Background: Polymer-based nanoparticles as drug-delivery systems offer new therapeutic opportunities.
Among them, ligand-mediated targeting, which increases selectivity and efficacy, allows controllable drug
delivery. The aim of the this research was to prepare and characterize poly(methyl methacrylate) (PMMA)
nanoparticles grafted with the –Arginine, Glycine, Aspartic Acid (RGD)– peptide sequence as a promising smart
drug delivery system for Paclitaxel (PTX), directed at the sites of integrin receptor overexpression.
Methods: Nanoparticles were characterized by FT-IR and Raman spectroscopy, dynamic light scattering, zeta
potential and transmission electron microscopy.
Results: RGD-PMMA-PTX size distribution was 17.58 ± 7.45 nm with a zeta potential of -38.73 ± 5.62 mV.
According to the boxLucas Model, PTX was incorporated into nanoparticles with an entrapment efficiency of
100% (evaluated by HPLC analysis). In vitro sustained release was determined, with the maximum release of
55% and 40% after 21 days at pH 5.3 and 7.4, respectively. The highest inhibition on cell proliferation was found
with RGD-PMMA-PTX nanoparticles (90 %).
Conclusion: The obtained results showed that RGD-PMMA-PTX represents an attractive and suitable therapeutic
approach for targeting overexpressed integrins in the cancer cells.