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http://hdl.handle.net/1843/56505| Type: | Artigo de Periódico |
| Title: | Long-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response |
| Authors: | Eliza Rocha Gomes Rodrigo Maia de Pádua Mônica Cristina de Oliveira Marcus Novais Izabella Thaís Silva André Luís Branco de Barros Elaine Amaral Leite Jennifer Munkert Alessandra Frade Geovanni Dantas Cassali Fernão Castro Braga |
| Abstract: | Cancer is an important public health problem, being one of the leading causes of death worldwide. Most antineoplastic agents cause severe toxic effects and some types of cancer do not respond or are resistant to the existing pharmacotherapy, necessitating the research and development of new therapeutic strategies. CardenolideshaveshownsignificantantitumoractivityduetotheirabilitytoinhibittheNa+K+ATPaseenzyme, and the expression of this enzyme is increased in tumor cells. Glucoevatromonoside containing peracetylated glucose hydroxyl groups (GEVPG) is a cardenolide derivative that has low solubility in aqueous media, which constitutes a barrier to its potential biological applications. In this context, the use of liposomes represents a promising strategy to deliver GEVPG, thus allowing its intravenous administration. In this study, long-circulating and fusogenic liposomes containing GEVPG (SpHL-GEVPG) were developed, and their chemical and physicochemical properties were evaluated. SpHL-GEVPG presented adequate properties, including a mean diameter of182.2 ± 2.7nm,a polydispersity index equalto 0.36 ± 0.03,a zetapotential of–2.37 ± 0.31mV, and a GEVPG entrapment of 0.38 ± 0.04mg/mL. Moreover, this formulation showed a good stability after having been stored for 30 days at 4°C. The cytotoxic studies against breast (MDA-MB-231, MCF-7, and SKBR-3) and lung (A549) cancer cell lines demonstrated that SpHL-GEVPG treatment significantly reduced the cell viability. In addition, the SpHL-GEVPG formulation presented a good selectivity toward these cancer cells. The evaluationofthetherapeuticefficacyofthetreatmentwithSpHL-GEVPGshowedapotentanticancereffectinan A549 human lung cancer xenograft model. SpHL-GEVPG administered at doses of 1.0 and 2.0mg/kg (i.v.) inducedantitumoreffectcomparable topaclitaxelgivenatdoseof10mg/kg(i.v.)tomice.Therefore,theresultsof the present work indicate the potential applicability of SpHL-GEVPG as a new anticancer formulation. |
| Subject: | Câncer de mama Morte - Causas |
| language: | por |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | FAR - DEPARTAMENTO DE PRODUTOS FARMACÊUTICOS |
| Rights: | Acesso Aberto |
| metadata.dc.identifier.doi: | https://doi.org/10.1016/j.biopha.2018.09.109 |
| URI: | http://hdl.handle.net/1843/56505 |
| Issue Date: | 2018 |
| metadata.dc.url.externa: | https://www.sciencedirect.com/science/article/pii/S0753332218343439?via%3Dihub |
| metadata.dc.relation.ispartof: | Biomedicine & Pharmacotherapy |
| Appears in Collections: | Artigo de Periódico |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| Long-circulating and fusogenic liposomes loaded with a glucoevatromonoside derivative induce potent antitumor response.pdf | 2 MB | Adobe PDF | View/Open |
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