Abstract

The aim of this study was to investigate the potential of Linum usitatissimum mucilage, a natural polymer, in developing a sustained release hydrogel for orally delivered drugs that require frequent dosing. For this purpose, nicorandil (a model drug)-loaded hydrogels with various feed ratios of Linum usitatissimum mucilage, acrylamide (monomer) and methylene bis-acrylamide (crosslinker) were prepared. The newly synthesized hydrogel formulations were probed fundamentally with respect to swelling behaviour, solvent penetration, and the release of the drug from the hydrogels. Later, the selected formulations were further characterized by Fourier-transform infrared spectroscopy, thermal analysis, X-ray diffraction analysis, and scanning electron microscopy. The swelling coefficient demonstrated a linear relation with the polymer ratio; however, an inverse behaviour in the case of monomer and crosslinker was observed. The drug release studies, performed at pH 1.2 and 4.5 and considering the dynamic environment of GIT, demonstrated that all formulations followed the Korsmeyer–Peppas model, displaying a slow drug release via diffusion and polymer erosion. FTIR analysis confirmed the successful grafting of acrylamide on linseed mucilage. Furthermore, scanning electron microscopy revealed a clear surface morphology with folds and pinholes in the hydrogel. Therefore, based upon the in-vitro outcomes, it can be concluded that a promising sustained release hydrogel can be prepared from natural polymer, Linum usitatissimum mucilage, offering many-fold benefits over the conventional synthetic polymers for oral delivery of drugs.

Highlights

  • The oral route of drug delivery is the most convenient way of administration but, at the same time, is associated with fluctuations in plasma drug concentrations that can be critical in certain diseases, for instance, cardiovascular problems [1]

  • Further, been reported in the literature that natural polymers extemporized formulations via grafting and that improvised graft co-polymerization results in superabsorbent hydrogels with a swelling rate that ranges from a fraction of a minute to hours [10,11]

  • Considering the physiochemical properties of the model drug, nicorandilnicorandil, the swelling studies were performed at a pH of 1.2 and 4.5, which mimic the acidic environment of the gastrointestinal track, as per USP

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Summary

Introduction

The oral route of drug delivery is the most convenient way of administration but, at the same time, is associated with fluctuations in plasma drug concentrations that can be critical in certain diseases, for instance, cardiovascular problems [1]. Based on one mechanism or the other, a number of sustained release drug delivery systems have been established, including liposomes, microspheres, nano-emulsions and hydrogels, to name a few [2]. Over the past few decades, studies on novel drug delivery systems in general, and hydrogels in particular, have been focused on the so-called biocompatible synthetic polymers, which have dominated the era because of their consistency and considerable purity. When it comes to the biocompatibility, the biodegradability, the safety, the complications of the synthetic processes and, the cost of production, there is no match to natural polymers. Considering the mentioned advantages, more and more natural polymers are being investigated in developing novel drug delivery systems under the umbrella of ‘naturapolyceutics’ for the delivery of all sorts of drugs

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