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

页码：101 / 105

页数：5

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