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脂质在经历多晶型相变时形成纳米孔和纳米颗粒。

Nanopore and Nanoparticle Formation with Lipids Undergoing Polymorphic Phase Transitions.

作者信息

Cholakova Diana, Glushkova Desislava, Tcholakova Slavka, Denkov Nikolai

机构信息

Department of Chemical and Pharmaceutical Engineering, Faculty of Chemistry and Pharmacy, Sofia University, 1 James Bourchier Avenue, 1164 Sofia, Bulgaria.

出版信息

ACS Nano. 2020 Jul 28;14(7):8594-8604. doi: 10.1021/acsnano.0c02946. Epub 2020 Jul 1.

Abstract

We describe several unexpected phenomena, caused by a solid-solid phase transition (gel-to-crystal) typical for all main classes of lipid substances: phospholipids, triglycerides, diglycerides, alkanes, . We discovered that this transition leads to spontaneous formation of a network of nanopores, spreading across the entire lipid structure. These nanopores are spontaneously impregnated (flooded) by water when appropriate surfactants are present, thus fracturing the lipid structure at a nanoscale. As a result, spontaneous disintegration of the lipid into nanoparticles or formation of double emulsions is observed, just by cooling and heating of an initial coarse lipid-in-water dispersion around the lipid melting temperature. The process of nanoparticle formation is effective even after incorporation of medical drugs of high load, up to 50% in the lipid phase. The role of the main governing factors is clarified, the procedure is optimized, and the possibility for its scaling-up to industrially relevant amounts is demonstrated.

摘要

我们描述了由所有主要类别的脂质物质(磷脂、甘油三酯、甘油二酯、烷烃等)典型的固-固相变(凝胶-晶体)引起的几种意外现象。我们发现这种转变会导致纳米孔网络的自发形成,该网络遍布整个脂质结构。当存在适当的表面活性剂时,这些纳米孔会被水自发填充(淹没),从而在纳米尺度上破坏脂质结构。结果,仅通过在脂质熔点附近对初始粗水包脂质分散体进行冷却和加热,就可以观察到脂质自发分解成纳米颗粒或形成双重乳液。即使在掺入高达脂质相50%的高负载药物后,纳米颗粒形成过程仍然有效。阐明了主要控制因素的作用,优化了该过程,并证明了将其扩大到工业相关量的可能性。

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