Design, statistical optimisation, characterisation and pharmacodynamic studies on Pioglitazone hydrochloride floating microparticles

J Microencapsul. 2014;31(4):406-14. doi: 10.3109/02652048.2013.863399. Epub 2014 Apr 3.

Abstract

The purpose of this study was to develop floating microparticles containing Pioglitazone HCl, for controlled release and perform pharmacodynamic studies. The FTIR and DSC studies revealed that there is no interaction between drug and excipients used. The 2(2) factorial design was employed to evaluate the effect of drug: polymer (total) and Eudragit RS 100: Eudragit RL 100. The floating microparticles were prepared by solvent evaporation technique. The predicted and actual values of drug release at 1 h, 8 h and drug entrapment were 38.307%, 77.76%, 84.25% and 38.712%, 76.237% and 84.62%, respectively. XRD and SEM studies showed reduced crystallinity of drug and spherical microparticles. Buoyancy studies revealed good floating of particles for 12 h. Pharmacodynamic studies showed significant reduction in blood glucose levels in male New Zealand rabbits. The results demonstrate the feasibility of the factorial design in successfully developing floating microparticles of Pioglitazone HCl for controlled release.

Keywords: Eudragit RS 100; Pioglitazone floating microparticles; RL 100; factorial design; pharmacodynamics.

MeSH terms

  • Animals
  • Blood Glucose / metabolism
  • Delayed-Action Preparations* / chemistry
  • Delayed-Action Preparations* / pharmacokinetics
  • Delayed-Action Preparations* / pharmacology
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Carriers* / pharmacology
  • Drug Evaluation, Preclinical
  • Hypoglycemic Agents* / chemistry
  • Hypoglycemic Agents* / pharmacokinetics
  • Hypoglycemic Agents* / pharmacology
  • Male
  • Pioglitazone
  • Rabbits
  • Thiazolidinediones*

Substances

  • Blood Glucose
  • Delayed-Action Preparations
  • Drug Carriers
  • Hypoglycemic Agents
  • Thiazolidinediones
  • Pioglitazone