Evaluation of parenteral depot insulin formulation using PLGA and PLA microparticles.
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.
Naha
Pratap C
PC
National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi 110067, India.
Kanchan
Vibhu
V
Panda
Amulya K
AK
D000818:Animals; D003921:Diabetes Mellitus, Experimental; D004337:Drug Carriers / Q000627:therapeutic use; D016503:Drug Delivery Systems; D005260:Female; D006801:Humans; D007003:Hypoglycemia; D007263:Infusions, Parenteral; D007273:Injections, Intramuscular; D007328:Insulin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000627:therapeutic use; D019344:Lactic Acid / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D011091:Polyesters; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013997:Time Factors
D004337:Drug Carriers; D007328:Insulin; D011091:Polyesters; D011108:Polymers; C018503:insulin, depot-; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide)