title: Bioflavonoid Fisetin Loaded α-Tocopherol-Poly(lactic acid)-Based Polymeric Micelles for Enhanced Anticancer Efficacy in Breast Cancers.
abstract: In this study, tocopherol based polymeric micelles were successfully prepared to enhance the anticancer effect of fisetin (FIS) in breast cancer cells.
  
  
  
  The drug-loaded carrier was characterized in terms of physicochemical and in vivo parameters.
  
  
  
  Compared to FIS, FIS-TPN showed higher cellular uptake in MCF-7 breast cancer cells as revealed by CLSM and flow cytometry. The cytotoxicity assay results clearly showed that the free FIS and FIS-TPN exhibited a typical dose-dependent toxic effect in MCF-7 breast cancer cells. Especially, enhanced cytotoxic effect of FIS was observed when loaded in a nanocarrier. Free FIS induced a ~11% apoptosis whereas FIS-TPN induced a significantly greater apoptosis of ~20% by the end of 24 h. At 48 h, similar trend continued and free FIS showed ~30% of apoptosis whereas ~42% cell apoptosis was observed in FIS-TPN treated group. Notably, migration of cancer cell was significantly inhibited when treated with FIS-TPN formulations. The FIS-TPN significantly reduced to tumor burden and H&E staining showed the lowest tumor volume and higher cell apoptosis.
  
  
  
  All the findings suggest that the fisetin-loaded TPGS-PLA polymeric micelles serve as a potential candidate and promising alternative for the effective treatment of breast cancers.
authors.affiliation: Department of General Surgery, The First Affiliated Hospital of Xinxiang Medical University, 453100, Xinxiang, People's Republic of China.
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.affiliation: Department of General Surgery, The First Affiliated Hospital of Xinxiang Medical University, 453100, Xinxiang, People's Republic of China.
authors.forename: De-Zhong
authors.initials: DZ
authors.lastname: Zhang
authors.affiliation: Department of Pathophysiology, Xinxiang Medical University, No. 602, Jinsui Avenue, Xinxiang, 453003, People's Republic of China. wangyx75@outlook.com.
authors.forename: Yu-Xia
authors.initials: YX
authors.lastname: Wang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D005260:Female; D005419:Flavonoids / Q000737:chemistry* / Q000494:pharmacology; D044948:Flavonols; D006801:Humans; D061986:MCF-7 Cells; D051379:Mice; D008823:Micelles; D011091:Polyesters / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry* / Q000494:pharmacology; D024502:alpha-Tocopherol / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D005419:Flavonoids; D044948:Flavonols; D008823:Micelles; D011091:Polyesters; D011108:Polymers; C033616:poly(lactide); D024502:alpha-Tocopherol; C017875:fisetin
keywords: anticancer; breast cancer; fisetin; polymeric micelles