Bleomycin in octaarginine-modified fusogenic liposomes results in improved tumor growth inhibition.

Bleomycin in octaarginine-modified fusogenic liposomes results in improved tumor growth inhibition.
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DOI:
10.1016/j.canlet.2012.06.008
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发表时间:
2013-07-01
期刊:
影响因子:
9.7
通讯作者:
Torchilin, Vladimir P.
Torchilin, Vladimir P.
中科院分区:
医学1区
文献类型:
--
作者:
Koshkaryev, Alexander;Piroyan, Aleksandr;Torchilin, Vladimir P.

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Bleomycin (BLM) is an example of an anticancer drug that should be delivered into cytosol for its efficient therapeutic action. With this in mind, we developed octaarginine (R8)-modified fusogenic DOPE-liposomes (R8-DOPE-BLM). R8-modification dramatically increased (up to 50-fold) the cell-liposome interaction. R8-DOPE-liposomes were internalized via macropinocytosis and did not end up in the lysosomes. R8-DOPE-BLM led to a significantly stronger cell death and DNA damage in vitro relative to all controls. R8-DOPE-BLM demonstrated a prominent anticancer effect in the BALB/c mice bearing 4T1 tumors. Thus, R8-DOPE-BLM provided efficient intracellular delivery of BLM leading to strong tumor growth inhibition in vivo.
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