Cancer-targeted Nucleic Acid Delivery and Quantum Dot Imaging Using EGF Receptor Aptamer-conjugated Lipid Nanoparticles

Min Woo Kim, Hwa Yeon Jeong, Seong Jae Kang, Moon Jung Choi, Young Myoung You, Chan Su Im, Tae Sup Lee, In Ho Song, Chang Gun Lee, Ki Jong Rhee, Yeon Kyung Lee, Yong Serk Park

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Abstract

Co-application of fluorescent quantum dot nanocrystals and therapeutics has recently become a promising theranostic methodology for cancer treatment. We developed a tumor-targeted lipid nanocarrier that demonstrates notable efficacy in gene delivery as well as tumor bio-imaging. Coupling of aptamer molecules against the EGF receptor (EGFR) to the distal termini of lipid nanoparticles provided the carrier with tumor-specific recognition capability. The cationic lipid component, referred to as O,O'-dimyristyl-N-lysyl glutamate (DMKE), was able to effectively complex with anionic small-interfering RNA (siRNA). The hydrophobic quantum dots (Q-dots) were effectively incorporated in hydrophobic lipid bilayers at an appropriate Q-dot to lipid ratio. In this study, we optimized the liposomal formula of aptamer-conjugated liposomes containing Q-dots and siRNA molecules (Apt-QLs). The anti-EGFR Apt-QLs exhibited remarkable EGFR-dependent siRNA delivery as well as fluorescence imaging, which were analyzed in cultured cancer cells and tumor xenografts in mice. These results imply that the formulation of Apt-QLs could be widely utilized as a carrier for tumor-directed gene delivery and bio-imaging.

Original languageEnglish
Article number9474
JournalScientific reports
Volume7
Issue number1
DOIs
Publication statusPublished - 2017 Dec 1

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Kim, M. W., Jeong, H. Y., Kang, S. J., Choi, M. J., You, Y. M., Im, C. S., Lee, T. S., Song, I. H., Lee, C. G., Rhee, K. J., Lee, Y. K., & Park, Y. S. (2017). Cancer-targeted Nucleic Acid Delivery and Quantum Dot Imaging Using EGF Receptor Aptamer-conjugated Lipid Nanoparticles. Scientific reports, 7(1), [9474]. https://doi.org/10.1038/s41598-017-09555-w