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Int J Pharm ; 404(1-2): 124-32, 2011 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-21093555

RESUMO

The goal of the present work was to develop a swellable hydrogel colonic delivery system, which would maximise the availability of the therapeutic agent at a site of inflammation, especially where the water is scarce. A novel method was developed to manufacture a biodegradable and reversible polyelectrolyte complex (PEC) containing chitosan and poly acrylic-acid (PAA). The PEC was analysed using FTIR and DSC, which confirmed the formation of non-permanent swollen gel-network at an alkaline pH. Pentosan polysulphate (PPS) was incorporated in a PEC and an activated partial thromboplastin time assay was developed to measure the release of PPS from PEC. In vitro studies suggested that the release of PPS was dependent on the initial drug loading and the composition of the PEC. The gel strength of the swollen network, determined using a texture analyser, was dependent on polymer composition and the amount of PPS incorporated. Bacterial enzymes were collected from the rat caecum and colon for the digestion studies and characterised for glucosidase activity, glucuronidase activity and protein content. The digestion of the reversible polyelectrolyte complexes was measured using a dinitro salicylic acid assay and an increased release of drug was also confirmed in the presence of bacterial enzymes.


Assuntos
Resinas Acrílicas/química , Anti-Inflamatórios/administração & dosagem , Bactérias/enzimologia , Quitosana/química , Colo/microbiologia , Portadores de Fármacos , Fármacos Gastrointestinais/administração & dosagem , Poliéster Sulfúrico de Pentosana/administração & dosagem , Administração Tópica , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/metabolismo , Anticoagulantes/administração & dosagem , Anticoagulantes/química , Coagulação Sanguínea/efeitos dos fármacos , Varredura Diferencial de Calorimetria , Química Farmacêutica , Digestão , Composição de Medicamentos , Fármacos Gastrointestinais/química , Fármacos Gastrointestinais/metabolismo , Glucosidases/metabolismo , Glucuronidase/metabolismo , Hidrogéis , Concentração de Íons de Hidrogênio , Cinética , Masculino , Tempo de Tromboplastina Parcial , Poliéster Sulfúrico de Pentosana/química , Poliéster Sulfúrico de Pentosana/metabolismo , Ratos , Ratos Sprague-Dawley , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Tecnologia Farmacêutica/métodos
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