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Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting
[Image: see text] The exploitation of curcumin for oral disease treatment is limited by its low solubility, poor bioavailability, and low stability. Surface-functionalized poly-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) have shown promising results to ameliorate selective delivery of drugs t...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2019
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6796886/ https://www.ncbi.nlm.nih.gov/pubmed/31646234 http://dx.doi.org/10.1021/acsomega.9b02086 |
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author | Akl, Mohamed A. Kartal-Hodzic, Alma Suutari, Teemu Oksanen, Timo Montagner, Isabella Monia Rosato, Antonio Ismael, Hatem R. Afouna, Mohsen I. Caliceti, Paolo Yliperttula, Marjo Samy, Ahmed M. Mastrotto, Francesca Salmaso, Stefano Viitala, Tapani |
author_facet | Akl, Mohamed A. Kartal-Hodzic, Alma Suutari, Teemu Oksanen, Timo Montagner, Isabella Monia Rosato, Antonio Ismael, Hatem R. Afouna, Mohsen I. Caliceti, Paolo Yliperttula, Marjo Samy, Ahmed M. Mastrotto, Francesca Salmaso, Stefano Viitala, Tapani |
author_sort | Akl, Mohamed A. |
collection | PubMed |
description | [Image: see text] The exploitation of curcumin for oral disease treatment is limited by its low solubility, poor bioavailability, and low stability. Surface-functionalized poly-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) have shown promising results to ameliorate selective delivery of drugs to the gastro-intestinal tract. In this study, curcumin-loaded PLGA NPs (C-PLGA NPs) of about 200 nm were surface-coated with chitosan (CS) for gastro-intestinal mucosa adhesion, wheat germ agglutinin (WGA) for colon targeting or GE11 peptide for tumor colon targeting. Spectrometric and zeta potential analyses confirmed the successful functionalization of the C-PLGA NPs. Real-time label-free assessment of the cell membrane-NP interactions and NP cell uptake were performed by quartz crystal microbalance coupled with supported lipid bilayers and by surface plasmon resonance coupled with living cells. The study showed that CS-coated C-PLGA NPs interact with cells by the electrostatic mechanism, while both WGA- and GE11-coated C-PLGA NPs interact and are taken up by cells by specific active mechanisms. In vitro cell uptake studies corroborated the real-time label-free assessment by yielding a curcumin cell uptake of 7.3 ± 0.3, 13.5 ± 1.0, 27.3 ± 4.9, and 26.0 ± 1.3 μg per 10(4) HT-29 cells for noncoated, CS-, WGA-, and GE11-coated C-PLGA NPs, respectively. Finally, preliminary in vivo studies showed that the WGA-coated C-PLGA NPs efficiently accumulate in the colon after oral administration to healthy Balb/c mice. In summary, the WGA- and GE11-coated C-PLGA NPs displayed high potential for application as active targeted carriers for anticancer drug delivery to the colon. |
format | Online Article Text |
id | pubmed-6796886 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-67968862019-10-23 Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting Akl, Mohamed A. Kartal-Hodzic, Alma Suutari, Teemu Oksanen, Timo Montagner, Isabella Monia Rosato, Antonio Ismael, Hatem R. Afouna, Mohsen I. Caliceti, Paolo Yliperttula, Marjo Samy, Ahmed M. Mastrotto, Francesca Salmaso, Stefano Viitala, Tapani ACS Omega [Image: see text] The exploitation of curcumin for oral disease treatment is limited by its low solubility, poor bioavailability, and low stability. Surface-functionalized poly-lactic-co-glycolic acid (PLGA) nanoparticles (NPs) have shown promising results to ameliorate selective delivery of drugs to the gastro-intestinal tract. In this study, curcumin-loaded PLGA NPs (C-PLGA NPs) of about 200 nm were surface-coated with chitosan (CS) for gastro-intestinal mucosa adhesion, wheat germ agglutinin (WGA) for colon targeting or GE11 peptide for tumor colon targeting. Spectrometric and zeta potential analyses confirmed the successful functionalization of the C-PLGA NPs. Real-time label-free assessment of the cell membrane-NP interactions and NP cell uptake were performed by quartz crystal microbalance coupled with supported lipid bilayers and by surface plasmon resonance coupled with living cells. The study showed that CS-coated C-PLGA NPs interact with cells by the electrostatic mechanism, while both WGA- and GE11-coated C-PLGA NPs interact and are taken up by cells by specific active mechanisms. In vitro cell uptake studies corroborated the real-time label-free assessment by yielding a curcumin cell uptake of 7.3 ± 0.3, 13.5 ± 1.0, 27.3 ± 4.9, and 26.0 ± 1.3 μg per 10(4) HT-29 cells for noncoated, CS-, WGA-, and GE11-coated C-PLGA NPs, respectively. Finally, preliminary in vivo studies showed that the WGA-coated C-PLGA NPs efficiently accumulate in the colon after oral administration to healthy Balb/c mice. In summary, the WGA- and GE11-coated C-PLGA NPs displayed high potential for application as active targeted carriers for anticancer drug delivery to the colon. American Chemical Society 2019-10-01 /pmc/articles/PMC6796886/ /pubmed/31646234 http://dx.doi.org/10.1021/acsomega.9b02086 Text en Copyright © 2019 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited. |
spellingShingle | Akl, Mohamed A. Kartal-Hodzic, Alma Suutari, Teemu Oksanen, Timo Montagner, Isabella Monia Rosato, Antonio Ismael, Hatem R. Afouna, Mohsen I. Caliceti, Paolo Yliperttula, Marjo Samy, Ahmed M. Mastrotto, Francesca Salmaso, Stefano Viitala, Tapani Real-Time Label-Free Targeting Assessment and in Vitro Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title | Real-Time Label-Free Targeting Assessment and in Vitro
Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title_full | Real-Time Label-Free Targeting Assessment and in Vitro
Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title_fullStr | Real-Time Label-Free Targeting Assessment and in Vitro
Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title_full_unstemmed | Real-Time Label-Free Targeting Assessment and in Vitro
Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title_short | Real-Time Label-Free Targeting Assessment and in Vitro
Characterization of Curcumin-Loaded Poly-lactic-co-glycolic Acid Nanoparticles for Oral Colon Targeting |
title_sort | real-time label-free targeting assessment and in vitro
characterization of curcumin-loaded poly-lactic-co-glycolic acid nanoparticles for oral colon targeting |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6796886/ https://www.ncbi.nlm.nih.gov/pubmed/31646234 http://dx.doi.org/10.1021/acsomega.9b02086 |
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