The Self-Assembly of Anticancer Camptothecin-Dipeptide Nanotubes: A Minimalistic and High Drug Loading Approach to Increased Efficacy

被引：73
|
作者：
Kim, Se Hye [1 ]
Kaplan, Jonah A. [2 ,3 ]
Sun, Yuan [1 ]
Shieh, Aileen [1 ]
Sun, Hui-Lung [4 ]
Croce, Carlo M. [4 ]
Grinstaff, Mark W. [2 ,3 ]
Parquette, Jon R. [1 ]
机构：
[1] Ohio State Univ, Dept Chem & Biochem, Columbus, OH 43210 USA
[2] Boston Univ, Dept Biomed Engn, Boston, MA 02215 USA
[3] Boston Univ, Dept Chem, Boston, MA 02215 USA
[4] Ohio State Univ, Dept Mol Virol Immunol & Med Genet, Columbus, OH 43210 USA
来源：
CHEMISTRY-A EUROPEAN JOURNAL | 2015年 / 21卷 / 01期
基金：
美国国家科学基金会;
关键词：
anti-cancer prodrugs; high drug loading; nanomedicines; self-assembly; MAMMALIAN TOPOISOMERASE-I; PLGA-BASED NANOPARTICLES; HUMAN SERUM-ALBUMIN; ANTITUMOR-ACTIVITY; GOLD NANOPARTICLES; PHARMACOKINETIC TRIAL; IRINOTECAN CPT-11; CARBON NANOTUBES; DELIVERY-SYSTEM; CANCER-THERAPY;
D O I：
10.1002/chem.201404520
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
20-(S)-Camptothecin (CPT)-conjugated dipeptides are reported that preassemble into nanotubes with diameters ranging from 80-120 nm. These nanoassemblies maintain a high (similar to 47%) drug loading and exhibit greater drug stability (i.e., resistance to lactone hydrolysis), and consequently greater efficacy against several human cancer cells (HT-29, A549, H460, and H23) in vitro compared with the clinically used prodrug irinotecan. A key and defining feature of this system is the use of the CPT-conjugated dipeptide as both the drug and precursor to the nanostructured carrier, which simplifies the overall fabrication process.
引用
收藏
页码：101 / 105
页数：5
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