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Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol

This work addresses the establishment and characterization of gellan gum:pectin (GG:P) biodegradable mucoadhesive beads intended for the colon-targeted delivery of resveratrol (RES). The impact of the polymer carrier system on the cytotoxicity and permeability of RES was evaluated. Beads of circular...

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Autores principales: Prezotti, Fabíola Garavello, Boni, Fernanda Isadora, Ferreira, Natália Noronha, Silva, Daniella de Souza e, Campana-Filho, Sérgio Paulo, Almeida, Andreia, Vasconcelos, Teófilo, Gremião, Maria Palmira Daflon, Cury, Beatriz Stringhetti Ferreira, Sarmento, Bruno
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6414934/
https://www.ncbi.nlm.nih.gov/pubmed/30966087
http://dx.doi.org/10.3390/polym10010050
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author Prezotti, Fabíola Garavello
Boni, Fernanda Isadora
Ferreira, Natália Noronha
Silva, Daniella de Souza e
Campana-Filho, Sérgio Paulo
Almeida, Andreia
Vasconcelos, Teófilo
Gremião, Maria Palmira Daflon
Cury, Beatriz Stringhetti Ferreira
Sarmento, Bruno
author_facet Prezotti, Fabíola Garavello
Boni, Fernanda Isadora
Ferreira, Natália Noronha
Silva, Daniella de Souza e
Campana-Filho, Sérgio Paulo
Almeida, Andreia
Vasconcelos, Teófilo
Gremião, Maria Palmira Daflon
Cury, Beatriz Stringhetti Ferreira
Sarmento, Bruno
author_sort Prezotti, Fabíola Garavello
collection PubMed
description This work addresses the establishment and characterization of gellan gum:pectin (GG:P) biodegradable mucoadhesive beads intended for the colon-targeted delivery of resveratrol (RES). The impact of the polymer carrier system on the cytotoxicity and permeability of RES was evaluated. Beads of circular shape (circularity index of 0.81) with an average diameter of 914 μm, Span index of 0.29, and RES entrapment efficiency of 76% were developed. In vitro drug release demonstrated that beads were able to reduce release rates in gastric media and control release for up to 48 h at an intestinal pH of 6.8. Weibull’s model correlated better with release data and b parameter (0.79) indicated that the release process was driven by a combination of Fickian diffusion and Case II transport, indicating that both diffusion and swelling/polymer chains relaxation are processes that contribute equally to control drug release rates. Beads and isolated polymers were observed to be safe for Caco-2 and HT29-MTX intestinal cell lines. RES encapsulation into the beads allowed for an expressive reduction of drug permeation in an in vitro triple intestinal model. This feature, associated with low RES release rates in acidic media, can favor targeted drug delivery from the beads in the colon, a promising behavior to improve the local activity of RES.
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spelling pubmed-64149342019-04-02 Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol Prezotti, Fabíola Garavello Boni, Fernanda Isadora Ferreira, Natália Noronha Silva, Daniella de Souza e Campana-Filho, Sérgio Paulo Almeida, Andreia Vasconcelos, Teófilo Gremião, Maria Palmira Daflon Cury, Beatriz Stringhetti Ferreira Sarmento, Bruno Polymers (Basel) Article This work addresses the establishment and characterization of gellan gum:pectin (GG:P) biodegradable mucoadhesive beads intended for the colon-targeted delivery of resveratrol (RES). The impact of the polymer carrier system on the cytotoxicity and permeability of RES was evaluated. Beads of circular shape (circularity index of 0.81) with an average diameter of 914 μm, Span index of 0.29, and RES entrapment efficiency of 76% were developed. In vitro drug release demonstrated that beads were able to reduce release rates in gastric media and control release for up to 48 h at an intestinal pH of 6.8. Weibull’s model correlated better with release data and b parameter (0.79) indicated that the release process was driven by a combination of Fickian diffusion and Case II transport, indicating that both diffusion and swelling/polymer chains relaxation are processes that contribute equally to control drug release rates. Beads and isolated polymers were observed to be safe for Caco-2 and HT29-MTX intestinal cell lines. RES encapsulation into the beads allowed for an expressive reduction of drug permeation in an in vitro triple intestinal model. This feature, associated with low RES release rates in acidic media, can favor targeted drug delivery from the beads in the colon, a promising behavior to improve the local activity of RES. MDPI 2018-01-08 /pmc/articles/PMC6414934/ /pubmed/30966087 http://dx.doi.org/10.3390/polym10010050 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Prezotti, Fabíola Garavello
Boni, Fernanda Isadora
Ferreira, Natália Noronha
Silva, Daniella de Souza e
Campana-Filho, Sérgio Paulo
Almeida, Andreia
Vasconcelos, Teófilo
Gremião, Maria Palmira Daflon
Cury, Beatriz Stringhetti Ferreira
Sarmento, Bruno
Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title_full Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title_fullStr Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title_full_unstemmed Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title_short Gellan Gum/Pectin Beads Are Safe and Efficient for the Targeted Colonic Delivery of Resveratrol
title_sort gellan gum/pectin beads are safe and efficient for the targeted colonic delivery of resveratrol
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6414934/
https://www.ncbi.nlm.nih.gov/pubmed/30966087
http://dx.doi.org/10.3390/polym10010050
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