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亮氨酸拉链型脂肽的温敏性及其在药物载体上的应用
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摘要
将自行设计的双亲性拉链型脂肽与磷脂混合制备得到一种新型的温敏性脂质体(Lipo-LPe)。该脂肽具有温敏性;在转变温度以上,由双螺旋结构转变为无规则单链结构。其游离在水溶液中和扦插在磷脂双分子层内都具备良好的温度可逆性。药物释放实验及抗肿瘤细胞实验均证明:在37℃条件下药物泄露被抑制,而在45℃条件下药物释放加速。同时,温度梯度实验也证明了该脂肽具备可逆的温控开关性能。Lipo-LPe展现了其作为一种新型温敏性及温控性药物载体的潜在应用前景,该研究也为其在临床上的应用提供了一个理论基础。
A novel thermo-sensitive liposome(Lipo-LPe) has been prepared by anchoring zipper-type amphipathic lipopeptides into liposomal bilayer.The designed lipopeptides were thermo-sensitive,they changed from double helix to single random coils above the melting temperature.These lipopeptides also showed good reversible thermo-sensitivity both being in free state and doping into liposomal bilayer.Drug release experiments and anti-tumor cell effect experiments both showed that drug leakage was restrained at 37℃ but accelerated at45℃.Drag release under an intermittent heating was performed and the reversibility of thermo-sensitive on/off switch was confirmed.Lipo-LPe presents a promising thermo-sensitive and temperature-controllable drug carrier,and this study provides a rationale for its application on clinic.
引文
[1]Shen,W.;Lammertink,R.G.H.;Sakata,J.K.;Kornfield,J.A.;Tirrell,D.A.Macromolecules,2005,38:3909.
    [2]Zahraa,S.A.;Wafa,T.A.;Jeroen,V.B.;Tam,T.B.;Alex,F.D.Acs Nano,2012,6(10):9335.

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