فهرست مطالب
Pharmaceutical Sciences
Volume:22 Issue: 4, Dec 2016
- تاریخ انتشار: 1395/10/10
- تعداد عناوین: 13
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Pages 215-216
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Pages 217-226BackgroundAlthough several cases of methimazole-induced liver injury are reported, but there is no clear idea on the mechanism of methimazole hepatotoxicity. N-methyl thiourea (NMT) is a postulated hepatotoxic metabolite for methimazole. The current investigation was designed to evaluate the effect of NMT on hepatocyte mitochondria as a target of xenobiotics-induced cellular injury.MethodsIsolated liver mitochondria from healthy mice were incubated with NMT (10 µM-160 mM) (in vitro). Furthermore, mice received NMT (10, 20, 40 and 80 mg/kg, i.p) then, their liver mitochondria were isolated and assessed (in vivo). Several mitochondrial indices including mitochondrial succinate dehydrogenase activity, mitochondrial membrane potential, mitochondrial swelling, reactive oxygen species, lipid peroxidation, and mitochondrial glutathione and ATP content were assessed.ResultsNMT caused a decrease in succinate dehydrogenase activity, an increase in mitochondrial ROS formation, lipid peroxidation, and swelling along with the collapse of mitochondrial membrane potential in both in vitro and in vivo experiments. Moreover, the level of glutathione and ATP was lower in NMT-exposed mitochondria.ConclusionOur data indicate that mitochondrial dysfunction might play a major role in the mechanism of liver injury induced by the methimazole hepatotoxic metabolite.Keywords: Hepatic injury, Antithyroids hepatotoxicity, Mitochondrial dysfunction, Endocrinology, Drug, induced liver Injury (DILI)
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Pages 227-233BackgroundFormaldehyde is widely used for industrial applications. Renal injury is an adverse effect associated with formaldehyde. Few studies have explored the potential benefits of protective factors on formaldehyde induced renal toxicity. This study evaluated the dose dependent effects of sodium selenite on the biochemical and histopathological effects of formaldehyde on murine kidney.MethodsForty eight adult Balb/c male mice were randomized into six groups: a control group, a formaldehyde group and experimental III-VI groups. Formaldehyde group was injected with 10 mg/kg formaldehyde and groups III-VI received intraperitoneally doses of 0.1, 0.2, 0.4, 0.8 mg/kg selenium. After two weeks, a stereological study was done in accordance with the principle of Cavalieri and serum concentrations of urea and creatinine were measured. Data were analyzed using ANOVA and SPSS software.ResultsGlomerosclerosis, necrosis and vacuolization were observed in the convoluted tubules of animals treated with formaldehyde. The biochemical markers, volume and count of glomeruli in the group treated with formaldehyde was significantly difference compared to the control group (PConclusionsA dose of 0.2 mg/kg of sodium selenite caused partial protective effect on the renal tissue and function in exposed to formaldehyde.Keywords: Formaldehyde, selenium, kidney, Mouse
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Pages 234-243BackgroundArtemisinin is a sesquiterpene lactone chemical extract from Artemisia annua, is poorly resolvable in water and a fast-acting blood active in treating the acute attack of malaria.MethodsArtemisinin was encapsulated within mPEG-PCL micelles with a single-step nano-precipitation method, leading to formation of ART/ mPEG-PCL micelles. mPEG-PCL copolymers was characterized in vitro by HNMR, FTIR and DSC techniques. Copolymers with artemisinin were self-assembled into micelles in aqueous solution. The consequential micelles were further characterized by various techniques such as DLS and AFM.ResultsThe results exhibited the successful formation of spherical artemisinin-loaded micelles. The artemisinin-loaded micelles showed high loading efficiency. The encapsulation efficiency of artemisinin was 63±2.31%. In vitro release of artemisinin from artemisinin-entrapped micelles followed remarkably sustained release profile.ConclusionThe results indicated that the successful formulation of artemisinin loaded mPEG-PCL micelles can improve the drug delivery of artemisinin. The results showed that nanomicelles can be promising drug delivery systems for sustaining release of artemisinin.Keywords: Artemisinin, Drug delivery, Micelles, mPEG, PCL
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Pages 244-250BackgroundWet agglomeration is a method wherein the crystals of dispersion are held together in aggregates by small amount of a liquid acting as an intercrystal binder. In present study, in order to study the possible modification of agglomerate structure, low concentrations of additives (0.1-1%) were added to binder liquid.MethodsPiroxicam agglomerates were produced by wet agglomeration method by three solvent systems including a good solvent (dimethylformamide or acetone), antisolvent (water) and a binder liquid (ethylacetate or isopropylacetate). Span 80, talc, ethylcellulose and Eudragit RS in different concentrations were used as additives. The agglomerates were evaluated for production yield of agglomerates, size, friability and drug release properties.ResultsThe results showed that formation of agglomerates was possible in presence of span and talc. However, no agglomerates could be obtained with polymers tested (ethylcellulose and Eudragit RS). Talc increased agglomerate size, whereas the obtained agglomerates were more susceptible to breakup. However, using span as opposed to talc resulted in agglomerates with higher strength but smaller particle size. The dissolution tests showed that both additives adversely affected the dissolution rate of piroxicam from the agglomerates.ConclusionResult of this study suggested that additives even in small amounts played a major role in agglomerate properties.Keywords: wet agglomeration, Span 80, Talc, Binder liquid
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Pages 251-259BackgroundAlthough the stabilizing effects of cyclodextrins (CDs) on the liquid protein formulations have been proven, there is no comprehensive data on evaluation of their effects on the lyophilized antibody powders. In this study, the influence of two CD derivatives namely beta-cyclodextrin (βCD) and hydroxypropyl beta-cyclodextrin (HPβCD) was compared with trehalose and mannitol regarding the molecular and thermodynamic stability of lyophilized IgG formulations as well as its biological activity.MethodsSugars were separately added to IgG solutions and lyophilization process was conducted. In each group of carbohydrates, the formulations with lowest amounts of aggregates were examined regarding the biological activity. The storage stability of selected formulations was subsequently determined following 1 and 3 month of storage at 45 °C.ResultsTrehalose and HPβCD in the ratios of 80% showed the most stabilizing effects by control of aggregated forms in the orders of 1.02% and 0.83%, respectively. Also, it was shown that trehalose and HPβCD could incomparably preserve IgG activity in values of 100% and 96.5%. The results of DSC and SEM analysis confirmed the existence of crystalline parts in mannitol and βCD formulations of antibody. During the storage time, the lowest rate constant of aggregation was observed in formulations containing trehalose 80% (0.16/month). All prepared formulations were beta-dominant and no fragmentation was detected.ConclusionMolecular, thermodynamic and biological stability of lyophilized IgG was more desirable in the presence of trehalose and HPβCD in comparison to mannitol and βCD.Keywords: Antibody, Lyophilization, Mannitol, Trehalose, Cyclodextrins, Stability
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Pages 260-266BackgroundProbiotics are live microorganisms bringing useful effects to the host through balancing intestine microbiota. This research was undertaken to determine the suitability of fig juice as raw material for production of probiotic juice by three species of lactic acid bacteria (Lactobacillus casei, Lactobacillus plantarum and Lactobacillus delbrueckii).MethodsHeat treated fig juices were inoculated (6 log CFU/ml) by three species inocula separately and incubated at 30 °C for 72 h. Changes in the pH, acidity, reducing sugar content and viable cell counts during the fermentation were monitored. Sensory characteristics of probiotic fig juice were also evaluated.ResultsL. delbrueckii grew well on fig juice; reached nearly 9 log CFU/ml after 48 h of fermentation at 30 °C. After 4 weeks of cold storage at 4 °C, the viable cell counts of L. delbrueckii and L. plantarum were still 6 and 5 log CFU/ml, respectively, in fermented fig juice; but L. casei was just survived until 2th week of cold storage time, reduced from 9 to 3 log CFU/ml. The results of the sensory evaluation showed that fermented fig juice samples were significantly different (PConclusionL. delbrueckii was the most suitable strain from the point of survivability among other species at the consumption time. Therefore, probiotic fig juice can serve as healthy beverage for vegetarians and consumers with lactose-allergy.Keywords: Fig juice, Probiotic, Lactobacillus, Survival, Nutraceutical
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Pages 267-271BackgroundIn this study we report the production and identification of alkaloid compounds from tissue culture derived from bulb scales of Galanthus transcaucasicus Fomin (Amaryllidaceae), a medicinally important plant.MethodsExplants were prepared from bulb scales of G. transcaucasicus in vitro. The alkaloid compounds were extracted and analyzed by GC/MS.ResultsIsolation of the alkaloid fraction of the produced bulblets and its GC/MS analysis led to the identification of an Amaryllidaceae alkaloid homolycorin. Moreover, galantamine was not detected in the alkaloid fraction.ConclusionAt the present study we report the first micropropagation work on G. transcaucasicus together with the isolation of alkaloid homolycorine from in vitro produced bulblets. The results indicated that G. transcaucasicus bulblets produce Amaryllidaceae alkaloids and could be a new source of bioactive compounds for possible pharmaceutical applications. Also, described method could be used for micropropagation of plantlets from G. transcaucasicus.Keywords: Alkaloid, Galanthus, Tissue culture, Homolycorine, Amaryllidaceae, GC, MS
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Pages 272-278BackgroundRecently, because of increasing concern regarding food safety containing chemical additives, remarkable attempts have been made and progress to develop natural antibacterial compounds such as essential oils.MethodsThis study was conducted to determine antibacterial activities of Ziziphora clinopodioides essential oil (ZEO) alone and in combination with different concentrations of nisin to increase shelf life and control Salmonella typhimurium and Staphylococcus aureus in milk stored at refrigerated temperature.ResultsThe dominant constituents of ZEO in our study were carvacrol (65.22%) and thymol (19.51%). The microbial population was decreased significantly with addition of ZEO and nisin, increased their concentrations and longer storage time. It was found that milk samples containing ZEO at 0.2% and nisin at 500 IU mL-1 had significantly lower microbial population (pConclusionsBased on our findings, ZEO and nisin extended the shelf life of milk and may be used as natural antibacterial compounds in food products such as milk and dairy products.Keywords: Milk, Nisin, Salmonella typhimurium, Staphylococcus aureus, Ziziphora clinopodioides essential oil
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Pages 279-284BackgroundInfection is a serious problem in medicine and appropriate antibiotic therapy is very important. Because of broad spectrum activity and low toxicity of β-lactam antibiotics, they are the most commonly used drugs. But, bacterial resistance to β-lactam antibiotics, has been considered as the global healthcare concern. The aim of study was to evaluate the antimicrobial resistance pattern and molecular characterization among ESBL-producing Escherichia coli isolated from patients with diarrhea admitted to a hospital in Ilam, Iran.MethodsTotally, fifty E. coli isolates were investigated. Confirmatory tests for phenotypic detection of ESBLs were performed. Molecular identification of the blaTEM and blaSHV genes was carried out by PCR method. To identify genetic relatedness among isolates, Randomly Amplified Polymorphic DNA (RAPD) analysis was performed.ResultsThe antibiotic susceptibility results showed that the most effective antibiotic was imipenem and minimum effect was related to gentamicin. Thirty-one isolates (62%) were ESBL-producing organisms according to phenotypic method. The distribution of blaTEM and blaSHV genes among ESBL-producing isolates were 20 (64.5%) and 6 (19.3%), respectively. RAPD-PCR typing among isolates gave us eight different types. Twelve isolates were clustered in genotype A and all of them were ESBL-producer.ConclusionThe present study showed noticeable incidence of ESBL-producing E. coli isolated from outpatients and hospitalized patients with diarrhea. Therefore, it seems that constant supervision is crucial to monitor the ESBL-producing microorganisms in hospitals and community.Keywords: ESBL, blaTEM, blaSHV, RAPD, PCR, Escherichia coli
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Pages 285-290BackgroundRecently, antimicrobial activity of medicinal plants have attained once more importance due to drug resistance of microbial isolates to common antibiotics as well as fewer side effects and low cost of herbal products comparing to chemical drugs. Eucalyptus globules (E. globulus) has been widely applied as a natural remedy in respiratory tract infections. The present study focused on the evaluation of antibacterial effect of two commercial products of E. globulus against common microbial causes of respiratory tract infections. To this end, two commercial products of E. globules including inhaler and oral soft capsule with standard expiration date, (in three different batch numbers) were purchased from the pharmacy stores of Tabriz city.MethodsThe antibacterial efficiency of these products were investigated using Minimum Inhibitory Concentration (MIC), Minimum Bactericidal Concentration (MBC) and disk diffusion methods against Staphylococcus aureus, Streptococcus pyogenes and Pseudomona aeruginosa.ResultsBased on the obtained results, these commercial products of E. globules showed significant inhibitory effects against Gram-positive bacteria. The findings also indicated that the Eucalyptus inhaler products had more inhibitory effects than Eucalyptus oral soft capsule, however batch to batch variations were of concern.ConclusionThis research presents optimistic result on using the Eucalyptus as an alternative antibacterial agent against respiratory tract pathogenic microorganisms.Keywords: Antibacterial effect, Eucalyptus globulus, Staphylococcus aureus, Streptococcus pyogenes, Pseudomonas aeruginosa
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Pages 291-295BackgroundPreliminary safety evaluation of polymer intended to use as drug delivery carrier is essential.MethodsIn this study polyacrylamide grafted bacterial cellulose (BC/AM) hydrogel was prepared by microwave irradiation initiated free radical polymerization. The synthesized hydrogel was subjected to in vitro cytotoxicity and acute gastrointestinal toxicity studies to evaluate its biological safety as potential oral drug delivery carrier.ResultsThe results indicate that hydrogel was non cytotoxic and did not show any histopathological changes in GI tract after a high dose of oral administration.ConclusionThe results revealed that hydrogel composed of bacterial cellulose and polyacrylamide is safe as oral drug delivery carrier.Keywords: Bacterial cellulose, Polyacrylamide, Cytotoxicity, Acute oral toxicity, Microwave, Irradiation
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Pages 296-301BackgroundFruits of Bunium persicum (Boiss.) B. Fedtsch (Apiaceae) has been used as spice, anti-flatulence and antiseptic agent for many years. In recent years the wild resources of the plant have been threatened by extinction. Domestication of such a plant saves its genetic resources from depletion. However, concerns remain about the possible changes due to development of chemotypes and changes in the composition and biological and pharmacological potentials.MethodsAnalyses of essential oils from fruits of wild and cultivated types was performed using Gas Chromatography/Mass Spectroscopy. Antimicrobial assessment was done by agar diffusionResultsThe main compounds of both oils were included γ-terpinene (30.77% and 27.57%), cuminaldehyde (20.49% and 21.1%), ρ-cymene (20.1% and 18.32%) and γ-terpinen-7-al (8.29% and 7.84%) respectively. Analytical results of both tested oils exhibited very close similarities in major compounds, whereas some differences in their percentages were observed. In vitro antimicrobial evaluation of volatile oils, total extract and the resultant fractions against Staphylococcus aureus, Escherichia coli and Candida albicans demonstrated some similarities and differences. Minimum inhibitory concentrations (MICs) of wild grown fruits essential oils ranged between 0.375-1.5 mg/ml, while those of cultivated one were 0.75-6.25 mg/ml. All extracts and fractions showed similarly minor antibacterial potential while anti-Candida albicans activity was much remarkable with MICs calculated 2.5-5 mg/ml for cultivated and 5 mg/ml for wild grown extracts and fractions.ConclusionIn conclusion, despite the substantial similarities in composition of both oils, the alteration in antimicrobial results may be caused by variety in concentration of major and minor compounds and their synergism or antagonism in mixture.Keywords: Antimicrobial, Apiaceae, Bunium persicum, Essential oil, Extract