生物相容性表面活性剂Tween 80的性能,用于形成适合新药加工的微乳

C. Prieto, L. Calvo
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引用次数: 78

摘要

本研究的目的是研究基于非离子、无毒和生物相容性表面活性剂Tween 80的正己烷/水乳液的相行为和结构。该系统是基于超临界流体形成纳米和封装颗粒的新制药技术的兴趣。然而,它表现出缺乏稳定性,表现为大面积的大乳液。为此,探讨了添加剂(醇类和卤水)和外部变量(温度)对其的影响。由于Tween 80的非离子特性,用卤水替代水的影响可以忽略不计。相反,醇(乙醇或1-丁醇)的存在增强了表面活性剂在油相中的溶解度,降低了混合物的粘度,从而提高了表面活性。将温度升高至云点(60°C)也得到了类似的结果。通过这些修饰,可以获得表面活性剂浓度相对较低(约30%)且组合物间隔较宽的微乳液,从而扩大了它们在药物制造(如受控药物输送、酶促反应或赋形剂加工)中的可能用途。对表面活性剂性能的了解可以进一步用于用更环保的溶剂(如超临界CO2)代替正己烷。
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Performance of the Biocompatible Surfactant Tween 80, for the Formation of Microemulsions Suitable for New Pharmaceutical Processing
The aim of this work was to investigate the phase behaviour and the structure of the n-hexane/water emulsions based on a nonionic, nontoxic and biocompatible surfactant, Tween 80. This system is of interest for new pharmaceutical techniques based on supercritical fluids to form nano- and encapsulated particles. However, it showed a lack of stability denoted by large areas of macroemulsion. For this reason, the effect of additives (alcohols and brine) and external variables (temperature) were explored. The replacement of water by brine caused negligible impact due to the nonionic character of Tween 80. On the contrary, the presence of an alcohol (ethanol or 1-butanol) enhanced the solubility of the surfactant in the oil phase and decreased the mixture viscosity, resulting in improved surface activity. Similar results were obtained by raising the temperature until the cloud point was reached (60°C). With these modifications, microemulsions at relatively low concentrations of surfactant (around 30%) and within a broad interval of compositions could be obtained, widening their possible use in pharmaceuticals manufacturing (such as controlled drug delivery, enzymatic reactions, or excipient processing). The understanding of the surfactant performance could be further used to substitute the n-hexane by a greener solvent, such as supercritical CO2.
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