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Artículo

Eudragit E100 as a drug carrier: The remarkable affinity of phosphate ester for dimethylamine

Guzman, Maria LauraIcon ; Manzo, Ruben HilarioIcon ; Olivera, Maria EugeniaIcon
Fecha de publicación: 09/2012
Editorial: American Chemical Society
Revista: Molecular Pharmaceutics
ISSN: 1543-8384
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Farmacología y Farmacia

Resumen

Therapeutic agents containing phosphate groups in their molecules have increasing therapeutic impact. The object of this study was to characterize the cationic polyelectrolyte Eudragit E100 (EuE100) as a carrier for drugs containing phosphate groups, using dexamethasone phosphate (DP) as a model. A series of EuE100-DP complexes was obtained by acid-base reaction in which DP neutralized 12.5-75% of the basic groups of EuE100. The solids obtained after solvent evaporation revealed by spectroscopic characterization the complete reaction between the components through the ionic interaction between the amine groups of EuE100 and the phosphate groups of DP. The reversibility of the counterion condensation, evaluated through the proton-withdrawing effect produced by the ionic exchange generated by titration with NaCl, showed a remarkable high affinity between EuE100 and DP. In line, drug delivery in bicompartimental Franz cells toward water as receptor medium was very slow (2% in 6 h). However, it was increased as water was replaced by NaCl solution, which upon diffusion generates ionic exchange. A sustained release of DP with noticeable zero order kinetics accounted for a remarkable high affinity, mainly due to the electrostatic attraction. The release rate remains constant regardless of the saline concentration of the media. Besides, the delivery control is maintained even in gastric simulated fluid, a property not informed previously for EuE100 complexes.
Palabras clave: CATIONIC POLYMETHACRYLATE , CONTROLLED RELEASE , PHOSPHATE ESTER
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/190741
URL: https://pubs.acs.org/doi/10.1021/mp300282f
DOI: http://dx.doi.org/10.1021/mp300282f
Colecciones
Articulos(CCT - CORDOBA)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - CORDOBA
Articulos(UNITEFA)
Articulos de UNIDAD DE INVESTIGACION Y DESARROLLO EN TECNOLOGIA FARMACEUTICA
Citación
Guzman, Maria Laura; Manzo, Ruben Hilario; Olivera, Maria Eugenia; Eudragit E100 as a drug carrier: The remarkable affinity of phosphate ester for dimethylamine; American Chemical Society; Molecular Pharmaceutics; 9; 9; 9-2012; 2424-2433
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