Liposomes derivatized with tetrabranched neurotensin peptides via click chemistry reactions
Liposomes derivatized with tetrabranched neurotensin peptides via click chemistry reactions
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DOI：
10.1039/c3nj00596h
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发表时间：
2013-01-01
影响因子：
3.3
通讯作者：
Morelli, Giancarlo
中科院分区：
文献类型：
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作者：
Accardo, Antonella;Ringhieri, Paola;Morelli, Giancarlo
神经降压素四聚体修饰的脂质体是通过使用脂质体后衍生化方法获得的，其中在外表面含有叠氮基功能的脂质体、DOPC/(C18)(2)-Peg9-N-3 (90/10)和修饰为存在C=C三键[(NT8-13)(4)-炔]的支链神经降压素肽之间进行点击化学反应。结果表明，脂质体后衍生化方法非常有效，并且点击化学程序对于纳米颗粒功能化非常有吸引力。脂质体的结构表征已通过动态光散射（DLS）测量进行。纯DOPC和混合DOPC/(C18)(2)-Peg9-N-3和DOPC/(C18)(2)-Peg-三唑-(NT8-13)(4)脂质体（摩尔比为90:10）的流体动力学半径分别为61+/-21nm、60+/-22nm和82+/-43nm。观察到非常有效的阿霉素负载，特别是 DOPC/ (C18)(2)-Peg9-N-3 脂质体，其载药量为 90%。
Liposomes decorated with neurotensin tetramers are obtained by using a post-liposomal derivatization method in which a click-chemistry reaction between liposomes containing azido functions on the external surface, DOPC/(C18)(2)-Peg9-N-3 (90/10), and branched neurotensin peptides modified for the presence of a C=C triple-bond [(NT8-13)(4)-alkyne] is performed. Results show that the post liposomal derivatization method is very efficient and that click-chemistry procedures are very attractive for nanoparticle functionalization. A structural characterization of liposomes has been performed by dynamic light scattering (DLS) measurements. The hydrodynamic radii of pure DOPC and mixed DOPC/(C18)(2)-Peg9-N-3 and DOPC/(C18)(2)-Peg-triazole-(NT8-13)(4) liposomes (at 90 : 10 molar ratio) are 61 +/- 21 nm, 60 +/- 22 nm and 82 +/- 43 nm, respectively. A very efficient doxorubicin loading has been observed, specially for DOPC/ (C18)(2)-Peg9-N-3 liposomes, with a drug loading content of 90%.