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Employing targeting ligands with high affinity to tumour receptors is an important strategy to increase treatment efficacy. The use of aptamers as targeting agent is increasingly prevalent in drug delivery systems. Mucin1 (MUC1) is a glycoprotein that is over-expressed on the surface of several cancer cells and plays an important role in metastasis and invasion. 5TR1-aptamer is a DNA aptamer, which targets MUC1 receptors. The present study investigated the anti-tumour activity and therapeutic effectiveness of 5TR1-aptamer-PEGylated liposomal doxorubicin (PLD) delivery system in C26 tumour-bearing mice. The in vitro experiments demonstrated enhanced cytotoxicity and cellular uptake of PLD at the presence of 5TR1 aptamer into MUC1C26 cell line. Biodistribution study indicated that aptamer conjugation increased tumour accumulation of PLDs. Pharmacokinetic analysis showed despite higher clearance rate, selective delivery of doxorubicin to tumour tissue was increased in the 5TR1-Doxil group. In C26-bearing tumour mice, treatment with 5TR1-Doxil exhibited significant deceleration in tumour growth and enhanced survival. The results suggested that 5TR1 aptamer is promising ligand for active targeting which improves therapeutic efficiency of PLD in cancer therapy.

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In this study, we have surface-functionalized PEGylated-nanoliposomal doxorubicin (DOX) with anti-EpCAM (epithelial cell adhesion molecule) aptamer via post-insertion of anti-EpCAM aptamer-conjugated DSPE-mPEG 2000 into Caelyx® (ED-lip). The size, charge, release profile, and cytotoxicity and cellular uptake of formulation were determined. The characterization of the ED-lip demonstrated the slightly increase in size and PDI along with the decrease in zeta potential which indicated that post-insertion efficiently done. The results of flow cytometry and fluorescent microscopy have shown that ED-lip enhanced the rate of cell uptake on C26 cell line compared to Caelyx®. The ED-lip also had more cytotoxic effects than Caelyx® which indicated the efficacy of anti-EpCAM aptamer as targeting ligand. The pharmacokinetic and tissue biodistribution of formulations in mice bearing C26 tumors demonstrated that ED-lip did not affect the distribution profile of DOX compared to Caelyx® in animal model. In addition, ED-lip effectively improved the tumor accumulation of DOX and promoted survival of animals compared to Caelyx®. These results suggest that the functionalization of Caelyx® with anti-EpCAM aptamer is promising in cancer treatment and merits further investigation.

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