화학공학소재연구정보센터
홈 로그인 로그아웃 연락처 사이트맵
Journal of Industrial and Engineering Chemistry, Vol.99, 204-213, July, 2021
DOI10.1016/j.jiec.2021.04.023  Export Citation
Cyclic RGDfK- and Sulfo-Cy5.5-functionalized mPEG-PCL theranostic nanosystems for hepatocellular carcinoma
Jee Yoon Park1, 2, Su Jung You2, Kyeongsoon Park3, Yeong Jun Song3, Ji Sun Park3, Dae Hyeok Yang2, Jae Kwang Kim4, Heung Jae Chun1, 2, †, and Gilson Khang5
  • 1Department of Biomedicine & Health Sciences, The Catholic University of Korea, Seoul 06591, Republic of Korea
  • 2Institute of Cell and Tissue Engineering, The Catholic University of Korea, Seoul 06591, Republic of Korea
  • 3Department of Systems Biotechnology, Chung-Ang University, Anseong-si, Gyeonggi-do 1546, Republic of Korea
  • 4Department of Internal Medicine, Bucheon St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, Bucheon-si, Gyeonggi-do 14647, Republic of Korea
  • 5Department of BIN Convergence Technology, Department of Polymer Nano Science & Technology, Jeonbuk National University, Jeonju 54896, Republic of Korea
E-mail:
Sorafenib (SF) is a standard, clinically-recognized therapy for treating hepatocellular carcinoma (HCC) patients. However, as a multikinase inhibitor, SF causes a systemic side effect. Therefore, there is an urgent need to selectively deliver the optimum dose of SF to the tumor site. The present study aimed to selectively target SF to HCC using a biocompatible drug carrier to increase the therapeutic efficacy, in turn, minimize the adverse effects. To this end, methoxy polyethylene glycol-polycaprolactone (mPEGPCL) di-block copolymer was selected as an amphiphilic carrier for SF that hydrophobic PCL core can encapsulate SF through self-assembly. Cyclic RGDfK (cRGD) was conjugated to the end of PEG-PCL (cRGD- PEG-PCL) for HCC targeting. Sulfo-Cyanine5.5 (S-Cy5.5) was also incorporated to PEG-PCL (S-Cy5.5-PEGPCL) for near-infrared fluorescence (NIRF) imaging. The composition, morphology and size distribution of nanoparticles (NPs) were characterized by 1H NMR, transmission electron microscopy (TEM) and dynamic light scattering (DLS), respectively. In addition, the ability of the integrin-mediated targeting of NPs for the selective delivery of SF was systemically investigated with Hep3B cell line and a nude mouse xenograft model. Consequently, it was found that S-Cy5.5-cRGD-PEG-PCL leads to the selective accumulation of SF into the tumor site and improve anticancer activity against HCC.
Keywords:Drug delivery systems;PEG-PCL nanoparticle;Active targeting;Sorafenib;Cyclic arginine.glycine.aspartic acid;peptide
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