前药
化学
紫杉醇
体内
药理学
生物发光成像
PEG比率
聚乙二醇
药物输送
生物结合
荧光素酶
生物化学
化疗
有机化学
转染
外科
生物技术
基因
经济
生物
医学
财务
作者
Simona Mura,Fatima Zouhiri,Stéphanie Lerondel,Andrei Maksimenko,Julie Mougin,Claire Gueutin,Davide Brambilla,Joachim Caron,Éric Śliwiński,Alain Lepape,Didier Desmaële,Patrick Couvreur
摘要
A new paclitaxel (Ptx) prodrug was designed by coupling a single terpene unit (MIP) to the hydroxyl group in position 2′ of the drug molecule. Using a squalene derivative of polyethylene glycol (SQ-PEG) as surface active agent, the resulting bioconjugate (PtxMIP) self-assembled in water leading to the formation of stable nanoparticles (PtxMIP_SQ-PEG NPs) with an impressively high drug loading (82%). In vivo, the anticancer activity of this novel Ptx nanoassembled prodrug was compared to the conventional Cremophor-containing formulation (Taxol) on a murine model of breast cancer lung metastasis induced by intravenous injection of 4T1 tumor cells, genetically modified to stably express firefly luciferase. Cell growth was assessed noninvasively by bioluminescence imaging (BLI) which enabled monitoring tumor metastatic burden in the same animals. PtxMIP_SQ-PEG nanoparticles slowed metastatic spread and were better tolerated than the Cremophor-containing formulation (i.e., free drug), thus demonstrating the potential of terpene-based nanoassembled prodrugs in the improvement of the therapeutic index of Ptx in balb/c mice.
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