Journal
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
Volume 127, Issue -, Pages 28-37Publisher
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jphotobiol.2013.06.008
Keywords
Chlorin; PEG; Folic acid; Water-solubility; Tumor targeting; Cytotoxicity
Categories
Funding
- National Natural Science Foundation of China [21072227, 61275216]
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Techniques to enhance tumor targeting and to improve the aqueous solubility of anticancer drugs and photosensitizers have recently been the focus of much research. In this study, a folate-PEG-conjugated chlorin was synthesized and characterized. Because of the use of PEG as a linker, the new chlorin displayed increased aqueous solubility, with a solubility of 40.1 mg/mL in PBS, and showed lower aggregation and cytotoxicity than its precursor, chlorin. Meanwhile, the introduction of folic acid to the new chlorin resulted in increased selectivity for folate-receptor-positive tumor cells (HeLa and Hep-2 cells); the cellular uptake of the new chlorin by HeLa and Hep-2 cells was strikingly higher than that of the precursor chlorin, and the photocytotoxicities of the new chlorin to HeLa and Hep-2 cells were 2.5 and 3.5 times greater than that of folate-free conjugate chlorin. During photodynamic therapy mediated by the new chlorin, both type I and type II reactions occur simultaneously. (C) 2013 Elsevier B.V. All rights reserved.
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