Multifunctional drug nanocarriers formed by cRGD-conjugated βCD-PAMAM-PEG for targeted cancer therapy.
Multifunctional drug nanocarriers formed by cRGD-conjugated βCD-PAMAM-PEG for targeted cancer therapy.
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DOI：
10.1016/j.colsurfb.2014.12.042
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发表时间：
2015-02-01
影响因子：
5.8
通讯作者：
Gong, Shaoqin
中科院分区：
文献类型：
--
作者：
Saraswathy, Manju;Knight, Gavin T.;Pilla, Srikanth;Ashton, Randolph S.;Gong, Shaoqin
聚酰胺胺 (PAMAM) 树枝状聚合物与羧甲基-β-环糊精 (βCD) 和聚乙二醇 (PEG) 缀合。然后将用作肿瘤靶向配体的环状 RGD 肽选择性地缀合到 PEG 臂的远端。所得的βCD-PAMAM-PEG-cRGD聚合物能够在水溶液中形成稳定且均匀的纳米颗粒（NP）。阿霉素 (Dox) 是一种模型疏水性抗癌药物，通过药物和 βCD 之间形成的包合物被有效封装在纳米颗粒中。 Dox 负载水平为 16.8 wt%。 U87MG 细胞系中 cRGD 缀合的 Dox 负载 NP 的细胞摄取量远高于非靶向 NP。此外，cRGD 缀合的 NP 的抗增殖作用优于游离药物和非靶向 NP。这些结果表明，由βCD-PAMAM-PEG-cRGD形成的具有高药物负载的纳米颗粒可以通过肿瘤靶向递送和增强细胞摄取来显着提高抗癌功效。
Polyamidoamine (PAMAM) dendrimer was conjugated with both carboxymethyl-β-cyclodextrin (βCD) and poly(ethylene glycol) (PEG). Cyclic RGD peptide, used as a tumor targeting ligand, was then selectively conjugated onto the distal ends of the PEG arms. The resulting βCD-PAMAM-PEG-cRGD polymer was able to form stable and uniform nanoparticles (NPs) in aqueous solution. Doxorubicin (Dox), a model hydrophobic anticancer drug, was effectively encapsulated in the NPs via an inclusion complex formed between the drug and βCD. The Dox loading level was 16.8 wt%. The cellular uptake of cRGD-conjugated Dox-loaded NPs in the U87MG cell line was much higher than that of non-targeted NPs. Furthermore, the anti-proliferative effect of the cRGD-conjugated NPs was superior to that of free drug and non-targeted NPs. These results suggest that NPs formed by βCD-PAMAM-PEG-cRGD with a high drug payload may significantly improve the anticancer efficacy by tumor-targeted delivery and enhanced cellular uptake.
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影响因子：
14
作者：
Guo, Jintang;Hong, Hao;Chen, Guojun;Shi, Sixiang;Zheng, Qifeng;Zhang, Yin;Theuer, Charles P.;Barnhart, Todd E.;Cai, Weibo;Gong, Shaoqin
通讯作者：
Gong, Shaoqin
DOI：
10.1016/0731-7085(90)80100-4
发表时间：
1990-01-01
影响因子：
3.4
作者：
BEKERS, O;BEIJNEN, JH;UNDERBERG, WJM
通讯作者：
UNDERBERG, WJM
影响因子：
5.8
作者：
Jevprasesphant, R;Penny, J;D'Emanuele, A
通讯作者：
D'Emanuele, A
影响因子：
4.9
作者：
Boswell, C. Andrew;Eck, Peter K.;Brechbiel, Martin W.
通讯作者：
Brechbiel, Martin W.
影响因子：
4.7
作者：
Hong, Seungpyo;Leroueil, Pascale R.;Holl, Mark M. Banaszak
通讯作者：
Holl, Mark M. Banaszak