Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique

Blanca Tobar-Grande,1 Ricardo Godoy,1 Paulina Bustos,2 Carlos von Plessing,1 Elias Fattal,3,4 Nicolas Tsapis,3,4 Claudia Olave,1 Carolina Gómez-Gaete11Departamento de Farmacia, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile; 2Departamento de Bioqu...

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Autores principales:	Tobar-Grande B, Godoy R, Bustos P, von Plessing C, Fattal E, Tsapis N, Olave C, G&oacute;mez-Gaete C
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/448de000c23d4209b67604771c19a7cc
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spelling	oai:doaj.org-article:448de000c23d4209b67604771c19a7cc2021-12-02T04:21:18ZDevelopment of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique1176-91141178-2013https://doaj.org/article/448de000c23d4209b67604771c19a7cc2013-05-01T00:00:00Zhttp://www.dovepress.com/development-of-biodegradable-methylprednisolone-microparticles-for-tre-a13155https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Blanca Tobar-Grande,1 Ricardo Godoy,1 Paulina Bustos,2 Carlos von Plessing,1 Elias Fattal,3,4 Nicolas Tsapis,3,4 Claudia Olave,1 Carolina Gómez-Gaete11Departamento de Farmacia, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile; 2Departamento de Bioquímica Clínica e Inmunología, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile; 3Univ Paris-Sud, Institut Galien Paris-Sud, Faculté de Pharmacie, Châtenay-Malabry, France; 4CNRS, UMR 8612, Faculté de Pharmacie, Châtenay-Malabry, FranceAbstract: In this work, microparticles were prepared by spray-drying using albumin, chondroitin sulfate, and hyaluronic acid as excipients to create a controlled-release methylprednisolone system for use in inflammatory disorders such as arthritis. Scanning electron microscopy demonstrated that these microparticles were almost spherical, with development of surface wrinkling as the methylprednisolone load in the formulation was increased. The methylprednisolone load also had a direct influence on the mean diameter and zeta potential of the microparticles. Interactions between formulation excipients and the active drug were evaluated by x-ray diffraction, differential scanning calorimetry, and thermal gravimetric analysis, showing limited amounts of methylprednisolone in a crystalline state in the loaded microparticles. The encapsulation efficiency of methylprednisolone was approximately 89% in all formulations. The rate of methylprednisolone release from the microparticles depended on the initial drug load in the formulation. In vitro cytotoxic evaluation using THP-1 cells showed that none of the formulations prepared triggered an inflammatory response on release of interleukin-1ß, nor did they affect cellular viability, except for the 9.1% methylprednisolone formulation, which was the maximum test concentration used. The microparticles developed in this study have characteristics amenable to a therapeutic role in inflammatory pathology, such as arthritis.Keywords: spray-drying, microparticles, methylprednisolone, chondroitin sulfate, hyaluronic acid, cytotoxic assaysTobar-Grande BGodoy RBustos Pvon Plessing CFattal ETsapis NOlave CG&oacute;mez-Gaete CDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 2065-2076 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Tobar-Grande B Godoy R Bustos P von Plessing C Fattal E Tsapis N Olave C G&oacute;mez-Gaete C Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
description	Blanca Tobar-Grande,1 Ricardo Godoy,1 Paulina Bustos,2 Carlos von Plessing,1 Elias Fattal,3,4 Nicolas Tsapis,3,4 Claudia Olave,1 Carolina Gómez-Gaete11Departamento de Farmacia, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile; 2Departamento de Bioquímica Clínica e Inmunología, Facultad de Farmacia, Universidad de Concepción, Concepción, Chile; 3Univ Paris-Sud, Institut Galien Paris-Sud, Faculté de Pharmacie, Châtenay-Malabry, France; 4CNRS, UMR 8612, Faculté de Pharmacie, Châtenay-Malabry, FranceAbstract: In this work, microparticles were prepared by spray-drying using albumin, chondroitin sulfate, and hyaluronic acid as excipients to create a controlled-release methylprednisolone system for use in inflammatory disorders such as arthritis. Scanning electron microscopy demonstrated that these microparticles were almost spherical, with development of surface wrinkling as the methylprednisolone load in the formulation was increased. The methylprednisolone load also had a direct influence on the mean diameter and zeta potential of the microparticles. Interactions between formulation excipients and the active drug were evaluated by x-ray diffraction, differential scanning calorimetry, and thermal gravimetric analysis, showing limited amounts of methylprednisolone in a crystalline state in the loaded microparticles. The encapsulation efficiency of methylprednisolone was approximately 89% in all formulations. The rate of methylprednisolone release from the microparticles depended on the initial drug load in the formulation. In vitro cytotoxic evaluation using THP-1 cells showed that none of the formulations prepared triggered an inflammatory response on release of interleukin-1ß, nor did they affect cellular viability, except for the 9.1% methylprednisolone formulation, which was the maximum test concentration used. The microparticles developed in this study have characteristics amenable to a therapeutic role in inflammatory pathology, such as arthritis.Keywords: spray-drying, microparticles, methylprednisolone, chondroitin sulfate, hyaluronic acid, cytotoxic assays
format	article
author	Tobar-Grande B Godoy R Bustos P von Plessing C Fattal E Tsapis N Olave C G&oacute;mez-Gaete C
author_facet	Tobar-Grande B Godoy R Bustos P von Plessing C Fattal E Tsapis N Olave C G&oacute;mez-Gaete C
author_sort	Tobar-Grande B
title	Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
title_short	Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
title_full	Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
title_fullStr	Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
title_full_unstemmed	Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
title_sort	development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/448de000c23d4209b67604771c19a7cc
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Development of biodegradable methylprednisolone microparticles for treatment of articular pathology using a spray-drying technique

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