Journal
COLLOIDS AND SURFACES B-BIOINTERFACES
Volume 159, Issue -, Pages 571-579Publisher
ELSEVIER
DOI: 10.1016/j.colsurfb.2017.08.014
Keywords
Transferrin; Doxorubicin; Fattigation-platform; Apo-transferrin-stearic acid conjugate; Self-assembled nanoparticles; Physicochemical characterization; Receptor-oriented cancer targeting
Funding
- Ministry of Food and Drug Safety, Republic of Korea [16173MFDS542]
- Ministry of Food & Drug Safety (MFDS), Republic of Korea [DY0002256287-16173기반연542-2] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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A major hurdle in cancer treatment is the precise targeting of drugs to the cancer site. As many cancer cells overexpress the transferrin receptor (TfR), the transferrin (Tf)-TfR interaction is widely exploited to target cancer cells. In this study, novel amphiphilic apo-Tf stearic acid (TfS) conjugates were prepared and characterized by Fourier transform infrared (FTIR) spectroscopy, matrix-assisted laser desorption/ionization-time of flight (MALDI-TOF) mass spectrometry, and trinitrobenzenesulfonic acid (TNBS) assay. The prepared TfS conjugates were readily self-assembled in water to form nanoparticles (NPs), consisting of TfS as a core of NPs, whose sizes and zeta potentials were determined by scanning electron microscopy (SEM), transmission electron microscopy (TEM), and a particle size analyzer. Hydrophilic water-soluble doxorubicin (DOX) was chosen as a model drug. DOX-loaded TfS NPs (NP + DOX), prepared by the adsorption of DOX on the NP surface via the incubation method, were analyzed for their cell targeting and killing efficiencies in TfR-overexpressing A549 and HCT116 cell lines by MTT assay, confocal microscopy, and fluorescence assisted cell sorting (flow cytometry). The data showed that NP + DOX exhibited improved cancer cell targeting and killing properties compared to that reported for free DOX. Further, the cytotoxic efficiency of NP + DOX was comparable to that of PEGylated liposomal product, Doxil, while its cellular uptake was higher than that of Doxil. Thus, this novel receptor-based TfS NP drug delivery system has great potential to target TfR-overexpressing cancer cells without off-target effects. (C) 2017 Elsevier B.V. All rights reserved.
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