目的为开发新型药物传递系统，本实验考察了非离子型双子(Gemini)表面活性剂及NaCl对氧氟沙星囊泡理化性质及包封率的影响。方法以Span80、胆固醇和双子表面活性剂为囊材，氧氟沙星为模型药物，用薄膜水化-超声法制备囊泡，考察对囊泡粒径、电位、稳定性等理化性质及包封率、体外释放行为的影响，优化出最佳处方。结果双子表面活性剂能显著提高囊泡包封率和粒径分布的均匀性，囊材最佳配比为Span80-CHOL-Gemini=1∶1∶1。水相中加入NaCl后，囊泡载药量明显增加，电位绝对值显著降低，NaCl最佳用量为10mg·mL-1。体外释放实验表明，双子表面活性剂囊泡具有明显的缓释效果。囊泡中氧氟沙星在7h时平均累积释放率为62。8%。结论双子表面活性剂囊泡对氧氟沙星具有明显的缓释作用，并具有耐盐性，双子表面活性剂有望成为一种新型药物缓释囊材。
Abstract
OBJECTIVE To study the influences of Gemini surfactant and sodium chloride(NaCl) on the physicochemical properties and encapsulation efficiency of ofloxacin niosomes for developing new drug delivery system. METHODS The non-ionic surfactant noisome was prepared by thin film hydration-ultrasonic method, taking non-ionic Gemini surfactant, Span80 and cholesterol as capsule wall materials and ofloxacin as model drug. And the influences of factors such as the amount of surfactant, salt and hydration volume etc on the vesicle size, Zeta potential, encapsulation efficiency, stability and in vitro release behaviors of the ofloxacin niosomes were studied and the optimal prescription was obtained. RESULTS The encapsulation efficiency and the particle size distribution of the niosomes were significantly improved by Gemini surfactant. And the best ratio of the capsule wall materials was as follows∶Span80-CHOL-Gemini=1∶1∶1. The influences of NaCl on the properties of the noisomes were as follows: the amount of drug loading was improved significantly and the absolute value of the Zeta potential decreased obviously with NaCl being added in the aqueous phase. The optimal NaCl concentration was 10 mg·mL-1. The in vitro release test showed that only 62.8% ofloxacin was released from the niosomes in 7 h in artificial gastric juice and artificial intestinal fluid, suggesting a good sustained release trend. CONCLUSION Gemini surfactant niosomes show significant salt tolerance and obviously decrease the release rate of ofloxacin. The non-ionic Gemini surfactant may be used as a capsule wall material for new drug release system.
关键词
囊泡 /
氧氟沙星 /
双子表面活性剂 /
包封率 /
体外释放
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Key words
niosome /
ofloxacin /
gemini surfactant /
encapsulation efficiency /
in vitro release
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中图分类号：
R944
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参考文献
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脚注
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基金
山东省科技攻关项目(2009GG10002076)
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