Effect of PLGA hydrophilia on the drug release and the hypoglucemic activity of different insulin-loaded PLGA microspheres

The effects of viscosity and hydrophilic characteristics of different PLGA polymers on the microencapsulation of insulin have been studied in vitro and in vivo after subcutaneous administration to hyperglycemic rats. Hydrophilic PLGA polymers produced a higher burst effect than the hydrophobic ones....

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Bibliographic Details
Published in:Journal of microencapsulation 2011-12, Vol.28 (8), p.791-798
Main Authors: Presmanes, C., de Miguel, L., Espada, R., Álvarez, C., Morales, E., Torrado, J.J.
Format: Article
Language:English
Subjects:
Animals
bioavailability
biodegradable polymers
Biological and medical sciences
calorimetry
Delayed-Action Preparations - chemistry
Drug Carriers - chemistry
Drug Compounding
drug release
General pharmacology
Hydrophobic and Hydrophilic Interactions
Hyperglycemia - drug therapy
Hypoglycemic Agents - administration & dosage
Hypoglycemic Agents - pharmacokinetics
Hypoglycemic Agents - therapeutic use
Insulin - administration & dosage
Insulin - pharmacokinetics
Insulin - therapeutic use
Lactic Acid - chemistry
Male
Medical sciences
Microspheres
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyglycolic Acid - chemistry
protein delivery
Rats
Rats, Wistar
Viscosity
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Summary:The effects of viscosity and hydrophilic characteristics of different PLGA polymers on the microencapsulation of insulin have been studied in vitro and in vivo after subcutaneous administration to hyperglycemic rats. Hydrophilic PLGA polymers produced a higher burst effect than the hydrophobic ones. Moreover, an incomplete insulin release was observed with the hydrophilic PLGA polymers in comparison with the hydrophobic ones. An explanation for that incomplete release can be the development of polymer-insulin interactions associated to the polymer hydrophilic/hydrophobic character, as detected by DSC analysis. Differences in the release rate of microsphere formulations lead to differences in the hypoglycemic action and the weight of animals. Hydrophobic PLGA was able to prolong the hypoglycemic action up to 4 weeks which is at least double than that obtained with hydrophilic PLGA of a similar viscosity. Comparing insulin microspheres with an immediate release formulation, microspheres can increase insulin relative bioavailability up to four times.
ISSN:0265-2048
1464-5246
DOI:10.3109/02652048.2011.621554