[10]-Gingerol-Loaded Nanoemulsion and its Biological Effects on Triple-Negative Breast Cancer Cells

Autor(es)

Zanesco-Fontes, Ideli ; Lopes Silva, Ana Carolina ; da Silva, Patricia Bento ; Duarte, Jonatas Lobato ; Di Filippo, Leonardo Delello ; Chorilli, Marlus ; Cominetti, Marcia Regina ; Baptista Moreno Martin, Ana Carolina

• Tipo de documento: Artigo Científico
• Fonte: AAPS PHARMSCITECH; v. 22, n. 5, p. 8-pg., 2021-05-18.

Resumo

The apoptotic, cytotoxic, and cytostatic activities for [10]-gingerol in triple-negative breast cancer cells (TNBCs) were already reported. However, despite these important antitumor activities, the compound has the disadvantage to have a hydrophobic characteristic, hindering in vivo administration. To surpass this issue, in this study we have created a [10]-gingerol-loaded nanoemulsion (10GNE) in order to increase the stability and solubility of the compound. The nanoemulsion was characterized and tested for its cytotoxic, cytostatic, and apoptotic effects on a panel of murine and human TNBC cell lines, as well as non-tumor cells, and compared with a [10]-gingerol-free nanoemulsion (NE) and with [10]-gingerol itself. Except for the murine 4T1.13 cell line, the IC50 of the free 10G molecule, after 72 h of incubation, was higher in all cell lines tested, both murine and human, demonstrating therefore the efficacy of the 10GNE regarding cytotoxicity. In murine tumor cells, 60 mu M 10GNE was able to arrest cell cycle at sub-G0 phase and induce apoptosis, leading to 48% and 78% of total cell death in 4T1.13 and 4T1Br4 murine tumor cells, respectively. This represents an improvement compared to 10G-free molecule that only induced 74% of total apoptosis at 100 mu M in 4T1Br4 cells. Taken together, our results show that nanoformulation preserved the [10]-gingerol cytotoxic and cytostatic properties and improved its apoptotic function on murine TNBC cell lines. These data open new perspectives to a more suitable drug-delivery approach for [10]-gingerol for TNBC treatment that should be further demonstrated using in vivo assays. (AU)

• Processo FAPESP: 18/17756-4 - Formulação do [10]-gingerol: estudos in vitro em células de câncer de mama triplo negativo
• Beneficiário: Ideli Zanesco Fontes Baptista
• Modalidade de apoio: Bolsas no Brasil - Iniciação Científica
• Processo FAPESP: 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos
• Beneficiário: Glaucius Oliva
• Modalidade de apoio: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs
• Processo FAPESP: 16/23202-6 - Efeitos sensibilizadores e mecanismos de ação do [10]-gingerol em combinação com a doxorrubicina para o tratamento de câncer de mama: estudos in vitro e in vivo
• Beneficiário: Ana Carolina Baptista Moreno Martin
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado