Abstract

Objective: The objective of the present study was to chemical modification, characterization and evaluation of mucoadhesive potentiality of Assam bora rice starch as potential excipients in the sustained release drug delivery system. Methods: The starch was isolated from Assam bora rice and esterified using thioglycolic acid and characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and Nuclear magnetic resonance (NMR). The 10% w/v gel formulation based on modified bora rice starch loaded with irinotecan (0.6%) was prepared and evaluated for various rheological properties, ex-vivo mucoadhesion using goat intestine and in vitro drug release study in phosphate buffer pH 6.8.Results: The chemical modification was confirmed by FT-IR and NMR studies with the presence of the peak at 2626.74 cm-1 and a singlet at 2.51 respectively due to–SH group. Ex-vivo mucoadhesion studies showed 6.6 fold increases in mucoadhesion of the modified starch with compared to native starch (46.3±6.79g for native starch; 308.7±95.31g for modified starch). In vitro study showed 89.12±0.84 % of drug release after 6 h in phosphate buffer pH 6.8 and the release kinetics followed Non-Fickian diffusion.Conclusion: The modified Assam bora rice starch enhanced a mucoadhesive property of the native starch and thus, can be explored in future as a potential excipient for the sustained release mucoadhesive drug delivery system.

Highlights

  • The bioadhesion is the term that refers to any kind of bond formed either between two biological surfaces or between a biological and a synthetic surface

  • The Differential scanning calorimetry (DSC) thermograms of native Starch and modified starch were presented in fig

  • While the DSC thermograms of modified starch shows a sharp endotherm at 81.11 ̊c with a heat of fusion 150.20 J/g

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Summary

Introduction

The bioadhesion is the term that refers to any kind of bond formed either between two biological surfaces or between a biological and a synthetic surface. The Mucoadhesive polymers which form noncovalent bonds such as hydrogen bonds, van der Waal’s forces, and ionic interactions have weak bioadhesion [1]. The mucoadhesive delivery systems gain the superiority by having some advantages over conventional systems such as–mucoadhesive delivery systems can be eagerly delivered on the site of action, this kind of systems allow for intimate contact of the formulation with the mucosal surface that enhance the permeability for macromolecules, these delivery systems can lengthen the residence period at the employed site of the dosage form [2, 3]. Thiolated polymers or thiomers covalently anchor with mucus by disulphide bonds and can mimic the natural mechanism of secreted mucus glycoprotein. The cysteine rich sub domain of mucus glycoprotein undergoes thiol/disulphide exchange reaction and forms disulphide bonds between polymer and mucus layer [4, 5]

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