Floating-bioadhesive gastroretentiveCaesalpinia pulcherrima-based beads of amoxicillin trihydrate forHelicobacter pylorieradication

Abstract

Context: An oral dosage form containing floating bioadhesive gastroretentive microspheres forms a stomach-specific drug delivery system for the treatment of Helicobacter pylori. Objectives: To prepare and evaluate controlled release floating bioadhesive gastroretentive chitosan-coated amoxicillin trihydrate-loaded Caesalpinia pulcherrima galactomannan (CPG)-alginate beads (CCA-CPG-A), for H. pylori eradication. Materials and methods: CCA-CPG-A beads were prepared by ionotropic gelation, using 2 3 factorial design with quantity of drug, combination of CPG with sodium alginate and concentration of calcium chloride as variables. Beads facilitated mucoadhesion to gastric mucosa with floating nature caused by chitosan coating for wide distribution throughout GIT. Developed beads were evaluated for characteristics like beads size-morphology, entrapment efficiency, DSC, XRD, FTIR, swelling ratio, in vitro mucoadhesion, in vitro drug release, in vitro floating and in vitro H. pylori growth inhibition studies. CCA-CPG-A beads were studied in Wistar rats for in vivo gastric mucoadhesion, in vivo H. pylori growth inhibition studies using PCR amplification of isolated DNA, rapid urease test. Result: Developed beads possess drug release of 79-92%, entrapment efficiency of 65-89%, mucoadhesion of 61-89%. In vivo mucoadhesion study showed more than 85% mucoadhesion of beads even after 7th hour. In vitro-in vivo growth inhibition study showed complete eradication of H. pylori. Discussion: CPG-alginate and chitosan in beads interacts with gastric mucosubstrate surface for prolonged gastric residence with floating bioadhesion mechanism for H. pylori eradication in rats. Conclusion: Floating bioadhesive CCA-CPG-A beads offer a promising drug delivery system for H. pylori eradication at lower dose, reduced adverse effect and enhance bioavailability.

Morphological, Release and Antibacterial Performances of Amoxicillin-Loaded Cellulose Aerogels

“…Besides, the peaks at 1163, and 1061 cm −1 correspond to the C–O asymmetric bridge stretching and the C–O–C pyranose ring skeletal vibration, respectively [ 27 ]. In the case of amoxicillin-loaded MC aerogels (curve b–c), a new peak appears at 1776 cm −1 , which is attributed to β lactam C=O stretching of amoxicillin [ 28 ]. Moreover, the peak intensity is highly enhanced with the increase of amoxicillin loading in the cellulose aerogel.…”

Orally administrated chitosan microspheres bind Helicobacter pylori and decrease gastric infection in mice

“…Focus has been given to understanding bacterial infection mechanisms and interaction with the host [19,20], identifying bacterial specific molecules that may represent potential targets, such as bacterial virulence factors, urease, flagella or surface adhesins [21][22][23]. The combination of these targets with improved encapsulation systems for local delivery of antibiotics (using micro-or nano-systems) [24][25][26][27][28][29][30][31][32][33], usage of compounds from natural sources [34][35][36][37][38][39][40][41] or vaccination [42][43][44][45] has allowed the development of more precise and efficient systems aiming H. pylori eradication.…”

Preparation and evaluation of floating tablets of pregabalin

“…Gastro-retentive systems (floating tablets, pellets or beads) were successfully developed and evaluated for several category of drugs like antihistamines (cetrizeine, famotidine, ranitidine), NSAIDS (ketorolac, celecoxib), antibiotics (metronidazole, ofloxacin, amoxicillin), antidiabetics (metformin, repaglinide) and many more [8][9][10][11][12][13][14][15][16][17] .…”