文献类型：期刊文献

英文题名：A designed lipopeptide with a leucine zipper as an imbedded on/off switch for lipid bilayers

作者：Wang, Sijia[1,2];Shen, Yinxing[1,2];Zhang, Junqi[3,4];Xu, Shouhong[1,2];Liu, Honglai[1,2]

机构：[1]E China Univ Sci & Technol, Key Lab Adv Mat, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Dept Chem, Shanghai 200237, Peoples R China;[3]Fudan Univ, Sch Basic Med Sci, Key Lab Med Mol Virol, Minist Hlth, 138 Yixueyuan Rd, Shanghai 200032, Peoples R China;[4]Fudan Univ, Sch Basic Med Sci, Key Lab Med Mol Virol, Minist Educ, 138 Yixueyuan Rd, Shanghai 200032, Peoples R China

年份：2016

卷号：18

期号：15

起止页码：10129

外文期刊名：PHYSICAL CHEMISTRY CHEMICAL PHYSICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000374350600030)】；

基金：Financial support for this study is provided by the National Natural Science Foundation of China (No. 21276074), the 111 Project (No. B08021) of China and the Fundamental Research Funds for the Centre Universities of China.

语种：英文

摘要：Thermo-sensitive drug carriers are receiving increasing attention for use with localized hyperthermia at abnormal tissue sites or to easily implement hyperthermia. In this study, a thermo-sensitive lipopeptide was designed, consisting of a carbon chain and a leucine zipper with an amino acid sequence CH3-(CH2)(4)-CO-NH-VAQLEVK-VAQLESK-VSKLESK-VSSLESK-COOH. They could form dimers by the hydrophobic force at body temperature and separate into single random coils above the melting temperature (T-m). The lipopeptide was mixed with phospholipids to form a hybrid liposome (Lipo-LPe). The T-m of the free lipopeptide and lipopeptide in Lipo-LPe was found to be 48.0 degrees C and 42.5 degrees C from circular dichroism data, respectively. Compared with the pure liposome, the phase-transition temperature (T-tr) of Lipo-LPe, which was obtained by differential scanning calorimetry, was increased by about 5 degrees C, showing an improvement of thermal stability. The drug release rate of Lipo-LPe was slightly decreased at body temperature but greatly increased at mild hyperthermia in vitro. Drug release under intermittent heating was performed, and the reversibility of thermo-sensitive on/off switch was confirmed. Furthermore, Lipo-LPe achieved the maximum amount of cell death under mild hyperthermia. We concluded that Lipo-LPe, as a novel thermo-sensitive drug carrier, provides a promising opportunity for controlling drug release.