Shih, Ying-HsiaYing-HsiaShihPeng, Cheng-LiangCheng-LiangPengChiang, Ping-FangPing-FangChiangMING-JIUM SHIEH2024-01-102024-01-102022-03-311999-4923https://scholars.lib.ntu.edu.tw/handle/123456789/638357The aim of this research was to evaluate the receptor tyrosine kinase inhibitor Sunitinib combined with SN-38 in polymeric micelles for antitumor efficacy in colorectal cancer. First, SN-38 and Sunitinib co-loaded micelles were developed and characterized. We studied cell viability and cellular uptake in HCT-116 cells. Then, subcutaneous HCT-116 xenograft tumors were used for ex vivo biodistribution, antitumor efficacy, and histochemical analysis studies. Results of cellular uptake and ex vivo biodistribution of SN-38/Sunitinib micelles showed the highest accumulation in tumors compared with other normal organs. In the antitumor effect studies, mice bearing HCT-116 tumors were smallest at day 28 after injection of SN-38/Sunitinib micelles, compared with other experiment groups (p < 0.01). As demonstrated by the results of inhibition on multi-receptors by Sunitinib, we confirmed that SN-38/Sunitinib co-loaded micelles to be a treatment modality that could inhibit VEGF and PDGF receptors and enhance the antitumor effect of SN-38 (p < 0.05). In summary, we consider that this micelle is a potential formulation for the combination of SN-38 and Sunitinib in the treatment of colorectal cancer.enSN-38; colorectal cancer; polymeric micelles; sunitinib[SDGs]SDG3journal article10.3390/pharmaceutics14040768354566022-s2.0-85128330699https://api.elsevier.com/content/abstract/scopus_id/85128330699