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Zeta potential changing nanoemulsions based on phosphate moiety cleavage of a PEGylated surfactant
Journal of Molecular Liquids ( IF 5.3 ) Pub Date : 2020-07-20 , DOI: 10.1016/j.molliq.2020.113868
Markus Kurpiers , Julian Dominik Wolf , Christian Steinbring , Sergey Zaichik , Andreas Bernkop-Schnürch

The aim of this study was to develop and evaluate a zeta potential changing nanoemulsion (NE) containing polyoxyethylene (9) nonylphenol monophosphate ester (PNPP) as emulsifier.

2% (v/v) of PNPP and 0.18% (5 μM) of cetyltrimethylammonium bromide (CTAB) were incorporated into the lipophilic NE preconcentrate (PEG-40 castor oil, glyceryl tricaprylate/tricaprate, propylene glycol dicaprylocaprate, propylene glycol monolaurate, highly purified diethylene glycol monoethyl ether; 20/20/10/30/20, v/v). After diluting the lipophilic preconcentrate, resulting NE was analyzed regarding droplet size, polydispersity index (PDI), storage stability and zeta potential change after incubation with intestinal alkaline phosphatase (IAP). Phosphate release due to cleavage by IAP was quantified by malachite green assay and toxicity as well as cellular uptake behavior on Caco-2 cells was determined. The NE containing PNPP and CTAB displayed a droplet size of 113 nm and a PDI of 0.20. It was stable over 4 h. A zeta potential change from −33.7 to +8.2 mV was observed due to cleavage of phosphate groups by isolated IAP. PNPP could be identified as non-toxic up to concentrations of 0.01% (v/v). Furthermore, an enhanced cellular uptake of the NE changing its zeta potential on Caco-2 cells was determined. Therefore, PNPP seems to be a promising tool for the development of zeta potential changing NE.



中文翻译:

基于PEG化表面活性剂的磷酸部分裂解的Zeta电位变化纳米乳液

这项研究的目的是开发和评估一种包含聚氧乙烯(9)壬基酚单磷酸酯(PNPP)作为乳化剂的Zeta电位变化纳米乳液(NE)。

将2%(v / v)PNPP和0.18%(5μM)的十六烷基三甲基溴化铵(CTAB)掺入亲脂性NE预浓缩物中(PEG-40蓖麻油,三辛酸甘油酯/三癸酸酯,丙二醇二辛酸癸酸酯,丙二醇单月桂酸酯,高度纯化的二甘醇单乙醚; 20/20/10/30/20,v / v)。稀释亲脂性预浓缩物后,分析所得的NE,与小肠碱性磷酸酶(IAP)孵育后的液滴大小,多分散指数(PDI),储存稳定性和Zeta电位变化。通过孔雀石绿分析定量了IAP裂解引起的磷酸盐释放,并测定了毒性以及细胞对Caco-2细胞的吸收行为。包含PNPP和CTAB的NE显示的液滴大小为113 nm,PDI为0.20。在4小时内稳定。zeta电位从-33变化。由于分离的IAP切割了磷酸基团,因此观察到7至+8.2 mV。PNPP最高浓度为0.01%(v / v)时,可以确定为无毒的。此外,确定了增强的NE吸收细胞,改变了其在Caco-2细胞上的ζ电势。因此,PNPP似乎是开发ζ电位改变NE的有前途的工具。

更新日期:2020-07-20
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