Abstract
The present study has been undertaken to apply the concept of nanoparticulate mucopenetrating drug delivery system for complete eradication of Helicobacter pylori (H. pylori), colonised deep into the gastric mucosal lining. Most of the existing drug delivery systems have failed on account of either improper mucoadhesion or mucopenetration and no dosage form with dual activity of adhesion and penetration has been designed till date for treating H. pylori induced disorders. In the present study, novel chitosan-alginate polyelectrolyte complex (CS-ALG PEC) nanoparticles of amoxicillin have been designed and optimized for various variables such as pH and mixing ratio of polymers, concentrations of polymers, drug and surfactant, using 33 Box-Behnken design. Various studies like particle size, surface charge, percent drug entrapment, in-vitro mucoadhesion and in-vivo mucopenetration of nanoparticles on rat models were conducted. The optimised FITC labelled CS-ALG PEC nanoparticles have shown comparative low in-vitro mucoadhesion with respect to plain chitosan nanoparticles, but excellent mucopenetration and localization as observed with increased fluorescence in gastric mucosa continuously over 6 hours, which clinically can help in eradication of H. pylori.
Highlights
Amoxicillin is a well tolerated, broad-spectrum, beta-lactam antibiotic for the treatment of a wide range of bacterial infections, including Helicobacter pylori (H. pylori)
The strategy for effective delivery of antibiotics to H. pylori has shifted to the use of mucoadhesive micro or nano particulate based delivery systems based on the fact that mucoadhesive particulate show longer retention in stomach and deliver the antibiotic locally in the stomach mucosa for longer duration [11]
CS-ALG PEC nanoparticles can be utilised as sustained release gastroretentive delivery system for antibiotics like Amoxicillin, Clarithromycin or Metronidazole in eradication of H. pylori where antibiotic formulations fail to deliver the minimum inhibitory concentration in gastric mucosa due to instability at low pH & short residence time in the stomach [12]
Summary
Amoxicillin is a well tolerated, broad-spectrum, beta-lactam antibiotic for the treatment of a wide range of bacterial infections, including Helicobacter pylori (H. pylori). The final concentration range selected for optimization study using Box Behnken design was 0.02–0.06 % w/v of CS, 0.1 % w/v of ALG, 0.01–0.04 % w/v of Amoxicillin and 0.0–0.025 % w/v solution of Pluronic F-127 (surfactant) as tabulated below: Tab. 1.
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