The self-assembly of anticancer camptothecin-dipeptide nanotubes: a minimalistic and high drug loading approach to increased efficacy.

20-(S)-Camptothecin (CPT)-conjugated dipeptides are reported that preassemble into nanotubes with diameters ranging from 80-120 nm. These nanoassemblies maintain a high (∼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.
AuthorsSe Hye Kim, Jonah A Kaplan, Yuan Sun, Aileen Shieh, Hui-Lung Sun, Carlo M Croce, Mark W Grinstaff, Jon R Parquette
JournalChemistry (Weinheim an der Bergstrasse, Germany) (Chemistry) Vol. 21 Issue 1 Pg. 101-5 (Jan 2 2015) ISSN: 1521-3765 [Electronic] Germany
PMID25384556 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S.)
Copyright© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Chemical References
  • Antineoplastic Agents, Phytogenic
  • Dipeptides
  • Drug Carriers
  • Prodrugs
  • Camptothecin
  • Antineoplastic Agents, Phytogenic (chemistry, pharmacology)
  • Camptothecin (chemistry, pharmacology)
  • Cell Line, Tumor
  • Cell Survival (drug effects)
  • Dipeptides (chemistry)
  • Drug Carriers (chemistry)
  • HT29 Cells
  • Humans
  • Microscopy, Fluorescence
  • Nanomedicine
  • Nanotubes (chemistry)
  • Prodrugs (chemistry, pharmacology)

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