Kwangmeyung Kima, 1, Jong Ho Kimb, 1, Hyungkyu Parka, Yoo-Shin Kimc, Kyeongsoon Parka, b, Heayun Nama, d, Seulki Leea, Jae Hyung Parkd, Rang-Woon Parkc, In-San Kimc, Kuiwon Choia, Sang Yoon Kime, Kinam Parkb, Ick Chan Kwona
a Biomedical Research Center, Korea Institute of Science and Technology, 39-1 Haweolgog-Dong, Sungbook-Gu, Seoul 136-791, South Korea
b Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West Lafayette, IN 47907, United States
c Advanced Medical Technology Cluster for Diagnosis and Prediction, Kyungpook National University, Daegu 700-422, South Korea
d Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Dongdaemun-gu, Seoul 130-701, South Korea
e Department of Otolaryngology, Asan Medical Center, College of Medicine, University of Ulsan, 388-1 Pungnap-dong, Songpa-gu, Seoul 138-736, South Korea
Corresponding authors. Kwon is to be contacted at Biomedical Research Center, Korea Institute of Science and Technology, 39-1 Haweolgog-Dong, Sungbook-Gu, Seoul 136-791, South Korea. Park, Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West Lafayette, IN 47907, United States.
1 These authors contributed equally to this paper
Theragnostic multifunctional nanoparticles hold great promise in simultaneous diagnosis of disease, targeted drug delivery with minimal toxicity, and monitoring of treatment. One of the current challenges in cancer treatment is enhancing the tumor-specific targeting of both imaging probes and anticancer agents. Herein, we report tumor-homing chitosan-based nanoparticles (CNPs) that simultaneously execute cancer diagnosis and therapy (cancer theragnosis). These CNPs are unique for their three distinctive characteristics, such as stability in serum, deformability, and rapid uptake by tumor cells. These properties are critical in increasing their tumor targeting specificity and reducing their nonspecific uptake by normal tissues. To develop these CNPs into novel theragnostic nanoparticles, we labeled them with Cy5.5, a near-infrared fluorescent (NIRF) dye, for imaging and also loaded them with paclitaxel (PTX-CNPs), an anticancer drug, for cancer treatment. Cy5.5 labeled PTX-CNPs exhibited significantly increased tumor-homing ability with low nonspecific uptake by other tissues in SCC7 tumor-bearing mice. Theragnostic nanoparticles, Cy5.5 labeled PTX-CNPs, are highly useful for simultaneous diagnosis of early-stage cancer and drug delivery.