Preparation and in vitro targeted antitumor effect of Coicis Semen oil-tripterine microemulsion co-modified with transferrin and folic acid / 中草药

ABSTRACT

Objective: A transferrin and folic acid co-modified Coicis Semen oil-tripterine microemulsion (Tf/FA-CT-MEs) was developed to improve the tumor targeting and thereby enhance the in vitro antitumor efficacy. Methods: FA-PEG 400 was synthesized by classic condensation and together with transferrin as targeting ligands. The structures were characterized by FT-IR and H-NMR. Tf/FA-CT-MEs were prepared by aqueous titration method using Coicis Semen oil as oil phase, followed by anchoring Tf on the surface of prepared particles mentioned-above in aqueous environment. The physiochemical properties and morphology were detected by dynamic light scattering (DLS) and transmission electron microscopy (TEM), respectively. The A549 and MCF-7 cellular uptake of various microemulsions was detected through employing fluorescein isothiocyanate (FITC) as a fluorescence probe. The in vitro antitumor efficacy of the microemulsions against A549 and MCF-7 cells were determined by MTT assay and cell apoptosis kit. Results: FA-PEG 400 was synthesized and characterized as a target ligand. The Tf/FA-CT-MEs with spherical shape had a small droplet size (52.52 ± 0.11) nm, narrow polydispersion index (PDI, 0.124 ± 0.019), and negative Zeta potential (-21.50 ± 1.70) mV, respectively, with good in vitro stability. In in vitro antitumor efficacy, the half proliferation inhibitory concentration (IC50) of Tf/FA-CT-MEs was 0.77 μmol/L on MCF-7 cell model and 0.85 μmol/L on A549 cell model. The cellular uptake results suggested that the fluorescence intensity of MCF-7 and A549 cells was 2782.33 ± 131.77 and 2762.91 ± 23.18 for 4 h, respectively. Besides, (70.60 ± 6.92)% of MCF-7 cells were induced to apoptosis by Tf/FA-CT-MEs. Conclusion: Tf/FA-CT-MEs could improve in vitro targeting and cytotoxicity toward MCF-7 cells. This study suggests that the modification with dul-targeted ligands could be a promising strategy for developing tumor-specific nanomedicines.