Evaluation of triazole-chelated lanthanides as chemically stabile bioimaging agents

Amruta Indapurkar, Brian Henriksen, Justin Tolman, James T. Fletcher

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Europium (Eu), dysprosium (Dy), samarium (Sm), and terbium (Tb) complexes were prepared using the neutral tridentate chelator 2,6-bis(1-benzyl-1,2,3-triazol-4-yl)pyridine and one equivalent of each lanthanide salt. The physicochemical, aerodynamic, and in vitro cellular properties of each lanthanide metal complex were studied to determine their viability as cell surface fluorescent probes. Each compound was characterized by electrospray ionization mass spectroscopy (ESI-MS), ultraperformance liquid chromatography (UPLC), differential scanning calorimetry (DSC), and thermogravimetic analysis (TGA). Upon excitation at 320 nm each complex displayed characteristic lanthanide-based fluorescence emission in the visible wavelength range with stokes shifts greater than 200 nm. Each complex was found to be chemically stable when exposed to pH range of 1-11 for 72 h and resistant to photobleaching. To simulate pulmonary administration of these fluorophores, the aerodynamic properties of the Eu and Tb complexes were determined using a next generation impactor (NGI). This measurement confirmed that the complexes retain their fluorescence emission properties after nebulization. Cellular cytotoxicity was determined on A-549 lung cancer cell line using methylthiazol tetrazolium (MTT) cytotoxicity assay at 24, 48, and 72 h postexposure to the complexes. The complexes showed a dose and time-dependent effect on the percent viability of the cells.

Original languageEnglish
Pages (from-to)2589-2598
Number of pages10
JournalJournal of Pharmaceutical Sciences
Volume102
Issue number8
DOIs
StatePublished - Aug 2013

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Lanthanoid Series Elements
Triazoles
Terbium
Europium
Cell Survival
Dysprosium
Fluorescence
Samarium
Photobleaching
Coordination Complexes
Differential Scanning Calorimetry
Chelating Agents
Fluorescent Dyes
Liquid Chromatography
Lung Neoplasms
Mass Spectrometry
Salts
Cell Line
Lung

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Evaluation of triazole-chelated lanthanides as chemically stabile bioimaging agents. / Indapurkar, Amruta; Henriksen, Brian; Tolman, Justin; Fletcher, James T.

In: Journal of Pharmaceutical Sciences, Vol. 102, No. 8, 08.2013, p. 2589-2598.

Research output: Contribution to journalArticle

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