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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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) |
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Nanomedicine Self-emulsifying Guava fruit Carotenoids Antitumoral Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 |
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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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