Tumor-homing peptide iRGD-conjugate enhances tumor accumulation of camptothecin for colon cancer therapy
- Authors
- Singh, Tejinder; Kim, Tae Wan; Murthy, Akula S. N.; Paul, Mohuya; Sepay, Nasim; Kong, Hye Jeong; Ryu, Jae Sung; Koo, Na Rim; Yoon, Sujeong; Song, Keon-Hyoung; Baek, Moo Jun; Jeon, Seob; Im, Jungkyun
- Issue Date
- Feb-2024
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Tumor -homing and tumor-penetrating peptide; iRGD; Drug delivery; Camptothecin; Colon cancer
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.265
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 265
- URI
- https://scholarworks.bwise.kr/sch/handle/2021.sw.sch/25951
- DOI
- 10.1016/j.ejmech.2023.116050
- ISSN
- 0223-5234
1768-3254
- 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.
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- Appears in
Collections - College of Medical Sciences > Department of Pharmaceutical Engineering > 1. Journal Articles
- College of Medicine > Department of General Surgery > 1. Journal Articles
- College of Medicine > Department of Obstetrics and Gynecology > 1. Journal Articles
- College of Engineering > Department of Chemical Engineering > 1. Journal Articles
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