载异烟肼聚己内酯微球的制备及其性质研究

Preparation and characterization of isoniazid-loaded poly(ε-caprolactone) microspheres

采用O/O溶剂挥发法制备载异烟肼聚己内酯微球。系统考察了活性剂浓度、内外油相体积、投药量对微球粒径、载药量和包封率的影响。结合内外油相初始粘度分析载药微球成球性,用IR、XRD、SEM对微球化学结构、结晶状态和表面形貌进行表征。通过优化得到平均粒径为28.73μm、载药量为2.36%、包封率为49.58%、外观圆整、表面多孔的载药微球。与O/W溶剂挥发法制备微球对比表明,O/O法有效地提高了载异烟肼聚己内酯微球载药量与包封率,是包覆亲水性小分子药物的可行方法,该载药微球可望用于骨和关节结核病的缓释治疗。

Microspheres of isoniazid（INH）-loaded poly（ε-caprolactone）（PCL） were fabricated by oil-in-oil（O/O） solvent evaporation method.In order to prepared PCL microspheres with high efficiency of drug content,technological parameters such as the concentration of surfactant in continuous phase,the volume ratio and initial viscosity of dispersed phase and continuous phase,the mass of INH added into solvent were investigated systematically.The chemical structure,crystallinity and morphology were characterized by IR,XRD and SEM.The microspheres prepared by optimized conditions display an average particle size of 28.73μm with 2.36wt% drug loading amount and 49.58% entrapment efficiency,presenting spherical shape and porous surface.Meanwhile the INH-loaded PCL microspheres were also prepared by oil-in-water（O/W） solvent evaporation method as the contrast.The results show that O/O solvent evaporation method has better drug loading and entrapment efficiency than O/W method.It is a feasible approach to encapsulate micromolecular and hydrophilic drugs for the releasing therapy of tuberculosis of bones and joints in the future.