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Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery

Despite a considerable number of new antibiotics under going clinical trials, treatment of intracellular pathogens still represents a major pharmaceutical challenge. The use of lipid nanocarriers provides several advantages such as protection from compound degradation, increased bioavailability, and...

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Autores principales: Hädrich, Gabriela, Vaz, Gustavo Richter, Bidone, Juliana, Yurgel, Virginia Campello, Teixeira, Helder Ferreira, Gonçalves Dal Bó, Alexandre, da Silva Pinto, Luciano, Hort, Mariana Appel, Ramos, Daniela Fernandes, Junior, Antonio Sergio Varela, Almeida da Silva, Pedro Eduardo, Dora, Cristiana Lima
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9611000/
https://www.ncbi.nlm.nih.gov/pubmed/36297456
http://dx.doi.org/10.3390/pharmaceutics14102022
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author Hädrich, Gabriela
Vaz, Gustavo Richter
Bidone, Juliana
Yurgel, Virginia Campello
Teixeira, Helder Ferreira
Gonçalves Dal Bó, Alexandre
da Silva Pinto, Luciano
Hort, Mariana Appel
Ramos, Daniela Fernandes
Junior, Antonio Sergio Varela
Almeida da Silva, Pedro Eduardo
Dora, Cristiana Lima
author_facet Hädrich, Gabriela
Vaz, Gustavo Richter
Bidone, Juliana
Yurgel, Virginia Campello
Teixeira, Helder Ferreira
Gonçalves Dal Bó, Alexandre
da Silva Pinto, Luciano
Hort, Mariana Appel
Ramos, Daniela Fernandes
Junior, Antonio Sergio Varela
Almeida da Silva, Pedro Eduardo
Dora, Cristiana Lima
author_sort Hädrich, Gabriela
collection PubMed
description Despite a considerable number of new antibiotics under going clinical trials, treatment of intracellular pathogens still represents a major pharmaceutical challenge. The use of lipid nanocarriers provides several advantages such as protection from compound degradation, increased bioavailability, and controlled and targeted drug release. Wheat germ agglutinin (WGA) is known to have its receptors on the alveolar epithelium and increase phagocytosis. The present study aimed to produce nanostructured lipid carriers with novel glycosylated amphiphilic employed to attach WGA on the surface of the nanocarriers to improve intracellular drug delivery. High-pressure homogenization was employed to prepare the lipid nanocarriers. In vitro, high-content analysis and flow cytometry assay was employed to study the increased uptake by macrophages when the nanocarriers were grafted with WGA. A lipid nanocarrier with surface-functionalized WGA protein (~200 nm, PDI > 0.3) was successfully produced and characterized. The system was loaded with a lipophilic model compound (quercetin; QU), demonstrating the ability to encapsulate a high amount of compound and release it in a controlled manner. The nanocarrier surface functionalization with the WGA protein increased the phagocytosis by macrophages. The system proposed here has characteristics to be further explored to treat intracellular pathogens.
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spelling pubmed-96110002022-10-28 Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery Hädrich, Gabriela Vaz, Gustavo Richter Bidone, Juliana Yurgel, Virginia Campello Teixeira, Helder Ferreira Gonçalves Dal Bó, Alexandre da Silva Pinto, Luciano Hort, Mariana Appel Ramos, Daniela Fernandes Junior, Antonio Sergio Varela Almeida da Silva, Pedro Eduardo Dora, Cristiana Lima Pharmaceutics Article Despite a considerable number of new antibiotics under going clinical trials, treatment of intracellular pathogens still represents a major pharmaceutical challenge. The use of lipid nanocarriers provides several advantages such as protection from compound degradation, increased bioavailability, and controlled and targeted drug release. Wheat germ agglutinin (WGA) is known to have its receptors on the alveolar epithelium and increase phagocytosis. The present study aimed to produce nanostructured lipid carriers with novel glycosylated amphiphilic employed to attach WGA on the surface of the nanocarriers to improve intracellular drug delivery. High-pressure homogenization was employed to prepare the lipid nanocarriers. In vitro, high-content analysis and flow cytometry assay was employed to study the increased uptake by macrophages when the nanocarriers were grafted with WGA. A lipid nanocarrier with surface-functionalized WGA protein (~200 nm, PDI > 0.3) was successfully produced and characterized. The system was loaded with a lipophilic model compound (quercetin; QU), demonstrating the ability to encapsulate a high amount of compound and release it in a controlled manner. The nanocarrier surface functionalization with the WGA protein increased the phagocytosis by macrophages. The system proposed here has characteristics to be further explored to treat intracellular pathogens. MDPI 2022-09-23 /pmc/articles/PMC9611000/ /pubmed/36297456 http://dx.doi.org/10.3390/pharmaceutics14102022 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Hädrich, Gabriela
Vaz, Gustavo Richter
Bidone, Juliana
Yurgel, Virginia Campello
Teixeira, Helder Ferreira
Gonçalves Dal Bó, Alexandre
da Silva Pinto, Luciano
Hort, Mariana Appel
Ramos, Daniela Fernandes
Junior, Antonio Sergio Varela
Almeida da Silva, Pedro Eduardo
Dora, Cristiana Lima
Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title_full Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title_fullStr Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title_full_unstemmed Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title_short Development of a Novel Lipid-Based Nanosystem Functionalized with WGA for Enhanced Intracellular Drug Delivery
title_sort development of a novel lipid-based nanosystem functionalized with wga for enhanced intracellular drug delivery
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9611000/
https://www.ncbi.nlm.nih.gov/pubmed/36297456
http://dx.doi.org/10.3390/pharmaceutics14102022
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