Formulation, Optimization, in vitro and in-vivo evaluation of levofloxacin hemihydrate Floating Tablets

Abstract The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.

Comparative characterization of cinnamon, cinnamaldehyde and kaempferol for phytochemical, antioxidant and pharmacological properties using acetaminophen-induced oxidative stress mouse model / Caracterización comparativa de canela, cinamaldehído y kaempferol para propiedades fitoquímicas, antioxidantes y farmacológicas utilizando el modelo de ratón con estrés oxidativo inducido por acetaminofeno

This study was aimed to explore the comparative efficacy of cinnamon bark extract, cinnamaldehyde and kaempferol against acetaminophen (APAP)-induced oxidative stress. Cinnamon bark extract, cinnamaldehyde and kaempferol were utilized or in-vivo analysis. From the results of in-vitro screening tests, cinnamon ethanolic extract was selected for in-vivo study in mouse model. For this, Balb/c albino mice were treated with cinnamon ethanolic extract (200 mg/kg), cinnamaldehyde (10 mg/kg) and kaempferol (10 mg/kg) orally for 14 days followed by single intraperitoneal administration of APAP during 8 hours. Blood and organ samples were collected for biochemical and histopathological analysis. The results showed that cinnamon bark ethanolic extract, cinnamaldehyde and kaempferol ameliorated APAP-induced oxidative stress and organ toxicity in mice. In conclusion, cinnamaldehyde and kaempferol possess comparable antioxidant potential even at 20-times less dose as compared to cinnamon bark ethanolic extract suggesting therapeutic potential in oxidative stress-related disorders.

Este estudio tuvo como objetivo explorar la eficacia comparativa del extracto de corteza de canela, cinamaldehído y kaempferol contra el estrés oxidativo inducido por acetaminofén (APAP). Se utilizaron extracto de corteza de canela, cinamaldehído y kaempferol para el análisis in vivo. De los resultados de las pruebas de detección in vitro, se seleccionó el extracto etanólico de canela para estudio in vivo en modelo de ratón. Para ello, los ratones albinos Balb/c fueron tratados con extracto etanólico de canela (200 mg/kg), cinamaldehído (10 mg/kg) y kaempferol (10 mg/kg) por vía oral durante 14 días, seguido de la administración intraperitoneal única de APAP durante 8 horas. Se recogieron muestras de sangre y órganos para análisis bioquímicos e histopatológicos. Los resultados mostraron que el extracto etanólico de la corteza de canela, el cinamaldehído y el kaempferol mejoraron el estrés oxidativo inducido por APAP y la toxicidad orgánica en ratones. En conclusión, el cinamaldehído y el kaempferol poseen un potencial antioxidante comparable, incluso a una dosis 20 veces menor en comparación con el extracto etanólico de la corteza de canela, lo que sugiere un potencial terapéutico en los trastornos relacionados con el estrés oxidativo.

Management of house fly, Musca domestica L. (Muscidae: Diptera), through botanical baits

ABSTRACT The house fly, Musca domestica L. (Diptera: Muscidae), is a major pest of all aspects of life, like the domestic, medical and veterinary and causal agent of several pathogenic diseases. The present study was conducted to evaluate the potential of different insecticide-free baits against house fly by incorporating flower methanol extract of Helianthus annuus (sunflower) and Tegetes erecta (marigold) at 10%, 20% and 30% bait formulation of corn syrup, dried milk and water. However, imidacloprid and thiacloprid (each at 5% concentration) were also included in the study for comparison. Results showed that insecticide baits were superior in causing mortality of adult house fly but dependent upon syrup. Overall, 20% baits of both extracts caused more than half population death of house fly within 48h. On the other hand, the mortality rate by 30% baits (from sunflower and marigold) had a similar impact as observed in case of imidacloprid and thiacloprid baits. Therefore, biological baits could play a more active and safer role in the management of house fly as compared to synthetic insecticides.

Termiticide activities of wood extractives of Ziziphus mauritiana (Rhamnaceae) against subterranean termites under field conditions

Abstract Synthetic wood preservatives are the causes of large-scale environmental pollution and few have been withdrawn from the commercial markets in the past years. The present studies focused on determination of naturally present extractives of Ziziphus mauritiana as less toxic wood protectant against subterranean termites. Firstly, natural resistance of Z. mauritiana heartwood against termite was determined by exposing stakes in the field. For the preparation of extractives, air-dried Z. mauritiana heartwood and bark shavings were soaked in 1 liter each of ethyl acetate, hexane, petroleum ether and water in a bottle separately. Different dipping treatment times (36 and 72 hours) at 10, 20 and 30% concentrations of extractives on Populus deltoides wooden stakes were used and stakes were exposed to termites in submerged manner. Combination of extractives in different solvents were included as separate experiment and finally, seasoning prior to extractives application on P. deltoides wooden stakes was also done and stakes were arranged in three replications for each treatment. Maximum mean percent weight loss (81.1%) was observed in case of P. deltoides followed by boiled Z. mauritiana (15.24%) in termite resistance test. Stakes treated with petroleum ether extracts had minimum weight loss alone or in combination with other extract's solvent in all experiments. Extractives in other solvents followed petroleum ether non-significantly but were significantly different from their respective control treatment, which had the highest weight loss (>60%). Transferring durability using extracts of Z. mauritiana increased resistance of non-durable P. deltoides against termites and extractives could be used as wood preservatives.

Role of MyD88-adaptor-like gene polymorphism rs8177374 in modulation of malaria severity in the Pakistani population

Abstract Introduction: The present study was designed to investigate the association between rs8177374 polymorphism and malaria symptoms due to exposure of Plasmodium vivax and Plasmodium falciparum. Materials and methods: A total of 454 samples were included in the study (228 malaria patients and 226 healthy individuals). Malaria patients, divided into P. vivax and P. falciparum groups on the basis of the causative species of Plasmodium, were categorized into mild and severe on the basis of clinical outcomes according to WHO criteria. Healthy individuals were used as controls. Allele specific PCR based strategy was used for the identification of rs8177374 SNP. Results: MyD88-adaptor-like gene polymorphism was associated with susceptibility to malaria (p < 0.001). C allele frequency (0.74) was higher in the population compared to T allele frequency (0.26). CT genotype increased the susceptibility of malaria (OR: 2.661; 95% CI: 1.722-4.113) and was positively associated with mild malaria (OR: 5.609; 95% CI: 3.479-9.044, p = 0.00). On the other hand, CC genotype was associated with severe malaria (OR: 3.116; 95% CI: 1.560-6.224, p = 0.00). P. vivax infection rate was higher in CT genotype carriers compared to other genotypes (OR: 3.616; 95% CI: 2.219-5.894, p < 0.001). Conclusion: MyD88-adaptor-like/TIR domain containing adaptor protein polymorphism for single nucleotide polymorphism rs8177374 is related with the susceptibility of malaria.

Enhanced ethanol production at commercial scale from molasses using high gravity technology by mutant S. cerevisiae

Abstract Very high gravity (VHG) technology was employed on industrial scale to produce ethanol from molasses (fermented) as well as by-products formation estimation. The effect of different Brix° (32, 36 and 40) air-flow rates (0.00, 0.20, 0.40, and 0.60 vvm) was studied on ethanol production. The maximum ethanol production was recorded to be 12.2% (v/v) at 40 Brix° with 0.2 vvm air-flow rate. At optimum level aeration and 40 Brix° VHG, the residual sugar level was recorded in the range of 12.5-18.5 g/L, whereas the viable cell count remained constant up to 50 h of fermentation and dry matter production increased with fermentation time. Both water and steam consumption reduced significantly under optimum conditions of Brix° and aeration rate with compromising the ethanol production. Results revealed VHG with continuous air flow is viable technique to reduce the ethanol production cost form molasses at commercial scale.

Effect of cellulose acetate phthalate and polyethylene glycol on physical properties and release of theophylline from microcapsules

ABSTRACT The present study describes the development of theophylline microcapsules by a non-solvent addition method and the effect of plasticizer addition on microencapsulation. The release was studied in distilled water and the data were analysed by various mathematical models for determining the mechanism of release. Prepared microcapsules were found to be spherical, free flowing and having more than 80% entrapped drug. The polymer - cellulose acetate phthalate and plasticizer - polyethylene glycol was considered to be affecting the properties of microcapsules including drug release (time for 50% drug release, T50). The formulation with the highest proportion of polymer and without plasticizer (F3) showed the slowest release with T50 = 4.3 h, while the formulation with lower proportion of polymer and 20% (w/w) plasticizer (F13 &14) showed the fastest release of drug with T50 values of 1.2 h and 1.3 h, respectively. The drug release from most of the formulations was found to be following Higuchi model. It is concluded from the results of the present study that cellulose acetate phthalate significantly affects the sustained release of the drug in water, whereas the addition of polyethylene glycol slightly enhances the drug release.

RESUMO O presente estudo descreve o desenvolvimento de microcápsulas de teofilina pelo método sem adição de solvente e o efeito da adição de plastificante na microencapsulação. A liberação foi estudada em água destilada e os dados foram analisados por vários modelos matemáticos para determinação do mecanismo de liberação. As microcápsulas preparadas mostraram-se esféricas, livres de corrente e com mais de 80% de fármaco encapsulado. O polímero - ftalato de acetato de celulose e o plastificante - polietileno glicol - afetaram as propriedades das microcápsulas, incluindo a liberação do fármaco (tempo para liberação de 50% do fármaco, T50). A formulação com a maior proporção de polímero e sem plastificante (F3) se mostrou como a de liberação mais lenta, com T50 = 4,3 h, enquanto as formulações com menor proporção de polímero e 20% de plastificante (m/m) (F13 &14) apresentaram a liberação mais rápida do fármaco, com T50 de 1,2 h e 1,3 h, respectivamente. A liberação do fármaco para a maioria das formulações seguiu o modelo de Higuchi. Concluiu-se, dos resultados do presente estudo, que o ftalato do acetato de celulose afeta significativamente a liberação controlada do fármaco em água, enquanto que a adição de polietileno glicol aumenta ligeiramente a liberação do fármaco.

Paederus beetles: the agent of human dermatitis

Background Rove beetles of the genus Paederus cause dermatitis when they come in contact with human skin. This condition is prevalent in some tropical and subtropical regions, such as in northern Pakistan, where it was recorded for the first time by US troops. Despite much research from other countries on this subject, few studies, mostly clinical, have been performed in a Pakistani context. A survey was carried out in villages, towns and cities of Punjab province, Pakistan, to explore the rove beetle population dynamics and to develop a model to elucidate the symptoms, preventive measures and treatment strategies for this dermatitis. Methods The prospective observational and patient surveys were performed bimonthly over a period of two years, in different districts of Punjab province. Collection was carried out in fields, gardens and houses during every visit with the aid of a pitfall trap, light trap, flight intercept trap, Berlese funnel trap and sweep netting. These traps were installed for four days during every visit. Interviews of ten individuals of different ages and sexes from each site were recorded during each visit. Results Out of 980 individuals, 26.4% were found to suffer from Paederus dermatitis. Lesions were most commonly found on the neck followed by the face. In July-August during the rainy season, this skin irritation was most prevalent and the population of these beetles peaked (36.2%). During May-June, the beetle population was lowest (7.85%) due to soil dryness. About 70% of such irritation cases were from individuals living in farming villages or in farmhouses. Their houses typically (80%) had broken doors and screen-less windows while 97% of the residents were unaware of how they may have come into contact with these beetles. In most cases (91% from villages/small towns and 24% from cities and adjoining areas) the local residents were unaware of modern treatment strategies. Paederus dermatitis is extremely frequent in villages with poor housing facilities and could be avoided via community awareness.(AU)

Synthesis and DPPH scavenging assay of reserpine analogues, computational studies and in silico docking studies in AChE and BChE responsible for Alzheimer's disease

Alzheimer's disease (AD) is a fast growing neurodegenerative disorder of the central nervous system and anti-oxidants can be used to help suppress the oxidative stress caused by the free radicals that are responsible for AD. A series of selected synthetic indole derivatives were biologically evaluated to identify potent new antioxidants. Most of the evaluated compounds showed significant to modest antioxidant properties (IC50 value 399.07 140.0±50 µM). Density Functional Theory (DFT) studies were carried out on the compounds and their corresponding free radicals. Differences in the energy of the parent compounds and their corresponding free radicals provided a good justification for the trend found in their IC50 values. In silico, docking of compounds into the proteins acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which are well known for contributing in AD disease, was also performed to predict anti-AD potential.

A doença de Alzheimer (DA) é uma doença neurodegenerativado sistema nervoso central, em rápido crescimento, e antioxidantes ajudam a suprimir o estresse oxidativo causado por radicais livres, responsávies pela DA. Avaliou-se, biologicamente, série de derivados sintéticos de indol selecionados para identificar novos antioxidantes. A maioria dos compostos avaliados apresentou de significativa a boa propriedade antioxidante (valor de IC50 399,07140.0 ± 50 µM). Eftuaram-se estudos de Teoria do Funcional de Densidade (DFT) com os compostos e os seus correspondentes radicais livres. As diferenças de energia entre os compostos protótipos e os radicais livres correspondentes proporcionaram boa justificativa para a tendência encontrada nos seus valores de IC50. O ancoramento in silico dos compostos com a acetilcolinesterase (AChE) e com a butirilcolinesterase (BChE), que contribuem para a DA, foi, também, realizado para prever o seu potencial anti-DA.

Effectiveness of halo-tolerant, auxin producing Pseudomonas and Rhizobium strains to improve osmotic stress tolerance in mung bean (Vigna radiata L.)

Halo-tolerant, auxin producing bacteria could be used to induce salt tolerance in plants. A number of Rhizobium and auxin producing rhizobacterial strains were assessed for their ability to tolerate salt stress by conducting osmoadaptation assay. The selected strains were further screened for their ability to induce osmotic stress tolerance in mung bean seedlings under salt-stressed axenic conditions in growth pouch/jar trials. Three most effective strains of Rhizobium and Pseudomonas containing ACC-deaminase were evaluated in combination, for their ability to induce osmotic stress tolerance in mung bean at original, 4, and 6 dS m-1 under axenic conditions. Results showed that sole inoculation of Rhizobium and Pseudomonas strains improved the total dry matter up to 1.4, and 1.9 fold, respectively, while the increase in salt tolerance index was improved up to 1.3 and 2.0 fold by the Rhizobium and Pseudomonas strains, respectively. However, up to 2.2 fold increase in total dry matter and salt tolerance index was observed due to combined inoculation of Rhizobium and Pseudomonas strains. So, combined application of Rhizobium and Pseudomonas strains could be explored as an effective strategy to induce osmotic stress tolerance in mung bean.

Influence of lead on growth and nutrient accumulation in canola (Brassica napus L.) cultivars.

Canola (Brassica napus L.) is commonly used as a hyper-accumulator for phytoextraction of heavy metals from soil and water. Like many other heavy metals, lead (Pb) contaminates soil, water and air and thus it is a great problem. This study was conducted to investigate toxic effects of Pb on growth and nutrient uptake in four canola cultivars. Each of four cultivars of canola (Con-II, Con-III, Legend and Shiralee) was subjected to four levels of Pb (0, 30, 60 and 90 mg Pb kg-1 of soil) from lead chloride [PbCl2]. Due to Pb toxicity, plant growth was adversely affected and relatively a severe reduction in root biomass (45.7%) was recorded. The Pb accumulation increased both in shoot and root, the highest being in root. The uptake of different nutrients, i.e., N, P, K, Ca, Mg, Zn, Cu and Mn was reduced (38.4, 32.8, 33.1, 49.6, 7.78, 52.0, 42.6 and 45.9%, respectively) in the shoots and that of N, Fe, Zn, and Cu in the roots (48.5, 33.2, 24.3 and 44.8%, respectively) of all canola cultivars. The root K, P, Zn and Mn and shoot P, Mg and Fe contents were less affected, the concentration of Pb, Ca and Mg in roots of all cultivars. Among canola cultivars Con-II and Con- III performed better than Legend and Shiralee in terms of growth (26.03%) and nutrient accumulation. Overall, plant growth and nutrient accumulation in the canola cultivars was hampered due to the presence of Pb.

Effects of breast cancer on physiological and psychological health of patients.

Objectives:-The breast cancer has great impact on physiological and psychological health of patients. This study was designed to investigate the psychological and physical effects of breast cancer. Patients and methods:-One hundred (100) patients were included in the study sample. All the patients were evaluated with the help of a questionnaire which developed with the help of psychologists. Results:-The results showed that the patient had high distress level at the time of diagnosis and during treatment.80% of patients reported that they do not get enough support by their husbands. Results also showed that treatment of breast cancer severely affects the fertility and no pregnancy was recorded during the treatment of breast cancer. Conclusions:-The results of the present study showed that the patients involved in CA breast undergo several psychological & physiological changes. During the treatment patient’s psychological treatment is must to boost the self esteem & to courage the patient to fight against the disease.

Leech infestation in oro-pharynx

Leech can infest human as ecto- and endoparasite. Endoparasitism occurs most commonly in respiratory passage usually by drinking contaminated water. The most likely manifestations of endoparasitism are haemoptysis, haematemesis, dyspnoea or blood stained saliva. We present a case of leech infestation in oropharynx in a young soldier resulting in haematemesis and blood stained saliva. High index of suspicion must be entertained if patient belong to some rural population where aquatic leeches are commonly found and presenting with such symptoms particularly unexplained bleeding from throat and or blood stained saliva