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Synthetic peptide-labelled micelles for active targeting of cells overexpressing EGF receptors

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Abstract

The goal of nanomedicine is to transport drugs to pathological tissues, reducing side effects while increasing targeting and efficacy. Aggregates grafted by bioactive molecules act as the active targeting agents. Among bioactive molecules, peptides, which are able to recognize overexpressed receptors on cancer cell membranes, appear to be very promising. The aim of this study was to formulate analog peptide-labeled micelles enabled to potentially deliver highly hydrophobic drugs to cancer cells overexpressing epidermal growth factor (EGF) receptor (EGFR). The selected synthetic peptide sequences were anchored to a hydrophobic moiety, aiming to obtain amphiphilic peptide molecules. Mixed micelles were formulated with Pluronic® F127. These micelles were fully characterized by physico-chemical methods, estimating the critical micellar concentration (CMC) by fluorescence. Their sizes were established by dynamic light scattering (DLS) analysis. Then, micelles were also tested in vitro for their binding capacity to human hepatocellular carcinoma (HCC) cell lines overexpressing EGFR.

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Acknowledgements

This work was funded by the MERIT Project of the Italian Ministero dell’Istruzione, dell’Università e della Ricerca (Ministry for Education, Universities and Research)—MIUR FIRB-MERIT n. RBNE08YYBM to M.C. and D.T. The authors are grateful to Mrs. Antonina Azzolina for the technical support provided.

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Correspondence to Diego Tesauro.

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Tesauro, D., Mastro, R., Cusimano, A. et al. Synthetic peptide-labelled micelles for active targeting of cells overexpressing EGF receptors. Amino Acids 51, 1177–1185 (2019). https://doi.org/10.1007/s00726-019-02755-w

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  • DOI: https://doi.org/10.1007/s00726-019-02755-w

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