Degradation behaviour of microspheres prepared by spray-drying poly(D,L-lactide) and poly(D,L-lactide-co-glycolide) polymers

Int J Pharm. 2006 Dec 1;326(1-2):139-47. doi: 10.1016/j.ijpharm.2006.07.030. Epub 2006 Jul 22.

Abstract

Polymeric microsphere degradation must be taken into account in the design of drug delivery systems to be injected in in vivo systems, thus a prior analysis of in vitro degradation behaviour of microspheres appears to be necessary. In this study degradation characteristics of poly(lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) microspheres prepared by the spray-drying technique have been examined. It was found that a slow decrease in molecular weight took place during the first stage of degradation, and the value of the rate constant decreased with the increase of the percentage of lactic acid of the polymer in a linear way. Thus, the period of time of this first stage decreased with the increase of content of glycolidyl units of the polymer, and it was the unique stage observed in PLA microspheres after 5 months of study. During this period of time, significant mass loss was not observed in the microspheres. The second stage of degradation of PLGA microspheres showed a larger rate constant, whose value increased with the content of glycolidyl units of the polymer. Mass loss was observed from number-average molecular weight about 6000. A sharp decrease of glass transition temperature (T(g)) was observed coinciding with the start of mass loss. This fact was accompanied by a physical change of the samples, fusion of microspheres to form large particles, which also fusion to form a unique mass of polymer; moment from that the degradation process was quicker.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biocompatible Materials*
  • Calorimetry
  • Delayed-Action Preparations
  • Drug Carriers
  • Glass
  • Hydrogen-Ion Concentration
  • Lactic Acid / chemistry
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Molecular Weight
  • Polyesters / chemistry*
  • Polyglactin 910 / chemistry*
  • Polymers / chemistry
  • Temperature
  • Time Factors

Substances

  • Biocompatible Materials
  • Delayed-Action Preparations
  • Drug Carriers
  • Polyesters
  • Polymers
  • Lactic Acid
  • Polyglactin 910
  • poly(lactide)