Formulation and in vitro evaluation of a thermoreversible mucoadhesive nasal gel of itopride hydrochloride

Drug Dev Ind Pharm. 2018 Nov;44(11):1857-1867. doi: 10.1080/03639045.2018.1504059. Epub 2018 Aug 24.

Abstract

Itopride hydrochloride (ITO HCl) is a prokinetic agent, used in the treatment of gastrointestinal motility disorders. The aim of the study was to develop stable mucoadhesive thermoreversible nasal gel to avoid first pass effect. ITO HCl was incorporated into the blends of thermoreversible polymers like poloxamer 407 and various mucoadhesive polymers in different concentrations to increase the contact of the formulations with nasal mucosa. The compatibility between the drug and the suggested polymers was studied by Fourier transform infrared and differential scanning calorimetry (DSC). The formulations were evaluated for clarity, pH, gelation temperature, mucoadhesive strength, gel strength, viscosity, and drug content. In addition, the in vitro drug release and the dissolution efficiency (DE)% were measured. The optimized formulations that showed the highest dissolution efficiency% (DE%) in saline phosphate buffer of pH 6.4 at 35 ± 0.5 °C were chosen for stability testing at temperatures of 4 ± 2 and 25 ± 2 °C/60 ± 5% RH. It was found that F1 and F17 that contain 18% w/v poloxamer 407 and 0.5% w/v of hydroxypropylmethyl cellulose K4M or methyl cellulose (MC), respectively, showed higher stability results as indicated by their higher t90 values (days).

Keywords: Itopride hydrochloride; mucoadhesive; nasal drug delivery; poloxamer 407; thermal gel.

MeSH terms

  • Administration, Intranasal
  • Benzamides / administration & dosage
  • Benzamides / chemistry*
  • Benzyl Compounds / administration & dosage
  • Benzyl Compounds / chemistry*
  • Drug Compounding
  • Drug Liberation
  • Drug Stability
  • Gels
  • Hydrogen-Ion Concentration
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Temperature
  • Viscosity

Substances

  • Benzamides
  • Benzyl Compounds
  • Gels
  • itopride