Biocompatibility and Targeting Efficiency of Encapsulated Quinapyramine Sulfate-Loaded Chitosan-Mannitol Nanoparticles in a Rabbit Model of Surra

Antimicrob Agents Chemother. 2018 Oct 24;62(11):e00466-18. doi: 10.1128/AAC.00466-18. Print 2018 Nov.

Abstract

Quinapyramine sulfate (QS) produces trypanocidal effects against the parasite Trypanosoma evansi but is often poorly tolerated and causes serious reactions in animals. The encapsulation of QS in chitosan-mannitol to provide sustained release would improve both the therapeutic effect of QS and the quality of life of animals treated with this formulation. QS was encapsulated into a nanoformulation prepared from chitosan, tripolyphosphate, and mannitol nanomatrix (ChQS-NPs). ChQS-NPs were well ordered in shape, with nanoparticle size, as determined by transmission electron microscopy and atomic force microscopy. Our research revealed dose-dependent effects on biosafety and DNA damage in mammalian cells treated with ChQS-NPs. ChQS-NPs were absolutely risk-free at effective as well as many times higher doses against T. evansi ChQS-NPs were effective in rabbits, as they killed the parasites, relieving the animals from the clinical symptoms of the disease. The extent of this protection was similar to that observed with the conventional drug at higher dosages (5 mg QS/kg of body weight). ChQS-NPs are safe, nontoxic, and more effective than QS and offer a promising alternative to drug delivery against surra in animal models. ChQS-NPs may be useful for the treatment of surra due to reduced dosages and frequency of administration.

Keywords: Trypanosoma evansi; chitosan; mannitol; nanoparticles; polymer therapeutics; quinapyramine sulfate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biocompatible Materials / administration & dosage*
  • Cell Line, Tumor
  • Chitosan / administration & dosage*
  • Disease Models, Animal
  • Drug Carriers / administration & dosage
  • Drug Delivery Systems / methods
  • HeLa Cells
  • Humans
  • Mannitol / administration & dosage*
  • Microscopy, Atomic Force / methods
  • Microscopy, Electron, Transmission / methods
  • Nanoparticles / administration & dosage*
  • Particle Size
  • Quality of Life
  • Quinolinium Compounds / pharmacology*
  • Rabbits
  • Trypanosoma / drug effects

Substances

  • Biocompatible Materials
  • Drug Carriers
  • Quinolinium Compounds
  • chitosan sulfate
  • Mannitol
  • Chitosan
  • quinapyramine