Clary L, Verderone G, Santaella C, Vierling P
Laboratoire de Chimie Bioorganique, UPRESA 6001 CNRS, Faculté des Sciences, Université de Nice-Sophia Antipolis, Nice, France.
Biochim Biophys Acta. 1997 Aug 14;1328(1):55-64. doi: 10.1016/s0005-2736(97)00076-x.
The release of encapsulated carboxyfluorescein (CF) from liposomes made from various fluorinated amido-connected double-chain phosphocholines and their membrane permeability have been investigated at 37 degrees C in buffer and in human serum. These fluorinated membranes and liposomes display lower permeability coefficients and are able to retain more efficiently encapsulated CF than any of their respective conventional counterparts. Several of these liposomes are as effective as the first generation of liposomes based on fluorinated phosphatidylcholines, indicating that the chemical junction (ester/amide) and nature of the unit (glycerol, diaminopropanol, serine, ethanolamine) connecting the hydrophobic chains to the phosphocholine polar head have no significant effect on permeability and CF release. Our results show further that a fluorinated intramembrane layer reduces significantly the permeability of membranes in a liquid-crystalline state, protects the liposomes from the destabilizing effects of serum, and even increases their stability (in terms of dye retention) in serum when the membranes are in the gel state.
在37摄氏度的缓冲液和人血清中，研究了由各种氟化酰胺连接的双链磷酸胆碱制成的脂质体中封装的羧基荧光素（CF）的释放及其膜通透性。这些氟化膜和脂质体显示出较低的渗透系数，并且比其各自的传统对应物更能有效地保留封装的CF。其中几种脂质体与基于氟化磷脂酰胆碱的第一代脂质体一样有效，这表明连接疏水链与磷酸胆碱极性头部的化学连接（酯/酰胺）和单元（甘油、二氨基丙醇、丝氨酸、乙醇胺）的性质对通透性和CF释放没有显著影响。我们的结果进一步表明，氟化的膜内夹层显著降低了液晶态膜的通透性，保护脂质体免受血清的破坏作用，并且当膜处于凝胶态时，甚至提高了它们在血清中的稳定性（就染料保留而言）。
