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
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Administration, Topical
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Animals
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Anterior Chamber / drug effects
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Anterior Chamber / metabolism
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Anti-Inflammatory Agents / administration & dosage*
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Anti-Inflammatory Agents / analysis
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Anti-Inflammatory Agents / pharmacokinetics
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Biological Availability
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Dexamethasone / administration & dosage
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Dexamethasone / analogs & derivatives*
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Dexamethasone / analysis
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Dexamethasone / pharmacokinetics
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Drug Delivery Systems
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Excipients* / chemical synthesis
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Excipients* / chemistry
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Excipients* / pharmacology
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Eye Diseases / drug therapy
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Hydrogels
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Ophthalmic Solutions / administration & dosage*
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Ophthalmic Solutions / analysis
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Ophthalmic Solutions / pharmacokinetics
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Phase Transition
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Polyethylene Glycols* / chemical synthesis
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Polyethylene Glycols* / chemistry
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Polyethylene Glycols* / pharmacology
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Polyglactin 910* / chemical synthesis
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Polyglactin 910* / chemistry
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Polyglactin 910* / pharmacology
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Rabbits
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Temperature
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Viscosity
Substances
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Anti-Inflammatory Agents
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Excipients
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Hydrogels
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Ophthalmic Solutions
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poly(lactic-co-glycolic acid)-polyethylene glycol-poly(lactic-co-glycolic acid)
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Polyglactin 910
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Polyethylene Glycols
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Dexamethasone
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dexamethasone acetate