Comparative study of three structurally related acid polyelectrolytes as carriers of basic drugs: Carbomer, Eudragit L 100 and Eudragit S 100

A detailed description of equilibrium and drug release properties of aqueous dispersions of complexes of model basic drugs (D) with three structurally related acid polyelectrolytes (PE) is reported. Thus, equilibrium properties of dispersions of polymetacrylates Eudragit L 100, and Eudragit S 100, n...

Descripción completa

Detalles Bibliográficos
Autores: Ardusso, Marina Silvana, Manzo, Ruben Hilario, Jimenez Kairuz, Alvaro Federico
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2010
País:Argentina
Institución:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/129872
Acceso en línea:http://hdl.handle.net/11336/129872
Access Level:acceso abierto
Palabra clave:Polyelectrolyte-drug complexes
Ionic pairs
Affinity
Species distribution
Drug release
https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
Descripción
Sumario:A detailed description of equilibrium and drug release properties of aqueous dispersions of complexes of model basic drugs (D) with three structurally related acid polyelectrolytes (PE) is reported. Thus, equilibrium properties of dispersions of polymetacrylates Eudragit L 100, and Eudragit S 100, neutralized with increasing proportions of Lidocaine, Metoclopramide and Atenolol, were compared with those of Carbomer that were previously reported. The proportions of PE condensed (RCOO-DH+) and free species (D and DH+) were determined on PE-Lidocaine and PE-Metoclopramide systems. Affinity constants for ionic pair formation (Kip) were calculated as a function of D loading. In agreement with the high degree of counterionic condensation observed, the three (PE-D) complexes placed on Franz type cells released D at slow rates as water was the receptor medium. Rates increased over 3 times as water was replaced by 0.9% NaCl solution. Similar average of Korsmeyer exponent n (0.61 (water) and 0.69 (NaCl)) were found in both media. The overall kinetic behavior suggests that, under the conditions assayed, the dissociation of RCOO-DH+ is the factor that controls releasing rates. Structure related properties of the PE-D systems were identified in order to expand their potential uses as drug carriers.