Fullerene-conjugated doxorubicin in cells.
The conjugation of fullerene with well-established drug molecules has been a representative strategy to impart fullerene-specific properties for improved formulation. However, conjugates involving fullerenes or other nanomaterials often differ significantly from the free drug molecules in cellular uptake and distributions. For the highly effective anticancer drug doxorubicin (DOX), its strong absorption and fluorescence in the visible spectral region enable the tracking of DOX-containing conjugates by optical techniques. In this work, a stoimetrically and structurally well-defined fullerene-DOX conjugate was studied in terms of fluorescence microscopy, including the fluorescence imaging with two-photon excitation, to examine the uptake and distribution in human breast cancer cells. The results suggested that the conjugate was distributed mostly in the cytoplasm, significantly different from free DOX molecules (predominantly in the cell nucleus, as already reported in the literature). Mechanistic implications of the results are discussed. Also discussed are potentials of conjugated DOX species as self-labeled fluorescent probes in bioimaging and other mechanistic investigations on drug delivery.
Liu
Jia-Hui
JH
Department of Chemistry and Laboratory for Emerging Materials and Technology, Clemson University, Clemson, South Carolina 29634-0973, USA.
Cao
Li
L
Luo
Pengju G
PG
Yang
Sheng-Tao
ST
Lu
Fushen
F
Wang
Haifang
H
Meziani
Mohammed J
MJ
Haque
Sk Anwarul
SA
Liu
Yuanfang
Y
Lacher
Sebastian
S
Sun
Ya-Ping
YP
D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D001943:Breast Neoplasms / Q000378:metabolism* / Q000473:pathology; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D037741:Fullerenes / Q000737:chemistry*; D006801:Humans
D000970:Antineoplastic Agents; D004337:Drug Carriers; D037741:Fullerenes; D004317:Doxorubicin