Abstract: Objective To construct MUC1-targeted nanoparticles and evaluate its cytotoxicity in vitro. Methods MUC1 aptamers were conjugated to the surface of nanoparticles which were made of poly (lactic-co-glycolic-acid) (PLGA) nanoparticles and loaded with paclitaxel (PTX). The MUC1-targeted nanoparticles (Apt-NP-PTX) were characterized by UV spectrophotometry and dynamic light scattering. Using MUC1-overexpressing MCF-7 breast cancer cell as experimental group, and HepG2 as control group, the specificity of the Apt-NP-PTX was detected by flow cytometry. The cytotoxicity and IC50 of Apt-NP-PTX against MCF-7 were evaluated using a standard MTS assay. Results The Apt-NP-PTX were about (225.3± 9.2) nm in size with an encapsulation efficiency of 83.6% ± 1.7%. The Apt-NP-PTX enhanced in vitro drug delivery and cellular toxicity to MUC1+ cancer cells, as compared with non-targeted nanoparticles that lack the MUC1 aptamer (P < 0.01) , with IC50 of 1.52 mg/L and 4.10 mg/L, respectively. Conclusion the Apt-NP-PTX can effectively enhance the PTX delivery to MUC1- overexpressing MCF-7 cells in vitro.

Key words: MUC1, Aptamer, Targeted drug delivery, Tumor