Dendrimer-encapsulated camptothecins:: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro
Dendrimer-encapsulated camptothecins:: Increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro
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DOI：
10.1158/0008-5472.can-06-2066
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发表时间：
2006-12-15
期刊：
影响因子：
11.2
通讯作者：
Grinstaff, Mark W.
中科院分区：
文献类型：
--
作者：
Morgan, Meredith T.;Nakanishi, Yuka;Grinstaff, Mark W.
本发明描述了一种由天然代谢产物甘油和琥珀酸组成的生物相容性聚酯树枝状聚合物，其用于抗肿瘤喜树碱10-羟基喜树碱和7-丁基-10-氨基喜树碱的包封。树枝状聚合物-药物复合物对四种不同的人癌细胞系[人乳腺癌（MCF-7）]的细胞毒性。结直肠腺癌（HT-29）、非小细胞肺癌（NCI-H460）和胶质母细胞瘤（SF-268）]，并且测量到低nmol/L IC 50值。MCF-7细胞中的细胞摄取和流出测量显示，当使用树枝状聚合物载体时，细胞摄取增加16倍，细胞内药物保留增加。
A biocompatible polyester dendrimer composed of the natural metabolites, glycerol and succinic acid, is described for the encapsulation of the antitumor camptothecins, 10-hydroxy-camptothecin and 7-butyl-10-aminocamptothecin. The cyto-toxicity of the dendrimer-drug complex toward four different human cancer cell lines [human breast adenocarcinoma (MCF-7). colorectal adenocarcinoma (HT-29), non-small cell lung carcinoma (NCI-H460), and glioblastoma (SF-268)] is also reported, and low nmol/L IC50 values are measured. Cellular uptake and efflux measurements in MCF-7 cells show an increase of 16-fold for cellular uptake and an increase in drug retention within the cell when using the dendrimer vehicle.