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Synthesis and Biophysical Characterization of an Odd-Numbered 1,3-Diamidophospholipid
Langmuir ( IF 3.9 ) Pub Date : 2018-02-18 00:00:00 , DOI: 10.1021/acs.langmuir.7b04227
Frederik Neuhaus 1, 2 , Dennis Mueller 1 , Radu Tanasescu 1 , Sandor Balog 3 , Takashi Ishikawa 4 , Gerald Brezesinski 5 , Andreas Zumbuehl 1, 2
Affiliation  

Nanomedicine suffers from low drug delivery efficiencies. Mechanoresponsive vesicles could provide an alternative way to release active compounds triggered by the basic physics of the human body. 1,3-Diamidophospholipids with C16 tails proved to be an effective building block for mechanoresponsive vesicles, but their low main phase transition temperature prevents an effective application in humans. As the main phase transition temperature of a membrane depends on the fatty acyl chain length, we synthesized a C17 homologue of a 1,3-diamidophospholipid: Rad-PC-Rad. The elevated main phase transition temperature of Rad-PC-Rad allows mechanoresponsive drug delivery at body temperature. Herein, we report the biophysical properties of Rad-PC-Rad monolayer and bilayer membranes. Rad-PC-Rad is an ideal candidate for advancing the concept of physically triggered drug release.

中文翻译:

奇数的1,3-二酰胺基磷脂的合成与生物物理表征

纳米药物的药物递送效率低。机械响应性囊泡可以提供释放由人体基本物理学触发的活性化合物的替代方法。具有C16尾巴的1,3-二酰胺基磷脂被证明是机械响应囊泡的有效构件,但是它们的低主相变温度阻碍了其在人体中的有效应用。由于膜的主要相变温度取决于脂肪酰基链的长度,因此我们合成了1,3-二酰胺基磷脂:Rad-PC-Rad的C17同源物。Rad-PC-Rad升高的主相变温度允许在体温下传递机械响应性药物。在这里,我们报告Rad-PC-Rad单层和双层膜的生物物理特性。
更新日期:2018-02-18
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