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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 ciclesonide solid lipid nanoparticle colloidal solution and investigate its physico-chemical properties. Methods: The method was investigated to determine the emulsion - solvent evaporation method for the preparation of ciclesonide nanoparticle colloidal solution. On the basis of the single factor such as the type and amount of carrier material, the type and amount of surfactant, the amount of water phase and so on, the response surface of the prescription was optimized to determine the optimal prescription composition and preparation process. The encapsulation efficiency and drug loading were measured by high-speed freeze centrifugation and ultraviolet spectrophotometry. The particle size and Zeta potential were measured by laser particle size analyzer. The morphology of the nanoparticles was observed by scanning electron microscopy. The drug nanoparticle colloidal solution was investigated in vitro stability. Results: Emulsification - solvent evaporation method was suitable for the preparation of ciclesonide nanoparticle colloidal solution. The composition of carrier materials, the mass ratio of drug to carrier material, and the amount of surfactant greatly influenced the particle size. The nanoparticles prepared by the best prescription were round and spherical, the average 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)%, 10.72 ± 0.23)%, the nanoparticle solution is not stable enough at room temperature. Conclusion: The formulation and preparation process of this study is suitable for the preparation of ciclesonide nanoparticle colloid solution. The relevant physical and chemical properties detection methods are feasible.