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In the present study, ethanolic extract of Clerodendrum serratum roots was investigated for its potential to reverse some features of bronchial asthma in ovalbumin-induced murine model of asthma. Clerodendrum serratum commonly called bharangi, (family Solanaceae) is a well-known anti-allergic drug in Asian folk system of medicines. In the present work, pharmacological studies are done to provide scientific evidence for therapeutic potential of plant in allergic asthma. Asthma was induced in experimental rats with allergen suspension of ovalbumin and aluminum hydroxide followed by treatment with dexamethasone (2.5 mg/kg, po) or C. serratum root extract (0.53 and 5.3 mg/kg, b. w., po). Biomarkers of inflammatory response including cell counts, immunoglobulin E, cytokines such as interleukin (IL) -4, -5, -1ß, tumor necrosis factor-a (TNF-a), leukotriene (LTD-4), and nitrite concentration in blood as well as bronchial (BAL) fluid were tested. Lung functions in asthmatic and treated animals were evaluated as breathing rate and tidal volume. Treatment with C. serratum extract markedly (p < 0.001, p < 0.01, and p < 0.05) diminished infiltration of inflammatory cells, IgE, cytokines, and nitrites in blood serum and bronchial fluid. Improvement in lung functions (p < 0.05) of asthmatic animals after CSE treatment also supports our findings. Results of the study suggest therapeutic potential of C. serratum in allergic asthma that can be related to ability of plant to attenuate response of inflammatory cells and thereby, production of inflammatory and proinflammatory cytokines in airways. [ABSTRACT FROM AUTHOR]

Introduction: Cuminum cyminum L. (Fam. Apiaceae) is a widely consumed spice. It is a rich sources of essential oils and has been actively researched for its chemical composition and biological activities. Aims: The study aimed to investigate the antiobesity effects of Cuminum cyminum L. distillates (CD) in high-fat-diet-induced obese rats. Methods: Twenty four male rats were randomly assigned to one of four groups: normal diet (ND), high fat diet (HFD), HFD + CD and HFD + orlistat. The CD was administered orally 7.75 ml/kg/twice a day for 4 weeks. Results: The CDtreated group significantly (p < 0.001) decreased the body weight gain, fat-pad weights, serum and hepatic lipids levels, insulin, glucose, leptin and pancreatic lipase activity in HFD-induced obese rats. The histological analysis revealed that the CD-treated group showed a remarkable reduction of macro vesicular steatosis in hepatic tissues and a significantly decreased number of lipid droplets and size of adipocytes compared to the HFD group. Conclusions: These findings demonstrate that CD treatment has a protective effect against a high-fat-diet-induced obesity in rats through the decreased activity in lipogenesis, as well as the increase in fatty acid oxidation and reduced intestinal absorption of dietary fat. [ABSTRACT FROM AUTHOR]

Context:Carica papayaLinn. (Caricaceae) leaf (CPL) juice has long been traditionally used in ethnomedicine for dengue fever. Objective:The study examines the effects of standardized CPL aqueous extract (SCPLE) on platelet count, extramedullary haematopoiesis (EMH), and immunomodulation in cyclophosphamide (CP)-induced animal model of thrombocytopenia. Materials and methods:The extract was analyzed for myricetin, caffeic acid,trans-ferulic acid, and kaempferol using HPTLC for standardization followed by UPLC-qTOF/MS fingerprinting for metabolite signature. The effects of SCPLE (50 and 150 mg/kg p.o.) on proliferative response of platelet count and total leucocyte count (TLC) were observed up to 14 days in Wistar rat. However, delayed-type hypersensitivity (DTH), haemagglutination titre (HT), andin vivocarbon clearance were examined as immunomodulatory parameters in albino mice at 150 mg/kg p.o. against CP. Results:The quantitative HPTLC estimation of SCPLE showed the presence of myricetin, caffeic acid,trans-ferulic acid, and kaempferol up to 280.16 ± 5.99, 370.18 ± 6.27, 1110.86 ± 2.97, and 160.53 ± 2.48 (μg/g), respectively. Twenty-four metabolites were identified using UPLC-qTOF/MS. Oral administration of SCPLE (150 mg/kg) in thrombocytopenic rats exhibited significant (p < 0.01) increase in thrombocytes (1014.83 × 103cells/mm3), DTH response (0.16 ± 0.004), and phagocytic index (63.15% increase) as compared to CP-induced thrombocytopenia group. Histopathological studies showed minimal fibrosis in spleen histology. Discussion and conclusions:Results suggest CPL can mediate the release of platelets providing the means for the treatment and prevention of dengue. [ABSTRACT FROM PUBLISHER]

Solubility and dissolution of a poor water-soluble drug are the two major barriers for formulation scientists in development of drug delivery. Many of the potent drugs do not show the therapeutic effects due to solubility issues but may show toxicity issues when used in high doses. Solid dispersion (SD) technology is an excellent tool for enhancing the solubility and dissolution and hence related bioavailability. Materials and Methods: SD of spironolactone (SPL) was developed using an inert carrier polyethylene glycol 4000 (PEG 4000) by the conventional fusion method and characterized for various characterization parameters. Results: Solubility of pure drug and SD of SPL in water was found to be 23.54 ± 1.75 μg/mL and 61.73 ± 1.26 μg/mL, respectively. The maximum cumulative percentage release from pure drug, SPL marketed product (tablet), physical mixture, and SPL SD at 60 min was 27.25 ± 1.83%, 35.64 ± 3.65%, 47.72 ± 2.45%, and 74.24 ± 3.25%, respectively in 0.1 N HCl. Conclusions: SD of SPL was developed successfully. The solubility of SPL SD was found to be significantly increased (P < 0.05) as compared to SPL active pharmaceutical ingredient (API) and physical mixture of PEG 4000 and SPL. The current study indicated that SD of SPL was a better option for enhancing solubility of a poorly soluble therapeutic agent. [ABSTRACT FROM AUTHOR]

Naringenin (NRG), predominant flavanone in grapefruits, possesses anti-inflammatory, anti-carcinogenic, hepato-protective and anti-lipid peroxidation effects. Slow dissolution after oral ingestion due to its poor solubility in water, as well as low bioavailability following oral administration, restricts its therapeutic application. The study is an attempt to improve the solubility and bioavailability of NRG by employing self-nanoemulsifying drug delivery technique. Preliminary screening was carried out to select oil, surfactant and co-surfactant, based on solubilization and emulsification efficiency of the components. Pseudo ternary phase diagrams were constructed to identify the area of nanoemulsification. The developed self-nanoemulsifying drug delivery systems (SNEDDS) were evaluated in term of goluble size, globule size distribution, zeta potential, and surface morphology of nanoemulsions so obtained. The TEM analysis proves that nanoemulsion shows a droplet size less than 50 nm. Freeze thaw cycling and centrifugation studies were carried out to confirm the stability of the developed SNEDDS. In vitro drug release from SNEDDS was significantly higher ( p < 0.005) than pure drug. Furthermore, area under the drug concentration time-curve (AUC0-24) of NRG from SNEDDS formulation revealed a significant increase ( p < 0.005) in NRG absorption compared to NRG alone. The increase in drug release and bioavailability as compared to drug suspension from SNEDDS formulation may be attributed to the nanosized droplets and enhanced solubility of NRG in the SNEDDS. [ABSTRACT FROM AUTHOR]

Diabetic cardiomyopathy plays a major role in morbidity and mortality among cardiovascular disorder-related complications. This study was designed to explore long-term benefits of Levosimendan (LEVO) along with Ramipril and Insulin. Diabetic cardiomyopathy was induced using streptozotocin (STZ) at the dose of 25 mg/kg/body weight/day for three consecutive days in Wistar rats. Rats were randomly divided into 10 groups and treatments were started after 2 weeks of STZ administration. A gradual but severe hyperglycemia (§§§p < 0.001) was observed in all STZ-treated groups except those received insulin (2  U/day). LEVO alone and in combination with Ramipril and Insulin normalized (**p < 0.01) mean arterial pressure and heart rate, restored catalase, superoxide dismutase, malondialdehyde, glutathione level and also attenuated (***p < 0.001) the raised serum levels of creatine kinase-heart type, lactate dehydrogenase, tumor necrosis factor-alpha, C-reactive protein, and caspase-3 level in heart tissue altered after STZ treatment. Myofibril degeneration, mitochondrial fibrosis and vacuolization occurred after STZ treatment, were also reversed by LEVO in combination with Ramipril and Insulin. The combination of LEVO with Ramipril and Insulin improved hemodynamic functions, maintained cardiac enzymes and ameliorated myofibril damage in diabetic cardiomyopathy. [ABSTRACT FROM AUTHOR]

Background: Increased use of the radioactive materials in the field of research, medical, nuclear power plant, and industry has increased the risk of accidental exposure. Intentional use of the radioisotopes by terrorist organizations could cause exposure/contamination of a number of the population. In view of the accidental contamination, there is a need to develop self-usable decontamination formulations that could be used immediately after contamination is suspected. Materials and Methods: Present work was planned to optimize and develop self-usable radiation decontamination cream formulation. Various pharmaceutical parameters were characterized. 99mTc- sodium pertechnetate was used as radiocontaminant. Static counts were recorded before and after decontamination using single photon emission computed tomography. Results: Decontamination efficacy of the cream was found to be 42% ± 3% at 0-0.5 h after the exposure. Primary skin irritancy test was satisfactory as no erythema or edema was observed visually after 2 weeks of the formulation application. Conclusion: The decontamination studies proved the potential of EDTA to remove the radiological contaminants effectively. [ABSTRACT FROM AUTHOR]

Objectives: Tigecycline has shown in vitro activity against Acinetobacter baumannii. Yet, published clinical experience with tigecycline use outside clinical trials is lacking. We describe, for the first time, bloodstream infection caused by tigecycline-non-susceptible A. baumannii occurring in patients receiving tigecycline for other indications. The possible mechanisms of resistance and pharmacokinetic limitations of the drug are addressed.Methods: The clinical records of involved patients were systematically reviewed. Tigecycline susceptibility testing was initially performed using the Etest method and confirmed by agar dilution. Involved isolates underwent PFGE and exposure to phenyl-arginine-β-naphthylamide (PAβN), an efflux pump inhibitor.Results: Two patients developed A. baumannii bloodstream infection while receiving tigecycline. Tigecycline was administered for other indications for 9 and 16 days, respectively, before the onset of A. baumannii infection. Patient 1 died of overwhelming A. baumannii infection and Patient 2 recovered after a change in antibiotic therapy. The MICs of tigecycline were 4 and 16 mg/L, respectively. Both isolates had a multidrug-resistant phenotype and were genotypically unrelated. After exposure to PAβN, the MICs reduced to 1 and 4 mg/L, respectively.Conclusions: To our knowledge, this is the first clinical description of bloodstream infection caused by tigecycline-non-susceptible A. baumannii. Such resistance appears to be at least partly attributable to an efflux pump mechanism. Given the reported low serum tigecycline levels, we urge caution when using this drug for treatment of A. baumannii bloodstream infection. [ABSTRACT FROM AUTHOR]