【摘要】 目的研究非离子表面活性剂囊泡对抗肿瘤药物5-氟尿嘧啶(5-Fu)的包封率及其释放行为的影响,为新型药物传输系统的研究提供一定的依据。方法以司盘40和胆固醇为主要原料,通过薄膜分散法制备了非离子表面活性剂囊泡,研究了该类囊泡对5-氟尿嘧啶的包封作用,包封率的影响因素以及被包封的5-氟尿嘧啶在模拟胃液及模拟肠液中的释放情况,并通过正交实验优化影响因素。结果 0.10 mol/L司盘40∶胆固醇=1∶1时形成的非离子表面活性剂囊泡对1.20 mg/mL的5-氟尿嘧啶的包封率是40%~55%;药物释放实验显示,在6 h,在模拟胃液和模拟肠液中游离的5-氟尿嘧啶释放率为95%,包封于囊泡中的5-氟尿嘧啶的释放率为25%。结论非离子表面活性剂囊泡对5-氟尿嘧啶具有较高的包封率及明显缓释作用。更多还原

【Abstract】 【Objective】 To investigate the entrapment efficiency and the release rate of 5-fluorouracil encapsulated into noiosomes,and provide the guidance for the study of the new drug delivery system.【Methods】 Niosomes were prepared with nonion surfactant span40 and cholesterol by ultrasonication.And the entrapment efficiency of 5-fluorouracil encapsulated into noiosomes and release profiles in simulated gastric and intestinal fluid were studied,and optimized 5-fluorouracil affecting factors through orthogonal test.【Results】 The results showed that the entrapment efficiency of 5-fluorouracil by noiosomes reached 40%～55% under the condition that the molar ratio of the span 40: Cholesterol equaled to 1 : 1 and the concentration of 5-fluorouracil was 1.20 mg/mL.The results also indicated that in simulated gastric and intestinal fluid,the release rate of 5-fluorouracil entrapped in niosomes was 25% after 6 h,however the release rate of free 5-fluorouracil was 95% under the same condition.【Conclusion】 The entrapment efficiency of 5-fluorouracil entrapped by niosomes was high enough and the release rate of the entrapped drug was slow obviously.更多还原