Development and Characterization of New Functionalized Polyurethanes for Sustained and Site-specific Drug Release in the Gastrointestinal Tract

The main objective of the present paper has been the development and study of two new biodegradable polyurethanes, PU(dithiodiethanol-DTDI) and PU[(iPr)Man-DTDI], to be used as sustained matrix forming excipients. Furthermore, their capacity to act as excipient for colon drug delivery systems has be...

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Bibliographic Details
Authors: Campiñez, María Dolores, Benito Hernández, Elena María, Romero Azogil, Lucía, Aguilar de Leyva, Mercedes Ángela, García Martín, María de Gracia, Galbis Pérez, Juan Antonio, Caraballo Rodríguez, Isidoro
Format: article
Status:Versión aceptada para publicación
Publication Date:2017
Country:España
Institution:Universidad de Sevilla (US)
Repository:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/162850
Online Access:https://hdl.handle.net/11441/162850
https://doi.org/10.1016/j.ejps.2017.01.017
Access Level:Open access
Keyword:Excipient efficiency
Matrix systems
Polyurethanes
SeDeM
Sustained release
Site-specific drug delivery
Description
Summary:The main objective of the present paper has been the development and study of two new biodegradable polyurethanes, PU(dithiodiethanol-DTDI) and PU[(iPr)Man-DTDI], to be used as sustained matrix forming excipients. Furthermore, their capacity to act as excipient for colon drug delivery systems has been evaluated. Thus, SeDeM diagrams have been obtained to investigate their suitability to be processed through a direct compression process. Matrices containing 10–30% w/w of the polymers and theophylline anhydrous as model drug have been manufactured. Release studies have been carried out using a modified dissolution assay simulating pH and redox conditions for the gastro intestinal tract, including colon. Drug dissolution data have been analyzed according to the main kinetic models and their Excipient Efficiencies for prolonged release have been calculated. The principal parameters of the SeDeM Expert system, such as the parametric profile (mean radius) and the good compression index obtained for the polymers are above the values considered as adequate for direct compression even without addition of flow agents. The obtained values for Excipient Efficiency show good ability of the polymer to control the drug release. Finally, in the case of PU(dithiodiethanol-DTDI), a clear increase in the release rate has been observed when the formulation is subjected to colon simulating conditions.