Elevated temperature accelerated release testing of PLGA microspheres

J Control Release. 2006 May 30;112(3):293-300. doi: 10.1016/j.jconrel.2006.02.015. Epub 2006 Apr 27.

Abstract

Drug release from four different poly(lactic-co-glycolic) acid (PLGA) microsphere formulations was evaluated under "real-time" (37 degrees C) and accelerated release testing conditions of elevated temperature (45, 53, 60 and 70 degrees C) and increase in flow rate (4-35 ml/min) using United States Pharmacopeia (USP) apparatus 4. Formulation 5 K (composed of low Mw PLGA) exhibited diffusion-controlled kinetics in "real-time". Whereas, formulations 25 K, 28 K and 70 K (composed of medium and high Mw PLGA) followed erosion-controlled kinetics at 37 degrees C. Temperature-induced degradation of the microspheres was studied by monitoring drug release rates, change in molecular weight and morphological changes. Drug release rates at elevated temperature were used to predict "real-time" release applying the Arrhenius equation. The energy of activation for dexamethasone release from PLGA microspheres was calculated as 19.14 kcal/mol. Molecular weight change measured by gel permeation chromatography followed first order kinetics for both "real-time" and accelerated release. All four formulations exhibited morphological changes (such as surface pore closing and geometry change) at elevated temperature with consequent reduction in burst release.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Chemistry, Pharmaceutical
  • Hot Temperature*
  • Lactic Acid / chemistry*
  • Lactic Acid / pharmacokinetics*
  • Microspheres*
  • Polyglycolic Acid / chemistry*
  • Polyglycolic Acid / pharmacokinetics*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry*
  • Polymers / pharmacokinetics*
  • Temperature

Substances

  • Polymers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid