| Autor: |
Shih YH; Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan., Peng CL; Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan., Chiang PF; Isotope Application Division, Institute of Nuclear Energy Research, Taoyuan 32546, Taiwan., Shieh MJ; Institute of Biomedical Engineering, College of Medicine and College of Engineering, National Taiwan University, Taipei 100, Taiwan.; Department of Oncology, National Taiwan University Hospital and College of Medicine, Taipei 100, Taiwan. |
| Jazyk: |
angličtina |
| Zdroj: |
Pharmaceutics [Pharmaceutics] 2022 Mar 31; Vol. 14 (4). Date of Electronic Publication: 2022 Mar 31. |
| DOI: |
10.3390/pharmaceutics14040768 |
| Abstrakt: |
The 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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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