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. 2011 Jul-Sep;79(3):673-94.
doi: 10.3797/scipharm.1011-05. Epub 2011 May 19.

Amoxicillin loaded chitosan-alginate polyelectrolyte complex nanoparticles as mucopenetrating delivery system for h. Pylori

Saahil Arora  1 , Sankalp Gupta, Raj K Narang, Ramji D Budhiraja
Affiliations

Amoxicillin loaded chitosan-alginate polyelectrolyte complex nanoparticles as mucopenetrating delivery system for h. Pylori

Saahil Arora et al. Sci Pharm. 2011 Jul-Sep.

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 3(3) 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.

Keywords: Box Behnken design; Factorial design; Helicobacter pylori; Mucopenetration; Stomach specific delivery system.

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Figures

Fig. 1.
Fig. 1.
Response surface plot showing effect of Drug and Chitosan concentration on a) Particle size (Y1), b) Zeta potential (Y2) and c) % Drug Entrapment (Y3).
Fig. 2.
Fig. 2.
Linear correlation plots between actual and predicted values of (a) Particle size; (b) Zeta potential; (c) Percent Drug Entrapment.
Fig. 3.
Fig. 3.
In vitro stability of amoxicillin in simulated gastric fluid (pH 1.2) (n = 3).
Fig. 4.
Fig. 4.
SEM micrograph of amoxicillin loaded CS-ALG polyanionic nanoparticles
Fig. 5.
Fig. 5.
FTIR spectra of CS-ALG PEC nanoparticles with Amoxicillin
Fig. 6.
Fig. 6.
In vitro release profiles of the optimised formulation of CS–ALG PEC nanoparticles in SGF, pH 1.2
Fig. 7.
Fig. 7.
In-vivo mucopenetration studies of CS-ALG PEC on Gastric mucosa (Digital microscope magnification-100X)
Fig. 8.
Fig. 8.
In-vivo mucopenetration studies of CS-ALG PEC on Gastric mucosa (Fluorescent microscope magnification-40X)
See this image and copyright information in PMC

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