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Int J Pharm ; 370(1-2): 75-80, 2009 Mar 31.
Article in English | MEDLINE | ID: mdl-19101617

ABSTRACT

The purpose of this report was to develop solvent-free biodegradable scleral plugs for vancomycin, amikacin and dexamethasone delivery for endophthalmitis treatment. To fabricate a biodegradable plug, polylactide-polyglycolide copolymers were pre-mixed with the drugs. The mixture was then compression molded and sintered to form a scleral plug of 1.4mm in diameter. An elution method was utilized to characterize the in vitro release characteristics of the antibiotics and the steroids over a 14-day period. The HPLC analysis and bacterial inhibition test showed that biodegradable scleral plugs released a high concentration resulting in significant activity of vancomycin and amikacin (well above the minimum inhibition concentrations) and dexamethasone in vitro, for the period of time needed to treat intraocular infection. A bacterial inhibition test was carried out to determine the relative activity of the released antibiotics. The activities of the eluted vancomycin and amikacin ranged from 69% to 89% and from 66% to 88%, respectively. In addition, the experimental result suggests that one will be able to reduce the drug release rate and prolong the total release period of the plugs by adopting a lower antibiotic/steroid to polymer ratio, increasing the sintering temperature, or increasing the compression pressures.


Subject(s)
Amikacin/chemistry , Anti-Bacterial Agents/chemistry , Dexamethasone/chemistry , Glucocorticoids/chemistry , Vancomycin/chemistry , Amikacin/administration & dosage , Amikacin/pharmacology , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/pharmacology , Chromatography, High Pressure Liquid , Delayed-Action Preparations , Dexamethasone/administration & dosage , Dexamethasone/pharmacology , Drug Delivery Systems/methods , Drug Stability , Drug Therapy, Combination , Endophthalmitis/drug therapy , Escherichia coli/drug effects , Glucocorticoids/administration & dosage , Glucocorticoids/pharmacology , Lactic Acid/chemistry , Microbial Sensitivity Tests , Polyglycolic Acid/chemistry , Polylactic Acid-Polyglycolic Acid Copolymer , Polymers/administration & dosage , Polymers/chemistry , Sclera , Staphylococcus aureus/drug effects , Vancomycin/administration & dosage , Vancomycin/pharmacology
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