Designing, structural determination and biological effects of rifaximin loaded chitosan- carboxymethyl chitosan nanogel

Abstract

Due to the poor solubility and permeability of rifaximin (RFX), it is not effective against intracellular pathogens although it shows strong activity against most bacteria. To develop an effective mucoadhesive drug delivery system with a targeted release in bacterial infection site, RFX-loaded chitosan (CS)/carboxymethyl-chitosan (CMCS) nanogel was designed and systematically evaluated. FTIR, DSC, and XRD demonstrated that the nanogel was formed by interactions between the positively charged NH₃⁺ on CS and CMCS, and the negatively charged COO on CMCS. RFX was encapsulated into the optimized nanogel in amorphous form. The nanogel was a uniform spherical shape with a mean diameter of 171.07 nm. It had excellent sustained release, strong mucin binding ability, and pH-responsive properties of quicker swelling and release at acidic pH. It showed low hemolytic ratio and high antioxidant activity. The present investigation indicated that the CS-nanogel could be potentially used as a promising bacterial responsiveness drug delivery system.

Keywords: Acetic acid; Bioadhesive; Carboxy methyl chitosan; Chitosan; DPPH; Mucin (from porcine stomach); Nanogel; Potassium bromide (KBr); Rifaximin; Tri polyphosphate; Triton X-100; pH-responsiveness.