Polysaccharides-based multiparticulated interpolyelectrolyte complexes for controlled benznidazole release

Int J Pharm. 2018 Jul 10;545(1-2):366-377. doi: 10.1016/j.ijpharm.2018.05.017. Epub 2018 May 7.

Abstract

Polysaccharides-based delivery systems and interpolyelectrolyte complexes (IPECs) are interesting alternatives to control the release of drugs, thereby improving therapies. Benznidazole (BZ) is the selected drug for Chagas disease pharmacotherapy. However, its side effects limit its efficacy and safety. We developed novel multiparticulated BZ-loaded IPECs based on chitosan and alginic acid, and investigated their physicochemical and pharmacotechnical properties. IPECs were obtained using the casting solvent method, followed by wet granulation. They presented ionic interaction between the biopolymers, revealed that free BZ was uniformly distributed and showed adequate flow properties for hard gelatin-capsule formulation. The multiparticles exhibited mucoadhesion properties and revealed modulation of BZ release, depending on the release media, in accordance with the fluid uptake. The IPECs developed possess interesting properties that are promising for the design of novel alternatives to improve Chagas disease pharmacotherapy, which would diminish BZ's adverse effects and/or allow a reduction in the frequency of BZ administration.

Keywords: Alginic acid; Benznidazole; Chitosan; Drug delivery; Polyelectrolyte complexes.

MeSH terms

  • Adhesiveness
  • Administration, Oral
  • Alginates / chemistry*
  • Capsules
  • Chagas Disease / drug therapy
  • Chagas Disease / parasitology
  • Chitosan / analogs & derivatives
  • Chitosan / chemistry*
  • Delayed-Action Preparations
  • Drug Carriers*
  • Drug Compounding
  • Drug Liberation
  • Gelatin / chemistry
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Kinetics
  • Models, Chemical
  • Nitroimidazoles / administration & dosage
  • Nitroimidazoles / chemistry*
  • Polyelectrolytes / chemistry*
  • Solubility
  • Solvents / chemistry
  • Technology, Pharmaceutical / methods
  • Trypanocidal Agents / administration & dosage
  • Trypanocidal Agents / chemistry*

Substances

  • Alginates
  • Capsules
  • Delayed-Action Preparations
  • Drug Carriers
  • Hexuronic Acids
  • Nitroimidazoles
  • Polyelectrolytes
  • Solvents
  • Trypanocidal Agents
  • Glucuronic Acid
  • Gelatin
  • Chitosan
  • benzonidazole