Promising self‑emulsifying drug delivery system loaded with lycopene from red guava (Psidium guajava L.) : in vivo toxicity, biodistribution and cytotoxicity on DU‑145 prostate cancer cells

• Autor(a) principal: Vasconcelos, Andreanne Gomes
• Data de Publicação: 2021
• Outros Autores: Barros, Ana Luisa A. N., Cabral, Wanessa Felix, Moreira, Daniel Carneiro, Silva, Ingrid Gracielle M. da, Carvalho, Amandda Évelin Silva de, Almeida, Miguel P. de, Albuquerque, Lucas Fraga Friaça, Santos, Raimunda C. dos, Brito, Ana Karolinne S., Araújo, Felipe Saldanha de, Arcanjo, Daniel Dias Rufino, Martins, Maria do Carmo Carvalho e, Borges, Tatiana Karla dos Santos, Báo, Sônia Nair, Plácido, Alexandra, Eaton, Peter, Kuckelhaus, Selma Aparecida Souza, Leite, José Roberto de Souza de Almeida
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UnB
• Texto Completo: http://repositorio2.unb.br/jspui/handle/10482/48314; https://doi.org/10.1186/s12645-021-00103-w; https://orcid.org/0000-0002-1096-3236
• topic: Nanomedicina; Goiaba; Carotenóides; Atividade antitumoral

Background: Self-emulsifying drug delivery systems (SEDDSs) have attracted atten‑ tion because of their efects on solubility and bioavailability of lipophilic compounds. Herein, a SEDDS loaded with lycopene purifed from red guava (nanoLPG) was pro‑ duced. The nanoemulsion was characterized using dynamic light scattering (DLS), zeta potential measurement, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FTIR), lycopene content quantifcation, radical scavenging activity and colloidal stability in cell culture medium. Then, in vivo toxicity and tissue distribution in orally treated mice and cytotoxicity on human prostate carcinoma cells (DU-145) and human peripheral blood mononuclear cells (PBMC) were evaluated. Results: NanoLPG exhibited physicochemical properties with a size around 200 nm, negative zeta-potential, and spherical morphology. The size, polydispersity index, and zeta potential parameters sufered insignifcant alterations during the 12 month storage at 5 °C, which were associated with lycopene stability at 5 °C for 10 months. The nanoemulsion showed partial aggregation in cell culture medium at 37 °C after 24 h. NanoLPG at 0.10 mg/mL exhibited radical scavenging activity equivalent to 0.043±0.002 mg Trolox/mL. The in vivo studies did not reveal any signifcant changes in clinical, behavioral, hematological, biochemical, and histopathological parameters in mice orally treated with nanoLPG at 10 mg/kg for 28 days. In addition, nanoLPG successfully delivered lycopene to the liver, kidney and prostate in mice, improved its cytotoxicity against DU-145 prostate cancer cells—probably by pathway independent on classical necrosis and apoptosis—and did not afect PBMC viability.