World Academy of Science, Engineering and Technology

Authors: P. S. Rajinikanth, Yeoh Suyu, Sanjay Garg

Abstract:

The present study is aim to prepare and evaluate the selfnanoemulsifying drug delivery (SNEDDS) system of a poorly water soluble drug valsartan in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. The present research work describes a SNEDDS of valsartan using labrafil M 1944 CS, Tween 80 and Transcutol HP. The pseudoternary phase diagrams with presence and absence of drug were plotted to check for the emulsification range and also to evaluate the effect of valsartan on the emulsification behavior of the phases. The mixtures consisting of oil (labrafil M 1944 CS) with surfactant (tween 80), co-surfactant (Transcutol HP) were found to be optimum formulations. Prepared formulations were evaluated for its particle size distribution, nanoemulsifying properties, robustness to dilution, self emulsication time, turbidity measurement, drug content and invitro dissolution. The optimized formulations are further evaluated for heating cooling cycle, centrifugation studies, freeze thaw cycling, particle size distribution and zeta potential were carried out to confirm the stability of the formed SNEDDS formulations. The prepared formulation revealed t a significant improvement in terms of the drug solubility as compared with marketed tablet and pure drug.

Keywords: Self Emulsifying Drug Delivery System, Valsartan, Bioavailability, poorly soluble drug.

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Authors: Rajan Rajabalaya, Li-Qun Tor, Sheba David

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Transdermal delivery of ondansetron hydrochloride (OdHCl) can prevent the problems encountered with oral ondansetron. In previously conducted studies, effect of amount of polyvinyl pyrrolidone, permeation enhancer and casting solvent on the physicochemical properties on OdHCl were investigated. It is feasible to develop ondansetron transdermal patch by using ethyl cellulose and polyvinyl pyrrolidone with dibutyl pthalate as plasticizer, however, the desired flux is not achieved. The primary aim of this study is to use dimethyl succinate (DMS) and propylene glycol that are not incorporated in previous studies to determine their effect on the physicochemical properties of an OdHCl transdermal patch using ethyl cellulose and polyvinyl pyrrolidone. This study also investigates the effect of permeation enhancer (eugenol and phosphatidylcholine) on the release of OdHCl. The results showed that propylene glycol is a more suitable plasticizer compared to DMS in the fabrication of OdHCl transdermal patch using ethyl cellulose and polyvinyl pyrrolidone as polymers. Propylene glycol containing patch has optimum drug content, thickness, moisture content and water absorption, tensile strength, and a better release profile than DMS. Eugenol and phosphatidylcholine can increase release of OdHCl from the patches. From the physicochemical result and permeation profile, a combination of 350mg of ethyl cellulose, 150mg polyvinyl pyrrolidone, 3% of total polymer weight of eugenol, and 40% of total polymer weight of propylene glycol is the most suitable formulation to develop an OdHCl patch. OdHCl release did not increase with increasing the percentage of plasticiser. DMS 4, PG 4, DMS 9, PG 9, DMS 14, and PG 14 gave better release profiles where using 300mg: 0mg, 300mg: 100mg, and 350mg: 150mg of EC: PVP. Thus, 40% of PG or DMS appeared to be the optimum amount of plasticiser when the above combination where EC: PVP was used. It was concluded from the study that a patch formulation containing 350mg EC, 150mg PVP, 40% PG and 3% eugenol is the best transdermal matrix patch compositions for the uniform and continuous release/permeation of OdHCl over an extended period. This patch design can be used for further pharmacokinetic and pharmacodynamic studies in suitable animal models.

Keywords: Ondansetron hydrochloride, dimethyl succinate, eugenol.

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Authors: Patrick Nwabueze Okechukwu, Ima Nirwana Soelaiman, Gabriele Anisah Ruth Froemming, Mohd Yusri Idorus, Norazlina Mohamed

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Supplementation of palm vitamin E has been reported to prevent loss of bone density in ovariectomised female rats. The mechanism by which palm vitamin E exerts these effects is still unknown. We hypothesized that palm vitamin E may act by preventing the protein expression changes. Two dimensional poly acyrilamide gel electrophoresis (2-D PAGE) and PD Quest software genomic solutions Investigator (proteomics) was used to analyze the differential protein expression profile in femoral and humeri bones harvested from three groups of rats; sham-operated rats (SO), ovariectomised rats (Ovx) and ovariectomised rats supplemented for 2 months with palm vitamin E. The results showed that there were over 300 valued spot on each of the groups PVE and OVX as compared to about 200 in SO. Comparison between the differential protein expression between OVX and PVE groups showed that ten spots were down –regulated in OVX but up-regulated in PVE. The ten differential spots were separately named P1-P10. The identification and understanding of the pathway of the differential protein expression among the groups is ongoing and may account for the molecular mechanism through which palm vitamin E exert its anti-osteoporotic effect.

Keywords: Palm vitamin E, ovariectomised, osteoporosis protein expression, 2-d-page.

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Authors: N. K. Fuloria, S. Fuloria

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Alpinia galanga is rhizome, generally known as Greater galangal and is selected for isolation of newer constituents accountable for various therapeutic activities. Present study is intended to isolate glycoside from Alpinia galanga rhizomes. Alpinia galanga methanolic extract was column chromatograph and eluted with ethyl acetate-methanol (99:1) to isolate compound β-Sitosterol Diarabinoside. Herein, the isolation and structural elucidation of new compound is described. Chemical investigation of methanolic extract of rhizomes of Alpinia galanga furnished a new compound β- Sitosterol Diarabinoside. The IR, NMR and MASS investigations of isolated compound confirmed its structure as β-Sitosterol Diarabinoside, which is isolated for the first time from a medicinal plant or any synthetic source.

Keywords: Alpinia galanga, methanolic extract, β-Sitosterol Diarabinoside.

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Authors: So-young Jung, Bu-chuhl Choe, Gi-young Shin, Jung-hun Kim, Young-zoo Chae

Abstract:

A sensitive and specific method for quantitative determination of aflatoxins(B1, B2, G1,G2), deoxynivalenol, fumonisin(B1,B2), ochratoxin A, zearalenone, T-2 and HT-2 in roasted and ground grains using liquid chromatography combined with tandem mass spectrometry. A double extraction using a phosphate buffer solution followed by methanol was applied to achieve effective co extraction of 11 mycotoxins. A multitoxin immunoaffinity column for all these mycotoxins was used to clean up the extract. The LODs of mycotoxins were 0.1~6.1 μg/kg, LOQs were 0.3~18.4 μg/kg. Forty seven samples collected from Seoul (Korea) for mycotoxin contamination monitoring. The results showed that the occurrence of zearalenone and deoxynivalenol were frequent. Zearalenone was detected in all samples and deoxynivalenol was detected in 80.9 % samples in the range 0.626 ~ 29.264 μg/kg and N.D ~ 48.332 μg/kg respectively. Fumonisins and ochratoxin A were detected in 46.8% samples and 17 % samples respectively, aflatoxins and T-2/HT-2 toxins were not detected all samples.

Keywords: LC-MS/MS, mycotoxins, roasted and ground grains.

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Authors: Diky Mudhakir, Satrialdi, Sukmadjaja Asyarie, Yeyet C. Sumirtapura

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Today, cancer remains one of the major diseases that lead to death. The main obstacle in chemotherapy as a main cancer treatment is the toxicity to normal cells due to Multidrug Resistance (MDR) after the use of anticancer drugs. Proposed solution to overcome this problem is the use of MDR efflux inhibitor of cinchona alkaloids which is delivered together with anticancer drugs encapsulated in the form of polymeric nanoparticles. The particles were prepared by the hydration method. The characterization of nanoparticles was particle size, zeta potential, entrapment efficiency and in vitro drug release. Combination nanoparticle size ranged 29-45 nm with a neutral surface charge. Entrapment efficiency was above 87% for the use quinine, quinidine or cinchonidine in combination with etoposide. The release test results exhibited that the cinchona alkaloids release released faster than that of etoposide. Collectively, cinchona alkaloids can be packaged along with etoposide in nanomicelles for better cancer therapy.

Keywords: Cinchona alkaloids, etoposide, MDR efflux inhitor, polymeric nanomicelles.

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Authors: Surender Singh Jadav, Venkatesan Jayaprakash, Arijit Basu, Barij Nayan Sinha

Abstract:

Chikungunya virus (CHICKV) is an arboviruses belonging to family Tagoviridae and is transmitted to human through by mosquito (Aedes aegypti and Aedes albopictus) bite. A large outbreak of chikungunya has been reported in India between 2006 and 2007, along with several other countries from South-East Asia and for the first time in Europe. It was for the first time that the CHICKV outbreak has been reported with mortality from Reunion Island and increased mortality from Asian countries. CHICKV affects all age groups, and currently there are no specific drugs or vaccine to cure the disease. The need of antiviral agents for the treatment of CHICKV infection and the success of virtual screening against many therapeutically valuable targets led us to carry out the structure based drug design against Chikungunya nSP2 protease (PDB: 3TRK). Highthroughput virtual screening of publicly available databases, ZINC12 and BindingDB, has been carried out using the Openeye tools and Schrodinger LLC software packages. Openeye Filter program has been used to filter the database and the filtered outputs were docked using HTVS protocol implemented in GLIDE package of Schrodinger LLC. The top HITS were further used for enriching the similar molecules from the database through vROCS; a shape based screening protocol implemented in Openeye. The approach adopted has provided different scaffolds as HITS against CHICKV protease. Three scaffolds: Indole, Pyrazole and Sulphone derivatives were selected based on the docking score and synthetic feasibility. Derivatives of Pyrazole were synthesized and submitted for antiviral screening against CHICKV.

Keywords: Chikungunya, nsP2 protease, ADME filter, HTVS, Docking, Active site.

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Authors: Jin Sun Oh, Kyung Ho Lee, S ang Gug Chung, Kyehan Rhee

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Microbubbbles incorporating ultrasound have been used to increase the efficacy of targeted drug delivery, because microstreaming induced by cavitating bubbles affects the drug perfusion into the target cells and tissues. In order to clarify the physical effects of microstreaming on drug perfusion into tissues, a preliminary experimental study of perfusion enhancement by a stably oscillating microbubble was performed. Microstreaming was induced by an oscillating bubble at 15 kHz, and perfusion of dye into an agar phantom was optically measured by histology on agar phantom. Surface color intensity and the penetration length of dye in the agar phantom were increased more than 70% and 30%, respectively, due to the microstreaming induced by an oscillating bubble. The mass of dye perfused into a tissue phantom for 30 s was increased about 80% in the phantom with an oscillating bubble. This preliminary experiment shows the physical effects of steady streaming by an oscillating bubble can enhance the drug perfusion into the tissues while minimizing the biological effects.

Keywords: Bubble, Mass Transfer, Microstreaming, Drug Delivery, Acoustic Wave.

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Authors: Raniah Al-Shalabi, Omaima Al- Gohary, Samar Afify, Eram Eltahir

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Acetaminophen (Paracetamol) tablets are popular OTC products among patients as analgesics and antipyretics. Paracetamol is marketed by a lot of suppliers around the world. The aim of the present investigation was to compare between many types of paracetamol tablets obtained from different suppliers (six brands produced by different pharmaceutical companies in middle east countries, and Panadol® manufactured in Ireland), by different quality control tests according to USP pharmacopeia.Using Non official tests-hardness and friability; official tests- disintegration, dissolution, and drug content. Additionally, evaluate the influence of temperatures 4°C, 25°C and 40°C at 75% relative humidity on the stability of the same brands in their original packaging has been conducted for two months. The results revealed that all paracetamol tablet brands complied with the official USP specifications. In conclusion, paracetamol tablets preferred to be stored at 25°C. All the tested brands being biopharmaceutically and chemically equivalent.

Keywords: Non official tests-hardness and friability, official tests –disintegration, dissolution, and drug content.

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Authors: Mehani M., Segni L.

Abstract:

The plant world is the source of many medicines. Recently, researchers have estimated that there are approximately 400,000 plant species worldwide, of which about a quarter or a third have been used by societies for medicinal purposes. The human uses of plants for thousands of years to treat various ailments, in many developing countries, much of the population trust in traditional doctors and their collections of medicinal plants to treat them. Essential oils have many therapeutic properties. In herbal medicine, they are used for their antiseptic properties against infectious diseases of fungal origin, against dermatophytes, those of bacterial origin. The aim of our study is to determine the antimicrobial effect of essential oils of the plant Trigonella focnum greacum on some pathogenic bacteria, it is a medicinal plant used in traditional therapy. The test adopted is based on the diffusion method on solid medium (Antibiogram), this method determines the sensitivity or resistance of a microorganism vis-à-vis the extract studied. Our study reveals that the essential oil of the plant Trigonella focnum greacum has a different effect on the resistance of germs. For staphiloccocus Pseudomonnas aeroginosa and Krebsilla, are moderately sensitive strains, also Escherichia coli and Candida albicans represents a high sensitivity. By against Proteus is a strain that represents a weak sensitivity.

Keywords: essential oil, microorganisme, antibiogram

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Authors: D. Mohd Nazrul Hisham, J. Mohd Lip, R. Suri, H. Mohamed Shafit, Z.Kharis, K. Shazlin, A. Normah, M.F. Nurul Nabilah

Abstract:

Presence of phytosterol compound in Durian seed (Durio zibethinus) or known as King of fruits has been discovered from screening work using reagent test. Further analysis work has been carried out using mass spectrometer in order to support the priliminary finding. Isolation and purification of the major phytosterol has been carried out using an open column chromatography. The separation was monitored using thin layer chromatography (TLC). Major isolated compounds and purified phytosterol were identified using mass spectrometer and nuclear magnetic resonance (NMR). This novel finding could promote utilization of durian seeds as a functional ingredient in food products through production of standardized extract based on phytosterol content.

Keywords: Agrowaste, durian, seed, phytosterol

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Authors: M. Petchsangsai, N. Wonglertnirant, T. Rojanarata, P. Opanasopit, T. Ngawhirunpat

Abstract:

The objective of the present study was to evaluate the potential of hollow microneedles for enhancing the transdermal delivery of Bovine Serum Albumin (MW~66,000 Da)-Fluorescein Isothiocyanate (BSA-FITC) conjugate, a hydrophilic large molecular compound. Moreover, the effect of different formulations was evaluated. The series of binary mixtures composed of propylene glycol (PG) and pH 7.4 phosphate buffer solution (PBS) was prepared and used as a medium for BSA-FITC. The results showed that there was no permeation of BSA-FITC solution across the neonatal porcine skin without using hollow microneedles, whereas the cumulative amount of BSA-FITC released at 8 h through the neonatal porcine skin was about 60-70% when using hollow microneedles. Furthermore, the results demonstrated that the higher volume of PG in binary mixtures injected, the lower cumulative amount of BSA-FITC released and release rate of BSA-FITC from skin. These release profiles of BSA-FITC in binary mixtures were expressed by Fick-s law of diffusion. These results suggest the utilization of hollow microneedle to enhance transdermal delivery of protein and provide useful information for designing an effective hollow microneedle system.

Keywords: Hydrophilic macromolecules, Microneedles, Propylene glycol, Transdermal drug delivery

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Authors: Mária Stachová, Lukáš Sobíšek

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Data mining incorporates a group of statistical methods used to analyze a set of information, or a data set. It operates with models and algorithms, which are powerful tools with the great potential. They can help people to understand the patterns in certain chunk of information so it is obvious that the data mining tools have a wide area of applications. For example in the theoretical chemistry data mining tools can be used to predict moleculeproperties or improve computer-assisted drug design. Classification analysis is one of the major data mining methodologies. The aim of thecontribution is to create a classification model, which would be able to deal with a huge data set with high accuracy. For this purpose logistic regression, Bayesian logistic regression and random forest models were built using R software. TheBayesian logistic regression in Latent GOLD software was created as well. These classification methods belong to supervised learning methods. It was necessary to reduce data matrix dimension before construct models and thus the factor analysis (FA) was used. Those models were applied to predict the biological activity of molecules, potential new drug candidates.

Keywords: data mining, classification, drug design, QSAR

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Authors: Ghulam Murtaza, Kalsoom Farzana

Abstract:

The aim of this article is to narrate the utility of novel simulation approach i.e. convolution method to predict blood concentration of drug utilizing dissolution data of salbutamol sulphate microparticulate formulations with different release patterns (1:1, 1:2 and 1:3, drug:polymer). Dissolution apparatus II USP 2007 and 900 ml double distilled water stirrd at 50 rpm was employed for dissolution analysis. From dissolution data, blood drug concentration was determined, and in return predicted blood drug concentration data was used to calculate the pharmacokinetic parameters i.e. Cmax, Tmax, and AUC. Convolution is a good biwaiver technique; however its better utility needs it application in the conditions where biorelevant dissolution media are used.

Keywords: Convolution, Dissolution, Pharmacokinetics, Salbutamol sulphate

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Authors: E. Aboutaleb, R. Dinarvand

Abstract:

The purpose of this work was to inspect the potential of vincristine-dextran complex loaded solid lipid nanoparticles for drug delivery to the brain. The nanoparticles were stained with a fluorescence dye and their plasma pharmacokinetic and brain concentrations were investigated following injection to rats. The result revealed a significant improvement in the plasma concentration profile of the SLN injected animals as well as a sharp increased concentration in the brains.

Keywords: Brain, Coumarin-6, Nanoparticles, SLN.

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Authors: Rungsinee Phongpradist, Sawitree Chiampanichayakul, Singkome Tima, Teruna J. Siahaan, Cory J. Berkland, Songyot Anuchapreeda, Chadarat Ampasavate

Abstract:

The expression of LFA-1 diverges from the physiological condition, thus active targeting carrier can provide the benefits from difference into LFA-1 expression in various conditions. Here, the selectivity of cIBR-conjugated nanoparticles (cIBR-NPs), in terms of uptake, was investigated using PBMCs, Mixed PBMCMolt- 3 cells and Molt-3 cells. The expressions of LFA-1 on Molt-3 cells, from flow cytometry and Western blot, possessed the highest level whereas PBMCs showed the lowest level. The kinetic uptake profiles of cIBR-NPs were obtained by flow cytometry, which the degree of cellular uptake presented a similar trend with the level of LFA-1 indicating the influence of LFA-1 expression on the cellular uptake of cIBR-NPs. The conformation of LFA-1 had a slight effect on the cellular uptake of cIBR-NPs. Overall we demonstrated that cIBR-NPs enhanced cellular uptake and improved the selectivity of drug carriers to LFA-1 on the leukemia cells, which related with the order of LFA-1 expression.

Keywords: cIBR, LFA-1, Molt-3, PBMCs

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Authors: Entela Haloci, Stefano Manfredini, Vilma Toska, Silvia Vertuani, Paola Ziosi, Irma Topi, Henri Kolani

Abstract:

Antifungal activities of ether and methanolic extracts of volatiles oils of Nigella Sativa seeds were tested against pathogenic bacterias and fungies strains.The volatile oil were found to have significant antifungal and antibacterial activities compare to tetracycline, cefuroxime and ciprofloxacin positive controls.The ether and methanolic esxtracts were compared to each other for antifungal and antibacterial activities and ether extracts showed stonger activity than methanolic one.

Keywords: Antifungal, antibacterial, essential oils, extraction, Nigella Sativa.

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Authors: Achara Dholvitayakhun, Nathanon Trachoo

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In this study, the forty Thai medicinal plants were used to screen the antibacterial activity against Campylobacter jejuni. Crude 95% ethanolic extracts of each plant were prepared. Antibacterial activity was investigated by the disc diffusion assay, and MICs and MBCs were determined by broth microdilution. The results of antibacterial screening showed that five plants have activity against C.jejuni including Adenanthera pavonina L., Moringa oleifera Lam., Annona squamosa L., Hibiscus sabdariffa L. and Eupotorium odortum L. The extraction of A. pavonina L. and A. squamosa L. produced an outstanding against C. jejuni, inhibiting growth at 62.5-125 and 250-500 μg/mL, respectively. The MBCs of two extracts were just 4-fold higher than MICs against C. jejuni, suggesting the extracts are bactericidal against this species. These results indicate that A. pavonina and A. squamosa could potentially be used in modern applications aimed at treatment or prevention of foodborne disease from C. jejuni.

Keywords: Antibacterial activity, Thai medicinal plants, Campylobacter jejuni

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Authors: Hong Ding, Fatiha Benslimane, Isra Marei, Chris R. Triggle

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Hyperglycaemia is a key factor that contributes to the development of diabetes-related microvascular disease and a major risk factor for endothelial dysfunction. In the current study, we have explored glucose-induced abnormal intracellular calcium (Ca2+ i) homeostasis in mouse microvessel endothelial cells (MMECs) in high glucose (HG) (40mmol/L) versus control (low glucose, LG) (11 mmol/L). We demonstrated that the exposure of MMECs to HG for 3 days did not change basal Ca2+ i, however, there was a significant increase of acetylcholine-induced Ca2+ entry. Western blots illustrated that exposure to HG also increased STIM1 (Stromal Interaction Molecule 1), but not Orai1 (the pore forming subunit), protein expression levels. Although the link between HG-induced changes in STIM1 expression, enhanced Ca2+ entry and endothelial dysfunction requires further study, the current data are suggestive that targeting these pathways may reduce the impact of HG on endothelial function.

Keywords: store-operated calcium entry, hyperglycaemia, STIM1, endothelial dysfunction

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Authors: Shujaat A. Khan, Ghulam Murtaza

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This presentation narrates the comparative analysis of the dissolution data nimesulide microparticles prepared with ethylcellulose, hydroxypropyl methylcellulose, chitosan and Poly(D,L-lactide-co-glycolide) as polymers. The analysis of release profiles showed that the variations noted in the release behavior of nimesulide from various microparticulate formulations are due to the nature of used polymer. In addition, maximum retardation in the nimesulide release was observed with HPMC (floating particles). Thus HPMC miacroparticles may be preferably employed for sustained release dosage form development.

Keywords: Nimesulide, microparticles, ethylcellulose, hydroxypropyl methylcellulose, chitosan and Poly(D, L-lactide-coglycolide).

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Authors: Leila Amjad, Zohreh Alizad

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Recent years have instance that there is a invigoration of interest in drug discovery from medicinal plants for the support of health in all parts of the world . This study was designed to examine the in vitro antimicrobial activities of the flowers and leaves methanolic and ethanolic extracts of Chenopodium album L. Chenopodium album Linn. flowers and leaves were collected from East Esfahan, Iran. The effects of methanolic and ethanolic extracts were tested against 4 bacterial strains by using disc,well-diffusion method. Results showed that flowers and leaves methanolic and ethanolic extracts of C.album don-t have any activity against the selected bacterial strains. Our study has indicated that ,there are effective different factors on antimicrobial properties of plant extracts

Keywords: Chennopodium album, antibacterial activity, extract

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Authors: Baharak Khoshkholgh-Sima, Soroush Sardari, Jalal Izadi Mobarakeh, Ramezan Ali Khavari-Nejad

Abstract:

There is an urgent need to develop novel Mycobacterium tuberculosis (Mtb) drugs that are active against drug resistant bacteria but, more importantly, kill persistent bacteria. Our study structured based on integrated analysis of metabolic pathways, small molecule screening and similarity Search in PubChem Database. Metabolic analysis approaches based on Unified weighted used for potent target selection. Our results suggest that pantothenate synthetase (panC) and and 3-methyl-2-oxobutanoate hydroxymethyl transferase (panB) as a appropriate drug targets. In our study, we used pantothenate synthetase because of existence inhibitors. We have reported the discovery of new antitubercular compounds through ligand based approaches using computational tools.

Keywords: In Silico, Ligand-based Virtual Screening, Metabolic Pathways, Mycobacterium tuberculosis

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Authors: Aditi Shukla, Ambarish S. Vidyarthi, Subir Samanta

Abstract:

The worldwide prevalence of H3N2 influenza virus and its increasing resistance to the existing drugs necessitates for the development of an improved/better targeting anti-influenza drug. H3N2 influenza neuraminidase is one of the two membrane-bound proteins belonging to group-2 neuraminidases. It acts as key player involved in viral pathogenicity and hence, is an important target of anti-influenza drugs. Oseltamivir is one of the potent drugs targeting this neuraminidase. In the present work, we have taken subtype N2 neuraminidase as the receptor and probable analogs of oseltamivir as drug molecules to study the protein-drug interaction in anticipation of finding efficient modified candidate compound. Oseltamivir analogs were made by modifying the functional groups using Marvin Sketch software and were docked using Schrodinger-s Glide. Oseltamivir analog 10 was detected to have significant energy value (16% less compared to Oseltamivir) and could be the probable lead molecule. It infers that some of the modified compounds can interact in a novel manner with increased hydrogen bonding at the active site of neuraminidase and it might be better than the original drug. Further work can be carried out such as enzymatic inhibition studies; synthesis and crystallizing the drug-target complex to analyze the interactions biologically.

Keywords: H3N2 Influenza, Neuraminidase, Oseltamiviranalogs, structure based drug designing

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Authors: Abalaka, M. E., Daniyan, S. Y., Adeyemo, S. O.

Abstract:

Studies were carried out to determine the in vitro susceptibility of the typhoid pathogens to combined action of Euphorbia hirta, Euphorbia heterophylla and Phyllanthus niruri. Clinical isolates of the typhoid bacilli were subjected to susceptibility testing using agar diffusion technique and the minimum inhibitory concentration (MIC) determined with tube dilution technique. These isolates, when challenged with doses of the extracts from the three medicinal plants showed zones of inhibition as wide as 26±0.2mm, 22±0.1mm and 18±0.0mm respectively. The minimum inhibitory concentration (MIC) revealed organisms inhibited at varying concentrations of extracts: E. hirta (S. typhi 0.250mg/ml, S. paratyphi A 0.125mg/ml, S. paratyphi B 0.185mg/ml and S. paratyphi C 0.225mg/ml), E. heterophylla (S. typhi 0.280mg/ml, S. paratyphi A 0.150mg/ml, S. paratyphi B 0.200mg/ml and S. paratyphi C 0.250mg/ml) and P. niruri (S. typhi 0.150mg/ml, S. paratyphi A 0.100mg/ml, S. paratyphi B 0.115mg/ml and S. paratyphi C 0.125mg/ml). The results of the synergy between the three plants in the ration of 1:1:1 showed very low MICs for the test pathogens as follows S. typhi 0.025mg/ml, S. paratyphi A 0.080mg/ml, S. paratyphi B 0.015mg/ml and S. paratyphi C 0.10mg/ml with the diameter zone of inhibition (DZI) ranging from 35±0.2mm, 28±0.4mm, 20±0.1mm and 32±0.3mm respectively. The secondary metabolites were identified using simple methods and HPLC. Organic components such as anthroquinones, different alkaloids, tannins, 6-ethoxy-1,2,3,4-tetrahydro-2,2,4-trimethyl and steroids were identified. The prevalence of Salmonellae, a deadly infectious disease, is still very high in parts of Nigeria. The synergistic action of these three plants is very high. It is concluded that pharmaceutical companies should take advantage of these findings to develop new anti-typhoid drugs from these plants.

Keywords: A Prevalence, Susceptibility, Synergistic, Typhoid pathogens.

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Authors: S. Angalaparameswari, T.S. Mohamed Saleem, M. Alagusundaram, S. Ramkanth, V.S. Thiruvengadarajan, K. Gnanaprakash, C. Madhusudhana Chetty, G. Pratheesh

Abstract:

The present research was designed to investigate the anti-microbial activity of aristolochic acid from the root of Aristolochia bracteata. From the methanolic & ethyl extract extracts of Aristolochia bracteata aristolochic acid I was isolated and conformed through IR, NMR & MS. The percentage purity of aristolochic acid I was determined by UV & HPLC method. Antibacterial activity of extracts of Aristolochia bracteata and the isolated compound was determined by disc diffusion method. The results reveled that the isolated aristolochic acid from methanolic extract was more pure than the compound from ethyl acetate extract. The various extracts (500μg/disc) of Aristolochia bracteata showed moderate antibacterial activity with the average zone of inhibition of 7-18 mm by disc diffusion method. Among the extracts, ethyl acetate & methanol extracts were shown good anti-microbial activity and the growth of E.coli (18 mm) was strongly inhibited. Microbial assay of isolated compound (Aristolochic acid I) from ethyl acetate & methanol extracts were shown good antimicrobial activity and the zone of inhibition of both at higher concentration 50 μg/ml was similar with the standard aristolochic acid. It may be concluded that the isolated compound of aristolochic acid I has good anti-bacterial activity.

Keywords: Aristolochic acid I, Anti-microbial activity, Aristolochia bracteata, Bacillus subtilis, E.coli

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Authors: N. Haghjou, M. J. Abdekhodaie, Y. L. Cheng, M. Saadatmand

Abstract:

Intravitreal injection (IVI) is the most common treatment for eye posterior segment diseases such as endopthalmitis, retinitis, age-related macular degeneration, diabetic retinopathy, uveitis, and retinal detachment. Most of the drugs used to treat vitreoretinal diseases, have a narrow concentration range in which they are effective, and may be toxic at higher concentrations. Therefore, it is critical to know the drug distribution within the eye following intravitreal injection. Having knowledge of drug distribution, ophthalmologists can decide on drug injection frequency while minimizing damage to tissues. The goal of this study was to develop a computer model to predict intraocular concentrations and pharmacokinetics of intravitreally injected drugs. A finite volume model was created to predict distribution of two drugs with different physiochemical properties in the rabbit eye. The model parameters were obtained from literature review. To validate this numeric model, the in vivo data of spatial concentration profile from the lens to the retina were compared with the numeric data. The difference was less than 5% between the numerical and experimental data. This validation provides strong support for the numerical methodology and associated assumptions of the current study.

Keywords: Posterior segment, Intravitreal injection (IVI), Pharmacokinetic, Modelling, Finite volume method.

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Authors: A. Maitarad, P. Maitarad

Abstract:

In order to find the particular interaction energy between cylcloguanil and the amino acids surrounding the pocket of wild type and quadruple mutant type PfDHFR enzymes, the MP2 method with basis set 6-31G(d,p) level of calculations was performed. The obtained interaction energies found that Asp54 has the strongest interaction energy to both wild type and mutant type of - 12.439 and -11.250 kcal/mol, respectively and three amino acids; Asp54, Ile164 and Ile14 formed the H-bonding with cycloguanil drug. Importantly, the mutation at Ser108Asn was the key important of cycloguanil resistant with showing repulsive interaction energy.

Keywords: Cycloguanil, DHFR, malaria disease, interactionenergy, quantum calculations

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Authors: G. Spada, E. Gavini, P. Giunchedi

Abstract:

Aim of this work was to compare the efficacy of two loading methods of proteins onto polymeric nanocarriers: adsorption and encapsulation methods. Preliminary studies of protein loading were done using Bovine Serum Albumin (BSA) as model protein. Nanocarriers were prepared starting from polylactic co-glycolic acid (PLGA) polymer; production methods used are two different variants of emulsion evaporation method. Nanoparticles obtained were analyzed in terms of dimensions by Dynamic Light Scattering and Loading Efficiency of BSA by Bradford Assay. Loaded nanoparticles were then submitted to in-vitro protein dissolution test in order to study the effect of the delivery system on the release rate of the protein.

Keywords: Drug delivery, nanoparticles, PLGA, proteinadsorption, protein encapsulation.

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Authors: M. M. Mon, S. S. Maw, Z. K. Oo

Abstract:

Antioxidant activities of ethanolic extracts of Ardisia japonica Blume., Ageartum conyzoides Linn., and Cocculus hirsutus Linn Diels. leaves was determined qualitatively and quantitatively in this research. 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical solution was used to investigate free radical scavenging activity of these leaves extracts. Ascorbic acid (Vitamin C) was used as the standard. In the present investigation, it is found that all of these extracts have remarkable antioxidant activities. The EC50 values of these ethanolic extracts were 12.72 μg/ml for A. japonica, 15.19 μg/ml for A. conyzoides, 10.68 μg/ml for C. hirsutus respectively. Among these Myanmar medicinal plants, C. hirsutus showed higher antioxidant activities as well as free radical scavenging activity than black tea (Camellia sinensis), the famous antioxidant, and A. japonica and A. conyzoides showed a rather lower antioxidant activity than tea extracts. According to results from bioassay with carrot discs infected with Agrobacterium tumefaciens, all extracts showed anti-tumor activity after 3 weeks of incubation. No gall was detected in carrot disks treated with C. hirsutus and A. japonica extracts in the dose of 100ppm and in carrot discs treated with A. conyzoides extract in the dose of 1000 ppm. Therefore, the research clearly indicates that these weedy plants of dry farm land are exceptionally advantageous for human health.

Keywords: Antioxidant, Anti-tumor activity, Carrot-discbioassay, DPPH

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Authors: Mahmood Ahmad, Asadullah Madni, Muhammad Usman, Abubakar Munir, Naveed Akhtar, Haji M. Shoaib Khan

Abstract:

This article demonstrated development of controlled release system of an NSAID drug, Diclofenac sodium employing different ratios of Ethyl cellulose. Diclofenac sodium and ethyl cellulose in different proportions were processed by microencapsulation based on phase separation technique to formulate microcapsules. The prepared microcapsules were then compressed into tablets to obtain controlled release oral formulations. In-vitro evaluation was performed by dissolution test of each preparation was conducted in 900 ml of phosphate buffer solution of pH 7.2 maintained at 37 ± 0.5 °C and stirred at 50 rpm. At predetermined time intervals (0, 0.5, 1.0, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, 20 and 24 hrs). The drug concentration in the collected samples was determined by UV spectrophotometer at 276 nm. The physical characteristics of diclofenac sodium microcapsules were according to accepted range. These were off-white, free flowing and spherical in shape. The release profile of diclofenac sodium from microcapsules was found to be directly proportional to the proportion of ethylcellulose and coat thickness. The in-vitro release pattern showed that with ratio of 1:1 and 1:2 (drug: polymer), the percentage release of drug at first hour was 16.91 and 11.52 %, respectively as compared to 1:3 which is only 6.87 % with in this time. The release mechanism followed higuchi model for its release pattern. Tablet Formulation (F2) of present study was found comparable in release profile the marketed brand Phlogin-SR, microcapsules showed an extended release beyond 24 h. Further, a good correlation was found between drug release and proportion of ethylcellulose in the microcapsules. Microencapsulation based on coacervation found as good technique to control release of diclofenac sodium for making the controlled release formulations.

Keywords: Diclofenac sodium, Microencapsulationtechnology, Ethylcellulose, In-Vitro Release Profile

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