Abstract:

BACKGROUND: Release microspheres of 5-fluorouracil-poly lactic-co-glycolic acid (5-Fu-PLGA) have a potential value in inhibition of scar formation of filtering bleb after glaucoma filtering surgery. However, the preparation of the microspheres is complicated, the drug loading is low, and the phenomenon of sudden release often exists.
OBJECTIVE: To compare the shape characteristics, drug loadings and releasing characteristics in vitro of 5-Fu-PLGA microspheres prepared with the emulsion solvent evaporation method and 5-Fu-PLGA slow-release membranes prepared with the spray technique in order to investigate preparation methods of 5-Fu controlled release formulations with more obvious sustained release activity in vitro.
METHODS: The 5-Fu-PLGA microspheres were prepared with the emulsion solvent evaporation method on the carrier of poly lactic-co-glycolic acid; the 5-Fu-PLGA slow-release membranes were prepared with spray technique on the carrier.
RESULTS AND CONCLUSION: The prepared microspheres had the regular morphology. The average particle size was        (4 447.4±359.8) nm, while the encapsulation efficiency and the drug loading were (86.68±1.92)% and (8.668±0.37)% respectively. The obtained membranes were with smooth surface. The diameter, thickness, drug loading and encapsulation efficiency of the membranes were 6.0 mm, (0.24±0.005) mm, (23.76±0.37)% and (95.04±1.36)% respectively. The drug performance of 5-Fu had not been influenced during preparation. The microspheres had the obvious sudden release in vitro. The slow-release membranes had sustained release activity in vitro, and its release curve was accordance with the Higuchi equation. It is indicated that the preparation is simple, the drug loading is high, the phenomenon of sudden release can be decreased, and the release time is longer of the slow-release membranes.