A new combination strategy of an active loading and active targeting approach was applied in this work. The
liposomes actively loaded with
Curcumin (CRM) (LipCRM) were decorated with
cholesterol tagged-anti-
nucleolin AS1411 aptamer (NCL) via a new post-insertion approach, utilizing the
cholesterol as a wedge to incorporate aptamer into the surface of the
liposome bilayer. A successful NCL post-insertion was verified by
agarose gel electrophoresis and dynamic light scattering (DLS). The cellular uptake of AptNCL-Lip was investigated using flow cytometry and Confocal
Laser Scanning Microscopy (CLSM) on two different human
breast cancer cell lines (MCF-7 and MDA-MB-231). The uptake and cytotoxicity of loaded CRM were investigated using flow cytometry and MTT assay. Our results showed successful post insertion of NCL aptamer to the surface of Lip. Also, higher cellular uptake was noted for AptNCL-Alexa-LipRhod compared to blank LipRhod in both cell lines. Moreover, CLSM showed prominent endocytosis and uptake of AptNCL-Alexa-LipRhod into the cytoplasm of
breast cancer cells. Furthermore, the results showed a significant increase in the uptake and cytotoxicity of AptNCL-LipCRM compared to LipCRM in both cell lines. Overall, our results demonstrate a successful post-insertion of
cholesterol-tagged aptamer into
liposomes and the possible combination between active loading and active targeting.