International Journal of Pharmaceutical Sciences and Drug Research

433-441

Authors: Asish Bhaumik1*, M. Chinna Eswaraiah2, Raja Chakraborty1

Neoplasia is a type of abnormal and excessive growth of tissue. The growth of a neoplasia is uncoordinated with that of the normal surrounding tissue, and it persists growing abnormally, even if the original trigger is removed. This abnormal growth usually forms a mass. The main objective of the present research work was the synthesis, characterization and evaluation of in vivo antitumour activity of some novel 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives. The in vivo antitumour activity of synthesized compounds was evaluated by HT 29 cell line induced malignant ascites on mouse model. The apoptosis of HT 29 cells was evaluated by using Gimsa and H33342 stain and the apoptosis ratios were analysed by FCM using AnnexinV-FITC/PI staining. The present experimental data displayed that the mortality was less in all groups except in tumour control group and all the synthesized compounds AB1-AB8 (100 mg/kg) significantly increased the PILS. While 5-FU increased the life span of 97.72%, and the PILS of synthesized compounds were found to be 45.45%, 59.09%, 68.18%, 56.81%, 38.63%, 84.09%, 77.27% and 90.90%. So the Synthesized compounds AB1-AB8 at the dose of 100 mg/kg significantly improved the overall survival of all treated animals and 5-FU was not significantly differed from each other in improving the overall survival of HT-29 cells. The apoptosis ratios of synthesized compounds were found as followed: AB1=26%; AB2=37.6%; AB3=43%; AB4=29%; AB5=24.1%; AB6=59.2%; AB7=48.2%; and AB8=63% respectively, while that of the Group-II (T. control) was 6.1%. When compared with standard drug 5-FU: 66.2%, it was indicated that compound AB8>AB6>AB7>AB3 were able to significantly induce HT-29 cells apoptosis.

447-453

Authors: Shrushti V. Somwanshi*, Sanjay S. Thonte

The present study aimed at preparing fast dissolving oral films of Eletriptan as a model drug which is used for the migraine treatment. Fast dissolving dosage forms have acquired great importance in pharmaceutical industry because of their unique properties. In the present research work various trials were carried out using different grades of HPMC E3, E6, and E15, maltodextrin DE6 and other polymers by solvent casting method. The prepared films were evaluated for film thickness, folding endurance, surface pH, morphological properties, % drug content and content uniformity, tensile strength, percent elongation, in vitro disintegration time and in vitro dissolution studies. The optimized formulation F24 prepared using HPMC E15 showed minimum disintegration time (10 sec), highest dissolution rate i.e. 99% of drug within 8 min and satisfactory physicochemical properties. The optimized film was evaluated for its bioavailability compared with pure drug as reference standard. Statistical analysis revealed that no significant difference between the bioavailability parameters of the film and the reference standard indicated that they exhibited comparable plasma level-time profiles. These findings suggest that the fast dissolving film containing Eletriptan is considered to be potentially useful for the treatment of migraine where quick onset of action is desirable.

460-473

Authors: P. R. Chetana1*, Vibha Vinayakumar Bhat1, Mohan A. Dhale2

In the present study, hetero-binuclear La(III) complexes were newly synthesized using well known bridging ligand N,N′-bis(2-pyridylmethyl)oxamide (2PMO, 1) and “complexes as ligands” [Cu(2PMO)] (2) and [Ni(2PMO)] (3). The newly synthesized mononuclear (4) as well as hetero-binuclear complexes (5 and 6) were characterized by analytical and spectroscopic techniques. The newly synthesized complexes were tested for their binding ability towards CT-DNA and chemical nuclease property towards SC pUC 19 DNA. The complexes were tested for antibacterial activities against Gram negative bacteria (E. coli and K. pneumonia) and Gram positive bacteria (B. subtilis and S. aureus), antioxidant activities by DPPH radical scavenging and ferrous-ion chelation methods and cytotoxicity against MCF-7 cell lines by MTT assay. The structure-activity relationship revealed that the newly synthesized hetero-binuclear complexes show potent DNA binding and chemical nuclease activities, antibacterial, antioxidant and cytotoxic activities.

480-486

Authors: Kaushal K. Chandrul1, Rajiv Dahiya2, Sunil Singh1*

Peptides are natural messenger molecules of human body and hence ideal lead compounds for the initiation of drug discovery research. They are the important organic compounds with potent biological activities. Peptides functions as hormones, enzymes enzyme inhibitors, or substrates or growth inhibitors or promoters, neurotransmitters and immunomodulators. Investigation of new and more potent analogs of molecules with already established activities from a key part of research in pharmaceutical field. It’s brings many modifications by manipulates the parent molecules structures serves to increase the activity of the compound, also eliminate adverse effect or toxicity associated with the parent drug. Cancer is the leading cause of deaths in world, We evaluated four natural cyclopeptides Diandrine A, Diandrine C, Fanlizhicyclopeptide A, Fanlizhicyclopeptide B, for cytotoxicity against HCT116 (Human Colorectal Carcinoma) & B16F10 (musculus skin melanoma) cells.

492-496

Authors: R. Shireesh Kiran1*, B. Chandra Shekar2, B. Nagendra Babu3

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (>24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16µg/mL, 8.00±1.23 h and 173 ± 26.34µg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.

362-371

Authors: I. Srinivas, D.V.R.N Bhikshapathi*

In the present study, immediate release solid dispersion of Repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. From in vivo studies, the AUC0→24 h and peak plasma concentration (Cmax) was doubled when compared with pure drug. In addition, in vitro dissolution efficiency was well correlated with in vivo pharmacokinetic parameters. The obtained results suggested that developed solid dispersion might be an efficacious approach for enhancing the solubility and bioavailability of Repaglinide.

379-385

Authors: Dhiraj Kumar1*, Susanta Kumar Panda2, Sudhir Kumar Sahoo2

A precise, accurate, economical and simple stability indicating RP-HPLC method was developed for the estimation of Amlodipine (AML) and Olmesartan (OLM) in bulk and pharmaceutical dosage form. Method was performed on a octadecyl silane column with dimensions 4.6 x 250 mm having particle size 5 micron. The mobile phase used in the method is TEA Buffer (pH 3.0) and acetonitrile in proportion of 25:75 respectively. The flow rate was maintained at 1.0 ml/ min and effluent was monitored at 258 nm. The drug was subjected to acid and alkali hydrolysis, oxidation, photolysis and heat as stress conditions. The method was validated for specificity, linearity, precision, accuracy, robustness and system suitability. The retention times were observed at 2.39 min and 3.33 min for AML and OLM respectively. The standard curve was found linear over a range of 05–35 µg/ml for AML and OLM. Similarly an average correlation coefficient was also obtained at 0.999 for AML and OLM. The limit of quantitation (LOQ) of this method was 2µg/ml for Amlodipine and Olmesartan. The absolute recovery was 100% for Amlodipine and 100.3 for Olmesartan. Degradation products produced as a result of stress studies did not interfere with the detection of AML and OLM and the assay can thus be considered stability-indicating.

394-405

Authors: Jeetu Gangil1*, Bhaswat S. Chakraborty2

Despite progress in antimalarial management and intensive care, the prevalence of malaria is growing and the mortality rate is very high. Yet even with timely treatment of quinine in maximum doses, the death in patients of severe malaria is very high. The successive synthesis of artemether and artesunate has supplied highly successful substitutes to quinine. This systematic review and meta-analysis approach provides a comparative outcome analysis of Artemisinin derivatives (intervention) and other antimalarials (comparison) in the paediatric and adult population. From the year 1985 to the year 2015, studies were recognized using database searches, citation searches of selected articles. The electronic databases searched engines: Pubmed, Web of Science, Global Health, Medline & Cochrane review of Journals up to April 2015. We selected published randomized controlled clinical trials information comparing artemisinin derivatives and quinine for the management of severe malaria in adult and paediatric population as per WHO malaria treatment guideline, any gender, age group less than or greater than 15 years who were diagnosed with severe malaria. The primary outcome was efficacy in terms of parasite clearance time (PCT), Parasite clearance at D7 and D28 and fever clearance time (FCT). The secondary outcome was the mortality and adverse events. We measured 95% confidence interval by the using of REVMAN software version 5.3 for meta-analysis and summarized the collected data on the basis of characteristics of inclusion criteria of articles. We included total 33 RCTs, enrolling 8396 paediatric and adult patients who were suffering from severe malaria. Artemisinin and its derivatives showed mean parasite clearance time (PCT) (MD -8.50 hours, 95% CI -9.41 to -7.60) and mean fever clearance time (FCT) (MD -9.51 hours, 95% CI -11.22 to -7.81) P<0.00001 statistically significant as compared to quinine therapy. Artemisinin and its derivatives showed a statistically significant clearance of parasites when compared to quinine at Day 7 (OR 0.41, 95% CI 0.21, 0.81, random effect model, P=0.01). Overall artemisinin derivatives has shown more parasite clearance at D28 than quinine group (Odds ratio 0.54, 95% CI 0.23, 1.29, random effect model, P=0.17). We evaluated secondary outcomes mortality which showed artemisinin or its derivatives a statistically significant mortality reduction as compared to quinine. (Odds Ratio 0.77, 95% CI 0.67 to 0.89; 27 trials, 8396 participants) P=0.0002 and also showed a statistically significant reduction in the adverse events as compared with quinine (RR0.73, 95% CI 0.62 to 0.87) P=0.003. An overall positive result was found with artemisinin derivatives across all evaluated outcomes.

410-417

Authors: B. Ram Prasad, D.V.R.N. Bhikshapathi*

The purpose of the present study was to develop and optimize multi-layered matrix tablets of Gliclazide trilayer tablets to achieve zero-order drug release for sustained plasma concentration. Gliclazide tablets were prepared by direct compression and consist of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC K 4M, K 15M and K100M), Guar gum and Eudragit L 100. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. In vivo bioavailability studies were carried out on the optimized formulation (EF14), mean time to attain peak drug concentration (Tmax) was 6.00 ± 0.14 and 4.02 ± 0.12 h for the optimized and marketed product respectively, while mean maximum drug concentration (Cmax) was 124.80 ± 1.02 ng/ml and 95.12 ± 1.05 ng/ml respectively. AUC0-α and AUC0-t for optimized formulation was significantly higher (p<0.05) as compared to marketed product. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a controlled release formulation of the drug. The EF14 was shown significant plasma concentration with controlled release and maintained for 24 hours with patient compliance by reducing the dosage frequency, when compared with marketed product in the efficient management of Diabetes mellitus.

213-216

Authors: E. Vadivel*, Poorva P. Dabholkar

From the last few decades the importance of search for natural polymer as pharmaceutical excipients has been increasing due to their various advantages. Natural polymer has been used in different pharmaceutical formulations. They are easily available, non-toxic, biodegradable and less cost. The synthetic polymers used as excipients suffer from many disadvantages such as high cost, toxicity, non-biodegradable and environmental pollution caused during their synthesis. In the present study, mucilage was isolated from the bark of Cinnamon verum. The mucilage was extracted using distilled water and isolated by the two methods such as precipitation with ethanol and acetone. The mucilage was characterized by various physicochemical properties such as solubility, pH, swelling index, loss on drying and preliminary phytochemical studies. The micrometric properties of mucilage such as bulk and tapped densities, Carr’s index, Hausner’s ratio and angle of repose were also evaluated. The result showed that extracted Cinnamon mucilage exhibited good flow properties (Angle of repose 20°.45”), loss on drying was 1.6%, Swelling index was 31.8% and pH was found to be 7.0. Extracted mucilage swells in water and slightly soluble in organic solvents. The preliminary phytoconstituents studies showed the presence of carbohydrates, mucilage and phenolic compounds. FT-IR studies show that presence of O-H and aliphatic C-H stretching. Results of evaluated parameters showed that cinnamon derived mucilage can be used as pharmaceutical excipients to formulate different dosage form. It has acceptable pH and organoleptic properties, so can be easily used in various dosage form.

227-232

Authors: Y. Bindu Vani, C. Haranath*, C. Surya Prakash Reddy, E. Bhargav

The present work is concerned with the formulation and evaluation of Piroxicam emulgel employing carbopol 934 and xanthan gum as polymers. The emulgel is prepared by combining the gel and emulsion. The gel in formulations were prepared by dispersing Carbopol 934 and xanthan gum separately in purified water with constant stirring at a moderate speed and then the pH was adjusted to 4 to 5.4 using Tri-ethanol amine (TEA). The oil phase in the emulsion consists of oleic acid and span-80. The aqueous phase in the emulsion was prepared using Tween-80, propylene glycol and distilled water. The prepared emulgel formulations were subjected to evaluation studies like Physical appearance, rheological studies, estimation of drug content and in-vitro drug release. The appearance of prepared emulgel was white. The pH of the emulgel was found to be 5.4. The in vitro drug release studies revealed that formulation F1 showed 85.20% and formulation F2 showed 79.23% of drug release at the end of 8 hrs. The drug release of F1 formulation follows zero order kinetics.

246-251

Authors: Ravi Shekhar1*, P. Sharma2

A new approach to zero- order drug delivery that includes geometric factors is described. Systems such as multilayered tablets and other geometrically altered devices have been created to perform this function. The multi-layered matrix system overcomes inherent disadvantages of non-linearity associated with diffusion controlled matrix devices by providing additional release surface with time to compensate for the decreasing release rate. These formulations designed to deliver the drug at predetermined rate, maintain therapeutically effective concentrations in systemic circulation for prolonged period of time. Recently, pharmaceutical research has focused on controlled drug delivery offer definite advantages over conventional release formulation of the same drug. Controlled delivery systems that can provide zero-order drug delivery have the potential for maximizing efficacy while minimizing dose frequency and toxicity. In the present study, guar gum was used as hydrophilic matrix carrier for designing oral controlled drug delivery systems of highly soluble drug lamivudine. Three layered matrix tablets of lamivudine prepared by wet granulation technique were subjected for various evaluating parameters and optimized.

260-267

Authors: G. Muralichand1, D. V. R. N. Bhikshapathi2*

The objective of this study was to develop solid dispersions of Nifedipine which has low aqueous solubility and bioavailability. Preliminary solubility studies were carried out using various hydrophilic polymers. The formulations were then optimized and evaluated by in-vitro dissolution studies, X-ray diffraction, FTIR and SEM. Formulation with 1:4:2 ratios of Nifedipine, Labrosol and SLS was found to be the best as it possessed better drug release properties compared to pure drug and other physical mixtures. The optimized formulation SD12 was found to have better drug release of 98.74 ± 5.19% in 90 minutes. From FTIR studies no interaction was takes place between drug and polymers. XRD peaks indicate the successful transformation of drug from crystalline to amorphous form. The final results indicate that the solid dispersion of Nifedipine remained stable over 90 days.

274-277

Authors: Prudence A Rodrigues1, P R Murugesan2, Anjana Balakrishnan1*, Megha Binoy1, Jithin Titus Jacob1

The objective of the present study is to analyse the effectiveness of carvedilol and metoprolol in the management of atrial fibrillation in post operative coronary artery bypass graft surgery patients. Atrial fibrillation occurs frequently soon after coronary artery bypass grafting and often results in increased mortality and morbidity. The incidence of post operative atrial fibrillation actually varies from 11% to 40% despite of the surgical technique and current guidelines recommend beta blockers as a medication for the prevention of atrial fibrillation after coronary artery bypass graft surgery. A prospective observational study was conducted on 100 subjects considering the inclusion and exclusion criteria and they were classified into carvedilol and metoprolol group. Heart rate was chosen as the primary parameter and statistical analysis was performed using student‘t’ test (p<0.05). There was a statistically significant decrease in the heart rate after therapy for both metoprolol and carvedilol but the difference in the effectiveness between carvedilol and metoprolol could not be significantly identified.

283-287

Authors: Edcy Edvi*, Angel Rose, Jose Celesti Sibi, Elsa Sandra Thomas, P A Sreeja

Medication Appropriate Index (MAI) is used to assess the quality of antibiotic prescribing. The aim of the study to determine the risk factors of obstructive airway disease and to assess the appropriateness of ongoing antibiotic therapy using medication appropriate index criteria. A 6 months study was carried out at Karuna Medical College Chittur. The patient details were collected in a specially designed data entry form and results were statistically analysed using chi square test. During the study period, a total of 202 patients were enrolled. Out of this, 150 (74%) were male patients and 52 (26%) were female patients and Distribution of risk factors, ex-smokers 34 (15%) were more prone to infective exacerbations, followed by smokers 34 (17%), alcoholics 33 (16%), allergies 12 (6%), ex-alcoholics 8 (4%) and patients with both smoking and alcoholism were 10 (5%). The most common problems were seen with indication (68%), duration of therapy (74%), and dose of antibiotic (81%), directions (68%), duplication (64%), effectiveness (75%) and expensiveness (68%). The level of significance was assessed and found to be significant. Males are more affected than females. The cigarette smoking influences the rate of influence of lung function by causing path physiologic changes in airways, including inflammation hyper responsiveness. Using medication appropriate index criteria when comparing inappropriate v/s marginal and inappropriate v/s appropriate both shows high level of significance which imply antibiotic therapy was inappropriate. It is found that inappropriate use of antibiotics will increase the burden of multi-drug resistance. Prescribing under generic name is considered economical and rational.

293-296

Authors: Garima Shrivastava*, Manjul Shrivastava

New Schiff base (2-[(1H-benzimidazol-2-ylimino) methyl]-4,6- diiodophenol) was synthesized by the condensation of aryl/hetero aromatic aldehyde (3,5diiodosalicylaldehyde) with 2- amino benzimidazole under conventional and microwave conditions and characterized through IR, HNMR and Mass spectral data and CHN analysis.

306-314

Authors: Marcos Reynoso, María E. Balderrama Coca, Ivana Y. Brodkiewicz, Gloria Jaime, Marina Perotti, Carola Schuff, Nancy R. Vera*

The chemical machinery of vegetables offers a great diversity of biological properties and plays a fundamental role in the field of pharmacology. The search for new drugs with fewer adverse effects represents a challenge for researchers. The objective of the present work was to carry out to investigate the medicinal properties and safety of extracts and essential oil from aerial parts of Clinopodium gilliesii (muña muña) and evaluate their antioxidant and anti-inflammatory activities in vivo. The extractions were carried out serially, using 96º alcohol (EE) and boiled distilled water (AE). The essential oil (EO) was obtained by steam dragging. The AE in vivo anti-inflammatory activity was determined by carrageenan induced plantar edema (acute inflammation) and granuloma formation by cotton disc (chronic inflammation) at oral doses of 250 and 500 mg/kg while that of the EO was established topically at doses of 50, 100µl/kg. In-vitro antioxidant activity was evaluated by DPPH depuration and inhibition of lipid peroxidation (β-carotene-linoleic acid method). Chemical study of the extracts was carried out by means of phytochemical screening and the essential oil was analyzed by GC-MS chromatography. The safety was evaluated with test of acute toxicity (48 h) and acute dermal toxicity (14 days). The results revealed that EE and EO had a significant acute and chronic anti-inflammatory activity, compared with positive patterns. EE (500 mg/kg), EO (100µl/kg), ibuprofen (100 mg/kg) and meprednisone (5 mg/kg) significantly reduced the weight of the exudate and cotton disc granuloma (24.17, 35.30, 45.56 and 57.17% respectively). The alcoholic and aqueous extracts presented important antioxidant activities with values higher than 90% (from 400μg/ml) in both methods and similar to the positive patterns (BHT and quercetin). The chromatographic profile of volatile oil compounds showed a great richness in terpene substances, pulegone, menthone and neomenthol, being its major constituents. The hydroalcoholic extracts revealed the presence of reducing compounds, polysaccharides, tannins, triterpenes, sterols and coumarins as major phytoconstituents. In the acute toxicity study, a single dose of 4000 and 8000 mg/kg b.w., produced no mortality and no clinical signs of disease were observed after 48 h. The essential oil at a single dose of 2000 and 5000 mg/kg of body weight did not produce treatment-related signs of toxicity or mortality in all rats tested during the 14 day observation period. These findings are encouraging to continue studies for the validation of popular use and development of a phytopharmaceutical with medicinal utility.

322-328

Authors: A. Laxmi Raj*, Y. Shravan Kumar

Nebivolol is a pharmaceutical drug used for the treatment of Hypertension. It is characterized with poor solubility which limits its absorption and dissolution rate which delays onset of action. In the present study, fifteen formulations of solid dispersions were prepared with 1:1:1, 1:5:2 and 1:3:1.5 ratios of drug: carrier: surfactant by solvent evaporation method. There was significant improvement in the rate of drug release from all 15 solid dispersions and the formulation (SD14) comprising Nebivolol: Kleptose HPB: SLS in 1:5:2 ratio has shown enhanced solubility about 42 folds and significant improvement in the rate of drug release i.e. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Nebivolol has been converted into an amorphous form from crystalline within the solid dispersion formulation. The present study demonstrated that formulation of Nebivolol solid dispersion is a highly effective strategy for enhancing the bioavailability of poorly water soluble drug Nebivolol.

335-341

Authors: Kota Ravi Kumar*, Gande Suresh

The present study was designed to formulate and evaluate the Olmesartan sodium alginate microspheres. Fourteen formulations batches of microspheres (S1-S14) were prepared by using ionotropic gelation method. Sodium alginate, calcium chloride, ethyl cellulose, HPMC K15M was selected in the formulations. The effect of polymer and cross-linking agent on particle size (68.18 ± 0.06), % yield (98.34%), entrapment efficiency (97.36%), and drug release were studied. From the evaluation parameters S11 was found to be optimized and the highest drug release 96.98 ± 5.28 with in 12 h in controlled manner when compared with other parameters. From release order kinetics the drug release from microspheres was followed zero order with anomalous Non fickian diffusion. The prepared microspheres compatibility studies and morphological studies were investigated by Fourier-transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM), found to be compatible with the polymers. Thus, Olmesartan microspheres could be the best choice in the effective management of hypertensive with better patient compliance for prolonged period of time.

111-117

Authors: Mamta Kumari*, Madan L. Kaushik

Skin cancer is the most common malignancy worldwide, including malignant melanoma and Non-malignant melanoma. The progressive increase in the incidence of skin cancers is observed, mainly in cutaneous melanomas over the last few decades. UV exposure is the most common cause of skin cancer, which occurs due to mutations in the DNA of skin cells. The mutation in MAPK pathway was the main cause of the skin cancer, in which BRAF gene undergoes 75 somatic mutations. The mutation in DNA suppressed the tumor suppressor gene p53, inactivates DNA repair gene and causes mutation in proto-oncogene results in the formation of oncogene which promote the cell growth, cell proliferation and cell reproduction by affecting the process of apoptosis. Skin cancer can be prevented by healthy dietary intervention and regular physical activity. In the current review, we highlight recent global trends in the treatments of skin cancer which involve chemotherapy, radiotherapy, photodynamic therapy, biological therapy and surgery. These therapies show the effectiveness by improving the survival rate and quality of life.

125-130

Authors: Medipalli Viswaja, D.V.R.N Bhikshapathi*

The objective of the present investigation is focused on the preparation of solid dispersions containing Nevirapine. The effect of various hydrophilic polymers on the aqueous solubility was studied. Kolliphor P188 was selected as carrier and solid dispersions were prepared by solvent evaporation technique. Evaluation of solid dispersion for percentage yield, drug content and solubility were most appropriate. Solid dispersions of drug: Kolliphor P188 and SLS (1:3:1 ratio) (SE9) shown higher dissolution rate i.e. 98.6% compared with and pure drug (37.5%) and other formulations. Powder X-ray diffraction performed on solid dispersion showed that Nevirapine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Nevirapine to an amorphous form. Therefore, the solid dispersions prepared by solvent evaporation method using Kolliphor P188 as hydrophilic carrier can be successfully used for improvement of solubility and dissolution of Nevirapine. Both in vitro dissolution testing and the in vivo studies demonstrated that the solubility and bioavailability of Nevirapine were significantly improved when formulated in a solid dispersion with Kolliphor P188 and SLS. The present study demonstrated that formulation of Nevirapine solid dispersion by solvent evaporation technique is a highly effective strategy for enhancing the bioavailability of poorly water soluble Nevirapine.

139-143

Authors: Darshan Bhatt1*, Padmini Thatavarthi2, B. Rajkamal1

A simple and sensitive reverse phase high performance liquid chromatographic method was developed and successively validated for the estimation of Canagliflozin. In the new method, Canagliflozin separation was carried out by the nonpolar inertsil ODS-3 (250 × 4.6 mm, 5μ) column with a mobile phase composition of Ammonium acetate buffer (pH-4.5) and Acetonitrile in the ratio of 30:70% v/v. Canagliflozin was determined at 252 nm using UV detection and the compound was eluted at the retention time of 4.5 min. As per International Conference on Harmonization (ICH) guidelines, the method was validated and the parameters were precision, accuracy, linearity, limit of detection, limit of quantitation and robustness. The chromatographic method was accurate, linear, specific, precise and robust. The results of method concluded that the proposed RP-HPLC method is useful, convenient and reliable in regular analysis of Canagliflozin in bulk and its formulation.

150-157

Authors: Brij Mohan Singh*, Ayushi Jain, Anoop Mishra

Cosmetics market has been increasing tremendously in the world and providing a way in which a person can change his or her appearance and make the product instantly noticeable and attractable. Most consumers use cosmetic and personal care products every day to protect their health, enhance their well-being and boost their self-esteem. Ranging from antiperspirants, fragrances, make-up and shampoos, to soaps, sunscreens and toothpastes, cosmetics play an essential role in all stages of our life and have important functional and emotional benefits. The cosmetics industry is a science-driven, fast paced and a highly innovative sector which grows four folds annually which makes a significant social and economic contribution to national and regional economies across worldwide. Through the purchase of goods and services and the payment of taxes the cosmetics industry generates multiple rounds of economic spending worldwide. Considering globalization of Cosmetics, the regulatory compliance with international regulations is the first step towards ensuring that are safe for humans and the environment, and to subsequently create or re-develop products that respond to the ever-changing expectations of consumers of international markets. The cosmetic industry, from manufacturers to traders, must be able to adapt to a constantly changing framework. Even if there is a tendency to unite cosmetic legislations across countries, enough differences remain and may result in lack of compliance and product recalls or sanctions. In this article, we examine and establish the need for harmonization of regulations globally.

165-172

Authors: Keerthi Priya, D.V. R. N. Bhikshapathi*

In the present investigation, self-nanoemulsifying drug delivery system (SNEDDS), of Lovastatin is being formulated to increase the solubility and bioavailability. The optimized Lovastatin SNEDDS formulation (F8) has a composition of Acrysol EL 135 as oil phase, Lauro glycol 90 and Capmul MCM as surfactant and co-surfactant respectively. Formulation F8 was found to be best formulation based on evaluation parameters. No drug precipitation or phase separation was observed in the optimized formulation. The particle size of the optimized formulation was found to be 4.9 nm & Z-Average of 71.5 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -13.7 mV which comply with the requirement of the zeta potential for stability. Furthermore, pharmacokinetic studies in rats indicated that compared to the pure drug, the optimized SMEDDS formulation significantly improved the oral bioavailability of Lovastatin. Therefore, from our results the study suggests that the Lovastatin loaded self-nanoemulsifying formulation has a great potential for clinical application.

186-193

Authors: Bosco Lawarence, Murugan K*

To evaluate the anti-metastatic potentialities of purified anthocyanin from Osbeckia aspera (L.) Blume. and O. reticulata Bedd. against selected human cancer cell lines such as HT29 colon, MG63 bone and HeLa cervical by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, apoptosis and DNA fragmentation test. Anthocyanin was extracted from the in vitro callus culture of the Osbeckia species, purified using amberlite column chromatography and fractionated by LC-MS/MS. Anthocyanin producing callus cultures were trialed on MS medium fortified with various combinations of phytohormones and sucrose. Significant callus formation in O. aspera was initiated in cultures containing 0.5 mg/L of 2, 4-D and 0.5 mg/L BA, while that in O. reticulata was initiated with 1.2 mg/L BA and 1.4 mg/L NAA. The same hormonal combinations on sub-culturing turned white friable callus into red compact callus. Purified anthocyanins obtained from O. aspera and O. reticulata contained Malvidin-3 -diglucoside, delphinidin, cyanindin aglycone and Peonidin. Osbeckia species displayed differential responses against the HT29 colon, MG63 bone and HeLa cervical cancer cell lines in terms of IC50 values of toxicity. O. aspera was more effective against HeLa cervical cell lines (23.7µg/ml) followed by HT29 colon (64.7µg/ml) as compared to O. reticulata. Poor selectivity index was noticed with bone cancer cell lines. The results were substantiated by apoptotic analysis and DNA fragmentation results. The overall results suggest that the purified anthocyanin of O. aspera and O. reticulata was excellent as antimetastatic and warrant further studies to isolate novel compounds for chemotherapeutic use.

201-205

Authors: Bhetanabotla Chandramowli1*, B M Syam Kumar1, D. V. R. N. Bhikshapathi2, Bigala B Rajkamal1

A simple, precise and accurate RP-HPLC technique was developed and the developed method was validated for the regular analysis of Boceprevir. Chromatographic analysis was performed by selecting X-Terra ODS ( C18) column (4.6 mm i.d. × 250 mm, 5μ), Acetonitrile : Phosphate buffer pH -3 ( 90 : 10% v/v) as mobile phase, 1.0 ml/min as flow rate and 20μl injection volume. The LC chromatographic peak was eluted at 3.6 min at 235 nm as UV detection wavelength. The developed method was validated as per the ICH guidelines and the Validation parameters were specificity, accuracy, linearity, precision, LOD and LOQ. Linear relationship for Boceprevir established in the concentration range of 50 to 150μg/mL. Accuracy in terms of percentage recovery found in the range between 98 to 101%. LOD and LOQ values were found to be 2.3 and 7.123μg/mL respectively. The results of the method established that the new RP-HPLC method is convenient and simple in regular analysis of Boceprevir in bulk and capsule formulation.

57-64

Authors: F-Z Ennacerie1, F Rhazi Filali1*, N Moukrad1, M Bouidra2, A Bentayeb2

The purpose of this study is to promote the plant spontaneous, harvested from the West of Morocco and streamline its use in quantifying the total phenolic content, assessing the antioxidant activity and testing the degree of toxicity on two types of eukaryotic cells plants and animals. The content, extracts aqueous and ethanolic flower buds and fruit, in phenolic compounds was determined according to the method Follin-Ciocalteu. The antioxidant activity was evaluated by two methods FRAP and DPPH. As for the cytotoxicity extracts, it has been evaluated by the test hemolysis and inhibition germination test of Lepidium sativum seeds. The different extracts of the two organs of this plant, have revealed richness in total polyphenols, especially those of the flower buds, as well as, an antioxidant activity, which is in the same order as that of vitamin C for the aqueous extract of flower buds. The effect hemolytic is shown positive for decoctat of flower buds. The ethanolic extract of fruits displayed an activity antimitotic expressed by the inhibition of elongation and growth seedlings of Lepedium sativum. The decoctat of flower exhibited an effect antigerminatif of moderate intensity which is reversible after rehydration of seed. Capparis Spinosa is a plant of quality pharmaceutical interesting for its activities antioxidant, antimitotic, healing, and for its wealth in phenolics compounds.

71-76

Authors: A.Aparna1, C.M. Shalina2, D.V.R.N.Bhikshapathi3*

The current objective of the investigation was to fabricate Pirenzepine loaded microspheres for the treatment of gastritis delivered through oral route. The microspheres were prepared by ionotropic gelation technique using sodium as alginate polymer and calcium chloride as cross-linking agent. The effect of polymer and cross-linking agent on particle size, shape, % yield, entrapment efficiency, and drug release were studied. The prepared microspheres morphology and physicochemical properties of were investigated by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Among the total S14 formulations, S7 formulation was optimized at 2.2% of sodium alginate, 7% of calcium chloride maintained100rpm for 10 min at room temperature. The optimized S7 formulation displayed the %EE 94.10%, particle size 82.45 ± 0.09µm, % yield 96.30% and swelling index of 95.13%. From In vitro drug release studies S7 shown 97.17 ± 0.28% up to 12 h in 0.1N HCl, and the drug release followed the zero order and Korsmeyer-Peppas model (R2 = 0.987, 0.995) respectively, indicating the possible drug release mechanism to be by erosion and diffusion. The marketed product showed the drug release of 95.23 ± 0.21% within 1 h. The optimized S7 formulation subjected to stability studies for 6months as per ICH guidelines, no appreciable difference was observed hence the S7 formulation found stable. The data obtained thus suggest that a micro particulate system can be successfully designed for sustained delivery of Pirenzepine and to improve its bioavailability.

85-94

Authors: Jeetu Gangil1*, Bhaswat S. Chakraborty2

Artemisinin and its derivatives such as artesunate, arteether and artemether are the primary and effective treatment of choice as per WHO malaria treatment guideline for the treatment of severe malaria although various endemic countries are using quinine for the treatment of severe malaria. The objective of this meta-analysis was to evaluate the efficacy and safety of artemisinin and its derivatives compared with quinine as parenteral antimalarial therapy for treating severe malaria in children. From the year 1990 to the year 2015, studies were identified using database searches, citation searches of selected articles. The electronic databases searched engines: Pubmed, Web of Science, Global Health, Medline & Cochrane review of Journals up to April 2015. We selected published randomized controlled clinical trials (RCTs) information comparing artemisinin derivatives with quinine and route of administration was either intravenous or intramuscular for treatment of severe malaria in paediatric population as per WHO malaria treatment guideline, any gender, age group up to 15 years of children who were diagnosed with confirmed malaria by RDT or slide test. The primary outcome was efficacy in terms of parasite clearance time (PCT) and fever clearance time (FCT) in paediatrics population. The secondary outcome was the mortality, coma resolution time (CRT) and neurological sequelae at the time of discharge in the paediatric population. We assessed identified articles on the basis of clinical trial eligibility, the risk of bias and extracted data as per objective of this research for the desired outcomes. We measured 95% confidence interval by the using of REVMAN software version 5.3 for meta-analysis and summarized the collected data on the basis of characteristics of inclusion criteria of articles such as risk ratio (RR) for dichotomous outcomes and mean difference (MD) for continuous outcomes. We included total 17 RCTs, enrolling 7220 paediatric patients who were suffering from severe or complicated malaria and these trials were conducted in various countries in the world. Artemisinin derivatives showed mean PCT (MD -8.53 hours, 95% CI -9.44 to -7.62) and mean FCT (MD -9.42 hours, 95% CI -11.12 to -7.71) shorter and statistically significant (P<0.00001) as compared with quinine therapy. We evaluated secondary outcomes mortality, mean coma resolution time (CRT) and the risk of neurological sequelae at the time of discharge in paediatric malaria patients which was observed; (RR 0.82, 95% CI 0.72 to 0.93; 17 trials, 7220 participants, P=0.002), (MD -5.37 hours, 95% CI -7.70 to -3.05; nine trials, 591 participants, P<0.00001) and (RR 1.07, 95% CI 0.89 to 1.28; nine trials, 5939 participants, P=0.49), respectively. This meta-analysis of RCT addresses the evidence for various aspects in the treatment of severe malaria in the paediatric population although limitation of availability of published information in studies furthermore research on paediatric malaria population is required to overcome from challenges drug resistance, patient compliance and less adverse effect.