Synthesis, characterization, and cytotoxicity evaluation of dextran-myristoyl-ECGKRK peptide conjugate.

Abstract The CGKRK peptide is a well-known tumor homing peptide with significant specificity for many types of cancer tissues. Herein, we described the synthesis of a novel drug delivery system based on dextran decorated with myristoyl-ECGKRK peptide. The myristoylated peptide was synthesized and conjugated to dextran via an ester bond followed by purification. FT-IR and NMR confirmed the success of the conjugation reaction, while the surface morphology examination revealed that the conjugate has a characteristic porous network-like structure. Dynamic-light scattering measurements indicated the ability of the conjugate to self-assemble into nanoparticles with an average size of 248 ± 6.33 nm, and zeta potential of 10.7 mV. The cytotoxicity profiles for the peptide, dextran, and dextran-peptide conjugate were evaluated against triple-negative breast cancer (MDA-MB-231), breast cancer cell lines (MCF-7), and human embryonic normal kidney cell line (HEK-293). The results revealed that myristoyl-ECGKRK was noncytotoxic on the two different breast cancer cell lines up to 50 μM, but the cell viability was minimally reduced to 85% at 50 μm in HEK-293 cells. Similarly, dextran showed a neglected cytotoxicity profile at all tested concentrations. The dextran conjugate was not toxic to the cells up to a concentration of 8.3 mg/mL.