Reaction of pectin and glycidyl methacrylate and ulterior formation of free films by reticulation

Int J Pharm. 2008 May 1;355(1-2):184-94. doi: 10.1016/j.ijpharm.2007.12.006. Epub 2007 Dec 23.

Abstract

In this work, low-methoxyl pectin was chemically modified by reaction with glycidyl methacrylate (GMA) to give a material with low hydrosolubility. After physio-chemical characterization by FT-IR, DSC, and TGA analyses, the methacrylated/modified pectin (Pect-GMA) was crosslinked after the addition of sodium persulfate (SP), that actuates as initiator, at 50 degrees C for 24 and 48h either in the presence or not of aqueous polymethacrylate dispersion (Eudragit RS 30 D) to obtain free films by Teflon plate "casting" process. Different Pect-GMA/Eudragit RS 30 D ratios and SP concentrations were used. The free films were characterized by the determination of water vapor transmission (WVT), the swelling index (Ieq%) in simulated gastric (SGF) and intestinal (SIF) fluids, and by scanning electron microscopy (SEM). The presence of ionized groups in Pect-GMA turned the films pH-dependent because Ieq% of swollen crosslinked Pect-GMA films was larger at pH 6.8 than at pH 1.2. This was confirmed by the large pore size observed in the micrographs of SIF-swollen lyophilized films. In this way, films containing Pect-GMA and Eudragit RS 30 D, a time-dependent polymer, may present a synergistic action that favors specific biodegradation of the film in distal end of the gastrointestinal tract (GIT) by enzymes produced by the colonic microflora, enabling the modification of the release kinetics of drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacteria / enzymology
  • Calorimetry, Differential Scanning
  • Chemical Phenomena
  • Chemistry, Physical
  • Colon / microbiology
  • Epoxy Compounds / chemistry*
  • Excipients
  • Hydrogen-Ion Concentration
  • Membranes, Artificial
  • Methacrylates / chemistry*
  • Microscopy, Electron, Scanning
  • Pectins / chemistry*
  • Permeability
  • Polysaccharides / chemistry
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Thermogravimetry
  • Water

Substances

  • Epoxy Compounds
  • Excipients
  • Membranes, Artificial
  • Methacrylates
  • Polysaccharides
  • Water
  • Pectins
  • glycidyl methacrylate