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Subconjunctival sustained release 5-fluorouracil for glaucoma filtration surgery
Li-jun Cui1, Nai-xue Sun, Xing-hua Li
1Department of Ophthalmology and Pharmacology, Xi-an Jiaotong University, Xi-an 710004, China.
Acta Pharmacologica Sinica
|August 23, 2008
Summary
A novel 5-fluorouracil-loaded poly (lactic acid) disc (5-FU-PLA-DS) demonstrated sustained drug release, effectively reducing intraocular pressure and prolonging filtration bleb survival in glaucoma surgery. This sustained delivery minimized 5-FU toxicity in rabbit eyes.
Area of Science:
- Ophthalmology
- Biomaterials Science
- Drug Delivery Systems
Background:
- Glaucoma filtration surgery success is often limited by scar tissue formation and drug toxicity.
- Sustained delivery of anti-metabolites like 5-fluorouracil (5-FU) can improve surgical outcomes but requires careful control to avoid toxicity.
Purpose of the Study:
- To characterize the release profile of a 5-fluorouracil-loaded poly (lactic acid) disc (5-FU-PLA-DS).
- To evaluate the efficacy and safety of sustained 5-FU delivery using 5-FU-PLA-DS in rabbit glaucoma filtration surgery.
Main Methods:
- 5-FU-PLA-DS were prepared using a microsphere accumulation method.
- In vitro release, drug loading, and entrapment efficiency were assessed.
- The discs were implanted in rabbit eyes undergoing trabeculectomy, with evaluations of intraocular pressure, inflammation, bleb morphology, and 5-FU levels in aqueous humor.
Main Results:
- The 5-FU-PLA-DS exhibited sustained release of 5-FU for 91 days at suppressive concentrations.
- Significantly greater intraocular pressure reduction and prolonged bleb/fistula persistence were observed in the 5-FU-PLA-DS group compared to controls.
- Reduced corneal toxicity and hyperemia were noted with the 5-FU-PLA-DS compared to intraoperative 5-FU application, with no toxic reactions in conjunctival biopsies.
Conclusions:
- The 5-FU-PLA-DS provides sustained intraocular release of 5-FU.
- This sustained delivery effectively reduces intraocular pressure and prolongs filtration bleb survival.
- The 5-FU-PLA-DS significantly mitigates the toxicity associated with 5-FU in glaucoma surgery.
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