氟尿嘧啶Gemini表面活性剂囊泡的制备及其体外释放研究

The preparation of the Fluorouracil Gemini surfactant noisome and the in vitro release behavior

目的为开发新型载体材料,研究了Gemini表面活性囊泡对水溶性药物氟尿嘧啶的包封作用及其体外释放行为的影响。方法采用薄膜分散法,利用非离子Gemini表面活性剂、Span60及胆固醇为囊材,以水溶性抗癌药物氟尿嘧啶为模型药物,制备非离子Gemini表面活性剂载药囊泡,通过包封率、粒径和电位的测定等优化出最佳的处方。利用智能药物溶出仪研究了Gemini表面活性剂囊泡在模拟胃液及模拟肠液中的释放行为。结果Gemini表面活性剂囊泡的最佳处方为:Gemini 80 nmol、Span60 65 nmol、CHOL 58 nmol、氟尿嘧啶溶液的浓度1 mg/mL、水化体积为20 ml。体外释放行为则表明,Gemini表面活性剂囊泡具有明显的缓释作用。结论 Gemini表面活性剂可作为缓释制剂的优良囊材,有着潜在的应用价值。

Objective： To study the influence of Gemini surfactant noisome on the encapsulation function for the water soluble Fluorouracil and the in vitro release behavior so as to develop new carrier material.Methods： The non-ionic surfactant noisome was prepared by thin film hydration-ultrasonic method,with non-ionic Gemini surfactant,span60 and cholesterol as capsule wall material,water soluble anti-cancer drug Fluorouracil as model drug.And the optimal prescription was obtained by measuring the zeta potential,size,size distribution and encapsulation efficiency.And the release behavior of the Fluorouracil encapsulated in the Gemini surfactant noisome in simulated gastric and intestinal was studied by using the dissolution test system.Results： The encapsulation efficiency and the particle size distribution of the noisome were significantly improved by gemini surfactant.And the optimal prescription was as follows： Gemini 80 nmol,Span60 65 nmol,CHOL58 nmol,concentration of Fluorouracil 1 mg/ml and Hydration volume 20 ml.The in vitro release study indicated that the loaded Gemini surfactant noisome showed a good sustained release trend.Conclusion： Gemini surfactant can be used as a good kind of wall material for sustained release preparation,which shows a good application prospect for the Gemini surfactant.