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

Abstract Background Self-emulsifying drug delivery systems (SEDDSs) have attracted attention because of their effects on solubility and bioavailability of lipophilic compounds. Herein, a SEDDS loaded with lycopene purified from red guava (nanoLPG) was produced. The nanoemulsion was characterized usi...

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Autores principales: Andreanne G. Vasconcelos, Ana Luisa A. N. Barros, Wanessa F. Cabral, Daniel C. Moreira, Ingrid Gracielle M. da Silva, Amandda É. Silva-Carvalho, Miguel P. de Almeida, Lucas F. F. Albuquerque, Raimunda C. dos Santos, Ana Karolinne S. Brito, Felipe Saldanha-Araújo, Daniel D. R. Arcanjo, Maria do Carmo C. Martins, Tatiana K. dos S. Borges, Sônia N. Báo, Alexandra Plácido, Peter Eaton, Selma A. S. Kuckelhaus, José Roberto S. A. Leite
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Publicado: BMC 2021
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spelling oai:doaj.org-article:96d0dd8b92374717be7fb9fc336122572021-11-14T12:11:53ZPromising 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 cells10.1186/s12645-021-00103-w1868-69581868-6966https://doaj.org/article/96d0dd8b92374717be7fb9fc336122572021-11-01T00:00:00Zhttps://doi.org/10.1186/s12645-021-00103-whttps://doaj.org/toc/1868-6958https://doaj.org/toc/1868-6966Abstract Background Self-emulsifying drug delivery systems (SEDDSs) have attracted attention because of their effects on solubility and bioavailability of lipophilic compounds. Herein, a SEDDS loaded with lycopene purified from red guava (nanoLPG) was produced. 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 quantification, 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 suffered insignificant 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 significant 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 affect PBMC viability. Conclusions Thus, nanoLPG stands as a promising and biosafe lycopene delivery system for further development of nanotechnology-based health products. Graphical AbstractAndreanne G. VasconcelosAna Luisa A. N. BarrosWanessa F. CabralDaniel C. MoreiraIngrid Gracielle M. da SilvaAmandda É. Silva-CarvalhoMiguel P. de AlmeidaLucas F. F. AlbuquerqueRaimunda C. dos SantosAna Karolinne S. BritoFelipe Saldanha-AraújoDaniel D. R. ArcanjoMaria do Carmo C. MartinsTatiana K. dos S. BorgesSônia N. BáoAlexandra PlácidoPeter EatonSelma A. S. KuckelhausJosé Roberto S. A. LeiteBMCarticleNanomedicineSelf-emulsifyingGuava fruitCarotenoidsAntitumoralNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancer Nanotechnology, Vol 12, Iss 1, Pp 1-29 (2021)
institution DOAJ
collection DOAJ
language EN
topic Nanomedicine
Self-emulsifying
Guava fruit
Carotenoids
Antitumoral
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
spellingShingle Nanomedicine
Self-emulsifying
Guava fruit
Carotenoids
Antitumoral
Neoplasms. Tumors. Oncology. Including cancer and carcinogens
RC254-282
Andreanne G. Vasconcelos
Ana Luisa A. N. Barros
Wanessa F. Cabral
Daniel C. Moreira
Ingrid Gracielle M. da Silva
Amandda É. Silva-Carvalho
Miguel P. de Almeida
Lucas F. F. Albuquerque
Raimunda C. dos Santos
Ana Karolinne S. Brito
Felipe Saldanha-Araújo
Daniel D. R. Arcanjo
Maria do Carmo C. Martins
Tatiana K. dos S. Borges
Sônia N. Báo
Alexandra Plácido
Peter Eaton
Selma A. S. Kuckelhaus
José Roberto S. A. Leite
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
description Abstract Background Self-emulsifying drug delivery systems (SEDDSs) have attracted attention because of their effects on solubility and bioavailability of lipophilic compounds. Herein, a SEDDS loaded with lycopene purified from red guava (nanoLPG) was produced. 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 quantification, 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 suffered insignificant 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 significant 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 affect PBMC viability. Conclusions Thus, nanoLPG stands as a promising and biosafe lycopene delivery system for further development of nanotechnology-based health products. Graphical Abstract
format article
author Andreanne G. Vasconcelos
Ana Luisa A. N. Barros
Wanessa F. Cabral
Daniel C. Moreira
Ingrid Gracielle M. da Silva
Amandda É. Silva-Carvalho
Miguel P. de Almeida
Lucas F. F. Albuquerque
Raimunda C. dos Santos
Ana Karolinne S. Brito
Felipe Saldanha-Araújo
Daniel D. R. Arcanjo
Maria do Carmo C. Martins
Tatiana K. dos S. Borges
Sônia N. Báo
Alexandra Plácido
Peter Eaton
Selma A. S. Kuckelhaus
José Roberto S. A. Leite
author_facet Andreanne G. Vasconcelos
Ana Luisa A. N. Barros
Wanessa F. Cabral
Daniel C. Moreira
Ingrid Gracielle M. da Silva
Amandda É. Silva-Carvalho
Miguel P. de Almeida
Lucas F. F. Albuquerque
Raimunda C. dos Santos
Ana Karolinne S. Brito
Felipe Saldanha-Araújo
Daniel D. R. Arcanjo
Maria do Carmo C. Martins
Tatiana K. dos S. Borges
Sônia N. Báo
Alexandra Plácido
Peter Eaton
Selma A. S. Kuckelhaus
José Roberto S. A. Leite
author_sort Andreanne G. Vasconcelos
title 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
title_short 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
title_full 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
title_fullStr 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
title_full_unstemmed 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
title_sort 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
publisher BMC
publishDate 2021
url https://doaj.org/article/96d0dd8b92374717be7fb9fc33612257
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