretentive Carriers for Curcumin-Loaded Solid Dispersion Based on Expandable Starch/Chitosan Films

“…The poor aqueous solubility and dissolution rate of curcumin may be improved by the formulation of solid dispersions. This strategy involves intimate mixing of hydrophilic polymers and bioactive compounds, for example, from plants, including curcumin, resveratrol, quercetin, and glycosides [9][10][11][12][13]. The bioavailability of curcumin may be further enhanced by employing gastroretentive drug delivery systems, which are designed to extend residence times in the stomach, resulting in prolonged drug release and thereby improving bioavailability.…”

Curculigoside attenuates Helicobacter pylori-induced inflammation and apoptosis of gastric mucosal epithelial cells via NF-κB pathway

“…Further investigation revealed that Cur suppressed H. pylori-induced ROS production and apoptosis. Interestingly, several studies of Cur have confirmed multiple biological activities, such as anti-inflammatory and anti-tumor effects [15]. Cur has been reported to mitigate hepatic ischemia/reperfusion-induced (HI-RI-induced) oxidative stress, inflammation, and apoptosis by activating the nuclear factor erythroid 2-related factor 2/heme oxygenase-1 (Nrf-2/HO-1) pathway [16].…”

Formulation and evaluation of raft forming pirenzepinedihydrochloride floating tablets for peptic ulcer

“…The 3D-response surface plots, 2D-contour plots and perturbation graphs generated by the Design Expert ® software were used to understand the relationship between the independent and dependent or response variables. [15][16][17][18][19][20] • The active drug nature and drug-excipients compatibility study was done prior to the formulation by Fourier transform infra-red (FTIR) by comparing spectral peaks in the spectra of PNZ drug and excipientswith standard reference spectra. 22 • Differential Scanning Calorimetry (DSC) • DSC is one of the most used calorimetric techniques, employed to characterize the solubility and physical state of drug in the complex.…”

“…Oral route has high patient acceptability, primarily due to ease of administration. 4 Over the years, oral dosage forms have become increasingly sophisticated with major role being played by control release drug delivery system. The Control release drug delivery system release drug at a predetermined rate, as determined by drug's pharmacokinetics and desired therapeutic concentration.…”