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.Uniterms: Naproxen/nanosuspension/anti-inflammatory activity. Naproxen/inclusion complex/antiinflammatory activity. Naproxen/solubility. Protease inhibition.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.Unitermos: Naproxeno/nanossuspensão/atividade anti-inflamatória. Naproxeno/complexo de inclusão/ atividade anti-inflamatória. Naproxeno/solubilidade. Inibição da protease.

Purpose: To investigate the anti-urolithiatic activity of the aqueous and alcoholic extracts ofMelia azedarach Linn leaves in calcium oxalate urolithiasis in male albino rats. Methods: The effect of oral administration of aqueous and ethanol extracts of Melia azedarach Linn leaves on calcium oxalate urolithiasis has been investigated. Lithiasis was induced by oral adminstration of ethylene glycol (0.75 %v/v) in male albino rats for 28 days. Each of the extract (250 mg/kg) was administered orally day 0 as a prophylactic regimen and from day 15 as a curative regimen. Regular administration of ethylene glycol caused hyperoxaluria in ethylene glycol-fed animals, leading to increased renal retention and excretion of oxalate, calcium and phosphate. Histopathological study, urine microscopy, serum analysis and biochemical analysis of kidney homogenate were performed. Results: Oxalate and calcium excretion in urine increased (p < 0.01) to 3.68 ± 0.01 and 4.5 ± 0.01 mg/24 h, respectively, in lithiatic control animals compared to (0.37 ± 0.01 and 1.27 ± 0.12 mg/24 h) for the normal control group. Treatment with aqueous or ethanol extract (250 mg/kg, p.o.) significantly (p < 0.01) reduced the elevated levels of calcium, oxalate and phosphate excretion in urine to 0.79 ± 0.01 and 1.09 ± 0.04 mg/24 h, respectively. Following treatment with the ethanol extract (250mg/kg), serum creatinine excretion was restored from 0.95 ± 0.01 mg/24 h to the normal level of 0.87 ± 0.01 mg/24 h. The results were comparable to those of the standard drug, allopurinol (50 mg/kg p.o.). Histopathological data for the kidney supported the foregoing results. Conclusions: The results demonstrate that the aqueous and ethanol extracts of Melia azedarach Linn leaves have potent antiurolithiatic activity against ethylene glycol-induced calcium oxalate urolithiasis in male albino rats.

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Background: The present study aimed at investigating the effect of ethanolic extract (EtAI), and aqueous extract (AqAI) of Aristolochia indica Linn roots on castor oil-induced diarrhoea and study on small intestinal transit. Phytochemical analysis of extracts was performed as per standard procedure. Materials and Methods:The oral toxicity study using Swiss albino mice was performed in accordance with OECD guidelines. The EtAI and AqAI extracts of Aristolochia indica Linn were studied for antidiarrhoeal property using castor oil-induced diarrhoeal model and charcoalinduced gastrointestinal motility test in Swiss albino mice. Results: Among the tested doses of 200 and 400 mg/kg body weight, the extracts reduced the frequency and severity of diarrhoea in test animals throughout the study period. At the same doses, the extract delayed the intestinal transit of charcoal meal in test animals as compared to the control and the results were statistically significant. Conclusion: Experimental findings showed that ethanol extract of Aristolochia indica Linn root possess significant antidiarrheal activity and may be a potent source of anti-diarrhoeal drug in future.

The aim of this study was to investigate the potent neuroprotective property of ethanol extract of Ocimum sanctum (EEOS) leaf (Holy basil, Family: Labiataea) against excitotoxicity induced neurodegeneration by using monosodium-L-glutamate (MSG) in Sprague-Dawley rats. The animals received EEOS (50, 100 and 200 mg/kg) and memantine (MMT, 20 mg/kg) daily for 7 days. On all the 7 days, MSG (2g/kg, i.p.) was administered one hour before drug treatment. The animals were observed for neurobehavioral performance on 1 st , 3 rd , 5 th and 7 th day. Oxidative damage and histopathological analysis were also assessed. EEOS (100 and 200 mg/kg, p.o.) and MMT (20 mg/kg, i.p.) administration significantly improved body weight and attenuated locomotor activity, rotarod performance and footfault test as compared with MSG treated group. In addition, EEOS was found to restore reduced glutathione (GSH), glutathione peroxidase (GPx), glutathione reductase (GR), catalase (CAT), super oxide dismutase (SOD) and Na +-K + ATPase. Conversely, the elevated level of lipid peroxidation and nitrite concentration in MSG treated group was attenuated significantly in EEOS group in comparison to MSG treated group. Histopathological evaluation showed that treatment with EEOS and MMT significantly attenuated neuronal death and increased the density of neurons after MSG treatment. Thus, these findings suggest that EEOS contains rosmarinic acid and ursolic acid in addition to other bioactive principles may have utility in the preventing and/or treating the neurodegenerative diseases and its protective effects may be due to the amelioration of excitotoxicity, oxidative stress, neurological and behavioral alterations. However, further studies are necessary to clearly define mechanism responsible.