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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 the formulation of in situ gels of thermo-sensitive α-asarone nanoparticles and to investigate their in vitro release behavior, providing a reference for the study of brain-targeting agents. Methods: Poloxamer 407 and poloxamer 188 were used as independent variables and gelation temperature was used as the dependent variable. Multivariate linear regression and binomial fitting were used to establish the mathematical relationship between the dependent variables and their respective variables. Point Design - Response Surface Methodology to Optimize Formulation of α - asarone Nano - particles in. The release characteristics of the preparation in vitro were investigated by artificial simulated nasal fluid. Results: The optimum formulation of α-asaronein nanoparticles in in situ gels was polluted at 21.85% poloxamer 407 and poloxamer 188 at a gelation temperature of 33.7 ± 0.1 ℃, Asarone cumulative release of 70.42% brain. CONCLUSION: The thermo-sensitive α-Asarone nanoparticle nasal in situ gel has better sustained-release effect. The preferred prescription may provide a reference for the development of new formulations of α-Asarone.