Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Marmara University, Haydarpasa, Istanbul, Turkey.
Pharm Dev Technol. 2012 Jan-Feb;17(1):118-24. doi: 10.3109/10837450.2010.529145. Epub 2010 Oct 26.
Ofloxacin (OFL), second-generation fluoroquinolone, is a broad-spectrum antibiotic which is active against both Gram-positive and Gram-negative bacteria. However, OFL has a short biological half life (8-9 h) and poor stability in serum and needs frequently repeated doses during the treatment. The objective of this study was to fabricate the fucospheres and chitosan microspheres containing a poorly soluble drug, OFL, and to compare the formulation parameters influencing the in vitro properties of microparticles such as size, zeta potential, encapsulation efficiency and drug release characteristics. Particle size of fucospheres and chitosan microspheres has been found to be 0.61-1.48 µm and 1.05-2.08 µm, respectively. The zeta potentials have changed between 5.6 mV and 28.0 mV for fucospheres; 22.3 mV and 42.4 mV for chitosan microspheres. The fucospheres have had higher drug encapsulation efficiency than those of chitosan microspheres. The particle size, surface charge, encapsulation efficiency and in vitro drug release from both fucospheres and chitosan microspheres have been affected by type and concentration of the polymers used. The release mechanism from most of the microsphere formulations has been fitted to Higuchi kinetic model. It can be concluded that OFL-encapsulated fucospheres can be a potential delivery system for antibiotics.
氧氟沙星（OFL）是第二代氟喹诺酮类药物，属于广谱抗生素，对革兰氏阳性菌和革兰氏阴性菌均有活性。然而，OFL 的生物半衰期（8-9 小时）较短，在血清中的稳定性差，在治疗过程中需要频繁重复给药。本研究的目的是制备载有疏水性药物氧氟沙星的藻酸盐微囊和壳聚糖微球，并比较影响微球体外性质的制剂参数，如粒径、Zeta 电位、包封率和药物释放特性。藻酸盐微囊和壳聚糖微球的粒径分别为 0.61-1.48μm 和 1.05-2.08μm。藻酸盐微囊的 Zeta 电位在 5.6mV 到 28.0mV 之间变化；壳聚糖微球的 Zeta 电位在 22.3mV 到 42.4mV 之间变化。藻酸盐微囊的载药包封率高于壳聚糖微球。藻酸盐微囊和壳聚糖微球的粒径、表面电荷、载药包封率和体外药物释放均受到所用聚合物的类型和浓度的影响。大多数微球制剂的释放机制均符合 Higuchi 动力学模型。可以得出结论，氧氟沙星包封的藻酸盐微囊可以作为抗生素的潜在给药系统。
