PLGA-PEG-PLGA hydrogel for ocular drug delivery of dexamethasone acetate

Drug Dev Ind Pharm. 2010 Oct;36(10):1131-8. doi: 10.3109/03639041003680826.

Abstract

Aim: This study aims to investigate the suitability of thermosensitive triblock polymer poly-(DL-lactic acid-co-glycolic acid) (PLGA)-polyethylene glycol (PEG)-PLGA as a matrix material for ocular delivery of dexamethasone acetate (DXA).

Methods: The copolymer was synthesized and evaluated for its thermosensitive and gelation properties. DXA in situ gel-forming solution based on PLGA-PEG-PLGA copolymer of 20% (w/w) was prepared and evaluated for ocular pharmacokinetics in rabbit according to the microdialysis method, which was compared to the normal eye drop.

Result: The copolymer with 20% (w/w) had a low critical solution temperature of 32 degrees C, which is close to the surface temperature of the eye. The C(max) of DXA in the anterior chamber for the PLGA-PEG-PLGA solution was 125.2 microg/mL, which is sevenfold higher than that of the eye drop, along with greater area under the concentration-time curves (AUC).

Conclusion: These results suggest that the PLGA-PEG-PLGA copolymer is potential thermosensitive in situ gel-forming material for ocular drug delivery, and it may improve the bioavailability, efficacy of some eye drugs.

MeSH terms

  • Administration, Topical
  • Animals
  • Anterior Chamber / drug effects
  • Anterior Chamber / metabolism
  • Anti-Inflammatory Agents / administration & dosage*
  • Anti-Inflammatory Agents / analysis
  • Anti-Inflammatory Agents / pharmacokinetics
  • Biological Availability
  • Dexamethasone / administration & dosage
  • Dexamethasone / analogs & derivatives*
  • Dexamethasone / analysis
  • Dexamethasone / pharmacokinetics
  • Drug Delivery Systems
  • Excipients* / chemical synthesis
  • Excipients* / chemistry
  • Excipients* / pharmacology
  • Eye Diseases / drug therapy
  • Hydrogels
  • Ophthalmic Solutions / administration & dosage*
  • Ophthalmic Solutions / analysis
  • Ophthalmic Solutions / pharmacokinetics
  • Phase Transition
  • Polyethylene Glycols* / chemical synthesis
  • Polyethylene Glycols* / chemistry
  • Polyethylene Glycols* / pharmacology
  • Polyglactin 910* / chemical synthesis
  • Polyglactin 910* / chemistry
  • Polyglactin 910* / pharmacology
  • Rabbits
  • Temperature
  • Viscosity

Substances

  • Anti-Inflammatory Agents
  • Excipients
  • Hydrogels
  • Ophthalmic Solutions
  • poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid)
  • Polyglactin 910
  • Polyethylene Glycols
  • Dexamethasone
  • dexamethasone acetate