Preparation of poly-l-lysine-based nanoparticles with pH-sensitive release of curcumin for targeted imaging and therapy of liver cancer in vitro and in vivo

Drug Delivery

Jae Kwang Kim¹  Kyeongsoon Park²  Dae Hyeok Yang³  Hyun Joo Kim⁴  Heung Jae Chun⁴ 

[1] Department of Internal Medicine, Bucheon St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, Bucheon, Republic of Kore;Department of Systems Biotechnology, Chung-Ang University, Anseong, Republic of Korea;Department of Internal Medicine, Bucheon St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, Bucheon, Republic of Kore;Institute of Cell and Tissue Engineering, College of Medicine, The Catholic University of Korea, Seoul, Republic of Korea;Institute of Cell and Tissue Engineering, College of Medicine, The Catholic University of Korea, Seoul, Republic of Korea;Department of Biomedical Sciences, College of Medicine, The Catholic University of Korea, Seoul, Republic of Korea;

关键词: Poly--lysine nanoparticles;    curcumin;    PEGylation;    cyanine 5.5;    theranosis;   

DOI  :  10.1080/10717544.2018.1461957

来源: publisher

【 摘 要 】

Poly-l-lysine (PLL) nanoparticle (NP) system was prepared for the controlled release of curcumin (CUR) by pH stimuli, and its theranostic efficacy on cancer was compared to that of CUR solution in vitro and in vivo. Deoxycholic acid (DOCA), methoxy polyethylene glycol (MPEG) and cyanine 5.5 (cy5.5) were conjugated to the amine group of PLL through condensation reaction (PLL-DOCA-MPEG-cy5.5), followed by encapsulation of CUR by dialysis method (PLL-DOCA-MPEG-cy5.5/CUR NPs). The composition, morphology and size distribution of PLL-DOCA-MPEG-cy5.5 NPs were characterized by proton nuclear magnetic resonance (1H NMR), transmission electron microscopy (TEM) and dynamic light scattering (DLS), respectively. In vitro tests exhibited that changes in the charge and size of the NPs at low pH led to the improved cellular uptake of CUR into human hepatoma Hep3B cell line by electrostatically absorptive endocytosis. PEGylation with MPEG was turn out to be very effective to have a prolonged blood circulation time, in turn increased the EPR effect. In addition, the incorporation of Cy5.5 into NPs provided successful biodistribution images in vivo and ex vivo. Our findings suggest that PLL-DOCA-MPEG-cy5.5/CUR NPs may have promising applications in cancer theranosis.

【 授权许可】

CC BY