Spray-dried microspheres based on methylpyrrolidinone chitosan as new carrier for nasal administration of metoclopramide

Eur J Pharm Biopharm. 2008 Feb;68(2):245-52. doi: 10.1016/j.ejpb.2007.05.002. Epub 2007 May 13.

Abstract

The work purpose was to study the application of 5-methylpyrrolidinone chitosan (MPC) for preparing mucoadhesive microparticles for the nasal administration of drugs. Microspheres were produced by the spray-drying technique using MPC; metoclopramide hydrochloride (MC) was chosen as model drug. Chitosan microparticles were prepared as a comparison. The microparticles obtained were characterised (encapsulation efficiency, morphology, size and drug release behaviour). In-vitro mucoadhesive tests, swelling tests and ex-vivo studies using sheep nasal mucosa were performed. The hydrogel formation from microspheres was studied in different media and at different pHs. Microspheres are able to control the in-vitro MC release. MPC microparticles show good in-vitro mucoadhesive properties and ex-vivo controlled permeation profiles. The hydrogel formation is dependent mainly on the medium used: ionically crosslinked hydrogel was hypothesized. These in-vitro and ex-vivo preliminary results show that spray-dried microspheres based on MPC could be a suitable nasal delivery system for the administration of metoclopramide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intranasal
  • Animals
  • Antiemetics / administration & dosage*
  • Chitosan / chemistry*
  • Drug Carriers
  • Hydrogels
  • Metoclopramide / administration & dosage*
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Pyrrolidinones / chemistry*
  • Sheep

Substances

  • Antiemetics
  • Drug Carriers
  • Hydrogels
  • Pyrrolidinones
  • methylpyrrolidinone chitosan
  • Chitosan
  • Metoclopramide