title: Non-invasive, real-time reporting drug release in vitro and in vivo.
abstract: We developed a real-time drug-reporting conjugate (CPT-SS-CyN) composed of a near-infrared (NIR) fluorescent cyanine-amine dye (CyN), a disulfide linker, and a model therapeutic drug (camptothecin, CPT). Treatment with dithiothreitol (DTT) induces cleavage of the disulfide bond, followed by two simultaneous intramolecular cyclization reactions with identical kinetics, one to cleave the urethane linkage to release the NIR dye and the other to cleave the carbonate linkage to release CPT. The released CyN has an emission wavelength (760 nm) that is significantly different from CPT-SS-CyN (820 nm), enabling easy detection and monitoring of drug release. A linear relationship between the NIR fluorescence intensity at 760 nm and the amount of CPT released was observed, substantiating the use of this drug-reporting conjugate to enable precise, real-time, and non-invasive quantitative monitoring of drug release in live cells and semi-quantitative monitoring in live animals.
authors: Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, 1304 West Green Street, Urbana, IL 61801, USA. jianjunc@illinois.edu.
authors: Yanfeng
authors: Y
authors: Zhang
authors: Qian
authors: Q
authors: Yin
authors: Jonathan
authors: J
authors: Yen
authors: Joanne
authors: J
authors: Li
authors: Hanze
authors: H
authors: Ying
authors: Hua
authors: H
authors: Wang
authors: Yuyan
authors: Y
authors: Hua
authors: Eric J
authors: EJ
authors: Chaney
authors: Stephen A
authors: SA
authors: Boppart
authors: Jianjun
authors: J
authors: Cheng
mesh_terms: D000818:Animals; D002166:Camptothecin / Q000737:chemistry; D002232:Carbocyanines / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005260:Female; D005456:Fluorescent Dyes / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D007259:Infrared Rays; D051379:Mice; D013050:Spectrometry, Fluorescence; D013997:Time Factors
chemical_list: D002232:Carbocyanines; D004337:Drug Carriers; D005456:Fluorescent Dyes; D002166:Camptothecin