Preparation, characterization and in vitro-targeted delivery of novel Apolipoprotein E-based nanoparticles to C6...

Apolipoprotein E (APOE) with its extraordinary features is readily assembled with hydrophobic compounds via its compact hydrophobic units (CHUs). These assemblies can then be converted to stable particles by protein-protein interactions via coiled coil regions (CCRs) which exist in APOE structure. Applying these features of APOE, we prepared novel nanoparticles called NAPOE, using no cross-linker. Vitamin D3 - a hydrophobic antitumor model - was loaded within the nanoparticles (NPs). The NPs were mostly spherical with the mean diameter and zeta potential of 94.39 ± 5.71 nm and -20 ± 0.3 mV, respectively. The molar ratio of VD3/APOE in NPs was 37.2 ± 0.61. The NPs targeted C6 glioma cells in vitro via over-expressed LDLRs. The efficiency of the NPs uptake to malignant C6 glioma cells was remarkable compared to non-tumor glial cells (p < 0.05). The releasing rate of hydrophobic cargo from the particles was high (p < 0.05) and reached to maximum, 12 h after targeting C6 cells. The size and drug loading of NPs were found to be controlled by the definite numbers of CCRs and CHUs in APOE. In conclusion, it is suggested that NAPOE NPs can facilitate the controlled delivery of hydrophobic drugs to the malignant C6 glioma cells according to the degree of invasiveness.