期刊
NANO RESEARCH
卷 9, 期 3, 页码 663-673出版社
TSINGHUA UNIV PRESS
DOI: 10.1007/s12274-015-0945-1
关键词
self-assembly; self-delivery; prodrug; tumor-targeting therapy
类别
资金
- National Natural Science Foundation of China [51125014, 51503227, 51233003]
- Natural Science Foundation of Hubei Province of China [2014CFB696, 2013CFA003]
A novel self-delivered prodrug system was fabricated for tumor-targeting therapy. In this nanosystem, the Arg-Gly-Asp-Ser (RGDS) tetrapeptide was used to improve the therapeutic index to integrin-overexpressing tumor cells. The antitumorous drug camptothecin was further appended to the epsilon-amino group of lysine by 20-O-succinyl linkage and controllably released via hydrolytic cleavage. Prodrug molecules self-assembled into fibrillar nano-architectures and achieved the capability of self-delivery after being injected subcutaneously into mice. Introduction of hydrophobic myristic acid favored the self-assembly and enhanced the cellular internalization of the prodrugs. In vitro and in vivo studies demonstrated that the self-assembled nanofibers could effectively target integrinoverexpressing tumorous cells and inhibit tumor growth via RGD-mediated specific targeting. Therefore, the traditional idea that fibrillar structures hold low therapeutic efficacy due to poor cell uptake can be challenged.
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