title: Novel self-nanoemulsifying formulation of quercetin: Implications of pro-oxidant activity on the anticancer efficacy.
abstract: The present work focuses on the anticancer potential of quercetin (QT) loaded self-nanoemulsifying drug delivery system (QT-SNEDDS) composed of Capmul MCM, Tween 20 and ethanol. In vitro cell culture studies revealed potential cell cytotoxicity of developed formulation mediated by its ability to induce DNA damage and apoptosis in MCF-7 cells. QT-SNEDDS at a dose of 50mg/kg demonstrated the antioxidant activity measured as function of prophylactic antitumor efficacy against DMBA induced breast tumors which revealed higher latency to the tumor growth as compared to free QT. This appreciation was further supported by normalized levels of tumor angiogenesis markers (MMP-2, MMP-9, TNF-α and IL-6). At higher doses (100mg/kg) the pro-oxidant activity was noted and exhibited significantly higher therapeutic anticancer efficacy (~65% tumor suppression) in the same model as compared to that of free QT (~20%). Finally, safety profile of developed formulation was established assessing various hepatotoxicity markers.
  
  
  BACKGROUND
  This basic science study focuses on the anticancer potential of a specific quercetin loaded self-nanoemulsifying drug delivery system. At higher doses significantly higher therapeutic anticancer efficacy (~65% tumor suppression) was noted in the same model as compared to that of free quercetin (~20%).
authors.affiliation: Department of Pharmaceutics, Centre for Pharmaceutical Nanotechnology, National Institute of Pharmaceutical Education and Research (NIPER), (Mohali) Punjab, India.
authors.forename: Amit K
authors.initials: AK
authors.lastname: Jain
authors.affiliation: Department of Pharmaceutics, Centre for Pharmaceutical Nanotechnology, National Institute of Pharmaceutical Education and Research (NIPER), (Mohali) Punjab, India.
authors.forename: Kaushik
authors.initials: K
authors.lastname: Thanki
authors.affiliation: Department of Pharmaceutics, Centre for Pharmaceutical Nanotechnology, National Institute of Pharmaceutical Education and Research (NIPER), (Mohali) Punjab, India. Electronic address: sanyogjain@niper.ac.in.
authors.forename: Sanyog
authors.initials: S
authors.lastname: Jain
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D004249:DNA Damage / Q000187:drug effects; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D006801:Humans; D015850:Interleukin-6 / Q000378:metabolism; D061986:MCF-7 Cells; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism; D020780:Matrix Metalloproteinase 9 / Q000378:metabolism; D011136:Polysorbates / Q000737:chemistry; D011794:Quercetin / Q000737:chemistry* / Q000494:pharmacology*; D017382:Reactive Oxygen Species / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D015850:Interleukin-6; D011136:Polysorbates; D017382:Reactive Oxygen Species; D014409:Tumor Necrosis Factor-alpha; D011794:Quercetin; D020778:Matrix Metalloproteinase 2; D020780:Matrix Metalloproteinase 9
keywords: Anticancer efficacy; Apoptosis; Prooxidant activity; Prophylactic; Quercetin; SNEDDS