星点设计-效应面法优化α-细辛脑纳米粒原位凝胶的处方及其体外释放性能考察

Optimization of Formulation of α-Asarone Nanoparticles in situ Gel and Investigation of Its Release Properties

目的:优选温敏型α-细辛脑纳米粒原位凝胶的处方并考察其体外释放行为,为脑靶向性制剂的研究提供参考。方法:以泊洛沙姆407和泊洛沙姆188质量分数为自变量,胶凝温度为因变量,通过多元线性回归及二项式拟合建立因变量与各自变量之间的数学关系,采用星点设计-效应面法优选α-细辛脑纳米粒原位凝胶的处方。以人工模拟鼻液为释放介质考察该制剂的体外释放特性。结果:α-细辛脑纳米粒原位凝胶的最佳处方组成为21.85%泊洛沙姆407和3.8%泊洛沙姆188;胶凝温度(33.7±0.1)℃,72 h内α-细辛脑的累积释放量70.42%。结论:温敏型α-细辛脑纳米粒鼻用原位凝胶具有较好的缓释作用,优选的处方可为α-细辛脑新型给药途径制剂的开发提供参考。

Objective： To optimize formulation of thermo-sensitive in situ nasal gel of α-asarone nanoparticles and investigate its in vitro release behavior. Method： With amounts of poloxamer 407 and poloxamer188 as independent variables,gelation temperature as an dependent variable,multilinear and quadratic models were used to estimate the relationship between dependent variable and independent variables and to select the formulation by central composite design-response surface methodology. Artificial simulated nasal fluid was applied as release medium to study in vitro release characteristics of α-asarone nanoparticles in situ gel. Result： Optimal formulation was as follows： poloxamer 407 of 21. 85% and poloxamer 188 of 3. 8%,gelation temperature was（ 33. 7 ± 0. 1） ℃. Within 72 hours,accumulative release of α-asarone was 70. 42%. Conclusion： α-asarone nanoparticles in situ gel possesses a superior sustained-release effect,the optimum formulation provides a basis for development of new administration routes and dosage forms of α-asarone.