Multimeric System of RGD-Grafted PMMA-Nanoparticles as a Targeted Drug- Delivery System for Paclitaxel

Author(s): Brenda Vianey Gibbens-Bandala, Blanca Eli Ocampo-García*, Guillermina Ferro-Flores, Enrique Morales-Avila, Alejandra Ancira-Cortez, Laura Jaimes-Aguirre

Journal Name: Current Pharmaceutical Design

Volume 23 , Issue 23 , 2017

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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.

Keywords: PMMA nanoparticles, drug delivery systems, targeted multimeric-RGD, pH-responsive nanoparticles, entrapment efficiency, transmission electron microscopy.

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Article Details

Year: 2017
Published on: 27 September, 2017
Page: [3415 - 3422]
Pages: 8
DOI: 10.2174/1381612823666170407143525
Price: $65

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