A conjugation of stearic acid to apotransferrin, fattigation-platform, as a core to form self-assembled nanoparticles: Encapsulation of a hydrophobic paclitaxel and receptor-driven cancer targeting

Abstract

In this study, apotransferrin (Tf)-stearic acid conjugate was newly synthesized via "fattigation method" to form self-assembled nanoparticles (NPs) containing a hydrophobic model drug, paclitaxel (PAC). Then, physicochemical properties and cellular behaviors such as transferrin receptor-driven targeting and cytotoxic efficiencies were evaluated. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) studies showed that the NPs had spherical shape and smooth surface. The particle size of PAC-loaded NPs was 326.97 +/- 2.03 nm with a loading and encapsulation efficiency of 7.94 +/- 1.60% (w/w) and 71.10 +/- 4.12% (w/w), respectively. In comparison to free PAC, PAC-loaded NPs showed a 7-fold reduction in the LC50 value in breast carcinoma cells (MCF-7), which indicated an increase in cytotoxicity owing to the effective targeting of cells. This observation was confirmed via confocal microscopy images that showed that transferrin receptor blocking inhibited NP uptake. This was further confirmed via flow cytometry data which showed the time-dependent uptake of NPs and their inhibition by transferrin receptor blockage. The results of this study reveal the advantages of NP-based drug delivery systems consisting of Tf as a core of NP for the receptor-driven targeting and subsequent killing of cancer cells. (C) 2017 Elsevier B.V. All rights reserved.