Drug nanocarriers for cancer chemotherapy based on microemulsions: The case of Vemurafenib analog PLX4720

Ioanna Theochari, Maria Goulielmaki, Dganit Danino, Vassiliki Papadimitriou*, Alexandros Pintzas, Aristotelis Xenakis

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

26 Scopus citations

Abstract

Oil-in-water (O/W) microemulsions based on Tween 80 as the emulsifier and triacetin as the dispersed oil phase were formulated to be used as delivery vehicles of Vemurafenib analog PLX4720. PLX4720 is a lipophilic antitumor drug against various cancer types correlated with the BRAFV600E mutation. The limits of the single-phase region corresponding to O/W microemulsions as described by ternary phase diagrams were examined. Droplet size measurements determined by dynamic light scattering (DLS) showed mean droplet diameters equal to 10 ± 0.1 nm both in the presence and in absence of the drug. Cryogenic-transmission electron microscopy (Cryo-TEM) images of the microemulsions showed the existence of small structures with uniform size distribution having also average diameters of approximately 10 nm. Electron paramagnetic resonance (EPR) spectroscopy applying the spin probing technique confirmed PLX4720 location in the oil cores excluding its participation in the surfactants monolayer. Furthermore, cell viability assays on colon cancer cell lines Colo-205 and HT29 showed that microemulsions did not exhibit any cytotoxicity when added in ratios between 0.005% v/v and 0.2% v/v. When the cells were treated with encapsulated PLX4720 at two different concentrations (0.063 and 0.12 μΜ) the same response as when dissolved in classic DMSO was observed.

Original languageEnglish
Pages (from-to)350-356
Number of pages7
JournalColloids and Surfaces B: Biointerfaces
Volume154
DOIs
StatePublished - 1 Jun 2017
Externally publishedYes

Keywords

  • Cell viability
  • Chemotherapy
  • Drug delivery
  • EPR
  • Microemulsions
  • PLX4720

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