PCM and TAT co-modified liposome with improved myocardium delivery: in vitro and in vivo evaluations.
PCM and TAT co-modified liposome with improved myocardium delivery: in vitro and in vivo evaluations.
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PCM 和 TAT 共修饰脂质体可改善心肌输送：体外和体内评估。
DOI：
10.1080/10717544.2016.1253121
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发表时间：
2017-11
期刊：
影响因子：
6
通讯作者：
Chen H
中科院分区：
文献类型：
--
作者：
Wang X;Huang H;Zhang L;Bai Y;Chen H
本研究将PCM和达特共修饰脂质体作为心肌给药的新型载体，并对其体内外性质进行了评价。采用薄膜水合法制备了含荧光探针香豆素-6的脂质体。PCM配体特异性结合原代心肌细胞（MCs）细胞外结缔组织中的PCM受体，而达特配体作为经典的细胞穿透肽使脂质体被MCs内化。制备了未修饰脂质体（L）、PCM修饰脂质体（PL）、TAT修饰脂质体（TL）以及PCM和达特共修饰脂质体（PTL）并进行了表征。MCs对各种脂质体的细胞摄取和细胞内分布表明PTL具有最佳的递送能力。肽抑制实验表明，PCM可抑制PL的摄取。但达特几乎不能抑制TL的摄取。此外，CCK-8实验表明脂质体具有较低的细胞毒性。冷冻切片的体内荧光图像和HPLC-荧光分析进一步证明PTL具有最高的心肌分布。结果表明，PCM和达特共修饰可以提高脂质体的心肌靶向性。
In this study, PCM and TAT co-modified liposome was developed as a novel drug carrier for myocardium delivery with evaluation of its in vitro and in vivo properties. Liposomes containing fluorescent probe coumarin-6 were prepared by thin-film hydration. The PCM ligands specifically bind to the PCM receptors in the extracellular connective tissue of primary myocardium cells (MCs), while the TAT ligands functioned as a classical cell penetrating peptide to make liposomes internalized by MCs. The unmodified liposome (L), PCM-modified liposome (PL), TAT-modified liposome (TL) and PCM and TAT co-modified liposome (PTL) were prepared and characterized. The cellular uptake and intracellular distribution of various liposomes by MCs demonstrated that PTL had the best delivery capability. Peptide inhibition assay indicated that the uptake of PL could be inhibited by PCM. However, TAT could almost not suppress the uptake of TL. In addition, the CCK-8 experiments showed that liposomes had low cytotoxicity. In vivo fluorescent images of frozen sections and HPLC-fluorescence analysis further demonstrated that PTL had highest myocardium distribution. The results of this study demonstrated that PCM and TAT co-modifying could improve the myocardial targeting ability of liposome.
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DOI：
10.1016/j.jconrel.2014.07.041
发表时间：
2014-12-10
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Won YW;Bull DA;Kim SW
通讯作者：
Kim SW
影响因子：
6
作者：
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通讯作者：
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DOI：
10.1016/j.jconrel.2015.06.017
发表时间：
2015-12-28
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Dasa SSK;Suzuki R;Gutknecht M;Brinton LT;Tian Y;Michaelsson E;Lindfors L;Klibanov AL;French BA;Kelly KA
通讯作者：
Kelly KA
影响因子：
3.5
作者：
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通讯作者：
Allen, TM
影响因子：
9.7
作者：
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Oku, Naoto