| Objective:Choosing antibiotic drug-Clindamycin (DA) as model drug, PLGA as thecarrier to prepare DA-PLGA biodegradable sustained-release formulations. And thento determinate the morphology，particle size，preparation condition，in vitro release,and antibacterial properties in vitro. In order to extend the partial antimicrobialduration through the preparation of DA-PLGA microspheres.Methods:(1) PLGA was used as carrier to prepare DA-PLGA microspheres by the doubleemulsion solvent evaporation method.(2) The entrapment efficiency and particle size evaluated and studied for theoptimization of condition, including stirring speed, PVA concentration，PLGAsolution concentration in water phase, and rate of charge.(3) The morphology and entrapment efficiency of microspheres was studied byultraviolet-visible spectrometer and scanning electron microscope (SEM).(4) The antibacterial properties of DA-PLGA were measured by K-B method invitro.Results:DA-PLGA microspheres were obtained for drug loading4.59±0.5%,entrapment efficiency86.3±1.5%, under the optimal conditions. The results ofmicroscope observation were the uniform size, surface smooth and particleroundness, at the mean diameter of700nm mostly. The results showed that the initialrelease was18.37%, the cumulative drug release ratio was77.92%within28d, withsignificant sustained-release effect, in vitro release of microspheres; the antibacterialactivity test in vitro revealed a significant inhibiting effect. Conclusion:In this paper, DA-PLGA microspheres were prepared by the double emulsionsolvent evaporation method. With good morphology, high encapsulation efficiency,and sustained effect of in vitro release by the optimal conditions. As the result, amicrosphere preparation method with stable quality was acquired which can get anideal sustained-release delivery system of clindamycin. |
