pH sensitive functionalized hyperbranched polyester based nanoparticulate system for the receptor-mediated targeted cancer therapy

ABSTRACT

The aim of this study is to develop a novel folic acid conjugated, DL-lysine modified, PEGylated, the 3rd generation hyperbranched polymer (HBP-PEG-Lys-FA) for use in receptor-mediated therapy. 5-fluorouracil, model anti-cancer drug, loaded nanoparticles were found an average size of 177 nm with loading efficiency of 23.18%. In vitro drug release studies demonstrated that nanoparticles showed pH-dependent release. HBP-PEG-Lys-FA were efficiently taken up by HeLa cells and specificity of targeted nanoparticles to folate receptors of cells was proved. It was concluded that the HBP-PEG-Lys-FA nanoparticles can provide an advantage on delivering of the drug efficiently into the cytosol for cancer therapy.

GRAPHICAL ABSTRACT

KEYWORDS:

• 5-fluorouracil
• cancer therapy
• hyperbranched polyester
• pH sensitive nanoparticles
• receptor-mediated targeting
• targeted drug carrier

Acknowledgements

The authors wish to thank Assoc. Prof. Dr. Kamber Demir and DVM Selin Yağcıoğlu from the Department of Reproduction & Artificial Insemination at Istanbul University for their help with fluorescence microscope and flow cytometry studies. We also wish to thank Dr. Hande Tekarslan from the Department of Pharmaceutical Technology at Istanbul University for experimental assistance with regard to cell culture studies.

Additional information

Funding

This work was supported by a grant of the Scientific Research Projects Coordination Unit of Istanbul University, project number 15349.