Influence of chitosan type on the properties of extruded pellets with low amount of microcrystalline cellulose

AAPS PharmSciTech. 2007 Aug 10;8(3):E64. doi: 10.1208/pt0803064.

Abstract

The purpose of this research was to study the influence of type of chitosan with different molecular weights, ie, 190 and 419 kDa, on properties of pellets prepared by extrusion/spheronization. The formulations, consisting of acetaminophen as model drug, chitosan, microcrystalline cellulose (MCC), and dibasic calcium phosphate dihydrate with/without sodium alginate, were extruded using a twin-screw extruder and water as the granulating liquid. With 30% wt/wt MCC and no added sodium alginate, spherical pellets were produced containing low and high molecular weight chitosan at a maximum amount of 60% and 40% wt/wt, respectively. With sodium alginate (2.5% wt/wt), pellets with either type of chitosan (60% wt/wt), MCC (17.5% wt/wt), and acetaminophen (20% wt/wt) could be produced indicating an improved pellet-forming ability. Type and amount of chitosan and added sodium alginate affected physical properties of pellets including size, roundness, crushing force, and drug release. Low molecular weight chitosan produced pellets with higher mean diameter, sphericity, and crushing force. Additionally, the pellets made of low molecular weight chitosan and added sodium alginate showed faster drug release in 0.1 N HCl but had slower drug release in pH 7.4 phosphate buffer. This indicated that drug release from pellets could be modified by the molecular weight of chitosan. In conclusion, the molecular weight of chitosan had a major influence on formation, physical properties, and drug release from the obtained pellets.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates
  • Cellulose / chemistry*
  • Chemistry, Pharmaceutical
  • Chitosan / chemistry*
  • Glucuronic Acid
  • Hexuronic Acids
  • Molecular Weight
  • Particle Size
  • Solubility

Substances

  • Alginates
  • Hexuronic Acids
  • Glucuronic Acid
  • Cellulose
  • Chitosan
  • microcrystalline cellulose