Synthesis of folate- pegylated polyester nanoparticles encapsulating ixabepilone for targeting folate receptor overexpressing breast cancer cells

P. Siafaka, M. Betsiou, A. Tsolou, E. Angelou, B. Agianian, M. Koffa, S. Chaitidou, E. Karavas, K. Avgoustakis, D. Bikiaris

Research output: Contribution to journalArticlepeer-review

45 Scopus citations

Abstract

Abstract: The aim of this study was the preparation of novel polyester nanoparticles based on folic acid (FA)–functionalized poly(ethylene glycol)–poly(propylene succinate) (PEG–PPSu) copolymer and loaded with the new anticancer drug ixabepilone (IXA). These nanoparticles may serve as a more selective (targeted) treatment of breast cancer tumors overexpressing the folate receptor. The synthesized materials were characterized by 1H-NMR, FTIR, XRD and DSC. The nanoparticles were prepared by a double emulsification and solvent evaporation method and characterized with regard to their morphology by scanning electron microscopy, drug loading with HPLC–UV and size by dynamic light scattering. An average size of 195 nm and satisfactory drug loading efficiency (3.5 %) were observed. XRD data indicated that IXA was incorporated into nanoparticles in amorphous form. The nanoparticles exhibited sustained drug release properties in vitro. Based on in vitro cytotoxicity studies, the blank FA–PEG–PPSu nanoparticles were found to be non-toxic to the cells. Fluorescent nanoparticles were prepared by conjugating Rhodanine B to PEG–PPSu, and live cell, fluorescence, confocal microscopy was applied in order to demonstrate the ability of FA–PEG–PPSu nanoparticles to enter into human breast cancer cells expressing the folate receptor. Graphical Abstract: [Figure not available: see fulltext.]

Original languageEnglish (US)
Article number275
Pages (from-to)1-14
Number of pages14
JournalJournal of Materials Science: Materials in Medicine
Volume26
Issue number12
DOIs
StatePublished - Dec 1 2015
Externally publishedYes

ASJC Scopus subject areas

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Biomedical Engineering

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