World Academy of Science, Engineering and Technology

Authors: Sanvidhan G. Suke

Abstract:

This article briefly reviews the role of Indian Pharmacopoeia Commission (IPC) for publications of Indian Pharmacopoeia (IP) and National formulary of India (NFI) to some of these anticipated changes, informs constituents about how they can remain updated about progress and upcoming modifications to official texts, and invites participation in the standards-setting process, which are helpful to the practitioners, researchers, educators and policy makers in the field of health care profession.

Keywords: Addendum, Indian Pharmacopoeia, Monograph, National Formulary of India.

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Authors: Ritu Shitak

Abstract:

Humans are social mammals, of the primate order. Our biology, our behaviour and our pathologies are unique to us. In our desire to understand, reduce solitary confinement one source of information is the many reports of social isolation of other social mammals, especially primates. A behavioural study was conducted in the department of pharmacology at Indira Gandhi Medical College, Shimla in Himachalpradesh province in India using white albino mice. Different behavioural parameters were observed by using open field, tail suspension, tests for aggressive behaviour and social interactions and the effect of isolation was studied. The results were evaluated and the standard statistics were applied. The said study was done to establish facts that isolation itself impairs social behaviour and can lead to alcohol dependence as well as related drug dependence.

Keywords: Albino Mice, Drug Dependence, Social isolation.

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Authors: Wan Azuati Wan Omar, Selva Rani John Jasudass, Siti Rohaiza Md Saad

Abstract:

Background: The objectives of this study were to assess patient’s knowledge of appropriate sublingual glyceryl trinitrate (GTN) use as well as to investigate how patients commonly store and carry their sublingual GTN tablets. Methodology: This was a cross-sectional survey, using a validated researcher-administered questionnaire. The study involved cardiac patients receiving sublingual GTN attending the outpatient and inpatient departments of Taiping Hospital, a non-academic public care hospital. The minimum calculated sample size was 92, but 100 patients were conveniently sampled. Respondents were interviewed on 3 areas, including demographic data, knowledge and use of sublingual GTN. Eight items were used to calculate each subject’s knowledge score and six items were used to calculate use score. Results: Of the 96 patients who consented to participate, majority (96.9%) were well aware of the indication of sublingual GTN. With regards to the mechanism of action of sublingual GTN, 73 (76%) patients did not know how the medication works. Majority of the patients (66.7%) knew about the proper storage of the tablet. In relation to the maximum number of sublingual GTN tablets that can be taken during each angina episode, 36.5% did not know that up to 3 tablets of sublingual GTN can be taken during each episode of angina. Fifty four (56.2%) patients were not aware that they need to replace sublingual GTN every 8 weeks after receiving the tablets. Majority (69.8%) of the patients demonstrated lack of knowledge with regards to the use of sublingual GTN as prevention of chest pain. Conclusion: Overall, patients’ knowledge regarding the self-administration of sublingual GTN is still inadequate. The findings support the need for more frequent reinforcement of patient education, especially in the areas of preventive use, storage and drug stability.

Keywords: Glyceryl trinitrate, knowledge, adherence.

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Authors: Travis J. Meyer, Jasodra Ramlall, Phyo Thu, Nidhi Gadura

Abstract:

For centuries humans have used the antimicrobial properties of copper to their advantage. Yet, after all these years the underlying mechanisms of copper mediated cell death in various microbes remain unclear. We had explored the hypothesis that copper mediated increased levels of lipid peroxidation in the membrane fatty acids is responsible for increased killing in Escherichia coli. In this study we show that in both gram positive (Staphylococcus aureus) and gram negative (Pseudomonas aeruginosa) bacteria there is a strong correlation between copper mediated cell death and increased levels of lipid peroxidation. Interestingly, the non-spore forming gram positive bacteria as well as gram negative bacteria show similar patterns of cell death, increased levels of lipid peroxidation, as well as genomic DNA degradation, however there is some difference in loss in membrane integrity upon exposure to copper alloy surface.

Keywords: Antimicrobial, copper, gram positive, gram negative.

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Authors: Zayed N. Alsulami, Asma F. Aldosseri, Ahmed S. Ezziden, Abdulrahman K. Alonazi

Abstract:

Children are more susceptible to medication errors than adults. Medication administration process is the last stage in the medication treatment process and most of the errors detected in this stage. Little research has been undertaken about medication errors in children in the Middle East countries. This study was aimed to evaluate how the paediatric nurses adhere to the medication administration policy and also to identify any medication preparation and administration errors or any risk factors. An observational, prospective study of medication administration process from when the nurses preparing patient medication until administration stage (May to August 2014) was conducted in Saudi Arabia. Twelve paediatric nurses serving 90 paediatric patients were observed. 456 drug administered doses were evaluated. Adherence rate was variable in 7 steps out of 16 steps. Patient allergy information, dose calculation, drug expiry date were the steps in medication administration with lowest adherence rates. 63 medication preparation and administration errors were identified with error rate 13.8% of medication administrations. No potentially life-threating errors were witnessed. Few logistic and administrative factors were reported. The results showed that the medication administration policy and procedure need an urgent revision to be more sensible for nurses in practice. Nurses’ knowledge and skills regarding to the medication administration process should be improved.

Keywords: Double checking, Medication administration errors, Medication safety, Nurses.

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Authors: J. Y. Tan, L. C. Lum, M. G. Lee, S. Mansouri, K. Hapgood, X. D. Chen, M. W. Woo

Abstract:

Folic acid (FA) is known to be an important supplement to prevent neural tube defect (NTD) in pregnant women. Similar to some commercial formulations, sodium bicarbonate solution is used as a solvent for FA. This work uses the antisolvent vapour precipitation (AVP), incorporating ethanol vapour as the convective drying medium in place of air to produce branch-like micro-structure FA particles. Interestingly, the dissolution rate of the resultant particle is 2-3 times better than the particle produce from conventional air drying due to the higher surface area of particles produced. The higher dissolution rate could possibly improve the delivery and absorption of FA in human body. This application could potentially be extended to other commercial products, particularly in less soluble drugs to improve its solubility.

Keywords: Absorption, antisolvent vapour precipitation, dissolution rate, folic acid.

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Authors: Deepak K. Semwal, Ruchi B. Semwal, Aijaz Ahmad, Guy P. Kamatou, Alvaro M. Viljoen

Abstract:

Kigelia africana (Lam.) Benth. (Bignoniaceae) is a reputed traditional remedy for various human ailments such as skin diseases, microbial infections, melanoma, stomach troubles, metabolic disorders, malaria and general pains. In spite of the fruit being widely used for purposes related to its antibacterial and antifungal properties, the chemical constituents associated with the activity have not been fully identified. To elucidate the active principles, we evaluated the antimicrobial activity of fruit extracts and purified fractions against Staphylococcus aureus, Enterococcus faecalis, Moraxella catarrhalis, Escherichia coli, Candida albicans and Candida tropicalis. Shade-dried fruits were powdered and extracted with hydroalcoholic (1:1) mixture by soaking at room temperature for 72 h. The crude extract was further fractionated by column chromatography, with successive elution using hexane, dichloromethane, ethyl acetate, acetone and methanol. The dichloromethane and ethyl acetate fractions were combined and subjected to column chromatography to furnish a wax and oil from the eluates of 20% and 40% ethyl acetate in hexane, respectively. The GC-MS and GC×GC-MS results revealed that linoleic acid, linolenic acid, palmitic acid, arachidic acid and stearic acid were the major constituents in both oil and wax. The crude hydroalcoholic extract exhibited the strongest activity with MICs of 0.125-0.5 mg/mL, followed by the ethyl acetate (MICs = 0.125-1.0 mg/mL), dichloromethane (MICs = 0.250-2.0 mg/mL), hexane (MICs = 0.25- 2.0 mg/mL), acetone (MICs = 0.5-2.0 mg/mL) and methanol (MICs = 1.0-2.0 mg/mL), whereas the wax (MICs = 2.0-4.0 mg/mL) and oil (MICs = 4.0-8.0 mg/mL) showed poor activity. The study concludes that synergistic interactions of chemical constituents could be responsible for the antimicrobial activity of K. africana fruits, which needs a more holistic approach to understand the mechanism of its antimicrobial activity.

Keywords: Kigelia Africana, traditional medicine, antimicrobial activity, Candida albicans, palmitic acid, synergistic interaction.

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Authors: N. K. Fuloria, S. Fuloria, R. Gupta

Abstract:

Esterification of p-bromo-m-cresol led to formation of 2-(4-bromo-3-methylphenoxy)acetate (1). 2-(4-Bromo-3-methyl phenoxy)acetohydrazide (2) is derived from Compound (1) by hydrazination. Compound (2) was reacted with different aromatic aldehydes to yield N-(substituted benzylidiene)-2-(4-bromo-3-methyl phenoxy)acetamide(3a-c). Cyclization of compound (3a-c) with thioglycolic acid yielded 2-(4-bromo-3-methylphenoxy)-N-(4-oxo-2- arylthiazolidin-3-yl) acetamide (4a-c). The newly synthesized compounds were characterized on the basis of spectral studies and evaluated for antibacterial and antifungal activities.

Keywords: Imines, Thiazolidinone, Schiff base, Antimicrobial.

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Authors: S. Buloyan, V. Mamikonyan, H. Hakobyan, H. Harutyunyan, H. Gasparyan

Abstract:

The liver is the strongest regenerating organ of the organism, and even with 2/3 surgically removed, it can regenerate completely. Hence liver cirrhosis may only develop when the regenerating system is off. We present the results of a comparative study of structural and functional characteristics of rat liver tissue under the conditions of toxic liver cirrhosis development, induced by carbon tetrachloride, and its prevention/treatment by natural compounds with antioxidant and immune stimulating action. Studies were made on Wister rats, weighing 120~140 g. Grape seeds extracts, separately and in combination with well-known anticirrhotic drug ursodeoxycholic acid (Urdoxa), have demonstrated effectiveness in prevention of liver cirrhosis development and its treatment.

Keywords: Carbon tetrachloride, GSE, liver cirrhosis, prevention, treatment.

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Authors: P. Narrima, C. Y. Looi, M. A. Mohd, H. M. Ali

Abstract:

Persea declinata (Bl.) Kosterm is a member of the Lauraceae family, widely distributed in Southeast Asia. It is from the same genus with avocado (Persea americana Mill), which is widely consumed as food and for medicinal purposes. In the present study, we examined the anticancer properties of Persea declinata (Bl.) Kosterm bark methanolic crude extract (PDM). PDM exhibited a potent antiproliferative effect in MCF-7 human breast cancer cells, with an IC50 value of 16.68 .g/mL after 48h of treatment. We observed that PDM caused cell cycle arrest and subsequent apoptosis in MCF-7 cells, as exhibited by increased population at G0/G1 phase, higher lactate dehydrogenase (LDH) release, and DNA fragmentation. Mechanistic studies showed that PDM caused significant elevation in ROS production, leading to perturbation of mitochondrial membrane potential, cell permeability, and activation of caspases-3/7. On the other hand, real-time PCR and Western blot analysis showed that PDM treatment increased the expression of the proapoptotic molecule, Bax, but decreased the expression of prosurvival proteins, Bcl-2 and Bcl-xL, in a dose-dependent manner. These findings imply that PDM could inhibit proliferation in MCF-7 cells via cell cycle arrest and apoptosis induction, indicating its potential as a therapeutic agent worthy of further development.

Keywords: Antiproliferative, apoptosis, MCF-7 human breast cancer, Persea declinata.

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Authors: Sihana Ahmeti Lika, Merita Dauti, Ledjan Malaj

Abstract:

The objective of this study is to analyze the prophylactic usage of low molecular weight heparin (LMWH) along pregnancy and the correlation between their usage and month/week of pregnancy, in the Department of Gynecology and Obstetrics, at Clinical Hospital in Tetovo. A retrospective study was undertaken during 01 January – 31 December 2012. Over of one year, the total number of patients was 4636. Among the 1447 (32.21%) pregnant women, 298 (20.59%) of them were prescribed LMWH. The majority of patients given LMWH, 119 (39.93%) were diagnosed hypercoagulable. The age group with the highest attendance was 25- 35, 141 patients (47.32%). For 195 (65.44%) patients, this was their first pregnancy. Earliest stage of using LMWH was the second month of pregnancy 4 (1.34%) cases. The most common patients were 70 women along the seventh month (23.49%), followed by 68 in the ninth month of pregnancy (22.81%). Women in the 28th gestational week, were found to be the most affected, a total of 55 (78.57%) were in that week. Clexane 2000 and Fraxiparine 0.3 were the most common for which low molecular weight heparin was prescribed. The number of patients which received Clexane 2000 was 84 (28.19%), followed by those with Fraxiparine 0.3 81 (27.18%). The administration of LMWH is associated with long hospitalization (median 14,6 days).

Keywords: Hypercoagulable state, low molecular weight heparin, month of pregnancy, pregnant women.

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Authors: A. Bouzabata, A. Boukhari

Abstract:

Curcuma longa L. (Zingiberaceae), commonly known as turmeric, has a long history of traditional uses for culinary purposes as a spice and a food colorant. The present study aimed to document the ethnobotanical knowledge about Curcuma longa, and to assess the variation in the herbalists’ experience in Northeastern Algeria. Data were collected using semi-structured questionnaires and direct interviews with 30 herbalists. Ethnobotanical indices, including the fidelity level (FL%), the relative frequency citation (RFC), and use value (UV) were determined by quantitative methods. Diversity in the level of knowledge was analyzed using univariate, non-parametric, and multivariate statistical methods. Three main categories of uses were recorded for C. longa: for food, for medicine, and for cosmetic purposes. As a medicine, turmeric was used for the treatment of gastrointestinal, dermatological, and hepatic diseases. Medicinal and food uses were correlated with both forms of preparation (rhizome and powder). The age group did not influence the use. Multivariate analyses showed a significant variation in traditional knowledge, associated with the use value, origin, quality, and efficacy of the drug. The findings suggested that the geographical origin of C. longa affected the use in Algeria.

Keywords: Curcuma longa, curcuma indices, ethnobotanical knowledge, variation.

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Authors: Mohammad Reza Naghavi, Farzad Alaeimoghadam, Hossein Ghafoori

Abstract:

Artemisia species, which are medically beneficial, are widespread in temperate regions of both Northern and Southern hemispheres among which Iran is located. About 35 species of Artemisia are indigenous in Iran among them some are widespread in all or most provinces, yet some are restricted to some specific regions. In this review paper, initially, GC-Mass results of some experiments done in different provinces of Iran are mentioned among them some compounds are common among species, some others are mostly restricted to other species; after that, medical advantages based on some researches on species of this genus are reviewed; different qualities such as anti-leishmania, anti-bacteria, antiviral as well as anti-proliferative could be mentioned.

Keywords: Artemisia, GC-Mass analysis, medical advantage.

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Authors: Nazedah Ain Ibrahim, Mohamed Mansor Manan

Abstract:

Information regarding early onset neonatal sepsis (EONS) pathogens may vary between regions. Global perspectives showed Group B Streptococcal (GBS) as the most common causative pathogens, but the widespread use of intrapartum antibiotics has changed the pathogens pattern towards gram negative microorganisms, especially E. coli. Objective of this study is to describe the pathogens isolated, to assess current treatment and risk of EONS. Records of 899 neonates born in three General Hospitals between 2009 until 2012 were retrospectively reviewed. Proven was found in 22 (3%) neonates. The majority was isolated with gram positive organisms, 17 (2.3%). All grams positive and most gram negative organisms showed sensitivity to the tested antibiotics. Only two rare gram negative organisms showed total resistant. Male was possible risk of proven EONS. Although proven EONS remains uncommon in Malaysia, nonetheless, the effect of intrapartum antibiotics still required continuous surveillance.

Keywords: Early onset neonatal sepsis, neonates, pathogens, gram positive, gram negative.

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Authors: Mohd. A. M. Rahim, Yahaya Hassan, Mathumalar L. Fahrni

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Second line antiretroviral therapy (ART) regimen is used when patients fail their first line regimen. There are many factors such as non-adherence, drug resistance as well as virological and immunological failure that lead to second line highly active antiretroviral therapy (HAART) regimen treatment failure. This study was aimed at determining predictor factors to treatment failure with second line HAART and analyzing median survival time. An observational, retrospective study was conducted in Sungai Buloh Hospital (HSB) to assess current status of HIV patients treated with second line HAART regimen. Convenience sampling was used and 104 patients were included based on the study’s inclusion and exclusion criteria. Data was collected for six months i.e. from July until December 2013. Data was then analysed using SPSS version 18. Kaplan-Meier and Cox regression analyses were used to measure median survival times and predictor factors for treatment failure. The study population consisted mainly of male subjects, aged 30- 45 years, who were heterosexual, and had HIV infection for less than 6 years. The most common second line HAART regimen given was lopinavir/ritonavir (LPV/r)-based combination. Kaplan-Meier analysis showed that patients on LPV/r demonstrated longer median survival times than patients on indinavir/ritonavir (IDV/r) based combination (p<0.001). The commonest reason for a treatment to fail with second line HAART was non-adherence. Based on Cox regression analysis, other predictor factors for treatment failure with second line HAART regimen were age and mode of HIV transmission.

Keywords: Adherence, antiretroviral therapy, second line, treatment failure.

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Authors: Aditya Arya, Hairin Taha, Ataul Karim Khan, Nayiar Shahid, Hapipah Mohd Ali, Mustafa Ali Mohd

Abstract:

This study has investigated the antidiabetic and antioxidant potential of Pseudovaria macrophylla bark extract on streptozotocin–nicotinamide induced type 2 diabetic rats. LCMSQTOF and NMR experiments were done to determine the chemical composition in the methanolic bark extract. For in vivo experiments, the STZ (60 mg/kg/b.w, 15 min after 120 mg/kg/1 nicotinamide, i.p.) induced diabetic rats were treated with methanolic extract of Pseuduvaria macrophylla (200 and 400 mg/kg·bw) and glibenclamide (2.5 mg/kg) as positive control respectively. Biochemical parameters were assayed in the blood samples of all groups of rats. The pro-inflammatory cytokines, antioxidant status and plasma transforming growth factor βeta-1 (TGF-β1) were evaluated. The histological study of the pancreas was examined and its expression level of insulin was observed by immunohistochemistry. In addition, the expression of glucose transporters (GLUT 1, 2 and 4) were assessed in pancreas tissue by western blot analysis. The outcomes of the study displayed that the bark methanol extract of Pseuduvaria macrophylla has potentially normalized the elevated blood glucose levels and improved serum insulin and C-peptide levels with significant increase in the antioxidant enzyme, reduced glutathione (GSH) and decrease in the level of lipid peroxidation (LPO). Additionally, the extract has markedly decreased the levels of serum pro-inflammatory cytokines and transforming growth factor beta-1 (TGF-β1). Histopathology analysis demonstrated that Pseuduvaria macrophylla has the potential to protect the pancreas of diabetic rats against peroxidation damage by downregulating oxidative stress and elevated hyperglycaemia. Furthermore, the expression of insulin protein, GLUT-1, GLUT-2 and GLUT-4 in pancreatic cells was enhanced. The findings of this study support the anti-diabetic claims of Pseudovaria macrophylla bark.

Keywords: Diabetes mellitus, Pseuduvaria macrophylla, alkaloids, caffeic acid.

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Authors: Pathan Imran Khan, Bhandari Anil, Kumar Amit

Abstract:

The present investigation was aimed to develop methodology for the standardization of Marichyadi Vati and its raw materials. Standardization was carried using systematic Pharmacognostical and physicochemical parameters as per WHO guidelines. The detailed standardization of Marichyadi Vati, it is concluded that there are no major differences prevailed in the quality of marketed products and laboratory samples of Marichyadi Vati. However, market samples showed slightly better amount of Piperine than the laboratory sample by both methods. This is the first attempt to generate complete set of standards required for the Marichyadi Vati.

Keywords: Marichyadi Vati, Standardization, Piperine.

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Authors: Gouda K. Helal, Marwa I. Shabayek, Heba A. El-Ramly, Heba A. Awida

Abstract:

The adverse effects of Clindamycin (Clind.) / Ibuprofen (Ibu.) combination on liver, kidney, blood elements and the significances of antioxidants (N-acetylcysteine and Zinc) against these effects were evaluated. The study includes: Group I; control n=30, Group II; patients on Clind.300mg/Ibu.400mg twice daily for a week n=30, Group III; patients on Clind.300mg/Ibu.400mg+Nacetylcysteine 200mg twice daily for a week n=15 and Group IV; patients on Clind.300mg/Ibu.400mg+Zinc50mg twice daily for a week n=15. Serum malondialdehyde (MDA), alanine transferase (ALT), aspartate transferase (AST), γ glutamyl transferase (GGT), creatinine, blood urea nitrogen (BUN) were measured. Applying one way ANOVA followed by Tuckey Kramer post test, Group II showed significant increase in ALT, AST, GGT, BUN and decrease in Hb, RBCs, platelets than Group I. Group III showed significant decrease in ALT, AST, GGT, BUN than Group II. Moreover, Group IV showed significant decrease in ALT, AST, GGT and increase in Hb, RBCs, and platelets than Group II. Conclusively, Adding Zinc or Nacetylcysteine buffer the oxidative stress and improve the therapeutic outcome of Clindamycin/Ibuprofen combination.

Keywords: Clindamycin, Ibuprofen, Adverse effects, Antioxidant, Zinc, N-acetylcysteine.

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Authors: M. Kumpugdee-Vollrath, J.-P. Krause, S. Bürk

Abstract:

Most of the drugs used for pharmaceutical purposes are poorly water-soluble drugs. About 40% of all newly discovered drugs are lipophilic and the numbers of lipophilic drugs seem to increase more and more. Drug delivery systems such as nanoparticles, micelles or liposomes are applied to improve their solubility and thus their bioavailability. Besides various techniques of solubilization, oil-in-water emulsions are often used to incorporate lipophilic drugs into the oil phase. To stabilize emulsions surface active substances (surfactants) are generally used. An alternative method to avoid the application of surfactants was of great interest. One possibility is to develop O/W-emulsion without any addition of surface active agents or the so called “surfactant-free emulsion or SFE”. The aim of this study was to develop and characterize SFE as a drug carrier by varying the production conditions. Lidocaine base was used as a model drug. The injection method was developed. Effects of ultrasound as well as of temperature on the properties of the emulsion were studied. Particle sizes and release were determined. The long-term stability up to 30 days was performed. The results showed that the surfactant-free O/W emulsions with pharmaceutical oil as drug carrier can be produced.

Keywords: Emulsion, lidocaine, Miglyol, size, surfactant, light scattering, release, injection, ultrasound, stability.

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Authors: Rawia M. Khalil, Ahmed A. Abd El Rahman, Mahfouz A. Kassem, Mohamed S. El Ridi, Mona M. Abou Samra, Ghada E. A. Awad, Soheir S. Mansy

Abstract:

Solid lipid nanoparticles (SLNs) have gained great attention for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Our work deals with the preparation of nystatin loaded solid lipid nanoparticles (NystSLNs) using the hot homogenization and ultrasonication method. The prepared NystSLNs were characterized in terms of entrapment efficiency, particle size, zeta potential, transmission electron microscopy, differential scanning calorimetry, rheological behavior and in vitro drug release. A stability study for 6 months was performed. A microbiological study was conducted in male rats infected with Candida albicans, by counting the colonies and examining the histopathological changes induced on the skin of infected rats. The results showed that SLNs dispersions are spherical in shape with particle size ranging from 83.26±11.33 to 955.04±1.09 nm. The entrapment efficiencies are ranging from 19.73±1.21 to 72.46±0.66% with zeta potential ranging from -18.9 to -38.8 mV and shear-thinning rheological Behavior. The stability studies done for 6 months showed that nystatin (Nyst) is a good candidate for topical SLN formulations. A least number of colony forming unit/ ml (cfu/ml) was recorded for the selected NystSLN compared to the drug solution and the commercial Nystatin® cream present in the market. It can be fulfilled from this work that SLNs provide a good skin targeting effect and may represent promising carrier for topical delivery of Nyst offering the sustained release and maintaining the localized effect, resulting in an effective treatment of cutaneous fungal infection.

Keywords: Candida infections, Hot homogenization, Nystatin, Solid lipid nanoparticles, Stability, Topical delivery.

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Authors: Najari Moghadam Sh., Qomi M., Raofie F., Khadiv J.

Abstract:

In this study, a liquid phase microextraction by hollow fiber (HF-LPME) combined with high performance liquid chromatography-UV detector was applied to preconcentrate and determine trace levels of Cyproheptadine in human urine and plasma samples. Cyproheptadine was extracted from 10 mL alkaline aqueous solution (pH: 9.81) into an organic solvent (n-octnol) which was immobilized in the wall pores of a hollow fiber. Then was back-extracted into an acidified aqueous solution (pH: 2.59) located inside the lumen of the hollow fiber. This method is simple, efficient and cost-effective. It is based on pH gradient and differences between two aqueous phases. In order to optimize the HF-LPME some affecting parameters including the pH of donor and acceptor phases, the type of organic solvent, ionic strength, stirring rate, extraction time and temperature were studied and optimized. Under optimal conditions enrichment factor, limit of detection (LOD) and relative standard deviation (RSD(%), n=3) were up to 112, 15 μg.L⁻¹ and 2.7, respectively.

Keywords: Biological samples, Cyproheptadine, hollow fiber, liquid phase microextraction.

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Authors: M. Hoxha, V. Capra, C. Buccellati, A. Sala, C. Cena, R. Fruttero, M. Bertinaria, G. E. Rovati

Abstract:

Today COXIBs are used in the treatment of arthritis and many other painful conditions in selected patients with high gastrointestinal risk and low cardiovascular (CV) risk. Previously, we have identified an unexpected mechanism of action of a traditional non-steroidal anti-inflammatory drug (NSAID) (diclofenac) and a specific inhibitor of cyclooxygenase-2 (COXIB) (lumiracoxib) demonstrating that they possess weak competitive antagonism at the thromboxane receptor (TP). We hypothesize that modifying the structure of a known COXIB so that it becomes also a more potent TP antagonist will preserve the anti-inflammatory and gastrointestinal safety typical of COXIBs and prevent the CV risk associated with long term therapy.

Keywords: Cyclooxygenase, inflammation, lumiracoxib, thromboxane A2.

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Authors: Amit Kumar, Ramendeep Grawal, Peeyush Sharma, Dinesh Puri, Anil Bhandari

Abstract:

The main perspective of the present study aims at overcoming solubility problems by using the technique of solid dispersion. Repaglinide is a BCS Class II drug, having low aqueous solubility and therefore, low bioavailability. Solid dispersions of repaglinide with different carriers Polyvinyl Pyrrolidone (PVP) and Ethyl Cellulose (EC) in different ratios were prepared by suspending method and Dissolving methods. In vitro release studies revealed that the F7 formulation showed extended drug release. So, the dissolution profile of solid dispersion containing EC and PVP K30 (1: 3) was selected as the best formulation because of its extended drug release among all formulations. In conclusion, solid dispersions of Repaglinide in PVP have shown to be a promising approach to improve the bioavailability of Repaglinide.

Keywords: Ethyl Cellulose, Glibenclamide, Polyvinyl Pyrrolidone, Repaglinide, Solid Dispersion.

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Authors: A. G. Abdellatif, H. M.Gargoum, A. A. Debani, M. Bengleil, S. Alshalmani, N. El Zuki, O. El Fitouri

Abstract:

In this study the administration of 660 mg/kg of the ethanolic extract of the Alhagigraecorum (Camel Thorn)to mice, showed a significant decrease in the level of transaminases in animals treated with a combination of CTE plus carbon tetrachloride (CCl₄) or acetaminophen as compared to animals receiving CCl₄ or acetaminophen alone. Histopatological investigation also confirmed that, camel thorn extract protects liver against damage-induced either by carbon tetrachloride or acetaminophen. On the other hand the cardiac toxicity produced by adriamycine was significantly increased in the presence of the ethanolic extract of camel thorn. Our study suggested that camel thorn can protect the liver against the injury produced by carbon tetrachloride or acetaminophen, with unexpected increase in the cardiac toxicity –induced by adriamycin in rodents.

Keywords: Acetaminophen, Adriamycin, Alhagi graecorum, Carbon tetrachloride.

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Authors: M. G. Tadros, S. M. Ezzat, M. M. Salama, M. A. Farag

Abstract:

In this study, the in vitro anticholinesterase activity of
the volatile oils of both O. basilicum and O. africanum was
investigated and both samples showed significant activity. The major
constituents of the two oils were isolated using several column
chromatographies. Linalool, 1,8-cineol and eugenol were isolated
from the volatile oil of O. basilicum and camphor was isolated from
the volatile oil of O. africanum. The anticholinesterase activities of
the isolated compounds were also evaluated where 1,8-cineol showed
the highest inhibitory activity followed by camphor. To confirm these
activities, learning and memory enhancing effects were tested in
mice. Memory impairment was induced by scopolamine, a
cholinergic muscarinic receptor antagonist. Anti-amnesic effects of
both volatile oils and their terpenoids were investigated by the
passive avoidance task in mice. We also examined their effects on
brain acetylcholinesterase activity. Results showed that scopolamineinduced
cognitive dysfunction was significantly attenuated by
administration of the volatile oils and their terpenoids, eugenol and
camphor, in the passive avoidance task and inhibited brain
acetylcholinesterase activity. These results suggest that O. basilicum
and O. africanum volatile oils can be good candidates for further
studies on Alzheimer’s disease via their acetylcholinesterase
inhibitory actions.

Keywords: Acetylcholinesterase, Ocimum africanum, Ocimum basilicum, passive avoidance.

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Authors: M. Kumpugdee-Vollrath, M. Tabatabaeifar, M. Helmis

Abstract:

Shellac is a natural polyester resin secreted by insects. Pectins are natural, non-toxic and water-soluble polysaccharides extracted from the peels of citrus fruits or the leftovers of apples. Both polymers are allowed for the use in the pharmaceutical industry and as a food additive. SSB Aquagold® is the aqueous solution of shellac and can be used for a coating process as an enteric or controlled drug release polymer. In this study, tablets containing 10 mg methylene blue as a model drug were prepared with a rotary press. Those tablets were coated with mixtures of shellac and one of the pectin different types (i.e. CU 201, CU 501, CU 701 and CU 020) mostly in a 2:1 ratio or with pure shellac in a small scale fluidized bed apparatus. A stable, simple and reproducible three-stage coating process was successfully developed. The drug contents of the coated tablets were determined using UV-VIS spectrophotometer. The characterization of the surface and the film thickness were performed with the scanning electron microscopy (SEM) and the light microscopy. Release studies were performed in a dissolution apparatus with a basket. Most of the formulations were enteric coated. The dissolution profiles showed a delayed or sustained release with a lagtime of at least 4 h. Dissolution profiles of coated tablets with pure shellac had a very long lagtime ranging from 13 to 17.9 h and the slopes were quite high. The duration of the lagtime and the slope of the dissolution profiles could be adjusted by adding the proper type of pectin to the shellac formulation and by variation of the coating amount. In order to apply a coating formulation as a colon delivery system, the prepared film should be resistant against gastric fluid for at least 2 h and against intestinal fluid for 4-6 h. The required delay time was gained with most of the shellac-pectin polymer mixtures. The release profiles were fitted with the modified model of the Korsmeyer-Peppas equation and the Hixson-Crowell model. A correlation coefficient (R²)> 0.99 was obtained by Korsmeyer-Peppas equation.

Keywords: Shellac, pectin, coating, fluidized bed, release, colon delivery system, kinetic, SEM, methylene blue.

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Authors: Imran Khan Pathan, Anil Bhandari, Peeyush K. Sharma, Rakesh K. Patel, Suresh Purohit

Abstract:

Floating tablets of Marichyadi Vati were developed with an aim to prolong its gastric residence time and increase the bioavailability of drug. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by wet granulation technique, using HPMC E50 LV act as Matrixing agent, Carbopol as floating enhancer, microcrystalline cellulose as binder, Sodium bi carbonate as effervescent agent with other excipients. The simplex lattice design was used for selection of variables for tablets formulation. Formulation was optimized on the basis of floating time and in vitro drug release. The results showed that the floating lag time for optimized formulation was found to be 61 second with about 97.32 % of total drug release within 3 hours. The vitro release profiles of drug from the formulation could be best expressed zero order with highest linearity r² = 0.9943. It was concluded that the gastroretentive drug delivery system can be developed for Marichyadi Vati containing Piperine to increase the residence time of the drug in the stomach and thereby increasing bioavailability.

Keywords: Piperine, Marichyadi Vati, Gastroretentive drug delivery, Floating tablet.

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Authors: D. S. Mohale, A. V. Chandewar

Abstract:

Aim- Study was undertaken to investigate the effect of altered behavioral condition like depression on various oxidative stress markers and biochemical parameters in rats. Methods- Rats were subjected for short (21 days) and long term (84 days) social isolation; the rats displayed an increase in depression on force swim test relative to control. Various markers of oxidative stress like lipid per oxidation (LPO), reduced glutathione (GSH), Supers oxide dismutase (SOD), catalase (CAT) and biochemical parameters like SGOT, SGPT, and blood glucose were determined. Results- There was significant increase in the level of LPO and decrease in the levels of GSH, SOD and CAT after long term isolation. Biochemical parameters were significantly altered after social isolation. Conclusion- Increased oxidative stress in depression which may leads to alteration of biochemical parameters.

Keywords: Depression, Glucose, LPO, Oxidative stress.

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Authors: Madhusudan Purohit, Stephen Philip, Bharathkumar Inturi

Abstract:

In this paper we report the quantitative structure activity relationship of novel bis-triazole derivatives for predicting the activity profile. The full model encompassed a dataset of 46 Bis- triazoles. Tripos Sybyl X 2.0 program was used to conduct CoMSIA QSAR modeling. The Partial Least-Squares (PLS) analysis method was used to conduct statistical analysis and to derive a QSAR model based on the field values of CoMSIA descriptor. The compounds were divided into test and training set. The compounds were evaluated by various CoMSIA parameters to predict the best QSAR model. An optimum numbers of components were first determined separately by cross-validation regression for CoMSIA model, which were then applied in the final analysis. A series of parameters were used for the study and the best fit model was obtained using donor, partition coefficient and steric parameters. The CoMSIA models demonstrated good statistical results with regression coefficient (r²) and the cross-validated coefficient (q²) of 0.575 and 0.830 respectively. The standard error for the predicted model was 0.16322. In the CoMSIA model, the steric descriptors make a marginally larger contribution than the electrostatic descriptors. The finding that the steric descriptor is the largest contributor for the CoMSIA QSAR models is consistent with the observation that more than half of the binding site area is occupied by steric regions.

Keywords: 3D QSAR, CoMSIA, Triazoles.

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Authors: Amr A. Fouad, Waleed H. Albuali, Iyad Jresat

Abstract:

The protective effect of thymoquinone (TQ) was investigated in rats exposed to testicular injury induced by sodium arsenite (10mg/kg/day, orally, for two days). TQ treatment (10mg/kg/day, intraperitoneal injection) was applied for five days, starting three day before arsenic administration. TQ significantly attenuated the arsenic-induced decreases of serum testosterone, and testicular reduced glutathione level, and significantly decreased the elevations of testicular malondialdehyde and nitric oxide levels resulted from arsenic administration. Also, TQ ameliorated the arsenic-induced testicular tissue injury observed by histopathological examination. In addition, TQ decreased the arsenic-induced expression of inducible nitric oxide synthase and caspase-3 in testicular tissue. It was concluded that TQ may represent a potential candidate to protect against arsenic-induced testicular injury. 

Keywords: Thymoquinone, arsenic, testes, rats.

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