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Multi-small molecule conjugations as new targeted delivery carriers for tumor therapy
| Content Provider | Scilit |
|---|---|
| Author | Shan, Lingling Liu, Ming Wu, Chao Zhao, Liang Li, Siwen Xu, Lisheng Cao, Wengen Gao, Guizhen Gu, Yueqing |
| Copyright Year | 2015 |
| Description | Multi-small molecule conjugations as new targeted delivery carriers for tumor therapy Lingling Shan,1 Ming Liu,2 Chao Wu,1 Liang Zhao,1 Siwen Li,3 Lisheng Xu,1 Wengen Cao,1 Guizhen Gao,1 Yueqing Gu3 1Institute of Pharmaceutical Biotechnology, School of Biology and Food Engineering, Suzhou University, Suzhou, People's Republic of China; 2Department of Biology, University of South Dakota, Vermillion, SD, USA; 3Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing, People's Republic of China In response to the challenges of cancer chemotherapeutics, including poor physicochemical properties, low tumor targeting ability, and harmful side effects, we developed a new tumor-targeted multi-small molecule drug delivery platform. Using paclitaxel (PTX) as a model therapeutic, we prepared two prodrugs, ie, folic acid-fluorescein-5(6)-isothiocyanate-arginine-paclitaxel (FA-FITC-Arg-PTX) and folic acid-5-aminofluorescein-glutamic-paclitaxel (FA-5AF-Glu-PTX), composed of folic acid (FA, target), amino acids (Arg or Glu, linker), and fluorescent dye (fluorescein in vitro or near-infrared fluorescent dye in vivo) in order to better understand the mechanism of PTX prodrug targeting. In vitro and acute toxicity studies demonstrated the low toxicity of the prodrug formulations compared with the free drug. In vitro and in vivo studies indicated that folate receptor-mediated uptake of PTX-conjugated multi-small molecule carriers induced high antitumor activity. Notably, compared with free PTX and with PTX-loaded macromolecular carriers from our previous study, this multi-small molecule-conjugated strategy improved the water solubility, loading rate, targeting ability, antitumor activity, and toxicity profile of PTX. These results support the use of multi-small molecules as tumor-targeting drug delivery systems. Keywords: multi-small molecules, paclitaxel, prodrugs, targeting, tumor therapy |
| Related Links | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4562733/pdf https://www.dovepress.com/getfile.php?fileID=26829 |
| Ending Page | 5591 |
| Page Count | 21 |
| Starting Page | 5571 |
| e-ISSN | 11782013 |
| DOI | 10.2147/ijn.s85402 |
| Journal | International Journal of Nanomedicine |
| Volume Number | 10 |
| Language | English |
| Publisher | Informa UK Limited |
| Publisher Date | 2015-09-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: International Journal of Nanomedicine Biomaterials Multi-small Molecules Paclitaxel Prodrugs Targeting Tumor Therapy |
| Content Type | Text |
| Resource Type | Article |
