Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method

Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method

Zaida Urbán-Morlán1, Adriana Ganem-Rondero1, Luz María Melgoza-Contreras2, José Juan Escobar-Chávez1,2, María Guadalupe Nava-Arzaluz1, David Quintanar-Guerrero11División de Estudios de Posgrado (...

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Autores principales: Zaida Urbán-Morlán, Adriana Ganem-Rondero, Luz María Melgoza-Contreras, et al
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2010
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Medicine (General)
R5-920
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spelling oai:doaj.org-article:5dfc9ae569324f04a855d1c85fa46e392021-12-02T07:15:35ZPreparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method1176-91141178-2013https://doaj.org/article/5dfc9ae569324f04a855d1c85fa46e392010-08-01T00:00:00Zhttp://www.dovepress.com/preparation-and-characterization-of-solid-lipid-nanoparticles-containi-a5071https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Zaida Urbán-Morlán1, Adriana Ganem-Rondero1, Luz María Melgoza-Contreras2, José Juan Escobar-Chávez1,2, María Guadalupe Nava-Arzaluz1, David Quintanar-Guerrero11División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán-Universidad Nacional Autónoma de México, Estado de México, México; 2Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, Calzada del Hueso, Colonia Villa Quietud, MéxicoAbstract: Solid lipid nanoparticles (SLNs) have been used for carrying different therapeutic agents because they improve absorption and bioavailability. The aim of the study was to prepare lipidic nanoparticles containing cyclosporine (CyA) by the emulsification-diffusion method and to study their physicochemical stability. Glyceryl behenate (Compritol® ATO 888) and lauroyl macrogolglycerides (Gelucire® 44/14) were used as carrier materials. Nanoparticles with good stability were obtained with Gelucire®, while it was difficult to obtain stable systems with Compritol®. Systems with Gelucire® were characterized by particle size, Z-potential, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), entrapment efficiency and in vitro release. Particle size and Z-potential were evaluated for at least three months. With a high CyA content (≥60 mg) in Gelucire® SLNs, variations in size were greater and particle size also increased over time in all batches; this effect may have been caused by a probable expulsion of the drug due to the lipid’s partial rearrangement. While the Z-potential decreased 10 mV after three months, this effect may be explained by the superficial properties of the drug that make the molecules to be preferably oriented at the solid-liquid interface, causing a change in the net charge of the particle. SEM confirmed size and shape of the nanoparticles. DSC studies evidenced that CyA affects the lipid structure by a mechanism still unknown. The entrapment efficiency was higher than 92%, and CyA release from SLNs was relatively fast (99.60% in 45 min).Keywords: emulsification-diffusion method, solid lipid nanoparticles, glyceryl behenate, lauroyl macrogolglycerides, dispersion stability, cyclosporine Zaida Urbán-MorlánAdriana Ganem-RonderoLuz María Melgoza-Contreraset alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 611-620 (2010)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Zaida Urbán-Morlán
Adriana Ganem-Rondero
Luz María Melgoza-Contreras
et al
Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
description Zaida Urbán-Morlán1, Adriana Ganem-Rondero1, Luz María Melgoza-Contreras2, José Juan Escobar-Chávez1,2, María Guadalupe Nava-Arzaluz1, David Quintanar-Guerrero11División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán-Universidad Nacional Autónoma de México, Estado de México, México; 2Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, Calzada del Hueso, Colonia Villa Quietud, MéxicoAbstract: Solid lipid nanoparticles (SLNs) have been used for carrying different therapeutic agents because they improve absorption and bioavailability. The aim of the study was to prepare lipidic nanoparticles containing cyclosporine (CyA) by the emulsification-diffusion method and to study their physicochemical stability. Glyceryl behenate (Compritol® ATO 888) and lauroyl macrogolglycerides (Gelucire® 44/14) were used as carrier materials. Nanoparticles with good stability were obtained with Gelucire®, while it was difficult to obtain stable systems with Compritol®. Systems with Gelucire® were characterized by particle size, Z-potential, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), entrapment efficiency and in vitro release. Particle size and Z-potential were evaluated for at least three months. With a high CyA content (≥60 mg) in Gelucire® SLNs, variations in size were greater and particle size also increased over time in all batches; this effect may have been caused by a probable expulsion of the drug due to the lipid’s partial rearrangement. While the Z-potential decreased 10 mV after three months, this effect may be explained by the superficial properties of the drug that make the molecules to be preferably oriented at the solid-liquid interface, causing a change in the net charge of the particle. SEM confirmed size and shape of the nanoparticles. DSC studies evidenced that CyA affects the lipid structure by a mechanism still unknown. The entrapment efficiency was higher than 92%, and CyA release from SLNs was relatively fast (99.60% in 45 min).Keywords: emulsification-diffusion method, solid lipid nanoparticles, glyceryl behenate, lauroyl macrogolglycerides, dispersion stability, cyclosporine
format article
author Zaida Urbán-Morlán
Adriana Ganem-Rondero
Luz María Melgoza-Contreras
et al
author_facet Zaida Urbán-Morlán
Adriana Ganem-Rondero
Luz María Melgoza-Contreras
et al
author_sort Zaida Urbán-Morlán
title Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
title_short Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
title_full Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
title_fullStr Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
title_full_unstemmed Preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
title_sort preparation and characterization of solid lipid nanoparticles containing cyclosporine by the emulsification-diffusion method
publisher Dove Medical Press
publishDate 2010
url https://doaj.org/article/5dfc9ae569324f04a855d1c85fa46e39
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