2. Academic Validation
  3. Tumor-homing peptide iRGD-conjugate enhances tumor accumulation of camptothecin for colon cancer therapy

Tumor-homing peptide iRGD-conjugate enhances tumor accumulation of camptothecin for colon cancer therapy

  • Eur J Med Chem. 2023 Dec 16:265:116050. doi: 10.1016/j.ejmech.2023.116050.
Tejinder Singh 1,  Tae Wan Kim 2,  Akula S N Murthy 1,  Mohuya Paul 1,  Nasim Sepay 1,  Hye Jeong Kong 2,  Jae Sung Ryu 2,  Na Rim Koo 1,  Sujeong Yoon 1,  Keon-Hyoung Song 3,  Moo Jun Baek 4,  Seob Jeon 5,  Jungkyun Im 6
Affiliations

Affiliations

  • 1 Department of Electronic Materials, Devices, and Equipment Engineering, Soonchunhyang University, Asan, 31538, Republic of Korea.
  • 2 Department of Medical Life Science, Soonchunhyang University, Asan, 31538, Republic of Korea.
  • 3 Department of Pharmaceutical Engineering, Soonchunhyang University, Asan, 31538, Republic of Korea.
  • 4 Department of Surgery, College of Medicine, Soonchunhyang University Cheonan Hospital, Cheonan, 31151, Republic of Korea.
  • 5 Department of Obstetrics and Gynecology, College of Medicine, Soonchunhyang University Cheonan Hospital, Cheonan, 31151, Republic of Korea. Electronic address: sjeon4595@gmail.com.
  • 6 Department of Electronic Materials, Devices, and Equipment Engineering, Soonchunhyang University, Asan, 31538, Republic of Korea; Department of Chemical Engineering, Soonchunhyang University, Asan, 31538, Republic of Korea. Electronic address: jkim5279@sch.ac.kr.
PMID: 38128233 DOI: 10.1016/j.ejmech.2023.116050
Abstract

Poor intracellular uptake of therapeutics in the tumor parenchyma is a key issue in Cancer therapy. We describe a novel approach to enhance tumor targeting and achieve targeted delivery of camptothecin (CPT) based on a tumor-homing internalizing RGD peptide (iRGD). We synthesized an iRGD-camptothecin conjugate (iRGD-CPT) covalently coupled by a heterobifunctional linker and evaluated its in vitro and in vivo activity in human colon Cancer cells. In vitro studies revealed that iRGD-CPT penetrated cells efficiently and reduced colon Cancer cell viability to a significantly greater extent at micromolar concentrations than did the parent drug. Furthermore, iRGD-CPT showed high distribution toward tumor tissue, effectively suppressed tumor progression, and showed enhanced antitumor effects relative to the parent drug in a mouse model, demonstrating that iRGD-CPT is effective in vivo Cancer treatment. These results suggest that intracellular delivery of CPT via the iRGD peptide is a promising drug delivery strategy that will facilitate the development of CPT derivatives and prodrugs with improved efficacy.

Keywords

Camptothecin; Colon cancer; Drug delivery; Tumor–homing and tumor-penetrating peptide; iRGD.

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Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-161095
    Anticancer agent