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Improved Antitumor Outcomes for Colon Cancer Using Nanomicelles Loaded with the Novel Antitumor Agent LA67
| Content Provider | Scilit |
|---|---|
| Author | Cui, Minhu Jin, Mingji Han, Mingfeng Zang, Yingda Li, Chuangjun Zhang, Dongming Huang, Wei Gao, Zhonggao Yin, Xuezhe |
| Copyright Year | 2020 |
| Description | Background: LA67 is a derivative of triptolide that exhibits strong antitumor activity. This derivative has a better safety profile than triptolide, but is limited by poor aqueous solubility. Aim and Methods: To improve solubility and further increase therapeutic efficacy, we prepared LA67-loaded polymeric micelles (LA67-PMs) using a film hydration method. The physicochemical properties of LA67-PMs were investigated, and the antitumor activity of this formulation against Colon26 (C26) cancer cell line was evaluated in vitro and in vivo with LA67 as a control. Results: Polymeric micelles containing LA67 had a particle size of 17.88 nm and a drug entrapment efficiency of 94.84%. This formulation dispersed completely in aqueous solution and exhibited slow, sustained release of LA67. Cellular uptake assay showed that LA67-PMs delivered LA67 to cancer cells with greater efficiency than free LA67, which resulted in increased LA67 accumulation in cancer cells. Cell counting kit 8 (CCK-8) assay showed that blank polymeric micelles (PMs) exhibited low toxicity and LA67-PMs exerted pronounced anti-proliferation effects against C26 cells. Furthermore, LA67-PMs induced apoptosis and repressed migration more effectively than free LA67. In vivo evaluation of antitumor activity showed that LA67-PMs inhibited tumor growth and distant organ metastasis to a greater extent than LA67, which resulted in improved survival rate. The potential mechanisms of these effects may have been induction of apoptosis, inhibition of cell proliferation, and neovascularization. Conclusion: Our study showed that LA67-PMs may be a promising formulation for treatment of colon cancer. |
| Related Links | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7245463/pdf https://www.dovepress.com/getfile.php?fileID=58234 |
| Ending Page | 3576 |
| Page Count | 14 |
| Starting Page | 3563 |
| e-ISSN | 11782013 |
| DOI | 10.2147/ijn.s241577 |
| Journal | International Journal of Nanomedicine |
| Volume Number | 15 |
| Language | English |
| Publisher | Informa UK Limited |
| Publisher Date | 2020-05-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: International Journal of Nanomedicine Oncology Polymeric Micelles Small Size Triptolide Derivatives Tumor Therapy |
| Content Type | Text |
| Resource Type | Article |
