SI-ATRP Decoration of Magnetic Nanoparticles with PHEMA and Post-Polymerization Modification with Folic Acid for Tumor Cells’ Specific Targeting

Abstract

Targeted nanocarriers could reach new levels of drug delivery, bringing new tools for personalized medicine. It is known that cancer cells overexpress folate receptors on the cell surface compared to healthy cells, which could be used to create new nanocarriers with specific targeting moiety. In addition, magnetic nanoparticles can be guided under the influence of an external magnetic field in different areas of the body, allowing their precise localization. The main purpose of this paper was to decorate the surface of magnetic nanoparticles with poly(2-hydroxyethyl methacrylate) (PHEMA) by surface-initiated atomic transfer radical polymerization (SI-ATRP) followed by covalent bonding of folic acid to side groups of the polymer to create a high specificity magnetic nanocarrier with increased internalization capacity in tumor cells. The biocompatibility of the nanocarriers was demonstrated by testing them on the NHDF cell line and folate-dependent internalization capacity was tested on three tumor cell lines: MCF-7, HeLa and HepG2. It has also been shown that a higher concentration of folic acid covalently bound to the polymer leads to a higher internalization in tumor cells compared to healthy cells. Last but not least, magnetic resonance imaging was used to highlight the magnetic properties of the functionalized nanoparticles obtained.

Solid-Phase Synthesized Copolymers for the Assembly of pH-Sensitive Micelles Suitable for Drug Delivery Applications

“…For biomedical applications, the pH-sensitive materials or assemblies that are stable at physiological pH (pH = 7.4) and unstable at lower pH (pH = 5.0–7.2) [ 1 , 2 , 3 , 4 , 5 ], together with the efficient carriers of a different nature [ 6 , 7 , 8 , 9 , 10 ], are of great interest [ 1 , 2 , 3 , 4 , 5 ]. Particularly, for drug delivery applications in cancer treatment, these types of materials, if properly tuned, enable the release of therapeutics within tumor tissues (pH = 6.5–7.2) [ 11 , 12 , 13 , 14 , 15 , 16 , 17 ], making the pH sensibility an excellent strategy for targeted chemotherapeutics delivery. A large variety of efficient, pH-sensitive drug carriers has been developed and reported in the last two decades [ 12 , 13 , 18 , 19 ].…”

In situ evaluation of in vivo sialylation with a dual-color imaging strategy

“…29 In the obtained Den-Gal/Cy5/FA probe, Gal is the substrate for the sialylation proceeding by a-2,3-sialyltransferase (ST3Gal) and a-2,6-sialyltransferase (ST6Gal), 30,31 and FA was used for receptor-mediated endocytosis of the probes into tumor cells. 32,33 By injecting the probes into the tumor region in a living mouse, SA groups were bound to the Gals on Den-Gal/Cy5/FA through sialylation (Fig. 1B).…”