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Int J Biol Macromol ; 92: 972-980, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27506120

RESUMO

The present study deals with the development of natural macromolecule gum Albizia stipulata (AS) based novel pharmaceutical excipient for the controlled-release of paracetamol (PC). Central composite design (CCD) two-factor, five-level was used for the optimization of independent variables AS gum and compression force (CF) based on desired response variable drug release (DR) of paracetamol matrix tablets (PCMT). The optimized PCMT was prepared by wet granulation method and screened for pre- and post- compression parameters, and were characterized. The optimized PCMT (F14) formulation showed favorable in vitro release of PC (65%) in 12h, and the release kinetics followed zero order anomalous diffusion mechanism. AS gum exerted significant (p<0.001) anticancer activity with 98.25% inhibition at 2000µg/mL (IC50=179.12µg/mL) against A549 cell line. PC and PCMT showed 78.56% inhibition (IC50 value=856.58µg/mL) and 93.68% inhibition (IC50 value=396.35µg/mL) respectively, symbolizing that the gum remarkably potentiated the anticancer effect of PC in formulation after 24h treatment by inducing apoptosis. This is the first report on A. stipulata gum as a promising biopolymer for drug delivery application in cancer therapeutics.


Assuntos
Albizzia/química , Antineoplásicos/uso terapêutico , Química Farmacêutica/métodos , Neoplasias/tratamento farmacológico , Gomas Vegetais/química , Células A549 , Acetaminofen/farmacologia , Análise de Variância , Antineoplásicos/farmacologia , Varredura Diferencial de Calorimetria , Morte Celular/efeitos dos fármacos , Forma Celular/efeitos dos fármacos , Preparações de Ação Retardada/farmacologia , Liberação Controlada de Fármacos , Humanos , Cinética , Neoplasias/patologia , Espectroscopia de Infravermelho com Transformada de Fourier , Comprimidos , Difração de Raios X
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