Evaluation of parenteral depot insulin formulation using PLGA and PLA microparticles

J Biomater Appl. 2009 Nov;24(4):309-25. doi: 10.1177/0885328208096238. Epub 2008 Nov 5.

Abstract

PLGA and PLA microparticles entrapping insulin are prepared by solvent evaporation method and are evaluated in diabetes-induced rat for its efficacy in maintaining blood sugar level from a single intramuscular dose. In vitro release of insulin from PLGA and PLA microparticles are 75.35 +/- 1.73% and 67.536 +/- 2.23%, respectively in 168 h (7 days). Released insulin from polymer particles are mostly in monomeric form without aggregation. Optimal use of stabilizers during particle formulation helps in reducing protein denaturation and thus results in stabilized insulin-loaded polymer particles. Intramuscular administration of insulin-loaded PLGA (50 : 50) and PLA microparticles (equivalent to 25 IU insulin/kg of animal weight) in alloxaninduced diabetic rats result in 53.86 +/- 4.2% and 39.52 +/- 6.7% reduction in blood glucose level, respectively in 96 h. This effect continued up to 7 days in case of PLGA and PLA microparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Diabetes Mellitus, Experimental
  • Drug Carriers / therapeutic use
  • Drug Delivery Systems*
  • Female
  • Humans
  • Hypoglycemia
  • Infusions, Parenteral*
  • Injections, Intramuscular
  • Insulin / administration & dosage*
  • Insulin / analogs & derivatives*
  • Insulin / metabolism*
  • Insulin / therapeutic use
  • Lactic Acid / chemistry*
  • Microspheres
  • Particle Size
  • Polyesters
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry*
  • Rats
  • Rats, Wistar
  • Time Factors

Substances

  • Drug Carriers
  • Insulin
  • Polyesters
  • Polymers
  • insulin, depot-
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • poly(lactide)