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1.  Role of Components in the Formation of Self-microemulsifying Drug Delivery Systems 
Pharmaceutical research is focused in designing novel drug delivery systems to improve the bioavailability of poorly water soluble drugs. Self-microemulsifying drug delivery systems, one among the lipid-based dosage forms were proven to be promising in improving the oral bioavailability of such drugs by enhancing solubility, permeability and avoiding first-pass metabolism via enhanced lymphatic transport. Further, they have been successful in avoiding both inter and intra individual variations as well as the dose disproportionality. Aqueous insoluble drugs, in general, show greater solubility in lipid based excipients, and hence they are formulated as lipid based drug delivery systems. The extent of solubility of a hydrophobic drug in lipid excipients i.e. oil, surfactant and co-surfactant (components of self-microemulsifying drug delivery systems) greatly affects the drug loading and in producing stable self-microemulsifying drug delivery systems. The present review highlighted the influence of physicochemical factors and structural features of the hydrophobic drug on its solubility in lipid excipients and an attempt was made to explore the role of each component of self-microemulsifying drug delivery systems in the formation of stable microemulsion upon dilution.
PMCID: PMC4502138  PMID: 26180269
Lipid based delivery systems; partition coefficient; solubility; electrostatic interaction; interfacial tension
2.  Formulation and Characterization of Pyrazinamide Polymeric Nanoparticles for Pulmonary Tuberculosis: Efficiency for Alveolar Macrophage Targeting 
Pyrazinamide, a highly specific agent against Mycobacterium tuberculosis is used as first-line drug to treat tuberculosis. The current work aims to formulate polymeric nanoparticles based drug delivery system to sustain the release profile and reduce the dosing frequency of pyrazinamide. Further aim was to target the macrophages within body fluid. These polymeric nanoparticles were prepared by simultaneous double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared dispersions were characterized for various biopharmaceutical parameters such as particle size, zeta potential, polydispersity index, drug loading capacity, entrapment efficiency and targeting to alveolar macrophages. The formulated polymeric nanoparticles were in the particle size range of 45.51 to 300.4 nm with a maximum drug entrapment efficiency of 80.9%. The stability study of optimized batch conducted at 40±2°/75±5% relative humidity showed no significant changes up to 90 days. X-Ray Diffraction spectrum exhibits the transformation of crystalline form of drug to amorphous in the formulation. Scanning Electron Microscope image showed nanoparticles spherical in shape with smooth surface. In vitro release profiles were biphasic in nature with burst release followed by controlled release over a period of 24 h obeying diffusion mechanism. In vivo and ex vivo studies results of the study show significant uptake of the nanoparticles by alveolar macrophages through fluorescent micrograph. Polymeric nanoparticles formulation of pyrazinamide could encompass significant uptake by alveolar macrophages, the high first-pass metabolism, sustain the release of drug leading to reduction in dose, toxicity and improvement of patient compliance.
PMCID: PMC4502139  PMID: 26180270
Double-emulsion; polymeric nanoparticles; pulmonary tuberculosis; alveolar macrophages
3.  Formulation Design and Optimization of Orodispersible Tablets of Quetiapine Fumarate by Sublimation Method 
The objective of present study was to formulate directly compressible orodispersible tablets of quetiapine fumarate by sublimation method with a view to enhance patient compliance. A full 32 factorial design was used to investigate the effect of two variables viz., concentration of Indion 414 and camphor. Indion 414 (3-5 % w/w) was used as superdisintegrant and camphor (5-15 % w/w) as subliming agent. The tablets were evaluated for thickness, weight variation, hardness, friability, content uniformity, wetting time, porosity, in vitro disintegration time and in vitro drug release. The formulation containing 5% w/w of Indion 414 and 5% w/w camphor was emerged as promising based on evaluation parameters. The disintegration time for optimized formulation was 18.66 s. The tablet surface was evaluated for presence of pores by scanning electron microscopy before and after sublimation. Differential scanning colorimetric study did not indicate any drug excipient incompatibility, either during mixing or after compression. The effect of independent variables on disintegration time, % drug release and friability is presented graphically by surface response plots. Short-term stability studies on the optimized formulation indicated no significant changes in drug content and in vitro disintegration time. The directly compressible orodispersible tablets of quetiapine fumarate with lower friability, greater drug release and shorter disintegration times were obtained using Indion 414 and camphor at optimum concentrations.
PMCID: PMC4502140  PMID: 26180271
Orodispersible tablet; factorial design; Indion 414; sublimation; quetiapine fumarate
4.  Evaluation of Cellular Antioxidant and Antiproliferative Activities of Five Main Phyllanthus Emblica L. Cultivars in China 
The cell-based antioxidant activity assay as more biological relevant assay was considered to be more accurate to predict antioxidant activity in vivo than chemical activity assays. In the present study, the five main Phyllanthus emblica L. cultivars in China were subjected for cellular antioxidant activity based on HepG2 cells as well as antiproliferative activity. Total phenolics, total flavonoids and oxygen radical absorbance capacity were also measured. The results showed that Qingyougan, Binggan and Boligan (832±100, 774±52 and 704±28 μmol of quercetin equivalents/100 g) had higher cellular antioxidant activity than Tianyougan and Yougan (553±50 and 457±24 μmol of quercetin equivalents/100 g) in phosphate buffered saline wash protocol whereas, Boligan (3735±217 μmol of quercetin equivalents/100 g) had the highest cellular antioxidant activity and Tianyougan (2025±171 μmol of quercetin equivalents/100 g) had the lowest cellular antioxidant activity in no phosphate buffered saline wash protocol. The highest and lowest antiproliferative activities were observed in Binggan and Tianyougan (median effective dose: 6.95±0.11 and 14.03±0.10 mg/ml), respectively. The significant correlation was only observed between total flavonoids and cellular antioxidant activity from no phosphate buffered saline wash protocol (R2 =0.908, P<0.05), and total flavonoids and antiproliferative activity (R2 =0.887, P<0.05), suggesting the major contribution of flavonoids to the bioactivities of emblica. Overall, the data obtained revealed that different Phyllanthus emblica L. cultivars had strong cellular antioxidant and antiproliferative activities, thus should be recommended to increase consumption for health.
PMCID: PMC4502141  PMID: 26180272
Phyllanthus emblica L.; cellular antioxidant activity; antiproliferative activity; oxygen radical absorbance capacity; phenolics; flavonoids
5.  Effect of Water Miscible Organic Solvents on p-Nitrophenol Hydroxylase (CYP2E1) Activity in Rat Liver Microsomes 
Organic solvents used for solubilization of the substrates/NCEs are known to affect the activity of cytochrome P450 enzymes. Further, this effect varies with the solvents used, the substrates and CYP450 isoforms in question. In the present study, we have investigated the effect of ten commonly used water miscible organic solvents (methanol, ethanol, 1-propanol, 2-propanol, acetonitrile, acetone, dimethyl sulphoxide, N,N-dimethyl formamide, dioxane and polyethylene glycol 400) on p-nitrophenol hydroxylase activity at 0, 0.1, 0.25, 0.5, 0.75 and 1% v/v concentration in rat liver microsomes. All the solvents studied showed concentration dependent inhibition of the p-nitrophenol hydroxylase activity except acetonitrile which showed activation of the activity at concentration range studied. Out of ten solvents studied, dioxane was found to be the most inhibitory solvent (inhibition >90% at 0.25% v/v concentration). Overall, solvents like dimethyl sulphoxide, dimethyl formamide and dioxane appeared to be unsuitable for characterizing p-nitrophenol hydroxylase (CYP2E1-mediated) reactions due to a high degree of inhibition. On the other hand, methanol and acetonitrile at concentrations <0.5% v/v appeared to be appropriate solvents for substrate solubilization while evaluating CYP2E1-mediated catalysis. The results of this study imply that caution should be exercised while choosing solvents for dissolution of substrate during enzyme studies in liver microsomes.
PMCID: PMC4502142  PMID: 26180273
CYP2E1; p-nitrophenol; p-nitrocatechol; RLM and HPLC
6.  Liquisolid Tablets for Dissolution Enhancement of a Hypolipidemic Drug 
This investigation was aimed to improve the dissolution rate of the poorly soluble drug lovastatin, by formulating it as a liquisolid compact. Different liquisolid compacts were prepared using mathematical formulae to calculate the required quantities of powder and liquid ingredients to produce acceptably flowable and compressible admixture. Avicel PH 200, Cab-O-Sil, sodium starch glycolate and PEG 400 were employed as carrier, coating material, disintegrant and non-volatile liquid vehicle, respectively. The various drug to liquid and carrier to coating ratio were used to prepare liquisolid compacts. The formulated liquisolid tablets were evaluated for weight variation, hardness, drug content, friability and disintegration time. The in vitro release characteristics of the drug from tablets formulated by direct compression and liquisolid technique were compared in two different dissolution media. The tableting properties of the liquisolid compacts were within the acceptable limits and drug release rates were distinctly higher as compared to directly compressed tablets. The FTIR spectra showed no interaction between drug-excipient and disappearance of the characteristic absorption band of lovastatin in liquisolid formulations could be attributed to the formation of hydrogen bonding between the drug and liquid vehicle, which resulted in dissolution enhancement. Thus, the liquisolid technique was found to be a promising approach for improving the dissolution of a poorly soluble drug like lovastatin.
PMCID: PMC4502143  PMID: 26180274
Liquisolid compacts; lovastatin; dissolution; carrier and coating material
7.  Appropriate Antibiotic Administration in Critically Ill Patients with Pneumonia 
Inappropriate initial antibiotics for pneumonia infection are usually linked to extended intensive care unit stay and are associated with an increased risk of mortality. This study evaluates the impact of inappropriate initial antibiotics on the length of intensive care unit stay, risk of mortality and the co-predictors that influences these outcomes. This retrospective study was conducted in an intensive care unit of a teaching hospital. The types of pneumonia investigated were hospital-acquired pneumonia and ventilator-associated pneumonia. Three different time points were defined as the initiation of appropriate antibiotics at 24 h, between 24 to 48 h and at more than 48 h after obtaining a culture. Patients had either hospital-acquired pneumonia (59.1%) or ventilator-associated pneumonia (40.9%). The length of intensive care unit stay ranged from 1 to 52 days (mean; 9.78±10.02 days). Patients who received appropriate antibiotic agent at 24 h had a significantly shorter length of intensive care unit stay (5.62 d, P<0.001). The co-predictors that contributed to an extended intensive care unit stay were the time of availability of susceptibility results and concomitant diseases, namely cancer and sepsis. The only predictor of intensive care unit death was cancer. The results support the need for early appropriate initial antibiotic therapy in hospital-acquired pneumonia and ventilator-associated pneumonia infections.
PMCID: PMC4502144  PMID: 26180275
Antibiotics; hospital-acquired pneumonia; ventilator-associated pneumonia; critical care
8.  The Impact of Clinical Pharmacist Support on Patients Receiving Multi-drug Therapy for Coronary Heart Disease in China 
The study determined pharmacist support on patients receiving multi-drug therapy for coronary heart disease by evaluating patient self-care ability, quality of life, and drug therapy compliance. In this study, ninety patients were randomly assigned to an experimental group (n=45) and a control group (n=45). The control group received conventional clinical care. The experimental group received clinical care plus pharmacist support that included medication review, patient education, lifestyle management, discharge guidance, and telephone follow-up. Eighty-five patients completed the study. Self-care ability and quality of life were evaluated before hospital discharge. The experimental group understood their condition better than the control group (P<0.05), the differences between the groups in understanding treatment goals, drug regimens, lifestyle modifications, psychogenic disorders, and satisfaction evaluations were more pronounced (P<0.01). At six-month follow-up, the difference between the groups in drug therapy compliance was P<0.01, as was success rate by intention-to-treat (77.8% vs. 48.9%) and per-protocol (81.4% vs. 52.4%). Two adverse drug reactions occurred in the experimental group and three in the control group. Pharmacist support improved self-care ability, quality of life, drug therapy compliance, and treatment success rate in coronary heart disease patients.
PMCID: PMC4502145  PMID: 26180276
Coronary heart disease; pharmacist; quality of life; clinical pharmacy service
9.  Development and Validation of Discriminating and Biorelevant Dissolution Test for Lornoxicam Tablets 
The establishment of biorelevant and discriminating dissolution procedure for drug products with limited water solubility is a useful technique for qualitative forecasting of the in vivo behavior of formulations. It also characterizes the drug product performance in pharmaceutical development. Lornoxicam, a BCS class-II drug is a nonsteroidal antiinflammatory drug of the oxicam class, has no official dissolution media available in the literature. The objective of present work was to develop and validate a discriminating and biorelevant dissolution test for lornoxicam tablet dosage forms. To quantify the lornoxicam in dissolution samples, UV spectrophotometric method was developed using 0.01M sodium hydroxide solution as solvent at λma×376 nm. After evaluation of saturation solubility, dissolution, sink conditions and stability of lornoxicam bulk drug in different pH solutions and biorelevant media, the dissolution method was optimized using USP paddle type apparatus at 50 rpm rotation speed and 500 ml simulated intestinal fluid as discriminating and biorelevant dissolution medium. The similarity factor (f2) were investigated for formulations with changes in composition and manufacturing variations, values revealed that dissolution method having discriminating power and method was validated as per standard guidelines. The proposed dissolution method can be effectively applied for routine quality control in vitro dissolution studies of lornoxicam in tablets and helpful to pharmacopoeias.
PMCID: PMC4502146  PMID: 26180277
Lornoxicam; biorelevant; discriminating; validation
10.  Formulation and Evaluation of Cefixime Trihydrate Matrix Tablets Using HPMC, Sodium CMC, Ethyl Cellulose 
The objective of the present work is to design sustained release matrix tablets of cefixime trihydrate by incorporating drug in a matrix made up of release retardant polymers, which prolong drug release leading to minimization of the peak and valley effect in the plasma and provide patient convenience. The effect of combination of polymers on parameters like release pattern, release mechanism of the drug were studied. Total nine formulations each containing 200 mg of drug were prepared by direct compression method. The formulations F-1, F-2, F-3 were prepared with a 1:1 drug to polymer ratio using hydroxypropyl methylcellulose, carboxymethyl cellulose sodium and ethyl cellulose. F-4 was prepared with a 1:1 ratio of hydroxypropyl methylcellulose, carboxymethyl cellulose sodium, F-5 as prepared with a 1:1 ratio of hydroxypropyl methylcellulose and ethyl cellulose, F-6 was prepared with a 1:1 ratio of carboxymethyl cellulose sodium and ethyl cellulose, F-7, F-8, F-9 were prepared by using polymers hydroxypropyl methylcellulose, carboxymethyl cellulose sodium and ethyl cellulose in the ratios of 0.5:0.5:1, 0.5:1:0.5, and 1:0.5:0.5. Designed matrix tablets were evaluated for various pre-compression and post-compression parameters. Formulation F-5 showed 102.15 % release at the end of 12 h and it is selected as the best formulation. All Formulations followed zero order with non-Fickian diffusion method.
PMCID: PMC4502147  PMID: 26180278
Sustained release; patient compliance; HPMC; Sodium CMC; ethyl cellulose
11.  Formulation and Solid State Characterization of Nicotinamide-based Co-crystals of Fenofibrate 
The present investigation deals with formulation of nicotinamide-based co-crystals of fenofibrate by different methods and solid-state characterization of the prepared co-crystals. Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods. The prepared molecular complexes were characterized by powder X-ray diffractometry, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy and in vitro dissolution study. Considerable improvement in the dissolution rate of fenofibrate from optimized co-crystal formulation was due to an increased solubility that is attributed to the super saturation from the fine co-crystals is faster because of large specific surface area of small particles and prevention of phase transformation to pure fenofibrate. In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate. Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.
PMCID: PMC4502148  PMID: 26180279
Co-crystal; nicotinamide; dissolution; fenofibrate
12.  Development and in vitro/in vivo Evaluation of a Silastic Intravaginal Ring for Mifepristone Delivery 
Preparation and in vitro/in vivo evaluation of mifepristone intravaginal ring formulations were investigated. In the present study, it is reported that a mifepristone intravaginal ring of reservoir design comprising of a mifepristone silicone elastomer core enclosed in a silicone layer. During the preparation of intravaginal ring solid dispersion method was employed which improved the release rate of drug from the intravaginal ring. In vitro release studies performed under sink conditions and the released drug amounts were estimated using UV spectrometry at 310 nm. In addition, the in vivo release profile of in-house devices was evaluated in female New Zealand white rabbits. The rabbit plasma samples were processed and analyzed using a validated HPLC-MS method. Norgestrel was used as internal standard, and plasma samples contained mifepristone and internal standard were deproteinized, and then subjected to HPLC-MS analysis under condition of electrospray ionization in the selected ion monitoring mode. The drug release from intravaginal ring made in house was constant for 21 days in rabbits, which suggested the mifepristone intravaginal ring release system would be useful in clinical practice in the future. The result indicated the in vitro/in vivo correlation is perfect, which explained in vitro release analysis method developed was feasible.
PMCID: PMC4502149  PMID: 26180280
Mifepristone; intravaginal ring; silicone elastomer; in vitro/in vivo correlation
13.  RP-HPLC Estimation of Imipramine Hydrochloride and Diazepam in Tablets 
A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v) on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 μg/ml for imipramine hydrochloride (r2=0.999) and in the range 5-30 μg/ml for diazepam (r2=0.9994), respectively. The limits of detection and quantitation were 0.03 and 0.1 μg/ml for imipramine hydrochloride and 0.02 and 0.07 μg/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam) studies, intraday and interday precision (<2%) and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets.
PMCID: PMC4502150  PMID: 26180281
Imipramine HCL; Diazepam; RP-HPLC; UV detection; Tablet dosage form
14.  A Stability Indicating HPLC Method for the Determination of Nitisinone in Capsules 
In this study a simple and efficient stability-indicating HPLC method with short run time was developed for the determination of nitisinone. The stress degradation of nitisinone was studied in different acidic, basic, oxidative, thermal and photolytic conditions. The chromatographic separation was achieved on a Nova-Pak C18 column using a mixture of 50 mM NaH2PO4 (pH 2.5) and acetonitrile (45:55, v/v) as mobile phase. UV detection was performed at 280 nm. Good linearity was observed over the concentration range of 0.5-50 μg/ml with r2>0.999. The within-day and between-day precision values were less than 2%. The proposed method could be used for the determination of nitisinone in the presence of its degradation products and also dosage form excipients for the quality control purposes.
PMCID: PMC4502151  PMID: 26180282
Nitisinone; stability-indicating; stress degradation; HPLC; UV detection
15.  Phytochemical Evaluation of Roots of Polygonum viscosum Buch-ham 
Phytochemical evaluation of the chloroform extract of roots of Polygonum viscosum has yielded six compounds, stigmasterol, 7,4-dimethylquercetin, kaempferol, quercetin, myricetin and scutellarein. Among the six compounds isolated and characterized by chemical and spectral (UV, NMR and Mass) analysis in the present phytochemical evaluation, stigmasterol was not reported earlier from P. viscosum. The compounds, 7,4’-dimethylquercetin, quercetin and scutellarein were reported from P. hydropiper. Kaempferol from P. amphibium, P. aviculare, P. convolvulus, P. hydropiper, P. lapathifolium and P. persicari a and myricetin from P. aviculare and P. lapathifolium were also reported earlier. This appers to be the first report of the occurrence of all the six compounds from P. viscosum.
PMCID: PMC4502152  PMID: 26180283
Polygonum viscosum; Polygonaceae; phytochemical evaluation; stigmasterol; 7,4’-dimethylquercetin; kaempferol; quercetin; myricetin; scutellarein
16.  Effect of Lycopene on Serum Nitrite-Nitrate Levels in Diabetic Rats 
The effect of lycopene on serum nitrate-nitrite levels was investigated in diabetic rats. In this investigation, 28 Wistar rats were divided into 4 groups, each of seven rats. These groups were control group, diabetes group, diabetes-lycopene group and lycopene group. The concentration of nitrite and nitrate was detected at high levels in diabetes group, diabetes-lycopene group and lycopene group as compared with the control group (P<0.05). Especially, the increase in the levels of nitrate in diabetes group and lycopene group was statistically significant when compared with diabetes-lycopene group and control group (P<0.05). In addition, we also determined the proportion of nitrite/nitrate for nitric oxide radical formation. Therefore, it is important to investigate the recovery and stability of nitrite and nitrate in samples. As a result of this study, it was observed that the amounts of nitrate and nitrite increased due to oxidative stress in diabetes and also application of antioxidant lycopene caused an increase in the amounts of nitrate and nitrite levels.
PMCID: PMC4502153  PMID: 26180284
Diabetic Rat; lycopene; nitrite-nitrate proportion
17.  Antioxidant and Hypoglycemic Activities of Exopolysaccharide by Submerged Culture of Inocutus Hispidus 
This work was to investigate the hypoglycemic and antioxidant activities of the exopolysaccharides produced in a stirred-tank bioreactor by Inocutus hispidus. The exopolysaccharides showed significant antioxidant activities, up to 70.7±2.5% inhibition of hydroxyl radicals, 50% inhibition of 2,2-diphenyl-1-picrylhydrazyl radicals, and a Trolox equivalent antioxidant capacity of 3.3 mM. The exopolysaccharide also showed notable hypoglycemic effects in streptozotocin-induced diabetic mice, reducing the plasma glucose, total cholesterol and triacylglycerol concentrations by 18.2±1.5, 20.9±0.8 and 14.4±0.4, respectively. The results demonstrated the potential of this EPS for human health protection against oxidative damage and hyperglycemia.
PMCID: PMC4502154  PMID: 26180285
Exopolysaccharides; Inocutus hispidus; fermentation; hypoglycemic effect; antioxidant
18.  D-002 (Beeswax Alcohols): Concurrent Joint Health Benefits and Gastroprotection 
Nonsteroidal antiinflammatory drugs include the traditional drugs and more selective COX-2 inhibitors. Traditional nonsteroidal antiinflammatory drug use is hampered by their gastrotoxicity, while COX-2-inhibitors increase the cardiovascular risk. The search of safer substances for managing inflammatory conditions is updated, a challenge wherein dual COX/5-LOX inhibitors have a place. This review summarizes the benefits of D-002, a mixture of higher aliphatic beeswax alcohols, on joint health and gastric mucosa. D-002 elicits gastroprotection through a multiple mechanism that involves the increased secretion and improved quality of the gastric mucus, the reduction of hydroxyl radical, lipid peroxidation, protein oxidation, neutrophil infiltration and the increase of antioxidant enzymes on the gastric mucosa. Consistently, D-002 inhibits NSAIDs, ethanol, pylorus-ligation and acetic acid-induced gastric ulceration in rats, and has reduced gastrointestinal symptoms in clinical studies. Early results found that D-002 was effective in the cotton pellet-induced granuloma and carrageenan-induced pleurisy model in rats, lowering pleural leukotriene B4 levels without causing gastrointestinal ulceration. However, D-002 effects on inflammation received little attention for years. Recent data have shown that D-002 inhibited both COX and 5-LOX activities with a greater affinity for 5-LOX and could act as a dual COX/5-LOX inhibitor. This mechanism might explain efficacy in experimental inflammatory and osteoarthritic models as well as clinical efficacy in osteoarthritic patients while supporting the lack of D-002 gastrotoxicity, but not the gastroprotective effects, which appear to be due to multiple mechanisms. In summary oral D-002 intake could help manage inflammatory conditions that impair joint health, while offering gastroprotection.
PMCID: PMC4442459  PMID: 26009643
Antiinflammatory agents; beeswax alcohols; D-002; gastroprotection; joint diseases; osteoarthritis
19.  Pharmacogenetics, Pharmacogenomics and Ayurgenomics for Personalized Medicine: A Paradigm Shift 
The value of health care can be increased tremendously through individualized medicine. With the promise of individualized medicine, healthcare professionals will be able to better predict disease risk, prevent development of disease and manage treatments more efficiently thereby allowing people to be healthier and active longer. The developments in the area of pharmacogenetics/pharmacogenomics can help the physicians achieve the target of personalized medicine. Personalized medicine will come to mean not just the right drug for the right individual, but the right drug for the specific disease affecting a specific individual. The use of personalized medicine will make clinical trials more efficient by lowering the costs that would arise due to adverse drug effects and prescription of drugs that have been proven ineffective in certain genotypes. The genotypic experiments have laid valuable insights into genetic underpinnings of diseases. However it is being realized that identification of sub-groups within normal controls corresponding to contrasting disease susceptibility could lead to more effective discovery of predictive markers for diseases. However there are no modern methods available to look at the inter-individual differences within ethnically matched healthy populations. Ayurveda, an exquisitely elaborate system of predictive medicine which has been practiced for over 3500 years in India, can help in bridging this gap. In contrast to the contemporary system of medicine, the therapeutic regimen in Ayurveda is implicated on tridoshas and prakriti. According to this system, every individual is born with his or her own basic constitution, which to a great extent regulates inter-individual variability in susceptibility to diseases and response to external environment, diet and drugs. Thus the researchers in India have demonstrated that integration of this stratified approach of Ayurveda into genomics i.e. Ayurgenomics could complement personalized medicine.
PMCID: PMC4442460  PMID: 26009644
Pharmacogenetics; pharmacogenomics; Ayurveda; ayurgenomics; personalized medicine
20.  Comparative Study to Predict Dipeptidyl Peptidase IV Inhibitory Activity of β-Amino Amide Scaffold 
Comparative study was performed on 34 β-amino amide derivatives as dipeptidyl peptidase IV inhibitors in order to determine their structural requirement to enhance the antidiabetic activities. Hologram quantitative structure activity relationships models utilized specialized fragment fingerprints (hologram length 353) which showed good predictivity with cross-validated q2 and conventional r2 values of 0.971 and 0.971, respectively. Models were validated and optimized by a test set of eight compounds and gave satisfactory predictive ability. Hologram quantitative structure activity relationships maps were helpful in prediction of the structural features of the ligands to account for the activity in terms of positively and negatively contributing towards activity. The information obtained from maps could be effectively use as a guiding tool for further structure modifications and synthesis of new potent antidiabetic agents.
PMCID: PMC4442461  PMID: 26009645
Dipeptidyl peptidase IV; fragment distinct; fragment size; hologram length; β-amino amide
21.  Combating Drug Resistant Pathogenic Bacteria Isolated from Clinical Infections, with Silver Oxide Nanoparticles 
The antibiogram study of methicillin resistant Staphylococcus aureus isolates revealed 100% resistance to vancomycin, bacitracin, erythromycin, ciprofloxacin and nalidixic acid. Eight isolates (53.3%) showed resistance to co-trimoxazole and one isolate to rifampicin, which was the drug of choice. An effort was made to evaluate the antimethicillin resistant Staphylococcus aureus activity of silver oxide (Ag2O) nanoparticles synthesized from Aspergillus terreus VIT 2013. Production of Ag2O nanoparticles was confirmed by color change of fungal filtrate and UV light absorption at 450 nm. X-ray diffraction pattern showed 2θ values at 27, 32, 38 and 57°, which corresponded to the cubic structure of Ag2O nanocrystals. Fourier transform infrared spectroscopy indicated the presence of primary amine, carbonyl group, NO2 and silver, revealing protein mediated nanoparticle production. The scanning electron microscope image showed freely dispersed Ag2O nanoparticles. The nanoparticles were active against all methicillin resistant isolates and hence can be used as antibacterial agents against drug resistant bacteria.
PMCID: PMC4442462  PMID: 26009646
Antibiogram; drug resistant MRSA; Aspergillus terreus VIT 2013; Ag2O nanoparticles; antibacterial activity
22.  Influence of Triazine Herbicide Exposure on Guppies (Poecilia sphenops) Aromatase Activities, Altered Sex Steroid Concentration and Vitellogenin Induction 
Atrazine, a herbicide is one the most toxic and sustaining pollutants in aquatic environment. It is detectable in surface water and in underground sources of drinking water. Many studies indicate that atrazine might be a potent endocrine disrupting xenobiotic. There are limited studies have revealed that the effects of atrazine on sex steroids hormones, vitellogenin and induction of aromatase, gonadosomatic index and hepatosomatic index. In this study, juvenile Poecilia sphenops fish was exposed to three different (0.83, 1.25 and 2.5 ppm) concentration of atrazine for 100 d. Changes in plasma and gonadal content and concentrations of sex steroids and vitellogenin protein in poecilia sphenops under laboratory conditions were assessed. The low level of the atrazine show estrogenic effect in males, as determined by a shortage of testosterone induction. Present study suggests that low induction of plasma vitellogenin and aromatase in male fish become suitable biomarkers of exposure to estrogenic chemicals.
PMCID: PMC4442463  PMID: 26009647
Poecilia sphenops; atrazine; sex steroid disruption; vitellogenin and aromatase
23.  Protective Effect of Total Phenolic Compounds from Inula helenium on Hydrogen Peroxide-induced Oxidative Stress in SH-SY5Y Cells 
Inula helenium has been reported to contain a large amount of phenolic compounds, which have shown promise in scavenging free radicals and prevention of neurodegenerative diseases. This study is to investigate the neuroprotective effects of total phenolic compounds from I. helenium on hydrogen peroxide-induced oxidative damage in human SH-SY5Y cells. Antioxidant capacity of total phenolic compounds was determined by radical scavenging activity, the level of intracellular reactive oxygen species and superoxide dismutase activity. The cytotoxicity of total phenolic compounds was determined using a cell counting kit-8 assay. The effect of total phenolic compounds on cell apoptosis due to hydrogen peroxide-induced oxidative damage was detected by Hoechst 33258 and Annexin-V/PI staining using fluorescence microscope and flow cytometry, respectively. Mitochondrial function was evaluated using the mitochondrial membrane potential and mitochondrial ATP synthesis by JC-1 dye and high performance liquid chromatography, respectively. It was shown that hydrogen peroxide significantly induced the loss of cell viability, increment of apoptosis, formation of reactive oxygen species, reduction of superoxide dismutase activity, decrease in mitochondrial membrane potential and a decrease in adenosine triphosphate production. On the other hand, total phenolic compounds dose-dependently reversed these effects. This study suggests that total phenolic compounds exert neuroprotective effects against hydrogen peroxide-induced oxidative damage via blocking reactive oxygen species production and improving mitochondrial function. The potential of total phenolic compounds and its neuroprotective mechanisms in attenuating hydrogen peroxide-induced oxidative stress-related cytotoxicity is worth further exploration.
PMCID: PMC4442464  PMID: 26009648
Total phenolic compounds; hydrogen peroxide; SH-SY5Y; apoptosis; neurodegenerative disease; neuroprotection
24.  In vitro Antioxidant and Pharmacognostic Studies of Leaf Extracts of Cajanus cajan (L.) Millsp 
Cajanus cajan (L.) Millsp is one of the second most dietary legume crops. The leaf extracts may be used as a potential source of natural antioxidant. The ash values, extractive values, total phenolic and flavonoid content, in vitro antioxidant activity of various leaf extracts as well as anatomical investigation of Cajanus cajan were carried out. Physicochemical parameters such as total, acid-insoluble and water-soluble ash values and moisture content of the leaf powder of C. cajan were found to be 9.50%, 1.40 g/100 g, 4.15 g/100 g drug and 6.72%, respectively. Percent yield of acetone, aqueous, ethanol, ethyl acetate and chloroform leaf extracts were 9.0, 10.6, 13.75, 8.7 and 5.8 g/100 g, respectively. Significant amount of phenolic and flavonoid content were observed. The results of the antioxidant activity were found to be concentration-dependent. The IC50 values for DPPH assay determined for aqueous and ethanol extracts were 0.69 and 0.79 mg/ml, respectively. Reducing power is increased with increasing amount of concentration in both aqueous and ethanol leaf extracts. The highest hydroxyl radical scavenging activity reached up to 83.67% in aqueous and 78.75% in ethanol extracts and in phosphomolybdenum assay the aqueous extract showed strong antioxidant capacity up to 55.97 nM gallic acid equivalents/g. It was found that the aqueous extract possessed highest antioxidant activity in all the assays tested. The antioxidant characteristics of leaf extracts are possibly because of the presence of polyphenols. Microscopic study showed the presence of collenchyma, fibres, xylem, phloem, epidermis, trichomes, palisade tissue, basal sheath, pith and cortex in leaf, petiole and pulvinus.
PMCID: PMC4442465  PMID: 26009649
Cajanus cajan; total phenolics; flavonoid; antioxidant; free radicals; hydroxyl radical scavenging activity
25.  Self Medication Practices among Medical Students of a Private Institute 
The study was undertaken to evaluate various aspects of self-medication in medical students. A prospective, cross-sectional, questionnaire-based study was carried out among 488 medical students selected by simple random sampling from January 2013 to June 2013. Data was collected and analyzed for counts and percentage. Students reported self-medication in the preceding one year was 71.7 % and the prevalence was more in final year students. Fever and headache were the most frequently reported illnesses, commonly used drugs were antipyretics and analgesics, obtained information through reading material, and reasons quoted were minor ailments and quick relief. Majority students agreed that medical knowledge is necessary for administration of medicine by self. Self-medication is highly prevalent in medical students, which is quite alarming.
PMCID: PMC4442466  PMID: 26009650
Self-medication; medical students; questionnaire; non-prescription drugs

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