Ravily V, Santaella C, Vierling P
Laboratoire de Chimie Moléculaire, URA CNRS 426 and Laboratoire de Chimie Bioorganique, EP CNRS 104, Faculté des Sciences, Université de Nice-Sophia Antipolis, France.
Biochim Biophys Acta. 1996 Nov 13;1285(1):79-90. doi: 10.1016/s0005-2736(96)00150-2.
The stability (with respect to encapsulated carboxyfluorescein release) of liposomes made from various fluorocarbon 1,2-or 1,3-di-O-alkylglycerophosphocholines (ether-connected) and their membrane permeability have been investigated in buffer and in human serum. Membranes and liposomes, whether formulated with fluorocarbon/fluorocarbon or mixed fluorocarbon/hydrocarbon, 1,2- or 1,3-di-O-alkylglycerophospholipids, display lower permeability coefficients and are able to retain more efficiently encapsulated CF, even when incubated in human serum, than any of their conventional counterparts. These fluorinated liposomes are as stable as the first generation of liposomes formulated with their fluorocarbon ester-connected 1,2-di-O-acylglycerophosphocholine analogs. These results further confirm that a fluorinated intramembranar layer reduces the permeability of membranes (more significantly when they are in a fluid state), protects them from the destabilizing effects of serum components and increases even the stability of the fluorinated liposomes whose membranes are in the gel state when incubated in human serum. The impact of the modular structure of the fluorinated phospholipids (number of fluorocarbon chains, ether vs. ester bond, 1,2- vs. 1,3-isomer, etc...) and structure/permeability/ stability relationships are also presented.
研究了由各种氟碳1,2 - 或1,3 - 二 - O - 烷基甘油磷酸胆碱（醚连接）制成的脂质体在缓冲液和人血清中的稳定性（相对于包裹的羧基荧光素释放）及其膜通透性。无论是用氟碳/氟碳还是混合氟碳/烃类1,2 - 或1,3 - 二 - O - 烷基甘油磷脂配制的膜和脂质体，与任何传统脂质体相比，都显示出更低的通透系数，并且即使在人血清中孵育时也能够更有效地保留包裹的CF。这些氟化脂质体与第一代用其氟碳酸酯连接的1,2 - 二 - O - 酰基甘油磷酸胆碱类似物配制的脂质体一样稳定。这些结果进一步证实，氟化的膜内脂质层降低了膜的通透性（当它们处于流体状态时更显著），保护它们免受血清成分的破坏作用，并且即使在人血清中孵育时，也增加了其膜处于凝胶状态的氟化脂质体的稳定性。还介绍了氟化磷脂的模块化结构（氟碳链的数量、醚键与酯键、1,2 - 与1,3 - 异构体等）的影响以及结构/通透性/稳定性关系。
