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Docetaxel immunonanocarriers as targeted delivery systems for HER2-positive tumor cells: preparation, characterization, and cytotoxicity studies

Authors Noori Koopaei M, Dinarvand R, Amini, Rabbani, Emami S, Ostad SN, Atyabi F

Published 8 September 2011 Volume 2011:6 Pages 1903—1912

DOI https://doi.org/10.2147/IJN.S23211

Review by Single-blind

Peer reviewer comments 3


Mona Noori Koopaei1, Rassoul Dinarvand1,2, Mohsen Amini3, Hojatollah Rabbani4, Shaghayegh Emami4, Seyed Nasser Ostad5, Fatemeh Atyabi1,2
1
Novel Drug Delivery Laboratory, Faculty of Pharmacy, 2Nanotechnology Research Center, 3Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; 4Monoclonal Antibody Research Center, Avesina Research Institute, ACECR, Tehran, Iran; 5Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Science, Tehran, Iran

Background: The objective of this study was to develop pegylated poly lactide-co-glycolide acid (PLGA) immunonanocarriers for targeting delivery of docetaxel to human breast cancer cells.
Methods: The polyethylene glycol (PEG) groups on the surface of the PLGA nanoparticles were functionalized using maleimide groups. Trastuzumab, a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) antigens of cancer cells, used as the targeting moiety, was attached to the maleimide groups on the surface of pegylated PLGA nanoparticles. Nanoparticles prepared by a nanoprecipitation method were characterized for their size, size distribution, surface charge, surface morphology, drug-loading, and in vitro drug release profile.
Results: The average size of the trastuzumab-decorated nanoparticles was 254 ± 16.4 nm and their zeta potential was -11.5 ± 1.4 mV. The average size of the nontargeted PLGA nanoparticles was 183 ± 22 nm and their zeta potential was -2.6 ± 0.34 mV. The cellular uptake of nanoparticles was studied using both HER2-positive (SKBR3 and BT-474) and HER2-negative (Calu-6) cell lines.
Conclusion: The cytotoxicity of the immunonanocarriers against HER2-positive cell lines was significantly higher than that of nontargeted PLGA nanoparticles and free docetaxel.

Keywords: nanoparticles, drug targeting, immunonanocarriers, trastuzumab, docetaxel, PLGA, HER2 receptor

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