Stability Evaluation of Ivermectin-Loaded Biodegradable Microspheres

AAPS PharmSciTech. 2015 Oct;16(5):1129-39. doi: 10.1208/s12249-015-0305-1. Epub 2015 Feb 21.

Abstract

A stability study was performed on ivermectin (IVM)-loaded biodegradable microparticles intended for injection in dogs. The rational was to evaluate the performances upon irradiation of a drug, such as IVM, with a few criticalities with respect to its stability, and toxicity. The goal was to provide valuable information for pharmaceutical scientists and manufacturers working in the veterinary area. The microspheres based on poly(D,L-lactide) and poly-(ε-caprolactone) and loaded with IVM and with the addition of alpha-tocopherol (TCP) as antioxidant were prepared by the emulsion solvent evaporation method and sterilized by gamma irradiation. Microsphere characterization in term of size, shape, polymer, and IVM stability upon irradiation was performed. The results show that the type of polymer significantly affects microsphere characteristics and performances. Moreover, suitably stable formulations can be achieved only by TCP addition.

Keywords: alpha-tocopherol; gamma irradiation; ivermectin; microspheres; poly(D,L-lactide); poly-(ε-caprolactone).

Publication types

  • Comparative Study

MeSH terms

  • Antioxidants / chemistry
  • Antiparasitic Agents / chemistry*
  • Antiparasitic Agents / radiation effects
  • Drug Carriers*
  • Drug Compounding
  • Drug Stability
  • Excipients / chemistry
  • Gamma Rays
  • Ivermectin / chemistry*
  • Ivermectin / radiation effects
  • Microspheres
  • Models, Chemical
  • Polyesters / chemistry*
  • Solubility
  • Veterinary Drugs / chemistry*
  • Veterinary Drugs / radiation effects
  • alpha-Tocopherol / chemistry

Substances

  • Antioxidants
  • Antiparasitic Agents
  • Drug Carriers
  • Excipients
  • Polyesters
  • Veterinary Drugs
  • polycaprolactone
  • poly(lactide)
  • Ivermectin
  • alpha-Tocopherol