Abstract
Radiation crosslinking was employed to obtain nanocarriers based on poly(acrylic acid)—PAA—for targeted delivery of radioactive isotopes. These nanocarriers are internally crosslinked hydrophilic macromolecules—nanogels—bearing carboxylic groups to facilitate functionalization. PAA nanogels were conjugated with an engineered bombesin-derivative—oligopeptide combined with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate chelating moiety, aimed to provide selective radioligand transport. 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium (DMTMM) toluene-4-sulfonate was used as the coupling agent. After tests on a model amine—p-toluidine—both commercial and home-synthesized DOTA-bombesin were successfully coupled to the nanogels and the obtained products were characterized. The radiolabeling efficiency of nanocarriers with 177Lu, was chromatographically tested. The results provide a proof of concept for the synthesis of radiation-synthesized nanogel-based radioisotope nanocarriers for theranostic applications.
Highlights
In recent years targeted nanotherapeutics have attracted significant attention
Such formulations should be designed in a way that assures that following functionalities are introduced: therapeutic moiety—a delivery vehicle or protein, carrying the therapeutic cargo; targeting ligand—a specific probe, e.g., a small organic molecule, peptide, or antibody able to bind with specific components of the cell, facilitating transport of the construct into the target site [5,6]
The objective of this paper is to present a novel approach to the development of nanoscale carriers based on poly(acrylic acid) nanogels for the targeted delivery of cancer diagnostic and therapeutic agents
Summary
In recent years targeted nanotherapeutics have attracted significant attention. Many carriers as well as targeting ligands have been intensively explored to enable reaching tumor cells in tailored, precise way. A growing body of evidence supports the feasibility of this approach, and an increasing number of formulations is entering clinical trials [1,2,3,4]. Such formulations should be designed in a way that assures that following functionalities are introduced: therapeutic moiety—a delivery vehicle or protein, carrying the therapeutic cargo; targeting ligand—a specific probe, e.g., a small organic molecule, peptide, or antibody able to bind with specific components of the cell, facilitating transport of the construct into the target site [5,6]. This provides the opportunity for the transport of biologically active compounds in a fluid-like manner, while protecting them against
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