Abstract
Targeted drug delivery by nanocarriers molecules can increase the efficiency of cancer treatment. One of the targeting ligands is folic acid (FA), which has a high affinity for the folic acid receptors, which are overexpressed in many cancers. Herein, we describe the preparation of the nanoconjugates containing quantum dots (QDs) and β-cyclodextrin (β-CD) with foliate-targeting properties for the delivery of anticancer compound C-2028. C-2028 was bound to the nanoconjugate via an inclusion complex with β-CD. The effect of using FA in QDs-β-CD(C-2028)-FA nanoconjugates on cytotoxicity, cellular uptake, and the mechanism of internalization in cancer (H460, Du-145, and LNCaP) and normal (MRC-5 and PNT1A) cells was investigated. The QDs-β-CD(C-2028)-FA were characterized using DLS (dynamic light scattering), ZP (zeta potential), quartz crystal microbalance with dissipation (QCM-D), and UV-vis spectroscopy. The conjugation of C-2028 with non-toxic QDs or QDs-β-CD-FA did not change the cytotoxicity of this compound. Confocal microscopy studies proved that the use of FA in nanoconjugates significantly increased the amount of delivered compound, especially to cancer cells. QDgreen-β-CD(C-2028)-FA enters the cells through multiple endocytosis pathways in different levels, depending on the cell line. To conclude, the use of FA is a good self-navigating molecule in the QDs platform for drug delivery to cancer cells.
Highlights
Faculty of Chemistry, Gdańsk University of Technology, Narutowicza Street 11/12, 80-233 Gdansk, Poland; Faculty of Chemistry, University of Warsaw, Pasteura Street 1, 02-093 Warsaw, Poland; Faculty of Chemistry, Warsaw University of Technology, Noakowskiego Street 3, 00-664 Warsaw, Poland;
We presented a new, efficient transporting platform for an anticancer drug—nanoconjugate of quantum dots and β-cyclodextrin labeled with a self-navigating molecule: folic acid (QDs-β-CD-FA)
The conjugation of unsymmetrical bisacridines derivative C-2028 with non-toxic QDs or QDs-β-CD-FA did not change the cytotoxic activity of this compound against cancer and normal cells
Summary
Navigating molecules-functionalized fluorescent agents, including folic acid- and transferrin-functionalized quantum dots can supply great assistance in surgery by tumor-specific fluorescence imaging [15] as well as drug targeting to cancer cells [22]. This strategy can allow for improving cancer therapy via enhancing the cytotoxicity and selectivity of drugs toward cancer cells while not affecting normal cells. UAs are the newest group of potential anticancer drugs among acridine derivatives conducted in our department for many years These compounds exhibited high cytotoxic and antitumor activity against many human tumors, including lung, pancreatic, prostate, and colon [26].
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