فهرست مطالب

Advanced Pharmaceutical Bulletin - Volume:6 Issue: 1, Mar 2016

Advanced Pharmaceutical Bulletin
Volume:6 Issue: 1, Mar 2016

  • تاریخ انتشار: 1395/01/09
  • تعداد عناوین: 20
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  • Mehdi Dadkhah, Giorgio Bianciardi Pages 1-4
    Predatory journals are a well-known issue for scholarly publishing and they are repositories for bogus research. In recent years, the number of predatory journals has risen and it is necessary to present a solution for this challenge. In this paper, we will discuss about a possible ranking of predatory journals. Our ranking approach is based on Beall’s criteria for detection of predatory journals and it can help editors to improve their journals or convert their questionable journals to non-predatory ones. Moreover, our approach could help young editors to protect their journals against predatory practice. Finally, we present a case study to clarify our approach.
    Keywords: Predatory journals, Ranking predatory journals, Journal selection, Academic ethic, Journal quality, Predatory journal criteria
  • Nahid Khaziri, Momeneh Mohamadi, Zeinab Aliyari, Jafar Soleimani Rad, Hamid Tayefi Nasrabadi, Hojjatollah Nozad Charoudeh* Pages 5-8
    Purpose
    Although bone marrow represents the main site for NK cell development and also distinct thymic-dependentNK cell pathway was identified, the cytokines effect on the NK cell generation from cord blood is unclear. Studies were identified the role of cytokines in the regulation of bone marrow and thymic NK cells. Previous studies reported that IL15 are critical for bone marrow dependent and IL7 is important for thymic NK cells. It is remain unclear the cytokines influence on the expantion of NK cells in cord blood mononuclear cells.
    Methods
    We evaluated cultured cord blood mononuclear cells suplememnted with combinations of cytokines using FACS in distinct time points. In this study, we presented the role of IL2, IL7 and IL15 as members of the common gamma receptor -chain (Il2rg) on the expansion NK cells from cord blood cells.
    Results
    By investigating cord blood mononuclear cells in vitro , we demonstrated that IL2 and IL15 are important for expansion of NK cells. IL2 in comparision with IL15 has more influences in NK cell expansion. In contrast IL-7 is dispensable for NK cell generation in cord blood.
    Conclusion
    Thus,IL-2Rg cytokines play complementary roles and are indispensable for homeostasis of NK cell development in cord blood. Probably these cytokines could help to use NK beneficials in engrafment of transplanted cells and Anti tumor activity of NK cells.
    Keywords: Cord blood, Mononclear cells, NK cell, IL2rg cytokines
  • Anayatollah Salimi *, Najme Hedayatipour, Eskandar Moghimipour Pages 9-16
    Purpose
    The purpose of the present investigation was to evaluate the effectiveness of different vehicles on drug permeability and microstructure of intercellular or lipids in SC layer of skin.
    Methods
    Pre-treated skin of rat using some vehicles including Labarac PG ,Transcutol P, tween 80, span 80 and propylene glycol (PG), were mounted on specialized design franzdiffusion cell was used to assess naproxen permeation and parameters such as permeability coefficients and state flux (Jss) were evaluated. Any differences in peak position and also change in symmetric and asymmetric stretching of C-H bond, lipid ester carbonyl stretching in SC, C=O stretching (Amide I) and C-N stretching of keratin (Amide II) absorbance using Fourier transform infrared spectroscopy (FTIR) were considered to investigate the enhancing mechanism. DSC method was utilized to compare their mean transition temperature (Tm) and enthalpies (ΔH).
    Results
    Steady-state flux (Jss), permeability coefficient (Kp) and diffusion coefficient (D) were significantly (p
    Conclusion
    It is concluded that naproxen permeation through rat skin may be facilitated by utilizing the vehicle systems. Lipid fluidization and lipid extraction are among suggested mechanisms.
    Keywords: Naproxen, Permeability, Mean transition temperature, Thermotropic behavior, Diffusion coefficient, Flux
  • Parisa Jourghanian, Solmaz Ghaffari, Mehdi Ardjmand, Setareh Haghighat, Mahdieh Mohammadnejad Pages 17-21
    Purpose
    curcumin is poorly water soluble drug with low bioavailability. Use of lipid systems in lipophilic substances increases solubility and bioavailability of poorly soluble drugs. The aim of this study was to prepare curcumin loaded Solid Lipid Nanoparticles (SLNs) with high loading efficiency, small particle size and prolonged release profile with enhanced antibacterial efficacy.
    Methods
    to synthesize stable SLNs, freeze- Drying was done using mannitol as cryoprotectant. Cholesterol was used as carrier because of good tolerability and biocompatibility. SLNs were prepared using high pressure homogenization method.
    Results
    optimized SLNs had 112 and 163 nm particle size before and after freeze drying, respectively. The prepared SLNs had 71% loading efficiency. 90% of loaded curcumin was released after 48 hours. Morphologic study for formulation was done by taking SEM pictures of curcumin SLNs.
    Results show the spherical shape of curcumin SLNs. DSC studies were performed to determine prolonged release mechanism. Antimicrobial studies were done to compare the antimicrobial efficacy of curcumin SLNs with free curcumin. DSC studies showed probability of formation of hydrogen bonds between cholesterol and curcumin which resulted in prolonged release of curcumin. Lipid structure of cholesterol could cause enhanced permeability in studied bacteria to increase antibacterial characteristics of curcumin.
    Conclusion
    the designed curcumin SLNs could be candidate for formulation of different dosage forms or cosmeceutical products.
    Keywords: Curcumin ⋅ Solid Lipid Nanoparticles ⋅ Sustained release ⋅ Freeze drying ⋅ Particle size
  • Zahra Molaeipour, Karim Shamsasanjan, Ali Akbari Movassaghpour, Parvin Akbarzadehlaleh, Fatemeh Sabaghi, Mahshid Saleh Pages 23-29
    Purpose
    Mesenchymal stem cells (MSCs) are key components of the hematopoietic stem cells (HSCs) niche. They control the process of hematopoiesis by secreting regulatory cytokines, growth factors and expression of important cell adhesion molecules for cell-tocell interactions. In this research, we have investigated the effect of bone marrow derived MSCs on monocytic differentiation of U937 cells line.
    Methods
    U937 cells were cultured in both direct co-culture with MSCs and MSCs conditioned medium (C.M) driven. This study used 1,25-dihydroxyvitamin D3(VitD3) as inductor of monocytic differentiation and U937 cells treated with VitD3 morphology was examined by Wright Giemsa staining. CD14 monocytic differentiation marker was measured by flow cytometry and monocytic gene expression was assessed by real time polymerase chain reaction (RT PCR).
    Results
    The results of flow cytometric analysis showed that CD14 expression of U937 increased. The higher effect of MSCs co-culture on CD14 expression in U937 cells was observed, compared to the conditioned medium. Among ten monocytic related genes which were screened that was observed increase in 5 genes in which CXCR4 and CSF2RA showed significant increase.
    Conclusion
    The results obtained show that MSCs have supportive effect on the monocytic differentiation of U937 cells. However, a distinct mechanism of that remains unclear.
    Keywords: Mesenchymal stem cells ⋅ U937 cells ⋅ Differentiation ⋅ Vitamin D3
  • Zahra Mardhiah Adib, Saeed Ghanbarzadeh, Maryam Kouhsoltani, Ahmad Yari Khosroshahi, Hamed Hamishehkar Pages 31-36
    Purpose
    In the present study the effect of particle size, as a substantial parameters in skin penetration, on the deposition depth and rate of SLNs in different layers of skin was explored.
    Methods
    SLNs in different particle size ranges (80, 333 and 971 nm) made of Precirol as solid lipid were prepared using hot melt homogenization technique and pigmented by Rhodamine B to be able to be tracked in the skin under inspection of fluorescent microscopy. After 0.5 h, 3 h, 6 h and 24 h of SLNs administration on rat skin, animals were sacrificed and exercised skins were sliced by a freeze microtome. SLNs were monitored in the skin structure under fluorescence microscope.
    Results
    The size of SLNs played a crucial role in the penetration to deep skin layers. The sub100 nm size range of SLNs showed the most promising skin penetration rate and depth mainly via hair follicles.
    Conclusion
    The results of the present study indicated that the selection of an appropriate size of particles may be a valuable factor impacting the therapeutic outcomes of dermal drug administration.
    Keywords: Solid lipid nanoparticle, SLN, Topical drug delivery, Skin penetration, Rhodamine B
  • Babak Haghshenas, Minoo Haghshenas, Yousef Nami, Ahmad Yari Khosroushahi, Norhafizah Abdullah, Abolfazl Barzegari, Rozita Rosli, Mohammad Saeed Hejazi Pages 37-47
    Purpose
    Probiotics are microorganisms, which show beneficial health effects on hosts once consumed in sufficient amounts. Among probiotic bacteria, the bioactive compounds from lactic acid bacteria (LAB) group can be utilized as preservative agents. LAB group can be isolated and characterized from traditional dairy sources. This study aimed to isolate, identify, and biologically characterize probiotic LAB strains from Iranian traditional dairy products.
    Methods
    A total of 19 LAB strains were identified by sequencing of their 16S rRNA genes. They were examined for adherence to human intestinal Caco-2 cells and tolerance to low pH/high bile salts and simulated in vitro digestion conditions. Moreover, they were evaluated further to assess their ability to prevent the adhesion of Escherichia coli 026 to the intestinal mucosa, inhibitory functions against pathogens, and sensitivity to conventional antibiotics.
    Results
    L. plantarum 15HN and E. mundtii 50H strains displayed ≥ 71% survival rates at low pH/high bile salts and ≥ 40% survival rates in digestive conditions. Their adherences to Caco-2 cells were 3.2×105 and 2.6×105 CFU mL-1 respectively and high values of antiadhesion capability were observed (≥36%). They inhibited the growth of 13 and 11 indicator pathogens respectively. Moreover, they were sensitive or semi-sensitive to seven and three out of eight antibiotics respectively.
    Conclusion
    L. plantarum 15HN and E. mundtii 50H, which were isolated from shiraz product, displayed above-average results for all of the criteria. Therefore, they can be introduced as novel candidate probiotics that could be used in the food industry.
    Keywords: Probiotic ⋅ Lactic acid bacteria ⋅ Adherence ⋅ Antimicrobial resistance
  • Yaghoub Yazdani, Shahram Azari, Hamid Reza Kalhor* Pages 49-56
    Purpose
    Tissue transglutaminase (TG2) is a unique multifunctional enzyme. The enzyme possesses enzymatic activities such as transamidation/crosslinking and non-enzymatic functions such as cell migration and signal transduction. TG2 has been shown to be involved in molecular mechanisms of cancers and several neurodegenerative diseases such as Alzheimer’s disease. The present study aimed at cloning and expression of full length human TG2 in Bac-to-Bac baculovirus expression system and evaluation of its activity.
    Methods
    pFastBac HTA donor vector containing coding sequence of human TG2 was constructed. The construct was transformed to DH10Bac for generating recombinant bacmid. The verified bacmid was transfected to insect cell line (Sf9). Expression of recombinant TG2 was examined by RT-PCR, SDS-PAGE and western blot analysis. Functional analysis was evaluated by fluorometric assay and gel electrophoresis.
    Results
    Recombinant bacmid was verified by amplification of a band near to 4500 bp. Expression analysis showed that the enzyme was expressed as a protein with a molecular weight near 80 kDa. Western blot confirmed the presence of TG2 and the activity assays including flurometric assay indicated that the recombinant TG2 was functional. The electrophoresis assay conformed that the expressed TG2 was the indeed capable of crosslinking in the presence of physiological concentration calcium ions.
    Conclusion
    Human TG2 was expressed efficiently in the active biological form in the Bacto-Bac baculovirus expression system. The expressed enzyme could be used for medical diagnostic, or studies which aim at finding novel inhibitors of the enzymes . To best of our knowledge, this is probably the first report of expression of full length human tissue transglutaminase (TG2) using the Bac-to-Bac expression system.
    Keywords: Tissue transglutaminase (TG2), Baculovirus, Bac, to, Bac, Sf9, Protein expressio
  • Mehdi Hassanpour Aghdam, Saeed Ghanbarzadeh, Yousef Javadzadeh, Hamed Hamishehkar* Pages 57-64
    Purpose
    Local therapy is a valuable and strategic approach in the treatment of lung associated diseases and dry powder inhalation (DPI) formulations play the key role in this plan. Transfersome has been introduced as a novel biocompatible vesicular system with potential for administration in pulmonary drug delivery. The present study was designed to prepare Itraconazole-loaded nanotrantransfersomal DPI formulation.
    Methods
    Itraconazole-loaded nanotransfersomes with three different types of surfactant in varying concentrations were prepared and characterized in the point of particle size distribution and morphology by laser light scattering and scanning electron microscopy (SEM) methods. The optimized transferosomal formulations were co-spray dried with mannitol and the aerosolization efficiency and aerodynamic properties of dry powders were determined by next generation impactor using a validated HPLC technique.
    Results
    The volume mean diameter of optimized nanotransfersomal formulation with lecithin:Span® 60 in the ratio of 90:10 was 171 nm with narrow size distribution pattern which increased up to 518 nm after drug loading. Different types of surfactant did not influence the particle size significantly. SEM images confirmed the formation of aggregated nanoparticles in the suitable range (1-5 µm) for the pulmonary drug delivery. Aerosolization evaluation of co-spray dried formulations with different amounts of mannitol indicated that 2:1 ratio of mannitol:transfersome (w:w) showed the best aerosolization efficiency (fine particle fraction (FPF)=37%). Increasing of mannitol significantly decreased the FPF of the optimized formulations.
    Conclusion
    The results of this study was introduced the potential application of nanotransfersomes in the formulation of DPIs for lung delivery of various drugs.
    Keywords: Pulmonary drug delivery, Dry powder inhaler, Transfersome, Itraconazole, DP
  • Fatemeh Namvar Vansofla, Leila Roshangar *, Azadeh Montaseri, Jafar Soleimani Rad Pages 65-69
    Purpose
    Cumulus cells have a critical role in normal oocyte development and fertilization. Prunus cerasus is an anthocyanin rich berry and performs strong antioxidant activity. The present study set to determine if Prunus cerasus can affect expression of HAS2 (hyaluronan synthase 2) and progesterone receptor in Cumulus cells and its consequences outcome of the in vitro fertilization.
    Methods
    60 female and 15 male adult mice were used for mating and IVF (in vitro fertilization). Prunus cerasus extraction was added to the diet of female mice for 30 days. Ovulation induction and oocytes collection were done as routine. The cumulus cells were dissected apart, and the expression of progesterone receptor and HAS2 was detected using RT-PCR (real-time polymerase chain reaction). Fertilization rate was evaluated by IVF. All data were analyzed using t-test.
    Results
    Data was showed that expression of progesterone receptor and HAS2 in cumulus cells of mice that received prunus cerasus increased. Moreover, oocyte fertilization rate also increased significantly.
    Conclusion
    Prunus cerasus as an antioxidant natural can become an important medication for improving oocyte quality and opening new opportunities for infertility treatment. It is concluded that Prunus cerasus consumption could improve fertility rate by increasing progesterone receptor and HAS2 activity in cumulus cells.
    Keywords: Cumulus cells, HAS2, Infertility, PGR, Prunus cerasus
  • Evgenii Plotnikov*, Vladimir Silnikov, Andrew Gapeyev, Vladimir Plotnikov Pages 71-74
    Purpose
    The problem of infectious diseases and drug resistance is becoming increasingly important worldwide. Silver is extensively used as an anti-infective agent, but it has significant toxic side effects. In this regard, it is topical to develop new silver compounds with high biological activity and low toxicity. This work is aimed to study DNA damage and chromosomal aberrations in blood cells under the influence of new silver-based compound of general formula C6H19Ag2N4LiO6S2, with antiviral activity.
    Methods
    The comet assay was applied for the genotoxic affects assessment on mice blood leukocytes. DNA damage was determined bases on the percentage of DNA in a comet tail (tail DNA), under the influence of silver complex in different concentrations. Genotoxic effect of the tested substance on the somatic cells was determined by chromosomal aberration test of bone marrow cells of mice.
    Results
    In the course of the experiments, no essential changes in the level of DNA damage in the cells were found, even at highest concentrations. The administration of the substance in doses up to 2.5 g/kg in mice did not cause any increase in the frequency of chromosomal aberration in bone marrow cells.
    Conclusion
    Taking into account known silver drug genotoxic properties, the use of a given complexed silver compound has possible great advantages for potential applications in the treatment of infectious diseases.
    Keywords: Genotoxicity, Antiviral compound, Chromosomal aberrations, Silver complex, Comet assay
  • Vinit Kumar Srivastava*, Abhishek Mishra, Sanjay Agrawal, Sanjay Kumar, Sunil Sharma, Raj Kumar Pages 75-81
    Purpose
    Dexmedetomidine and magnesium sulfate have been used in anesthesia as adjuvant to provide hemodynamic stability and anesthetic agents sparing effect. We compared these effects of dexmedetomidine and magnesium sulfate in spine surgeries.
    Methods
    Ninety patients were randomly assigned to three groups. Group D received dexmedetomidine loading dose 1 µg/kg over a period of 15 minutes and maintenance 0.5 µg/kg/h throughout the surgery. Group M received magnesium sulfate loading dose 50 mg/kg over a period of 15 minutes and maintenance 15 mg/kg/h throughout the surgery. Group C received same volume of normal saline. Heart rate (HR) and blood pressure values were recorded at various intervals. The induction and maintenance doses of anesthetics and recovery parameters were also recorded.
    Results
    Heart rate in group D and group M were significantly decreased (p
    Conclusion
    Dexmedetomidine is more effective than magnesium sulfate for maintaining the hemodynamic stability in spine surgeries. Both these drugs also reduce the requirements of anesthetic agents. Recovery from dexmedetomidine is as rapid as control group compared to magnesium sulfate.
    Keywords: Dexmedetomidine, Magnesium sulfate, Hemodynamics, Spine surgery
  • Sunethra Kalvakuntla, Mangesh Deshpande, Zenab Attari, Koteshwara Kunnatur B.* Pages 83-90
    Purpose
    Nanosuspension in drug delivery is known to improve solubility, dissolution and eventually bioavailability of the drugs. The purpose of the study was to compare particle size of nanosuspensions prepared by the first generation approach and H96 approach and to evaluate the effectiveness of H96 approach.
    Methods
    The nanosuspension of aprepitant was prepared by HPH and H96 approach. The prepared nanosuspensions were characterized for their particle size and zeta potential. The optimized nanosuspension was further evaluated for DSC, FT-IR, solubility and dissolution.
    Results
    The optimized nanosuspension (NCLH5) prepared using combination of tween 80 and poloxamer 188 as stabilizer, showed particle size of 35.82 nm and improved solubility and dissolution profile over pure drug. NCLH5 was chosen optimized formulation and further evaluated for other parameters after lyophilization. Lyophilization resulted in increase in particle size. The solubility and dissolution studies showed favorable increase in the performance. The FT-IR and DSC analysis showed change in the crystallinity after nanosizing.
    Conclusion
    The observations indicated that lyophilization prior to high pressure homogenization resulted in efficient particle size reduction yielding smaller particles than first generation preparation technique. H96 is a good and easy alternative to achieve efficient particle size reduction of drug in lesser time and increase its solubility and dissolution.
    Keywords: Lyophilization, Nanosuspension, Particle size, Second generation approach, High pressure homogenization
  • Khadijeh Nasiri, Mohammadreza Nassiri *, Mojtaba Tahmoorespur, Alireza Haghparast, Saeed Zibaee Pages 91-98
    Purpose
    Bovine Rotavirus and Bovine Coronavirus are the most important causes of diarrhea in newborn calves and in some other species such as pigs and sheep. Rotavirus VP8 subunit is the major determinant of the viral infectivity and neutralization. Spike glycoprotein of coronavirus is responsible for induction of neutralizing antibody response.
    Methods
    In the present study, several prediction programs were used to predict B and Tcells epitopes, secondary and tertiary structures, antigenicity ability and enzymatic degradation sites. Finally, a chimeric antigen was designed using computational techniques. The chimeric VP8-S2 antigen was constructed. It was cloned and sub-cloned into pGH and pET32a() expression vector. The recombinant pET32a()-VP8-S2 vector was transferred into E.oli BL21CodonPlus (DE3) as expression host. The recombinant VP8-S2 protein was purified by Ni-NTA chromatography column.
    Results
    The results of colony PCR, enzyme digestion and sequencing showed that the VP8-S2 chimeric antigen has been successfully cloned and sub-cloned into pGH and pET32a().The results showed that E.coli was able to express VP8-S2 protein appropriately. This protein was expressed by induction of IPTG at concentration of 1mM and it was confirmed by Ni–NTA column, dot-blotting analysis and SDS-PAGE electrophoresis.
    Conclusion
    The results of this study showed that E.coli can be used as an appropriate host to produce the recombinant VP8-S2 protein. This recombinant protein may be suitable to investigate to produce immunoglobulin, recombinant vaccine and diagnostic kit in future studies after it passes biological activity tests in vivo in animal model and or other suitable procedure.
    Keywords: Bovine Rotavirus, Bovine Coronavirus, Epitope, Expression, Recombinant protein
  • Fatemeh Habibi, Farhad Ghadiri Soufi, Rafighe Ghiasi, Amir Mahdi Khamaneh, Mohammad Reza Alipour* Pages 99-103
    Purpose
    The purpose of the present study is to evaluate the expression of miR-146a gene, its adaptor genes (TRAF6, NF-KB, and IRAK1), and possible changes in the cellular signaling pathway in diabetic hippocampus tissue.
    Methods
    Male Sprague–Dawley rats are randomly selected and divided into control and diabetic (n=6) groups. Diabetes induced by the single-dose injection of nicotinamide [110 mg/kg, (i.p.)], 15 min before streptozotocin (50 mg/kg; i.p.) in 12-h fasted rats. The rats are kept at the laboratory for two months. After anaesthetization, hippocampus of the rats was removed in order to measure the expression of miR-146a, NFK-B, IRAK1, and TRAF6 genes using real-time PCR and activity of NF-KB as well as amount of apoptosis rate using ELISA.
    Results
    The results indicated a reduction in expression of miR-146a and an increase in expression of IRAK1, NF-KB, and TRAF6 genes in the hippocampus of diabetic rats compared to control. Also it reveals an increase in the activity of NF-KB and apoptosis rate in the hippocampus of diabetic rats.
    Conclusion
    Our results report the probability that reduction of miR-146a expression in the negative feedback loop between miR-146a and NF-KB increases NF-kB expression and thus intensifies inflammation and apoptosis in hippocampus.
    Keywords: Diabetes, Hippocampus, TRAF6, IRAK1, NF, KB, miR, 146a
  • Parviz Vahedi, Jafar Soleimanirad, Leila Roshangar*, Hajar Shafaei, Seyedhosein Jarolmasjed, Hojjatollah Nozad Charoudeh Pages 105-110
    Purpose
    The goal of this study has been to evaluate adipose tissue derived stem cells (ADSCs) from infrapatellar fat pad and characterize their cell surface markers using antihuman antibodies, as adipose tissue derived stem cells (ADSCs) have great potential for cellular therapies to restore injured tissues.
    Methods
    Adipose tissue was obtained from infrapatellar fat pad of sheep. Surface markers evaluated by flow cytometry. In order to evaluate cell adhesion, the Polycaprolactone (PCL) was sterilized under Ultraviolet (UV) light and about 1×105 cells were seeded on PCL. Then, ASCs- PCL construct were evaluated by Scanning Electron Microscopy (Mira3 Te Scan, Czech Republic).
    Results
    We showed that adipose tissue derived stem cells (ADSCs) maintain their fibroblastic-like morphology during different subcultures and cell adhesion. They were positive for CD44 and CD90 markers and negative for CD31 and Cd45 markers by human antibodies.
    Conclusion
    Our results suggest that ASCs surface markers can be characterized by antihuman antibodies in sheep. As stem cells, they can be used in tissue engineering.
    Keywords: Anti, Human Antibodies, Infrapatellar fat pad adipose tissue, CD markers, ASCs
  • Mehran Mesgari Abbasi, Hadi Valizadeh, Hamed Hamishekar, Leila Mohammadnejad, Parvin Zakeri, Milani* Pages 111-118
    Purpose
    P-glycoprotein (P-gp) plays a major role in oral absorption of drugs. Induction or inhibition of P-gp by drugs contributes to variability of its transport activity and often results in clinically relevant drug-drug interactions. The purpose of this study was to investigate the effect of cetirizine, a second generation H1 antihistamine, on P-gp function and expression in vitro and in situ.
    Methods
    The in-vitro rhodamin-123 (Rho123) efflux assay in Caco-2 cells was used to study the effect of cetirizine on P-gp function. Western blot analysis was used for surveying the effect of cetirizine on expression of P-gp in Caco-2 cells. Rat in situ single-pass intestinal permeability technique was used to calculate the intestinal permeability of a known P-gp substrate (digoxin) in the presence of cetirizine. The amounts of digoxin and cetirizine in intestinal perfusion samples were analyzed using a HPLC method.
    Results
    The results showed significant increase in Rho123 uptake (P
    Conclusion
    Therefore it is concluded that cetirizine is a P-gp inhibitor and this should be considered in co administration of cetrizine with other P-gp substrate drugs. Further investigations are required to confirm our results and to determine the mechanism underlying P-gp inhibition by cetirizine.
    Research
    Keywords: Cetirizine ⋅ Digoxin ⋅ Intestinal permeability ⋅ P_glycoprotein
  • Mitra Jelvehgari, Hadi Valizadeh *, Sanam Ziapour, Mahdieh Rahmani, Seyed Hassan Montazam, Saieede Soltani Pages 119-130
    Purpose
    Sumatriptan succinate (Sum) is a Serotonin 5- HT1 receptor agonist, used in the treatment of migraine. It is absorbed rapidly but incompletely when taken orally and underwent first - pass metabolism, resulting in a low bioavailability of about 15%. The aim was to design mucoadhesive buccal discs and sublingual films of Sum and metoclopramide (Met) combined to improve their bioavailability.
    Methods
    In the current study, the microparticles and films were prepared by emulsion solvent diffusion (ESD) and solvent casting methods, respectively. Buccal-mucoadhesive microparticles and films with different drug to polymer ratios were prepared and characterized by encapsulation efficiency, particle size, DSC (Differential Scanning Calorimetric), folding endurance, mucoadhesive property and drug release studies.
    Results
    The best drug/s to polymer ratios in films and microparticles were 1:2.7:8 (SM2) and 1:4:6 (SM4), respectively. The film of SM2 showed 11.01 mg weight, 123 µm thickness and 300 folding endurance. The production yield was 107.33% for SM4 microparticles, 323.59 µm for mean particle size and 94.53% for loading efficiency (for Sum) and 104.18% (for Met). The DSC showed no stable characteristic of Sum and Met in the drug loaded films/discs and revealed amorphous form and transition of hydrate to anhydrous form for Met. The films exhibited very good mucoadhesive properties and shorter retention time (15-30 s) in comparison with the discs (130 min). The results showed that the discs prepared had slower release than the films (p
    Conclusion
    Films and discs of Sum-Met combinations were successfully prepared with improved release and mucoadhesive properties.
    Keywords: Mucoadhesive ? Buccal ? Transmucosal ? Sumatriptan ? Metoclopramide
  • Keyvan Yousefi, Sanaz Hamedeyazdan, Mohammadali Torbati, Fatemeh Fathiazad* Pages 131-136
    Purpose
    In the present study we aimed to quantify marrubiin, as the major active compound, in the aerial parts of Marrubium vulgare from Iran using a HPTLC-densitometry technique.
    Methods
    Quantitative determination of marrubiin in M. vulgare methanol extract was performed by HPTLC analysis via a fully automated TLC scanner. Later on, the in vitro antioxidant activity of the M. vulgare methanol extract was determined using 1,1diphenyl-2-picryl-hydrazil (DPPH) free radical scavenging assay. Furthermore, total phenolics and flavonoids contents of the methanol extract were quantified, spectrophotometrically.
    Results
    The amount of marrubiin was calculated as 156 mg/g of M. vulgare extract. The antioxidant assay revealed a strong radical scavenging activity for the M. vulgare methanol extract with RC50 value of 8.24μg/mL. Total phenolics and flavonoids contents for M. vulgare were determined as 60.4 mg gallic acid equivalent and 12.05 mg quercetin equivalent per each gram of the extract, correspondingly.
    Conclusion
    The presented fingerprint of marrubiin in M. vulgare extract developed by HPTLC densitometry afforded a detailed chemical profile, which might be useful in the identification as well as quality evaluation of herbal medications based on M. vulgare. Besides, the considerable antioxidant activity of M. vulgare was associated with the presence of marrubiin along with phenolics and flavonoids exerting a synergistic effect.
    Keywords: Marrubium vulgare ⋅ Marrubiin ⋅ Folin_Ciocalteau ⋅ Free radicals ⋅ TLC scanner ⋅ Densitometry
  • Hashem Alaani*, Yasmin Alnukkary Pages 137-141
    Purpose
    A simple stability-indicating RP-HPLC assay method was developed and validated for quantitative determination of Chloramphenicol, Dexamethasone Sodium Phosphate and Tetrahydrozoline Hydrochloride in ophthalmic solution in the presence of 2amino-1-(4-nitrophenyl)propane-1,3-diol, a degradation product of Chloramphenicol, and Dexamethasone, a degradation product of Dexamethasone Sodium Phosphate.
    Methods
    Effective chromatographic separation was achieved using C18 column (250 mm, 4.6 mm i.d., 5 μm) with isocratic mobile phase consisting of acetonitrile - phosphate buffer (pH 4.0; 0.05 M) (30:70, v/v) at a flow rate of 1 mL/minute. The column temperature was maintained at 40°C and the detection wavelength was 230 nm.
    Results
    The proposed HPLC procedure was statistically validated according to the ICH guideline, and was proved to be stability-indicating by resolution of the APIs from their forced degradation products.
    Conclusion
    The developed method is suitable for the routine analysis as well as stability studies.
    Keywords: Chloramphenicol ⋅ Dexamethasone Sodium Phosphate ⋅ Tetrahydrozoline Hydrochloride ⋅ HPLC ⋅ Ophthalmic Solution ⋅ Stability_indicatin