Asialoglycoprotein receptors distributing on the surface of hepatic parenchymal cells could
specifically recognize galactose residues. Therefore, galactose residues can be applied in
hepatocellar carcinoma targeted therapy through binding to the asialoglycoprotein receptors. A drug
carrier containing of near infrared (NIR) fluorescence dye (MPA) and galactose was constructed by
covalently conjugation process and named as GAL-MPA. The optical properties, cell viability, cell
affinity and in vivo bio-distribution of this drug carrier were evaluated respectively. The results
demonstrated that the drug carrier was provided with NIR fluorescence after conjugated with MPA.
The low bio-toxicity and high hepatic cells affinity facilitated this drug carrier for in vivo biomedical
application. Finally, the in vivo dynamic distribution of GAL-MPA confirmed this drug carrier was a
promising candidate for tumor-targeting imaging and therapy.
Mucin 1 (MUC1) is a cell surface mucin broadly expressed in mucosal tissues. The aberrant expression of MUC1 under-glycosylated forms has been reported in various carcinomas of the epithelium, such as breast, pancreatic and ovarian cancers. Using the Systematic Evolution of Ligands by Exponential Enrichment (SELEX) methodology, aptamers previously selected against MUC1 glycoprotein with high affinities and specificities. In this study, we developed two targeted near-infrared fluorescent probes for tumor in-vivo diagnostics using a MUC1 aptamer(APT) as targeted ligand and near-infrared fluorescent dye (ICG-Der-02) as labelling. MUC1 aptamer conjugated ICG-Der-02 (APT-ICG-Der-02) displayed a great selectivity to MUC1 positive cell line MCF7 and MCF7 xenograft-bearing nude mice. To improve the high targeting of the probe to the tumor cells, PEG, with high biocompatibility, non immunogenicity and long circulation, was conjugated to the probe .The new probe (APT-PEG-ICG-Der-02) showed better tumour uptake and clearance, and also displayed a great selectivity to MCF7 tumor-bearing nude mice. Data obtained demonstrate a high potential of the targeted near-infrared fluorescent probes in cancer early diagnosis.