环索奈德纳米粒制备及其性质

Preparation and property of ciclesonide nanoparticles

目的:制备环索奈德固体脂质纳米粒胶体溶液,对其理化性质进行考察。方法:经方法考察,确定采用乳化-溶剂挥发法制备环索奈德纳米粒胶体溶液。在载体材料种类及用量、表面活性剂种类及用量、水相用量等单因素考察基础上,对处方组成进行了响应面优化,确定了最佳处方组成和制备工艺。用高速冷冻离心法和紫外分光光度法测定了包封率、载药量,激光粒径仪测定了粒径、Zeta电位,扫描电镜观察了纳米粒形态,并考察了药物纳米粒胶体溶液的体外稳定性。结果:乳化-溶剂挥发法适合制备环索奈德纳米粒胶体溶液,载体材料组成、药物与载体材料质量比、表面活性剂用量对其粒径影响较大。最佳处方制备的纳米粒呈圆整球状,平均粒径为(96.6±18.4)nm,Zeta电位为(-12.7±2.2)mV,包封率为(94.3±1.4)%,载药量为(10.72±0.23)%,纳米粒溶液在室温条件下不够稳定。结论:研究中处方及制备工艺适合制备环索奈德纳米粒胶体溶液,相关理化性质检测方法可行。

OBJECTIVE To prepare the colloid solution of solid lipid nanoparticles containing ciclesonide, and examine its physicochemical property. METHODS To optimize the technique of preparation, the colloid solution of solid lipid nanoparti cles containing ciclesonide was prepared by the emulsiomsolvent evaporation method. The optimum formulation and the preparation process were obtained by the response surface methodology, based on the single factor analysis including the kind and quantity of the carrier material and the surface active agent, the quantity of the aqueous phase etc.. The entrapment efficiency and drug loading was measured by the high-speed refrigerated centrifuge and UV spectrophotometry; the particle size and Zeta potential was measured by the laser particle sizer; the surface of nanoparticles was observed by the scanning electronic microscope; and its stability in vitro was inspected. RESULTS The emulsion-solvent evaporation method was suitable for preparing the colloid solution of solid lipid nanoparticles containing ciclesonide. The following factors such as the component of carrier material, the mass ratio of the drug and the carrier material, and the quantity of the surface active agent greatly influenced on the particle size. The particulate prepared was regular ellipse, symmetrical. The mean particle size was （96. 6 ± 18.4） nm, the Zeta potential was （ - 12. 7 ± 2. 2） mV, the entrapment efficiency was （94. 3 ± 1.4） %, the drug loading was （ 10. 72 ±0. 23） %, but the aqueous solution of solid lipid nanoparticles was not enough stable at the room temperature. CONCLUSION The formulation and preparation process in study were suitable for preparing the colloid solution of solid lipid nanoparticles containing ciclesonide. The relevant test method is feasible for its physicochemical property.