Fabrication of Non-Ionic Surfactant Vesicular Gel for Effective Treatment of Rheumatoid Arthritis.

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.

Development of a Validated HPLC Method for the Estimation of Metformin HCl and Propranolol HCl.

The present investigation targets to develop a simple, specific, sensitive and accurate reverse phase high performance liquid chromatographic (RP-HPLC) method in human plasma for the estimation of metformin HCl and propranolol HCl from bulk drug and also from the marketed products. Human plasma samples were subjected to correct procedure for protein precipitation by methanol and protein free plasma samples were directly injected into HPLC C18 column. Chromatographic determination was performed on a reversed phase C18 column (3.9 mm X 300 mm, particle size 5 μm) using a mixture of acetonitrile and 0.1M pH 4.5 potassium dihydrogenortho phosphate buffer (mL) (40:60) at a flow rate of 0.8 mL/min and maintained at a pressure of 140 to 150 Kg/cm2. The retention time for metformin HCl and propranolol HCl was found to be 9.084 min and 6.132 min respectively at 232 nm without any interference of endogenous compounds in the plasma. The method was linear in the range between 50-2000 ng/mL. The peak areas were reproducible as indicated by low coefficient of variation. It was found that the excipients in the tablet dosage form do not interfere in the quantification of active drug by proposed method.

Comparative Quality Control Evaluation of Atenolol Tablets Marketed in Kuala Lumpur, Malaysia.

Background: The emergent of many pharmaceutical companies producing their own generic type of drugs after the patent of innovator drugs expired can improve the general healthcare delivery systems as well as decreasing the healthcare costs. But it also raises a few issues with one of it is the widespread of substandard and counterfeit product. Postsurveillance study to assess product parameter of various generics drug marketed is crucial. This kind of monitoring reduces a country’s economical burden on health issues from diseases due to fraudulent and substandard drugs usage. Purpose: The main objective of this study is to perform a comparative evaluation of the physicochemical properties of five commercially available leading brands of Atenolol tablets marketed in Kuala Lumpur. Method: The quality control parameters of five different brands of atenolol tablets were atenolol tablet assessed included uniformity of content, uniformity of weight, friability, crushing strength, disintegration and dissolution tests as well as content uniformity of the tablets. All the tablets were assessed for conformity with British Pharmacopoeia (BP) standards. Results: All the five brands of the tablets passed the British Pharmacopoeia (BP) standards for weight uniformity, disintegration, friability, content uniformity and hardness tests. Conclusion: The quality control parameters of all five top selling brands of atenolol tablets marketed in Kuala Lumpur analyzed passed all the BP and USP quality specifications and were physically and chemically equivalent.

Effects of nanosuspension and inclusion complex techniques on the in vitro protease inhibitory activity of naproxen

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.