Jones M N, Francis S E, Hutchinson F J, Handley P S, Lyle I G
Department of Biochemistry and Molecular Biology, University of Manchester, UK.
Biochim Biophys Acta. 1993 Apr 22;1147(2):251-61. doi: 10.1016/0005-2736(93)90010-w.
Proteoliposomes having surface-bound succinylated concanavalin A (s-conA) have been prepared from a range of phospholipid mixtures by sonication (SUV) and reverse phase evaporation (REV) covering a range of size (weight-average diameter (dw)) from approx. 35 to 310 nm and weight-average number of protein molecules per liposomes (Pw) from approx. 50 to 3000. The targeting of the proteoliposomes to adsorbed biofilms of the bacteria Streptococcus sanguis and Streptococcus mutans has been assessed from the extent of inhibition of an enzyme-linked immunosorbent assay (ELISA) for bacterial cell surface antigens. The surface-bound lectin enhances targeting relative to 'naked' liposomes of comparable concentration by factors of 2-50 depending on the liposomal lipid composition and Pw. The effect of the bactericide Triclosan on the thermal properties and permeability characteristics of liposomes has been studied. At and above a molar ratio of Triclosan to lipid of 0.6, Triclosan eliminates the gel to liquid-crystalline phase transition in dipalmitoylphosphatidylcholine (DPPC) containing liposomes and increases the bilayer permeability of both liposomes and proteoliposomes to D-glucose. The proteoliposomes have been used to deliver Triclosan to S. sanguis biofilms and the inhibition of growth of the bacteria after treatment with liposomally delivered Triclosan has been determined using a microtitre plate re-growth assay and compared with growth inhibition by 'free' Triclosan. It is shown that for short exposure times (1 to 2 min) proteoliposomally delivered Triclosan is a more effective growth inhibitor than free Triclosan. The results are discussed in terms of the targeting, retention and subsequent release of Triclosan into the bacterial biofilms.
通过超声处理（SUV）和反相蒸发（REV），从一系列磷脂混合物中制备了表面结合有琥珀酰化伴刀豆球蛋白A（s - ConA）的蛋白脂质体，其大小范围（重均直径（dw））约为35至310 nm，每个脂质体的重均蛋白质分子数（Pw）约为50至3000。已根据用于细菌细胞表面抗原的酶联免疫吸附测定（ELISA）的抑制程度，评估了蛋白脂质体对血链球菌和变形链球菌吸附生物膜的靶向性。取决于脂质体的脂质组成和Pw，与浓度相当的“裸”脂质体相比，表面结合的凝集素可将靶向性提高2至50倍。研究了杀菌剂三氯生对脂质体热性质和通透性特征的影响。当三氯生与脂质的摩尔比达到及高于0.6时，三氯生消除了含二棕榈酰磷脂酰胆碱（DPPC）的脂质体中的凝胶态到液晶态的转变，并增加了脂质体和蛋白脂质体对D - 葡萄糖的双层通透性。已使用蛋白脂质体将三氯生递送至血链球菌生物膜，并使用微量滴定板再生长测定法确定了脂质体递送的三氯生处理后细菌的生长抑制情况，并与“游离”三氯生的生长抑制作用进行了比较。结果表明，在短暴露时间（1至2分钟）内，脂质体递送的三氯生比游离三氯生是更有效的生长抑制剂。根据三氯生在细菌生物膜中的靶向性、保留和随后的释放对结果进行了讨论。
