Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies

Lucía Martín-Banderas,1 Josefa Álvarez-Fuentes,1 Matilde Durán-Lobato,1 José Prados,2 Consolación Melguizo,2 Mercedes Fernández-Arévalo,1 Mª Ángeles Hol...

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Autores principales: Prados J, Melguizo C, Holgado MÁ, Fernández-Arévalo M, Durán-Lobato M, Álvarez-Fuentes J, Martín-Banderas L
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Publicado: Dove Medical Press 2012
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spelling oai:doaj.org-article:c981da4f4e864f6fa24e36f5448c44e12021-12-02T06:00:45ZCannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies1176-91141178-2013https://doaj.org/article/c981da4f4e864f6fa24e36f5448c44e12012-11-01T00:00:00Zhttp://www.dovepress.com/cannabinoid-derivate-loaded-plga-nanocarriers-for-oral-administration--a11595https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Lucía Martín-Banderas,1 Josefa Álvarez-Fuentes,1 Matilde Durán-Lobato,1 José Prados,2 Consolación Melguizo,2 Mercedes Fernández-Arévalo,1 Mª Ángeles Holgado11Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, Seville, Spain; 2Institute of Biopathology and Regenerative Medicine (IBIMER), School of Medicine, University of Granada, Granada, SpainAbstract: CB13 (1-Naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone)-loaded poly(lactic-co-glycolic acid nanoparticles (NPs) were produced by nanoprecipitation and tested for their in vitro release behavior and in vitro cytotoxicity assays. The effects of several formulation parameters such as polymer type, surfactant concentration, and initial drug amount were studied. NPs had a particle size 90–300 nm in diameter. Results obtained show that the main influence on particle size was the type of polymer employed during the particle production: the greater the hydrophobicity, the smaller the particle size. In terms of encapsulation efficiency (%), high values were achieved (~68%–90%) for all formulations prepared due to the poor solubility of CB13 in the external aqueous phase. Moreover, an inverse relationship between release rate and NP size was found. On the other hand, low molecular weight and low lactide content resulted in a less hydrophobic polymer with increased rates of water absorption, hydrolysis, and erosion. NPs showed no cytotoxicity and may be considered to be appropriate for drug-delivery purposes.Keywords: neuropathic pain, CB13, nanoprecipitationPrados JMelguizo CHolgado MÁFernández-Arévalo MDurán-Lobato MÁlvarez-Fuentes JMartín-Banderas LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 5793-5806 (2012)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Prados J
Melguizo C
Holgado MÁ
Fernández-Arévalo M
Durán-Lobato M
Álvarez-Fuentes J
Martín-Banderas L
Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
description Lucía Martín-Banderas,1 Josefa Álvarez-Fuentes,1 Matilde Durán-Lobato,1 José Prados,2 Consolación Melguizo,2 Mercedes Fernández-Arévalo,1 Mª Ángeles Holgado11Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, Seville, Spain; 2Institute of Biopathology and Regenerative Medicine (IBIMER), School of Medicine, University of Granada, Granada, SpainAbstract: CB13 (1-Naphthalenyl[4-(pentyloxy)-1-naphthalenyl]methanone)-loaded poly(lactic-co-glycolic acid nanoparticles (NPs) were produced by nanoprecipitation and tested for their in vitro release behavior and in vitro cytotoxicity assays. The effects of several formulation parameters such as polymer type, surfactant concentration, and initial drug amount were studied. NPs had a particle size 90–300 nm in diameter. Results obtained show that the main influence on particle size was the type of polymer employed during the particle production: the greater the hydrophobicity, the smaller the particle size. In terms of encapsulation efficiency (%), high values were achieved (~68%–90%) for all formulations prepared due to the poor solubility of CB13 in the external aqueous phase. Moreover, an inverse relationship between release rate and NP size was found. On the other hand, low molecular weight and low lactide content resulted in a less hydrophobic polymer with increased rates of water absorption, hydrolysis, and erosion. NPs showed no cytotoxicity and may be considered to be appropriate for drug-delivery purposes.Keywords: neuropathic pain, CB13, nanoprecipitation
format article
author Prados J
Melguizo C
Holgado MÁ
Fernández-Arévalo M
Durán-Lobato M
Álvarez-Fuentes J
Martín-Banderas L
author_facet Prados J
Melguizo C
Holgado MÁ
Fernández-Arévalo M
Durán-Lobato M
Álvarez-Fuentes J
Martín-Banderas L
author_sort Prados J
title Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
title_short Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
title_full Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
title_fullStr Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
title_full_unstemmed Cannabinoid derivate-loaded PLGA nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
title_sort cannabinoid derivate-loaded plga nanocarriers for oral administration: formulation, characterization, and cytotoxicity studies
publisher Dove Medical Press
publishDate 2012
url https://doaj.org/article/c981da4f4e864f6fa24e36f5448c44e1
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