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Phase Behavior of Non-Ionic Surfactant-Medium Chain Triglyceride-Water Microemulsion Systems
Journal of Surfactants and Detergents ( IF 1.6 ) Pub Date : 2021-05-07 , DOI: 10.1002/jsde.12510
Shannon P. Callender 1 , Shawn D. Wettig 1, 2
Affiliation  

Microemulsion systems have garnered tremendous interest in the pharmaceutical sector for a variety of drug delivery applications. Non-ionic surfactants are often the preferred surfactant class given their uncharged nature, enhanced oral safety profile, and generally regarded as safe status as compared to other surfactant classes (Myers, Surfactant science and technology, 2005, p. 29), (Malmsten, Handbook of microemulsion science and technology, 1999, p. 755), (Grove & Mullertz, Chapter 5-liquid self-microemulsifying drug delivery systems, 2007), (Liu et al., Water-insoluble drug formulation, 2008), (Hauss, Advanced Drug Delivery Reviews, 2007, 59, pp. 667–676), (Balazs, Solubility, delivery and ADME problems of drugs and drug-candidates, 2011, p. 68). In this work, the phase behavior and microemulsion formation potential of four commonly used non-ionic surfactants, PEG-40 hydrogenated castor oil, Poloxamer 188, Polysorbate 80, and d-α-tocopherol polyethylene glycol succinate were studied via ternary phase diagram (TPD) mapping using a medium chain triglyceride, Miglyol 812. Results indicated notable differences in phase behavior despite similarities in hydrophilic–lipophilic balance value (13–15). All surfactants produced Winsor Type I, oil-in-water microemulsions at water concentrations above 40% wt/wt. Winsor Type II water-in-oil microemulsions were difficult to obtain even at high oil concentrations of ≥70% wt/wt. Winsor III microemulsions, though rare, were generally obtained in the middle regions of the TPD between 10% and 30% wt/wt water while Winsor IV microemulsions dominated at high surfactant concentrations of ≥45% wt/wt. Opaque emulsion areas were particularly notable in wax state surfactants. Polysorbate 80 and PEG-40 hydrogenated castor oil demonstrated a high degree of synergism as well as the largest oil-in-water (o/w) and water-in-oil (w/o) microemulsion formation potential rendering them suitable for a number of enteral and parenteral applications.

中文翻译:

非离子表面活性剂-中链甘油三酯-水微乳液体系的相行为

微乳液系统在制药领域的各种药物输送应用中引起了极大的兴趣。非离子表面活性剂通常是首选的表面活性剂类别,因为它们不带电荷,口服安全性更高,并且与其他表面活性剂类别相比通常被认为是安全的(Myers,Surfactant science and technology,2005,第 29 页),(Malmsten Handbook of microemulsion science and technology, 1999, p. 755), (Grove & Mullertz, Chapter 5-liquid self-microemulsifying drug delivery systems, 2007), (Liu et al., 水不溶性药物制剂, 2008), (Hauss ,Advanced Drug Delivery Reviews, 2007, 59, pp. 667–676),(Balazs,药物和候选药物的溶解度、递送和 ADME 问题,2011 年,第 68 页)。在这项工作中,d -α-生育酚聚乙二醇琥珀酸酯的研究是通过使用中链甘油三酯 Miglyol 812 的三元相图 (TPD) 映射。结果表明尽管亲水-亲油平衡值相似,但相行为存在显着差异 (13-15)。所有表面活性剂均以高于 40% wt/wt 的水浓度产生 Winsor I 型水包油微乳液。即使在 ≥ 70% wt/wt 的高油浓度下也难以获得 Winsor II 型油包水微乳液。Winsor III 微乳液虽然很少见,但通常在 10% 至 30% wt/wt 水的 TPD 中间区域获得,而 Winsor IV 微乳液在 ≥ 45% wt/wt 的高表面活性剂浓度下占主导地位。不透明乳液区域在蜡态表面活性剂中尤为显着。
更新日期:2021-07-14
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