Gustavo Richter Vaz1, Gabriela Hädrich1, Juliana Bidone2, Jamile Lima Rodrigues1, Mariana Corrêa Falkembach1, Jean-Luc Putaux3,4, Mariana Appel Hort1, José Maria Monserrat5, Antônio Sergio Varela Junior6, Helder Ferreira Teixeira2, Ana Luiza Muccillo-Baisch1, Ana Paula Horn7, Cristiana Lima Dora1. 1. Laboratório de Nanotecnologia Aplicada à Saúde, Programa de Pós-Graduação em Ciências da Saúde, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil. 2. Laboratório de Desenvolvimento Galênico, Programa de Pós-graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brazil. 3. Université Grenoble Alpes, Centre de Recherches sur les Macromolécules Végétales, Grenoble, France. 4. CNRS, Centre de Recherches sur les Macromolécules Végétales, Grenoble, France. 5. Instituto de Ciências Biológicas, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil. 6. Laboratório de Reprodução Animal Comparada -Instituto de Ciências Biológicas, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil. 7. Laboratório de Neurociências -Instituto de Ciências Biológicas, Universidade Federal do Rio Grande, Rio Grande, RS, Brazil.
Abstract
BACKGROUND: Curcumin (CUR) has properties that can be useful for the treatment of Alzheimer's disease. Such properties are the inhibition of amyloid-β-protein (Aβ) aggregation, Aβ-induced inflammation, and activities of β-secretase and acetylcholinesterase. However, previous studies have revealed that CUR exhibited low bioavailability and difficulties in reaching the brain. OBJECTIVE: To overcome such drawbacks, this study aims at developing nasal lipid nanocarriers loaded with CUR to effectively target the brain. METHODS: The lipid nanocarriers (NE) were prepared using the hot solvent diffusion associated with the phase inversion temperature methods. Physico-chemical and morphological characterizations and in vitro drug release of the nanocarriers were carried out. The CUR permeation/retention was analyzed in Franz-type diffusion cell using porcine nasal mucosa. Confocal laser scan and histopathological studies were also performed. RESULTS: The results showed that the NE sizes ranged between 18 nm and 44 nm with negative zeta potential. The CUR content ranged from 0.24 to 1.50 mg/mL with an encapsulation efficiency of 99%. The profiles of CUR release indicated a biphasic kinetics. CUR-NE permeation across the porcine nasal mucosa was higher when compared to free CUR. These results have also been validated through an analysis on a confocal microscopy. In addition, no toxicity on the nasal mucosa has been observed in a histopathological analysis. CONCLUSION: These results suggest that it is possible to develop NEs with a high content of CUR and small particle size. Such an encapsulation increases the potential of CUR permeation across the porcine nasal mucosa.
BACKGROUND:Curcumin (CUR) has properties that can be useful for the treatment of Alzheimer's disease. Such properties are the inhibition of amyloid-β-protein (Aβ) aggregation, Aβ-induced inflammation, and activities of β-secretase and acetylcholinesterase. However, previous studies have revealed that CUR exhibited low bioavailability and difficulties in reaching the brain. OBJECTIVE: To overcome such drawbacks, this study aims at developing nasal lipid nanocarriers loaded with CUR to effectively target the brain. METHODS: The lipid nanocarriers (NE) were prepared using the hot solvent diffusion associated with the phase inversion temperature methods. Physico-chemical and morphological characterizations and in vitro drug release of the nanocarriers were carried out. The CUR permeation/retention was analyzed in Franz-type diffusion cell using porcine nasal mucosa. Confocal laser scan and histopathological studies were also performed. RESULTS: The results showed that the NE sizes ranged between 18 nm and 44 nm with negative zeta potential. The CUR content ranged from 0.24 to 1.50 mg/mL with an encapsulation efficiency of 99%. The profiles of CUR release indicated a biphasic kinetics. CUR-NE permeation across the porcine nasal mucosa was higher when compared to free CUR. These results have also been validated through an analysis on a confocal microscopy. In addition, no toxicity on the nasal mucosa has been observed in a histopathological analysis. CONCLUSION: These results suggest that it is possible to develop NEs with a high content of CUR and small particle size. Such an encapsulation increases the potential of CUR permeation across the porcine nasal mucosa.
Authors: María L Del Prado-Audelo; Isaac H Caballero-Florán; Jorge A Meza-Toledo; Néstor Mendoza-Muñoz; Maykel González-Torres; Benjamín Florán; Hernán Cortés; Gerardo Leyva-Gómez Journal: Biomolecules Date: 2019-02-08
Authors: Clementine Wallet; Marco De Rovere; Jeanne Van Assche; Fadoua Daouad; Stéphane De Wit; Virginie Gautier; Patrick W G Mallon; Alessandro Marcello; Carine Van Lint; Olivier Rohr; Christian Schwartz Journal: Front Cell Infect Microbiol Date: 2019-10-24 Impact factor: 5.293
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