Gemini表面活性剂对类脂囊泡理化性质及pH敏感性的影响

Effects of gemini surfactant on the physical-chemical properties and pH sensitivity of niosome

目的为开发新型药物传递系统,本文考察了非离子型Gemini表面活性剂对pH敏感类脂囊泡理化性质及pH敏感度的影响。方法以Tween 20、胆固醇、胆固醇半琥珀酸酯(CHEMS)为囊材,用薄膜水化-超声法制备pH敏感类脂囊泡,通过粒度、电位、包封率、囊泡于不同pH下的释放速率以及在牛血清中培育后囊泡荧光强度的变化等探讨CHEMS、Gemini对囊泡理化性质及pH敏感性的影响。结果含有Gemini表面活性剂的pH敏感类脂囊泡,体系分布均匀,包封率高,在酸性环境中可快速释药,且Gemini表面活性剂对pH敏感类脂囊泡的pH敏感性没有明显影响,在牛血清中pH敏感Gemini类脂囊泡仍然可保持其较好的pH敏感性。结论 pH敏感双子表面活性剂囊泡,可用于向某些病理组织靶向输送药物,有望开发为一种理想的新型药物传递系统。

Objective In order to explore the new DDS, the effects of gemini surfactant on the physical-chemical properties and pH sensitivity of pH sensitive niosome were investigated. Methods The pH sensitive noisome was prepared by thin film hydration-ultrasonic method, taking Gemini surfactant, Tween 20, cholesterol and CHEMS as wall material. And the influence of CHEMS and Gemini surfactant on the physical-chemical properties of the noisome were studied by using DLS to measure the variation of vesicle size, PDI, zeta potential and encapsulation efficiency with the increasing concentration of the above two substances. The release rate in different pH buffer solution of the noisome and the fluorescent intensity of the niosome in different buffer solution was also determined after being incubated in the bovine serum for 2h to investigate the pH sensitivity of the noisome.Results The obtained pH sensitive Gemini noisome was almost a monodisperse vesicular system with high encapsulation efficiency high pH sensitivity and the quick release of the enveloped drug in acid environment, moreover the pH sensitive Gemini noisome can hold it＇s pH sensitivity in the buffer solution containing the bovine serum. Conclusion The prepared pH sensitive noisome can be used to transport of drugs to the target site,and might be explored to an ideal drug delivery system.