Ravi

Angiogenesis is the development of new blood vessels. A wealthy number of ion channels are found on the endothelial cells. These ion channels play a vital action in cell proliferation and in related angiogenesis. We aimed to investigate the effects of Nifedipine (L-Type voltage gated calcium channel blocker). The anti-angiogenic activities of Nifedipine was investigated by measuring its effects on number of branches formed, angiogenic score, number of sprouts formed, weight of sponge implanted, Hemoglobin content and histopathological studies by in-vitro (aortic ring assay) and in-vivo (sponge implantation method) methods. The test and standard drug (Bevacizumab) groups were compared with the control group using One-way ANOVA, followed by post hoc test, the Dennett’s test to compare mean of all the groups with the control mean. The results revealed that Nifedipine treatment led to significant inhibition of proliferation and related angiogenesis in the dose dependent manner and were quite comparable with the standard antiangiogenic drug Bevacizumab. These scientific findings indicate the clinical benefits of Nifedipine in pathological situations involving excessive angiogenesis. Negative regulation of cell cycle progression at various checkpoints and cell migration may be the underlying molecular mechanisms for antiangiogenic action.

The safety of human exposure to an ever- increasing number and diversity of electromagnetic field EMF sources both at work and at home has become a public health issue. Deficient sperm production may be affected by factors such as radiation and other environmental toxins. Raised body temperature for any reason, and raising scrotal temperature by sitting in sofa or in hot water for a long period of time, can reduce sperm production. Healthy young men who watched more than 20 hours of TV each week had a 44 per cent lower sperm count than those who watched almost no TV. Radiations and excessive heat to the genitalia have damaging effect on the testicles. Hence individuals having direct contact with or exposure to such chemicals have high chances of having primary or secondary infertility. . Intense exercise didn't raise sperm count if accompanied by lots of hours in front of the TV.

A Molecular docking study on novel Acetamide derivatives as specific Mono amino oxidase (MAO) A inhibitory agents was performed with a set of 40 compounds to analyze their inhibitory action.  For this, compounds were designed on the basis of available literature and used as Ligands for molecular interaction. The structure of molecular target Mono Amino Oxidase A (MAO A) was retrieved from the PDB database (PDB ID 2Z5X). For comparative analysis Clorgyline, a well-known specific MAO A inhibitor was taken as the standard. Computational docking analysis was performed using PyRx, AutoDock Vina option based on scoring functions. Among 40 compounds the top 11 hits were recognized as promising MAO A inhibitors, according to their docking scores and selected for further study of interaction and visualization. Phenyl sulphanyl derivative with chlorobenzyl amino moiety (Code AD31) showed an optimum binding affinity and stable complex with a molecular target MAO A  with the binding energy of -8.3  kcal/mol as compared to the standard (-7.6 kcal/mol). These results indicated that proposed modification in Acetamide derivatives may produce potent and specific MAO A inhibitors to treat depression with lesser side effects.

The purpose of this research work was to formulate fast dissolving film of cefpodoxime proxetil for oral delivery in order to improve oral bioavailability of drug with poor solubility. Cefpodoxime proxetil (CP) is the drug candidate belonging to BCS class IV with poor solubility and poor permeability is and limited oral bioavailability, an orally administered, extended spectrum, semi-synthetic β- lactum antibiotic of cephalosporin class. To improve oral bioavailability, cefpodoxime proxetil nanosuspension was prepared using solvent-antisolvent precipitation technique. Nanosuspension was characterized on the basis of drug concentration in organic phase, temperature, solvent-antisolvent ratio and the time period of stirring on the particle size systematically. Particle size and zeta potential of nanosuspension was observed at 755.6nm and −22.6mV, respectively. Solvent casting method be used in the formation of film, utilizing HPMC E50 as film former, PEG 400 as plasticizer and tween 80 as surfactant. The optimized fast dissolving film formulation F1 showed uniformity of weight (0.091mg), folding endurance (149) drug content uniformity (99.5%), surface pH (6.8) disintegration time (32 seconds in 6.8 PB) and in- vitro drug release 94.2% in 7 min. So, it is concluded from comparison studies between fast dissolving film (FDF) containing pure drug and nanosuspension, fast dissolving film containing cefpodoxime proxetil nanosuspension gives faster and high drug release.

The aim of present investigation was to develop nanoemulsion gel of ketoconazole for topical delivery and comparison with the marketed preparation. Ketoconazole, BCS class II antifungal agent with broad spectrum activity is a poorly soluble and highly permeable drug. Due to its poor solubility, it is incompletely absorbed after oral dosing and bioavailability varies. The drug efficacy of topical formulation can be limited by instability due to its poor solubility in the vehicle and low permeability. Therefore, to overcome these shortcomings of conventional system nanoemulsion have been used as drug carrier in topical treatment of fungal infection, especially in dermatology. Pseudo-ternary phase diagram was constructed on triplot software to identify nanoemulsion area using different concentrations of oil, Smix (surfactant and co- surfactant) and water. 2% Carbopol 980 as gelling agent and 0.5% DMSO as permeation enhancer was used in topical gel formulation. The formulations was characterized on the basis of pH, drug content, viscosity and in-vitro diffusion study. The optimized formulation was found to have pH 7.4 and drug content 98.90%. In-vitro diffusion study of nanoemulsion gel showed 80.375% release within 8 hrs. Drug release of ketoconazole nanoemulsion gel when compared with marketed formulation showed 80.375% release within 8 hrs as compare to 52.125% for marketed preparation (Ketoconazole cream 2%, H&H Pharmaceutical). So, it is concluded that by incorporating ketoconazole nanoemulsion in topical gel provided sustained release along with improved solubility and permeability.

Michelia champaca, a healthful plant and it's normally utilized in people medication to treat varied diseases. The aim of the study was to evaluate the hepatoprotective & invivo antioxidant activities of Michelia champaca against carbon tetrachloride induced liver injury in rats. The methanol extract of Michelia champaca at dose of 250 and 500 mg/kg were administered orally once daily for seven days. Serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), total bilirubin (TB), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) and total protein (TP) were estimated from serum. In-vivo antioxidant activity of methanol extract of Michelia champaca was evaluated by various assays including catalase (CAT), superoxide dismutase (SOD), reduced glutathione, glutathione peroxidase (GPx), glutathione reductase (GRD) and malondialdehyde (MDA) levels in liver tissues. Histopathological examination of the liver sections was carried out to support the induction of hepatotoxicity. The results of the study indicated that, methanol extract of Michelia champaca 500 mg/kg showed a major decrease in SGPT, SGOT, TB, ALP, LDH levels that were all elevated within the carbon tetra chloride treated group. The Michelia champaca extract showed considerably redoubled the degree of CAT, SOD, GSH, GPx, GRD and reduce the degree of MDA. Michelia champaca leaves extract therapy also protective effects against histopathological alterations. From the above study it can be concluded that methanol extract of Michelia champaca had hepatoprotective & antioxidant activities against carbon tetra chloride induced hepatic damage in experimental animals.

Development of amphiphilic drug-lipid complexes is a potential approach for improving delivery of the drugs by increasing solubility, release profile and oral bioavailability. Rutin, a polyphenolic flavonoid, shows several biological effects like capillary protectant, anti-oxidant, anti-inflammatory, anti-aging, cardio-protective, anti-thrombotic and neuroprotective, but its use is limited due to its low aqueous solubility. To overcome this limitation, phospholipid complex of Rutin was developed to improve its aqueous solubility for better absorption through the gastrointestinal tract and this might result in improved bioavailability. The Rutin phytosomes prepared by solvent evaporation method using different ratios of Rutin and Soybean phosphatidylcholine (1:1, 1:2 and 1:3) was evaluated for percentage yield, compatibility studies by infra-red spectroscopy, particle size, poly dispersity index, zeta potential, drug content and were found to be within the acceptable range. Surface morphology by scanning electron microscopy, solubility studies, in-vitro drug release and stability studies also were carried out. The phospholipid complex of Rutin was found to be fluffy and porous with rough surface. The water solubility of Rutin was improved from 0.058mg/ml to 0.475 mg/ml in the prepared Phytosomes. The in-vitro drug release studies showed that there is no drug release from pure drug and F1 formulation up to 120min in acidic buffer pH 1.2; while in phosphate buffer pH 7.4 showed releases about 49.3% and 92.85% respectively, which indicates the significant enhancement of dissolution of Rutin phytosomes compared to pure drug. Stability studies suggested that the formulations were stable. In this study, Phytosomes could be successfully tailored for Rutin with improved dissolution characteristics which is promising for lowering the influence of exogenous factors and increasing drug delivery.

Drug utilization study is one of the fundamental watchtowers of promoting rational use of medicine for the treatment of various diseases. Often drugs are not used keeping in mind their safety and efficacy. To study the drug utilization pattern of psychotropic drugs in psychiatric outpatient department of Government General Hospital, Kakinada. A  Descriptive observational study was carried out in psychiatric outpatient department for duration of 3months.patients of either sex and ages in between 15-80years suffering from a psychiatric illness and started on atleast one psychotropic drug were selected. Patients below 15years age, pregnant and lactating women, patients who are not willing to co-operate, patients with intellectual disability were excluded from the study. 202 patients were enrolled for 3months study. The most affected gender was females (59.4%).commonly affected age group was between 26-35 years(30.6%).the average number of drugs per encounter for males is 3.158 and for females is 3.291.the percentage of drugs supplied form hospital pharmacy and percentage of drugs prescribed by generic names was 95.4%.all the drugs were prescribed from National Essential List Of Medicines (100%). Schizophrenia was the most commonly diagnosed psychiatric disorders followed by mood disorders. Antipsychotics (35.7%) are most commonly prescribed class of drugs followed by Benzodiazepines (21.2%), Olanzapine (19.2%) was most commonly prescribed antipsychotic drug. All the psychotropic drugs were prescribed from National Essential List Of Medicines. Atypical antipsychotics were prescribed more often than typical antipsychotics Owing to their fewer incidences of extra pyramidal side effects. Among atypical antipsychotics olanzapine was commonly prescribed.

The purpose of present work was for formulation and characterization of Clopidrogrel floating tablets to improve bioavailability and to minimize the side effects of the drug. FTIR studies were conducted for drug polymer compatibility. The Clopidrogrel sustained release floating tablets were formulated by wet granulation method.  Tablets were subjected to pre and post compressional evaluation studies. The different concentrations of HPMC K4M, HPMC K15M, xanthan gum, guargum, and sodium bi carbonate 25% w/w is used as gas generating agent and micro cellulose crystalline MCC are used in different concentrations (75%, 50%, 25%) as diluent. The tablets were tested for thickness, weight variation, hardness, friability, drug content; In vitro floating parameters and drug release studies were also conducted. Compatibility studies revealed that there is no interaction between drug and polymers in the formulations. The flow properties were within the limits and the granular bed exhibited uniform flow and ease for compression. Clopidogrel floating tablets showed uniform post compressional properties with minimum standard deviation. The formulations showed minimum floating lag time and prolonged duration of floating. In vitro drug release of clopidogrel was sustained up to 12 h. Clopidrogrel release followed zero order, first order, Higuchi drug release kinetics for drug release. The peppas diffusion coefficient ranged from 0.455 - 0.895 indicating drug release by non fickian diffusion followed by erosion. The F4 floating tablet was optimized formulation which showed 100% release sustained for 12 h. The stability studies indicated stability of drug in the optimized formulation against temperature and humidity.

The present study was undertaken to investigate the Diuretic and antiurolithiatic activities of Ethanolic leaf extract of Sida Acuta in Albino rats. Ethanolic leaf extract was administered to experimental rats orally at doses of 200mg/kg and 400mg/kg (each p.o). Furosemide (5mg/kg) was used as a standard. The diuretic effect of the extract was evaluated by measuring the urine volume and determining sodium, potassium, chloride and bicarbonate contents. In In vitro antiurolithiatic activity Calcium oxalate crystallization was induced by the addition of 0.01M sodium oxalate solutions in synthetic urine. The effect of extract (100, 300 and 500μg/ml) was studied by time course measurement of absorbance. In-vivo Urolithiasis was induced in male rats by administering ethylene glycol (0.75%) in drinking water to groups II-V except normal control (Group I) for 28 days. Groups I, II and III served as normal control, positive control (hyperurolithiatic), and standard (cystone 750mg/kg), respectively, Groups IV and V served as curative regimen. Oxalate, calcium, phosphate were monitored in urine. Serum calcium, creatinine and uric acid were also recorded. The extract of Sida acuta was safe and exhibited no gross behavioral changes in the rats. A significant diuretic effect was observed from the experimental animals treated with extract of Sida acuta individually compared to the control. The results obtained suggest potential usefulness of extract of Sida acuta leaf as an antiurolithiatic agent.