Preparation, Characterization and in Vitro Release of Ciprofloxacin Polylactic Acid Microspheres

Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were preparedusing solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonalexperiment was used to optimize the method of CFX-PLA-MS preparation. Microspheres werecharacterized in terms of morphology, size, encapsulation efficiency, drug loading and in vitro drugrelease. Results The physical state of CFX-PLA-MS was determined by scanning electron microscopy(SEM) and differential scanning calorimetry (DSC) . Microspheres formed were spherical with smoothsurfaces. Drug was enveloped in microspheres without mixing physically with PLA. The averageparticle size was 280.80 ± 0.15 μm, with over 90% of microspheres falling in the range of 250 -390 μm. The encapsulation efficiency was 65.8% ± 0.58% and the drug loading was 34.1% ± 0.51% .In vitro release study revealed a profile of sustained release of Ciprofloxacin from CFX-PLA-MS. Theaccumulated release percentage and half-life (T_(1/2) of Ciprofloxacin microspheres were 84.0% in53.2 h, and 31.9 h, respectively. Higuchi equation was Q= -0.0043 + 0.003 9 t^(1/2), r = 0.9941.Conclusion Ciprofloxacin microspheres have been successfully prepared and sustained release of CFXfrom microspheres is achieved.

环丙沙星聚乳酸微球制备工艺的研究

目的 :通过正交设计试验筛选出制备环丙沙星聚乳酸微球的最佳工艺。方法 :用正交试验设计优化环丙沙星聚乳酸微球制备工艺 ,用电子显微镜观察微球表面形态 ,差示扫描热分析确证含药微球的形成 ,及对微球的平均粒径、粒度分布、载药量、包封率、工艺重现性进行了研究。结果 :环丙沙星聚乳酸微球的形态圆整 ,且药物确已被包裹在微球中 ,微球的平均粒径为 2 80 .80± 0 .15 μm ,粒径在 2 5 0～ 390 μm左右的占总数的 90 %以上 ,载药量为 (34.1± 0 .5 1) % ,包封率为 (6 8.5± 0 .5 8) % ,最佳工艺条件重现性良好。结论 :本研究获得了制备环丙沙星聚乳酸微球的较满意的工艺。