فهرست مطالب

Advanced Pharmaceutical Bulletin - Volume:7 Issue:3, 2017
  • Volume:7 Issue:3, 2017
  • تاریخ انتشار: 1396/07/10
  • تعداد عناوین: 20
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  • Behzad Mansoori, Ali Mohammadi, Sadaf Davudian, Solmaz Shirjang, Behzad Baradaran* Pages 339-348
    Anticancer drugs resistance is a complex process that arises from altering in the drug targets. Advances in the DNA microarray, proteomics technology and the development of targeted therapies provide the new strategies to overcome the drug resistance. Although a design of the new chemotherapy agents is growing quickly, effective chemotherapy agent has not been discovered against the advanced stage of cancer (such as invasion and metastasis). The cancer cell resistance against the anticancer agents can be due to many factors such as the individual’s genetic differences, especially in tumoral somatic cells. Also, the cancer drug resistance is acquired, the drug resistance can be occurred by different mechanisms, including multi-drug resistance, cell death inhibiting (apoptosis suppression), altering in the drug metabolism, epigenetic and drug targets, enhancing DNA repair and gene amplification. In this review, we outlined the mechanisms of cancer drug resistance and in following, the treatment failures by common chemotherapy agents in the different type of cancers.
    Keywords: Drug resistance, Cancer, Multi-drug resistance, microRNA, Epigenetic, Cell death inhibiting
  • Samaneh Rashtbari, Gholamreza Dehghan*, Reza Yekta, Abolghasem Jouyban, Mehrdad Iranshahi Pages 349-357
    Purpose
    The study on the interaction between various compounds and macromolecules such as enzymes has been very important for monitoring the alteration of structural and functional properties of them. Resveratrol (3, 5, 4-trihydroxy-stilbene; RES) is a biologically active phytoallexin found in grapes and other food products. This article shows an interaction of native bovine liver catalase (BLC) with natural antioxidant product, trans resveratrol (tRES) using multispectroscopic methods.
    Methods
    The interaction between BLC and tRES is performed using UV-vis absorption, fluorescence and circular dichroism (CD) spectroscopy and molecular docking study.
    Results
    In vitro kinetic studies indicated that tRES can decrease BLC activity through uncompetitive inhibition. The results of spectroscopic methods represented that the binding of tRES with BLC can change the micro-region around aromatic amino acids (tryptophan (Trp) and tyrosine (Tyr)) and quench intrinsic fluorescence of BLC by a static mechanism. According to fluorescence quenching data analysis, it was revealed that tRES has one binding site on BLC. The thermodynamic parameters were obtained, which demonstrated that tRES can bind to BLC by van der Waals forces and hydrogen bonds. Molecular docking results indicated that tRES binds to BLC away from heme group and near to the Tyr 324 and Phe 265. These results are in agreement with the experimental results.
    Conclusion
    The inhibitory effect of tRES on BLC demonstrated that excessive consumption of the antioxidants could be resulted in hazardous effects.
    Keywords: Bovine liver catalase, Molecular docking, Spectroscopy, Trans resveratrol, Uncompetitive inhibition
  • Reza Vajdi-Hokmabad, Mojtaba Ziaee, Saeed Sadigh-Eteghad, Siamak Sandoghchian Shotorbani, Javad Mahmoudi * Pages 359-365
    Purpose
    Modafinil is a vigilance-enhancing drug licensed for narcolepsy. The use of modafinil leads to various neuromodulatory effects with very low abuse potential. A body of evidence suggested that modafinil may have anti-parkinsonian effects. This study was designed to evaluate whether modafinil could improve motor dysfunction in the 6hydroxydopamine (6-OHDA)-induced rat model of Parkinson’s disease.
    Methods
    Male Wistar rats (180-220 g, n= 98) were used in this study. Parkinsonism was induced by injection of 6-hydroxydopamine (10 μg/2μl in 0.2 % ascorbic acid-saline) into the right striatum. Parkinsonian rats received intraperitoneal (ip) injections of modafinil (50, 75, and 100 mg/kg) and catalepsy-like immobility was assessed by the bar test (BT). Furthermore, involvement of dopamine D1 and D2 receptors in modafinil’s antiparkinsonian effects was studied. For this purpose, parkinsonian animals were pretreated with SCH23390 and raclopride (the dopamine D1 and D2 receptor anatgonists, respectively) or SCH23390 raclopride, and then assessed by the BT.
    Results
    Modafinil (100 mg/kg) showed anti-cataleptic effects in the BT. Notably, the effect of modafinil in the BT was reversed in parkinsonian rats pretreated with raclopride (1.25 mg/kg) and/or SCH23390 raclopride (0.75 and 1.25 mg/kg, respectively), but not in those pretreated with SCH23390 (0.75 mg/kg).
    Conclusion
    Acute administration of modafinil improves 6-OHDA-induced motor impairment possibly through activation of dopamine D2 receptors.
    Keywords: 6-hydroxydopamine, Dopaminergic neurotransmission, Modafinil, Parkinson's disease, Rat
  • Elias Adikwu, Bonsome Bokolo * Pages 367-374
    Purpose
    The therapeutic benefit derived from the clinical use of tramadol (TD) has been characterized by hepatotoxicity due to misuse and abuse. The implications of drug-induced hepatotoxicity include socio-economic burden which makes the search for remedy highly imperative. The present study investigated the protective effects of melatonin (MT) and nacetylcysteine (NAC) on TD-induced hepatotoxicity in albino rats.
    Methods
    Forty five adult rats used for this study were divided into nine groups of five rats each. The rats were pretreated with 10mg/kg/day of NAC, 10mg/kg/day of MT and combined doses of NAC and MT prior to the administration of 15 mg/kg/day of TD intraperitoneally for 7 days respectively. At the termination of drug administration, rats were weighed, sacrificed, and serum was extracted and evaluated for liver function parameters. The liver was harvested, weighed and evaluated for oxidative stress indices and liver enzymes.
    Results
    Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, total bilirubin, conjugated bilirubin, and malondialdehyde levels were significantly (P
    Conclusion
    Based on the findings in this study, melatonin and n- acetylcysteine could be used clinically as remedies for tramadol associated hepatotoxity.
    Research
    Keywords: Tramadol, Liver, Toxicity, Antioxidants, Pretreatment, Rat
  • Sri Handayani, Ratna Asmah Susidarti, Riris Istighfari Jenie, Edy Meiyanto* Pages 375-380
    Purpose
    The aim of this study is to observe the synergistic effect of two active compounds of secang, brazilin and brazilein, combined with cisplatin on WiDr colon cancer cells.
    Methods
    Cytotoxic activities of brazilin (Bi) and brazilein (Be) in single and in combination with cisplatin (Cisp) were examined by MTT assay. Synergistic effect was analyzed by combination index (CI) parameter. Apoptosis and cell cycle profiles were observed by using flow cytometry.
    Results
    The result of MTT assay showed that IC50 value of brazilin and brazilein on WiDr cancer cells were 41 µM and 52 µM respectively. The combination of ½ IC50 of Bi-Cisp reduced cells viability up to 64% and showed synergistic effect with CI value less than 1 (CI = 0.8). The combinations of ½ IC50 of Be-Cisp also reduced cells viability up to 78% and showed synergistic effect (CI=0.65). Combination of Bi-Cisp and Be-Cisp induced apoptosis higher than the single treatments. Further analysis on the cell cycle progression showed that single treatment of ½ IC50 of Be and Bi induced S-phase and G2/M-phase accumulation, while combination of Be-Cisp and Bi-Cisp enhanced S-phase accumulation.
    Conclusion
    Both combination of Bi-Cisp and Be-Cisp showed synergistic effect on WiDr cells through induction of apoptosis and halted the cell cycle progression, thus, WiDr cells growth were significantly reduced.
    Keywords: Brazilin, Brazilein, Caesalpinia sappan, L., Cisplatin, Synergistic effect, WiDr cells
  • Elham Safarzadeh, Abbas Delazar, Tohid Kazemi, Mona Orangi, Dariush Shanehbandi, Solmaz Esnaashari, Leila Mohammadnejad, Saeed Sadigh-Eteghad, Ali Mohammadi, Mehrdad Ghavifekr Fakhr, Behzad Baradaran * Pages 381-389
    Purpose
    Breast cancer is the most frequent malignancy diagnosed in women both in developed and developing countries. Natural products especially those from herbal origin have high potential in producing drug components with a source of novel structures. The present study was designed to explore the cytotoxic effects and the cell death mechanism of Scrophularia atropatana extracts.
    Methods
    MTT assay was employed to evaluate the cytotoxic activity of the extracts of S. atropatana on the MCF-7 as well as non-malignant cells. Furthermore, induction of apoptosis was evaluated by TUNEL assay, cell death detection ELISA, DNA fragmentation test, western blotting and Real Time PCR.
    Results
    In vitro exposures of the MCF-7 cells with different concentration of S. atropatana extract significantly inhibited their growth and viability and induced apoptosis in the MCF7 cells. Cleavage PARP protein, decrease in the mRNA expression levels of bcl-2 and increase expression of Caspase-3 and Caspase-9 mRNA, highlights that the induction of apoptosis was the main mechanism of cell death. Moreover the expression study of Caspase-9 mRNA showed that, the extracts have induced apoptosis via intrinsic mitochondrial pathway.
    Conclusion
    Our results demonstrated that dichloromethane extract of Scrophularia atropatana has an apoptotic effects and it can be developed as anticancer agents.
    Keywords: Scrophularia atropatana, Breast cancer, Extract, Apoptosis, MCF-7, Cytotoxic
  • Afsaneh Vazin, Iman Karimzadeh *, Atiyeh Zand, Nazafarin Hatami-Mazinani, Dena Firouzabadi Pages 391-397
    Purpose
    To evaluate colistin use according to global standard drug consumption in intensive care units of a referral hospital in Shiraz, Iran
    Methods
    A prospective, interventional study was performed during an 11 month period on 100 patients admitted to ICUs of a teaching hospital being treated with colistin for at least 3 subsequent doses. Required demographic, clinical, and paraclinical data were gathered by a pharmacist. Fifteen indexes were considered to evaluate colistin use. A clinical pharmacist reviewed indication and dose of colistin at the time of prescribing this agent.
    Results
    In our study population, pneumonia (69%) was the main indication of colistin. In 87% of patients, colistin administration was based on microbiological laboratory evidence. Continuation of therapy was inappropriate in 5% of cases. By the intervention of the clinical pharmacist, colistin was discontinued in all patients in whom empirical therapy was continued incorrectly. None of the patients received loading dose of colistin. The maintenance dose, dose interval, and duration of treatment of colistin were appropriate in 76%, 71%, and 100% of patients, respectively. For none of the patients, the pharmacokinetic dosing method was used. In all patients, serum creatinine and WBC count were evaluated on daily basis. The sum indexes of colistin use were relevant to standard guidelines in 67.33% of the cases.
    Conclusion
    The results of this study highlight the necessity of the pharmaceutical care team participation in all stages of treatment with antibiotics. After pharmacist interventions, some criteria of colistin utilization were corrected and brought closer to standard values.
    Keywords: Colistin guideline, Adherence, Clinical Pharmacist, Intensive care unit
  • Prabhakar Panzade*, Giridhar Shendarkar, Sarfaraj Shaikh, Pavan B. Rathi Pages 399-408
    Purpose
    Cocrystallisation of drug with coformers is a promising approach to alter the solid sate properties of drug substances like solubility and dissolution. The objective of the present work was to prepare, formulate and evaluate the piroxicam cocrystal by screening various coformers.
    Methods
    Cocrystals of piroxicam were prepared by dry grinding method. The melting point and solubility of crystalline phase was determined. The potential cocrystal was characterized by DSC, IR, XRPD. Other pharmaceutical properties like solubility and dissolution rate were also evaluated. Orodispersible tablets of piroxicam cocrystal were formulated, optimized and evaluated using 32 factorial design.
    Results
    Cocrystals of piroxicam-sodium acetate revealed the variation in melting points and solubility. The cocrystals were obtained in 1:1 ratio with sodium acetate. The analysis of Infrared explicitly indicated the shifting of characteristic bands of piroxicam. The X-Ray Powder Diffraction pattern denoted the crystallinity of cocrystals and noteworthy difference in 2θ value of intense peaks. Differential scanning calorimetry spectra of cocrystals indicated altered endotherms corresponding to melting point. The pH solubility profile of piroxicam showed sigmoidal curve, which authenticated the pKa-dependent solubility. Piroxicam cocrystals also exhibited a similar pH-solubility profile. The cocrystals exhibited faster dissolution rate owing to cocrystallization as evident from 30% increase in the extent of dissolution. The orodispersible tablets of piroxicam cocrystals were successfully prepared by direct compression method using crosscarmelose sodium as superdisintegrant with improved disintegration time (30 sec) and dissolution rate.
    Conclusion
    The piroxicam cocrystal with modified properties was prepared with sodium acetate and formulated as orodispersible tablets having faster disintegration and greater dissolution rate.
    Keywords: Cocrystal, Dissolution, Factorial design, Orodispersible tablet, Piroxicam, Solubility
  • Behzad Jafari, Maryam Hamzeh-Mivehroud, Ali Akbar Alizadeh, Mehdi Sharifi, Siavoush Dastmalchi * Pages 409-418
    Purpose
    Receptor tyrosine kinase (RTK) inhibitors are widely used pharmaceuticals in cancer therapy. Fibroblast growth factor receptors (FGFRs) are members of RTK superfamily which are highly expressed on the surface of carcinoma associate fibroblasts (CAFs). The involvement of FGFRs in different types of cancer makes them promising target in cancer therapy and hence, the identification of novel FGFR inhibitors is of great interest. In the current study we aimed to develop an alignment independent three dimensional quantitative structure-activity relationship (3D-QSAR) model for a set of 26 FGFR2 kinase inhibitors allowing the prediction of activity and identification of important structural features for these inhibitors.
    Methods
    Pentacle software was used to calculate grid independent descriptors (GRIND) for the active conformers generated by docking followed by the selection of significant variables using fractional factorial design (FFD). The partial least squares (PLS) model generated based on the remaining descriptors was assessed by internal and external validation methods.
    Results
    Six variables were identified as the most important probes-interacting descriptors with high impact on the biological activity of the compounds. Internal and external validations were lead to good statistical parameters (r2 values of 0.93 and 0.665, respectively).
    Conclusion
    The results showed that the model has good predictive power and may be used for designing novel FGFR2 inhibitors.
    Keywords: 3D?QSAR, Docking, GRIND descriptors, Tyrosine kinase inhibitors, FGFR2
  • Vandana Kr, Prasanna Raju Yalavarthi *, Harini Chowdary Vadlamudi, Jagadesh Kumar Yadav Kalluri, Arun Rasheed Pages 419-425
    Purpose
    Albendazole is a poorly soluble drug which limits its oral bioavailability. The study was focussed to enhance the solubility by in-situ micronization.
    Methods
    Albendazole microcrystals were prepared by solvent change method using gum karaya and hupu gum as stabilizing agents and the effect of each stabilizer on the prepared microcrystals were studied. FT-IR, DSC, XRD and SEM analysis were performed as a part of characterization studies. The formulations were evaluated for micromeritics, solubility and drug release. The microcrystals that had shown optimized properties were filled into suitable capsules.
    Results
    The formulations showed reduction in particle size with uniform size distribution and three folds increase in drug release. The microcrystals had shown more than 100-folds increase in solubility compared to pure drug. Surface energy, enthalpy and crystalline nature of microcrystals were found to be reduced. Microcrystals containing gum karaya had shown more drug release. The filled-in capsules also showed increase in drug release rate. The solubility enhancement of albendazole microcrystals was mainly due to the surface adsorption of the stabilizing agents that led to reduction in surface energy and crystalline nature as substantiated by the DSC and XRD studies. The type of stabilizing agent had significant effect on dissolution rate. High affinity of albendazole with gum karaya led to faster drug release profiles.
    Conclusion
    The study proved that in-situ micronization is an effective technique to enhance the solubility and dissolution rate of poorly soluble drugs like albendazole.
    Keywords: Particle engineering, Stabilizers, Adsorption, Enthalpy, Dissolution efficiency, Surface energy
  • Zahra Sobhani, Soliman Mohammadi Samani *, Hashem Montaseri, Elham Khezri Pages 427-432
    Purpose
    Chitosan is a natural mucoadhesive polymer with antibacterial activity. In the present study, chitosan (CS) nanoparticles were investigated as a vehicle for delivery of antibiotic, ciprofloxacin hydrochloride.
    Methods
    Ionotropic gelation method was used for preparation chitosan nanoparticles. The effects of various factors including concentration of CS, concentration of tripolyphosphate (TPP), and homogenization rate on the size of nanoparticles were studied. The effects of various mass ratios of CS to ciprofloxacin hydrochloride on the encapsulation efficiency of nanoparticles were assessed.
    Results
    The particles prepared under optimal condition of 0.45% CS concentration, 0.45% TPP concentration and homogenizer rate at 6000 rpm, had 72 nm diameter. In these particles with 1:0.5 mass ratio of CS to ciprofloxacin hydrochloride, the encapsulation efficiency was 23%. The antibacterial activity of chitosan nanoparticles and ciprofloxacin-loaded nanoparticles against E.coli and S.aureus was evaluated by calculation of minimum inhibitory concentration (MIC). Results showed that MIC of ciprofloxacin loaded chitosan nanoparticles was 50% lower than that of ciprofloxacin hydrochloride alone in both of microorganism species. Nanoparticles without drug exhibited antibacterial activity at higher concentrations and MIC of them against E.coli and S.aureus was 177 and 277 µg/ml, respectively.
    Conclusion
    Therefore chitosan nanoparticles could be applied as carrier for decreasing the dose of antibacterial agents in the infections.
    Keywords: Chitosan, Ciprofloxacin, MIC, Nanoparticle, Tripolyphosphate
  • Carolina Harder, Akila Lara De Oliveira, Andreia Borges Scriboni, AdElia Cristina Oliveira Cintra, Raphael Schezaro-Ramosm., Aacute, Rcio Galdino Dos Santos, Karina Cogo-MUller, Regina Yuri Hashimoto Miura, Rafael Stuani Floriano, Sandro Rostelato-Ferreira, Yoko Oshima-Franco * Pages 433-439
    Purpose
    Bothrops snakes are responsible for more than 70 % of snakebites every year in Brazil and their venoms cause severe local and systemic damages. The pharmacological properties of medicinal plants have been widely investigated in order to discover new alternative treatments for different classes of diseases including neglected tropical diseases as envenomation by snakebites. In this work, we have investigated the ability of Vochysia haenkeana stem barks extract (VhE) to neutralize the neuromuscular effects caused by Bothropstoxin-I (BthTX-I), the major phospholipase A2 (PLA2) myotoxin from B. jararacussu venom.
    Methods
    The biological compounds of VhE were analysed under thin layer chromatography (TLC) and its neutralizing ability against BthTX-I was assessed through twitch-tension recordings and histological analysis in mouse phrenic nerve-diaphragm (PND) preparations. The antimicrobial activity of VhE was assessed against S. aureus, E. coli and P. aeruginosa strains. The aggregation activity of VhE was analysed under protein precipitation assay.
    Results
    VhE showed the presence of phenolic compound visualized by blue trace under TLC. VhE abolished the neuromuscular blockade caused by BthTX-I applying the pre-toxin incubation treatment and partially neutralized the BthTX-I action under post-toxin incubation treatment; VhE contributed slightly to decrease the myotoxicity induced by BthTX-I. The neutralizing mechanism of VhE may be related to protein aggregation. VhE showed no antimicrobial activity.
    Conclusion
    V. haenkeana extract which has no antimicrobial activity exhibited neutralizing ability against the neuromuscular blockade caused by BthTX-I and also contributed to decrease its myotoxicity. Protein aggregation involving phenolic compounds may be related in these protective effects.
    Keywords: Antimicrobial activity, Antiophidian activity, Bothropstoxin-I, Myotoxicity, Neurotoxicity, V. haenkeana extract
  • Mahbubeh Hashemia, Vahid Ramezani *, Mohammad Seyedabadi, Ali Mohammad Ranjbar, Hossein Jafari, Mina Honarvar, Hamed Fanaei Pages 441-450
    Purpose
    Recurrent aphthous stomatitis (RAS) is the most common painful ulcerative disease of oral mucosa happening in ~20% of people. Aimed to develop Myrtus communis L. (Myrtle) containing oral patches, we applied box-behnken design to evaluate the effect of polymers such as Polyvinyl pyrrolidone (PVP), Gelatin, Methylcellulose (MC) and Pectin.
    Methods
    The patches properties such as tensile strength, folding endurance, swelling index, thickness, mucoadhesive strength and the pattern of myrtle release were evaluated as dependent variables. Then, the model was adjusted according to the best fitted equation with box behnken design.
    Results
    The results indicated that preparation of myrtle patch with hydrophilic polymers showed the disintegration time up to 24h and more. Using of polyvinyl pyrrolidone as a water soluble polymer and a pore-former polymer led to faster release of soluble materials from the patch to 29 (min-1). Also it decreases swelling index by increasing the patch disintegration. Gelatin and Pectin, with rigid matrix and water interaction properties, decreased the swelling ratio. Pectin increased the tensile strength, but gelatin produced an opposite effect. Thinner Myrtle patch (about 28µm) was obtained by formulation of methyl cellulose with equal ratio with polyvinyl pyrrolidone or gelatin.
    Conclusion
    Altogether, the analysis showed that the optimal formulation was achieved with of 35.04 mg of Gelatin, 7.22 mg of Pectin, 7.20 mg of polyvinyl pyrrolidone, 50.52 mg of methyl cellulose and 20 mg of Myrtle extract.
    Keywords: Myrtus communis, Oral patch, Methyl cellulose, Gelatin, Polyvinyl pyrrolidone, Pectin
  • Neeraj Upmanyu, Pawan Kumar Porwal * Pages 451-459
    Purpose
    Desmopressin acetate (DDAPV), a synthetic analogue of vasopressin, has been recommended to be used in diabetes insipidus, mild forms of hemophilia and Von Willebrand disease. The DDAPV is available for adminstration via different routes viz. oral, parenteral and nasal, however its dose is very less in case of nasal sprays (20 µg) and parenteral route (4 µg) compared to oral route (0.1 to 0.3 mg in tablet). A sensitive and selective method is needed to be developed and validated for assay of low concentrations of DDAPV in its pharmaceutical dosage form i.e. nasal spray.
    Methods
    Simple and specific HPLC-Fluorescecne method has been proposed for the quantitation of DDAPV at nanogram level in nasal formulations for the first time. DAPV, DDAPV EP impurity-B, chlorobutanol, benzalkonoium chloride were successfully derivatised with Ortho-Phthalaldehyde (OPA) and co-eluted on a C8 (50×2.1 mm, 3.5 µm particle size, 120Å) with mobile phase composed of 0.1% trifluroacetic acid, acetonitrile and Isopropyl alcohol in ratio of 70:25:5. The emission was measured at 450nm and flow rate was 0.8ml/min. The reaction was optimized in the terms of pH, stability of formed fluorophore and time consumed during the reaction.
    Results
    The maximal fluorescence intensity was reached when the solutions were mixed for 3 min, and remained constant for at least 30 min at 20-25ºC. The calibration curve was found linear from 50 to 5000 ng/ml with weight of 1/X2. The limit of detection was 10ng/ml and precision was less than 2.0.
    Conclusion
    The developed HPLC-fluorescence assay method was successfully applied for quantitation of DDAPV in nasal spray. HPLC-Fluorescence method was specific, sensitive, precise and accurate for determination of DDAPV. The method was able to quantify DDAPV at 50ng/ml with sufficient accuracy and precision. The validated HPLCFluorescence was successfully applied.
    Keywords: Desmopressin acetate (DDAPV), Ortho-Phthaldehyde, Spectrofluorometric, HPLC-Fluorescence, Derivatization, Nasal spray
  • Pravin Gupta *, Manish Kumar, Darpan Kaushik Pages 461-467
    Purpose
    Various floating and pulsatile drug delivery systems suffer from variations in the gastric transit time affecting the bioavailability of drugs. The objective of the study was to develop Pantoprazole Sodium (PAN) microballoons that may prolong the gastric residence time and could enhance the drug bioavailability.
    Methods
    Microballoons were prepared using Eudragit®L100 by adopting emulsion solvent diffusion method with non-effervescent approach, in vitro studies were performed and the in vivo evaluation was carried out employing ethanol induced ulceration method. Optimization and validation were carried out through Design Expert® software.
    Results
    The results demonstrate an increase in percentage yield, buoyancy, encapsulation efficacy and swelling. Particles were in the size range 80-100 µm following zero order release pattern. SEM study revealed their rough surface with spherical shape, internal cavity and porous walls. DSC thermo gram confirms the encapsulation of drug in amorphous form. Significant anti ulcer activity was observed for the prepared microballoons. The calculated ulcer index and protection were 0.20±0.05 and 97.43 % respectively for LRS-O (optimized formulation).
    Conclusion
    This kind of pH dependent drug delivery may provide an efficient dosage regimen with enhanced patient compliance.
    Keywords: Eudragit, Gastro retentive drug delivery, Gastric residence time, Non-effervescent, Optimization
  • Marli Gerenutti *, Adriana Michel Vieira Martinez, Cristiane De Cassia Bergamaschi Pages 469-472
    Purpose
    To verify the effectiveness of a pharmaceutical care model developed by the Specialized Municipal Assistance Service in Sorocaba, Brazil, on adherence to ART among patients infected with HIV.
    Methods
    A cohort study compared adherence to ART in two groups of patients: intervention group (patients assisted with pharmaceutical care, n=130) and non-intervention group (patients attended by the habitual dispensing process, n=229). Antiretroviral adherence was measured by the number of pharmacy refill records in a six-month period. The relationship between the use of other drugs for the treatment of opportunistic infections and the adherence rate in the intervention group and the correlation between adherence and viral load and CD4 lymphocytes were also assessed.
    Results
    Higher adherence rates were observed in the intervention group (p
    Conclusion
    The pharmaceutical care model developed by the SAME improved patient adherence to ART as well as clinical outcomes.
    Keywords: Adherence rates, Antiretroviral agents, Maintenance of antiretroviral therapy, Medication adherence, Pharmaceutical care
  • Puxvadee Chaikul *, Tawanun Sripisut, Setinee Charom, Kanchanapa Sathirachawan, Naphatsorn Ditthawuthikul Pages 473-477
    Purpose
    The study aimed to characterize the fatty acid profile of Camellia oleifera (tea) seed oil and evaluate for cytotoxicity and activities on melanogenesis and antioxidant activity assays in order to utilize as the functional oil.
    Methods
    The fatty acid profile of oil was analyzed by gas chromatography/mass spectrometry (GC/MS). The cytotoxicity was performed by sulforhodamine B (SRB) assay in B16-F10 melanoma cells and 3T3-L1 cells. The melanogenesis assay, including melanin content and activities of tyrosinase and tyrosinase-related protein-2 (TRP-2), and antioxidant activity were evaluated.
    Results
    Three major fatty acids of oil were oleic acid (87.93±0.19%), stearic (5.14±0.06%) and palmitic (5.08±0.12%) acids. The non-cytotoxicity of 5% tea seed oil demonstrated the cell viabilities of 94.59±3.41% in B16-F10 melanoma cells and 97.57±1.62% in 3T3-L1 cells. Tea seed oil exhibited the inhibitory activity on melanogenesis assay via inhibition of tyrosinase and TRP-2 activities. The antioxidant activity of 3% tea seed oil appeared the cellular protection with cell viability of 90.38±7.77%.
    Conclusion
    The results of study have shown the potential utilization of tea seed oil as the functional oil in several products, including health, food and cosmetic products.
    Keywords: Tea seed oil, Cytotoxicity, Melanogenesis, Antioxidant, Cosmetic
  • Mahsa Esmaeillou, Gholamreza Zarrini *, Mohammad Ahangarzadeh Rezaee, Javid Shahbazi Mojarrad, Ali Bahadori Pages 479-483
    Purpose
    Many antimicrobial medications are available to combat infections. However, the indiscriminate use of antibiotics has produced antibiotic resistance in the case of many bacterial pathogens. This study focuses on the development of nanoparticles (NPs) that enhance the in vitro antibiotic activity of vancomycin against multi-drug resistant (MDR) organisms.
    Methods
    Spherical shaped thioglycolic acid-stabilized silver nanoparticles (TGA-AgNPs) were prepared by using a simple chemical reduction method. Then, vancomycin was conjugated to the terminal carboxyl of TGA in the presence of N-Hydroxysuccinimide (NHS) and N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (EDC). Afterwards, the antibacterial activity of these nanoconjugates was examined by using the minimum inhibitory concentration (MIC) assay against MDR bacteria.
    Results
    The rate of vancomycin bound to the AgNPs was 19.6%. The MIC values of vancomycin (Van)-capped AgNPs against tested pathogens were in the range of (3.2, 1.6, 0.8, 0.4, 0.2, 0.1, 0.05, and 0.025 µl/ml). The MIC was 0.1 µg/ml for VRE, MIC≤0.02 µg/ml for MRSE, and 0.05 µg/ml for S. aureus. The MIC corresponded to the MBC for all bacterial species.
    Conclusion
    This study indicated that some antimicrobial agents like vancomycin can be conjugated with AgNPs. This can lead to increased antimicrobial activity against MDR microorganisms.
    Keywords: Vancomycin, Silver nanoparticles, Antibacterial agent, Multi-drug resistance bacteria
  • Pragati Rawat *, Swatantra Agarwal, Siddhi Tripathi Pages 485-490
    Purpose
    Tissue conditioners are used for healing of abused oral tissues. They may harbour microorganisms causing oral diseases such as candidiasis compromising the health of the patient. Also, addition of antifungal agents into tissue conditioner may alter its properties. This study compares the anti-fungal property and mechanical properties of tissue conditioner containing different antifungal agents.
    Methods
    Three antifungal agents, one synthetic – fluconazole, and two natural - oregano oil and virgin coconut oil were added into the tissue conditioner (Viscogel) in different concentrations. The antifungal property, tensile bond strength and viscoelasticity of Viscogel containing these antifungal agents were assessed after 24 hours, three days and seven days.
    Results
    While, the highest antifungal activity was shown by Viscogel containing fluconazole, the maximum tensile bond strength was found to be of Viscogel alone (control). Although Viscogel alone and in combination of fluconazole showed deterioration in viscoelasticity, Viscogel in combination of natural agents showed no significant changes over the period of seven days.
    Conclusion
    Incorporation of the natural agents in the tissue conditioner can be used as an effective alternative to systemic or topical synthetic antifungal agents.
    Keywords: Candida albicans, Viscoelasticity, Tensile bond strength, Fluconazole, Oregano oil, Virgin coconut oil
  • Niloofar Bazazzadegan, Marzieh Dehghan Shasaltaneh, Kioomars Saliminejad, Koorosh Kamali, Mehdi Banan, Hamid Reza Khorram Khorshid * Pages 491-494
    Purpose
    Sporadic Alzheimer’s disease (AD) accounts for over 95% of cases. Possible mechanisms of AD such as inflammation and oxidative stresses in the brain motivate researchers to follow many therapies which would be effective, especially in the early stages of the disease. IMOD, the herbal extract of R. Canina, T. Vulgare and U. Dioica plant species enriched with selenium, has anti-inflammatory, immunoregulatory and protective effects against oxidative stress.
    Methods
    In this study three AD-related genes, DAXX, NFκβ and VEGF, were chosen as candidate to investigate the neuroprotective effect of the extract by comparing their expression levels in the hippocampus of rat model of sporadic AD, using qPCR in the herbal-treated and control groups. The therapeutic effects on learning and memory levels were evaluated by Morris Water Maze (MWM) test.
    Results
    Gene expression results were indicative of significant up-regulation of Vegf in rat’s hippocampus after treatment with the herbal extract comparing to model group (P-value= 0.001). The MWM results showed significant changes in path length and time for finding the hidden platform in all groups during test and the same change in the treated comparing to the control group in memory level.
    Conclusion
    It could be concluded that the herbal extract may have significant effect on gene expression but not on behavioral level.
    Short
    Keywords: Alzheimer's disease, Gene expression, Herbal extract, Rat model