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.
Department of Chemistry and Biochemistry, The Ohio State University, 100 W. 18th Ave. Columbus, OH 43210 (USA), Fax: (+1) 614-292-1685.
Se Hye
SH
Kim
Jonah A
JA
Kaplan
Yuan
Y
Sun
Aileen
A
Shieh
Hui-Lung
HL
Sun
Carlo M
CM
Croce
Mark W
MW
Grinstaff
Jon R
JR
Parquette
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology; D002166:Camptothecin / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004151:Dipeptides / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D019073:HT29 Cells; D006801:Humans; D008856:Microscopy, Fluorescence; D050997:Nanomedicine; D043942:Nanotubes / Q000737:chemistry*; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology
D000972:Antineoplastic Agents, Phytogenic; D004151:Dipeptides; D004337:Drug Carriers; D011355:Prodrugs; D002166:Camptothecin
anti-cancer prodrugs; high drug loading; nanomedicines; self-assembly