ABSTRACT
Rheumatoid Arthritis (RA) is a chronic, inflammatory auto immune disorder with unknown aetiology. Though various efficacious treatment options are currently available to treat RA, failure to cure is unpredictable. Hence the present study aimed to evaluate Piroxicam (PC) loaded non-ionic surfactant vesicular carrier as transdermal patches. MethodsTransdermal patches of PC- niosomes were formulated by solvent casting method using different polymers. The prepared formulation was examined for physico - chemical and morphological characteristics and drug release studies were performed by Franz diffusion cell method. ResultsThe results of physico-chemical characterizations show that all formulations were with optimum range and morphological characterization shows that the prepared niosomes are spherical in shape. Drug release characteristic of all formulations was performed and the result exhibits that formulation TN4 (PC encapsulated niosomal gel transdermal patch) shows highest % drug release (95.13%) when compared to other formulation. The release data was fitted with release kinetics and results shows zero order with non Fickian diffusion mechanism. ConclusionsPC encapsulated vesicular carrier as transdermal patches is a promising drug delivery system to enhance the solubility of poorly soluble drugs. It also enhances the residence time of drug at absorption site. Hence this approach could be beneficial for the effective management of RA.
ABSTRACT
This study investigated the effects of nanosuspension and inclusion complex techniques on in vitro trypsin inhibitory activity of naproxen—a member of the propionic acid derivatives, which are a group of antipyretic, analgesic, and non-steroidal anti-inflammatory drugs. Nanosuspension and inclusion complex techniques were used to increase the solubility and anti-inflammatory efficacy of naproxen. The evaporative precipitation into aqueous solution (EPAS) technique and the kneading methods were used to prepare the nanosuspension and inclusion complex of naproxen, respectively. We also used an in vitro protease inhibitory assay to investigate the anti-inflammatory effect of modified naproxen formulations. Physiochemical properties of modified naproxen formulations were analyzed using UV, IR spectra, and solubility studies. Beta-cyclodextrin inclusion complex of naproxen was found to have a lower percentage of antitryptic activity than a pure nanosuspension of naproxen did. In conclusion, nanosuspension of naproxen has a greater anti-inflammatory effect than the other two tested formulations. This is because the nanosuspension formulation reduces the particle size of naproxen. Based on these results, the antitryptic activity of naproxen nanosuspension was noteworthy; therefore, this formulation can be used for the management of inflammatory disorders.
O objetivo do presente estudo foi investigar a atividade anti-inflamatória in vitro de nanossuspensões e do complexo de inclusão contendo naproxeno. Esse fármaco é derivado de ácido propiônico, com ação analgésica, antipirética e antiinflamatória. A obtenção dessas formulações teve por finalidade o aumento da solubilidade e da atividade anti-inflamatória do fármaco. Os métodos por precipitação em solução aquosa por evaporação e por empastagem foram modificados para a obtenção da nanossuspensão e do complexo de inclusão, respectivamente. Para a avaliação da atividade anti-inflamatória das formulações utilizou-se ensaio in vitro modificado de inibição de tripsina. As propriedades físico-químicas das formulações propostas foram determinadas utilizando espectroscopia UV e de infravermelho, além de estudos de solubilidade. O complexo de inclusão de naproxeno apresentou menor atividade antitripsina, quando comparado ao composto livre e à nanossuspensão. Em conclusão, entre as formulações avaliadas, a nanossuspensão de naproxeno apresentou maior efeito anti-inflamatório. Esse efeito foi devido à redução da dimensão das partículas de naproxeno para a escala nanométrica. Com base nos resultados obtidos, a atividade da nanossuspensão de naproxeno foi notável. Dessa forma, essa formulação apresenta potencial para o tratamento de distúrbios inflamatórios.