Abstract:

BACKGROUND: The bioavailability of ordinary eye drops is generally low due to short pre-corneal residence time related to tear turnover and nasolachrymal absorption.
OBJECTIVE: To prepare controlled release microspheres of chitosan-gelatin containing levofloxacin for ophthalmic delivery, and to investigate their physiochemical properties and release profiles in vitro.
METHODS: Chitosan-gelatin microspheres containing levofloxacin were prepared by spray drying method. The surface morphology, particle size distribution and zeta potential, drug-loading rate and encapsulation efficiency, and drug release profiles in vitro of the microspheres were detected by scanning electron microscopy, laser particle size analyzer, high performance liquid chromatography and dynamic dialysis respectively.
RESULTS AND CONCLUSION: The results showed that the prepared microspheres had a regular shape and narrow particle size distribution with the average particle size of (126 7.4±115.3) nm, the drug loading rate of (18.31±0.22)% and the encapsulation efficiency of (91.53±1.12)%. The release profile in vitro was in line with the first order equation of [Ln (1-Q)=  -0.699 1t-0.086 4, r2=0.945 1]. Chitosan-gelatin microspheres containing levofloxacin were successfully prepared by spray drying method with acceptable particle size distribution, suitable release period, and high drug stability.