فهرست مطالب

Research in Pharmaceutical Sciences
Volume:9 Issue: 1, Feb 2014

  • تاریخ انتشار: 1392/03/06
  • تعداد عناوین: 8
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  • F. Farvadi, Am Tamaddon, Ss Abolmaali, Z. Sobhani, Gh Yousefi Pages 1-10
    Single-walled carbon nanotubes (SWNTs) are among the promising nano-devices for delivery of therapeutic agents. Yet the drastic hydrophobic natures of SWNTs make their handling and hence application difficult.Several researches have been conducted to make them more hydrophilic and water dispersible and less toxic. Among the different approaches, dispersion methods exploit different reagents such as surfactants and block copolymers. The question is whether these so called dispersed SWNTs are stable enough and suitable for biomedical applications. Herein we aimed to functionalize SWNT surface by dioleoylphosphatidylethanolamine-polyethylene glycol (PL-PEG) and sodium deoxycholate (SDC) micelles and compare their efficacy in SWNT stabilization for biomedical application such as delivery of doxorubicin. Shortening and water dispersion of SWNTs were carried out by ultrasonication in aqueous solutions at different concentrations of SDC or PL-PEG micelle and assessed by UV-Vis-NIR spectroscopy. The stability of SWNT dispersions were assessed over the time and in the presence of salt by macroscopic observation and UV-Vis-NIR spectroscopy. Doxorubicin loading and release were carried out under different pH conditions. SWNT dispersions were stable in water for at least several weeks at room temperature, but SDC prepared dispersions were prone to agglomeration in the presence of salt and doxorubicin. The critical PL-PEG concentration for stability in physiologic conditions was about 5 times its critical micelle concentration. Doxorubicin loading was pH dependent and its release was triggered in acidic condition of tumor medium.
  • Ss Chowdhury, Mn Islam, Ha Jung, Js Choi Pages 11-22
    In an attempt to develop alternative medicine for the treatment of diabetes and related complications, the antidiabetic potential of the fruits of Crataegus pinnatifida was evaluated. The antidiabetic potential of the methanol (MeOH) extract as well as different solvent soluble fractions of the fruits of C. pinnatifida was evaluated via α-glucosidase, protein tyrosine phosphatase 1B (PTP1B), rat lens aldose reductase (RLAR), and advanced glycation end products (AGEs) formation inhibitory assays. The MeOH extract showed potent inhibitory activity against α-glucosidase, PTP1B, and AGEs formation with IC50 values of 122.11, 3.66 and 65.83 μg/ml respectively, while it showed moderate inhibitory activity against RLAR with the IC50 value of 160.54 μg/ml. Among different fractions, the ethyl acetate (EtOAc) and the dichloromethane (CH2Cl2) fractions were found as active fractions exhibiting potential α-glucosidase, PTP1B, RLAR inhibitory, and AGEs formation inhibitory activities. Seven compounds including hyperoside, chlorogenic acid, ursolic acid, oleanolic acid, 3-epicorosolic acid, β-sitosterol, β-sitosterol glucoside were isolated from these two fractions. 3-Epicorosolic acid showed both potent α-glucosidase and PTP1B inhibitory activities with IC50 values of 30.18 and 4.08 μg/ml respectively. Moreover, kinetic study revealed that 3-epicorosolic acid showed mixed type inhibition against PTP1B, while it showed uncompetitive inhibition against α-glucosidase. Therefore, these results suggest that the fruits of C. pinnatifida and its constituents have potential antidiabetic activity which might be used as a functional food for the treatment of diabetes and associated complications.
  • Ln Madhu, Ns Kumari Pages 23-29
    Protection of biological systems against radiation damage is of paramount importance during accidental and unavoidable exposure to radiation. Several physico-chemical and biological factors collectively contribute to the damage caused by radiation and are, therefore, targets for developing radioprotectors. Chemicals capable of scavenging free radicals, relieving oxidative stress, promoting antioxidant activity and modulating immune response have been some of the radioprotectors extensively investigated with limited success. It has long been known that some of the most effective radioprotective agents are those which contain sulphydryl groups. 4-amino-5-mercapto-3-methyl-1, 2, 4-triazole (AMMT) is one of the well-known 1, 2, 4 triazole derivatives with functional sulphydryl group. The present study reports an evaluation of radical scavenging and radioprotective properties of sulphydryl group containing triazole derivative. The lethal dose of electron beam radiation (EBR) was studied by survival assay. The dose reduction factor (DRF) of AMMT was calculated using the ratio between LD50 of EBR with and without AMMT treatment. Radical scavenging property of AMMT was assessed by DPPH radical scavenging assay. The clastogenic effects of EBR were recorded by Micronucleus test in bone marrow cells and DNA fragmentation assay in mice hepatic cells. The survival assay results showed that the LD50 of EBR was 10 Gy. The calculated DRF for AMMT was found to be 1.2. DPPH radical scavenging assay showed a positive result when it was compared with the standard glutathione. Treatment of mice with 100 mg of AMMT for 15 days before irradiation significantly (P<0.05) reduced the frequency of micronucleus formation in bone marrow cells and also reduced the DNA fragmentation in hepatic cells. The results obtained in the present study indicated that AMMT has a protective effect against the EBR-induced mortality and clastogenicity.
  • G. Haghi, A. Hatami, A. Safaei, M. Mehran Pages 31-37
    Chamomile (Matricaria chamomilla L.) is a widely used medicinal plant possessing several pharmacological effects due to presence of active compounds. This study describes a method of using ultra performance liquid chromatography (UPLC) coupled with photodiode array (PDA) detector for the separation of phenolic compounds in M. chamomilla and its crude extracts. Separation was conducted on C18 column (150 mm × 2 mm, 1.8 µm) using a gradient elution with a mobile phase consisting of acetonitrile and 4% aqueous acetic acid at 25°C. The method proposed was validated for determination of free and total apigenin and apigenin 7-glucoside contents as bioactive compounds in the extracts by testing sensitivity, linearity, precision and recovery. In general, UPLC produced significant improvements in method sensitivity, speed and resolution. Extraction was performed with methanol, 70% aqueous ethanol and water solvents. Total phenolic and total flavonoid contents ranged from 1.77 to 50.75 gram (g) of gallic acid equivalent (GAE)/100 g and 0.82 to 36.75 g quercetin equivalent (QE)/100 g in dry material, respectively. There was a considerable difference from 40 to 740 mg/100 g for apigenin and 210 to 1110 mg/100 g for apigenin 7-glucoside in dry material.
  • V. Sabale, V. Patel, A. Paranjape Pages 39-48
    Mucoadhesive drug delivery systems were developed to sustain drug delivery via various mucus membranes for either local or systemic delivery of poorly absorbed drugs such as peptides and proteins as well as drugs that are subjected to high first-pass metabolism. The present study was undertaken to use isolated Calendula mucilage as a mucoadhesive agent and to formulate controlled release buccoadhesive tablets with an intention to avoid hepatic first-pass metabolism as well as to enhance residence time of drug in the buccal cavity. The mucilage was isolated from the Calendula petals by aqueous extraction method and characterized for various physiochemical parameters as well as for its adhesive properties. By using direct compression technique, tablets were prepared containing dried mucilage and chlorpheniramine maleate (CPM) as a model drug. Three batches of tablets were prepared and evaluated containing three mucoadhesive components namely Methocel K4M, Carbopol 974P and isolated Calendula mucilage in 16.66%, 33.33 % and 50 % (1:2:3 ratio) resulting in 9 different formulations. FTIR studies between mucilage and CPM suggested the absence of a chemical interaction between CPM and Calendula mucilage. The results of the study showed that the isolated mucilage had good physicochemical and morphological characteristics and tablets conformed to the pharmacopoeial specifications. Also in vitro release studies showed controlled action of drug with increasing the concentration of the isolated Calendula mucilage as a mucoadhesive agent in the formulations. Permeability studies indicated that permeability behavior was not statistically different (P>0.05) by changing the mucoadhesive component. The formulated mucoadhesive tablets for buccal administration containing 75 mg Calendula mucilage showed controlled drug release. Thus, mucoadhesive natural Calendula mucilage based buccal tablets for controlled release were successfully formulated.
  • A. Mostajeran, A. Gholaminejad, G. Asghari Pages 49-57
    Turmeric (Curcuma longa L.) is a perennial rhizomatous plant from the family of Zingibraceae, native in South Asia. The main components of turmeric are curcuminoids and essential oil which are responsible for turmeric characteristic such as odor and taste. Due to the large areas of saline land in Iran and less information related to cultivation of turmeric, in this research, the effect of salinity on growth, curcumin and essential oil of turmeric was evaluated. Rhizomes were planted in coco peat and perlite for germination. Then uniform germinated rhizomes transferred to hydroponic condition containing Hoagland''s solution. Two months old plants were exposed to salinity (0, 20, 60 and 100 mM NaCl) for two months via hydroponic media using Hoagland’s solution. Then dry weight of different plant parts, chlorophyll, curcumin and essential oil components of turmeric were determined. The result indicated that, dry weight reductions in 100 mM NaCl were 191%, 141%, 56%, 30% in leaf, pseudo-stem, root and rhizome, respectively (This is almost equal to 6.9, 2.87, 0.34 and 0.23 mg plant-1 mM-1NaCl reduction of dry weight, respectively). The reductions in chlorophyll a and b are almost 3.32 and 0.79 µg/gFW respectively due to one unit addition of NaCl (P < 0.05). The addition of curcumin of rhizome for four months old plant versus three months were almost 5 fold for 0 mM NaCl and 2 fold for 100 mM NaCl due to one month of delay in harvest. Low salinity has positive effect in curcumin production but higher salinity (higher than 60 mM) had adverse effect and causes 24% reduction of curcumin compared to control plants. There were more para-cymene and terpineol in volatile oils of turmeric rhizome than the other components, most of the volatile oil compounds were unchanged or varied slightly as salinity changed.
  • N. Sethi, R. Bhatti, Mps Ishar Pages 59-67
    Nicotinic ligands have been studied as novel therapeutic interventions in pain therapeutics since a long time. Several nicotinic agonists have been withdrawn from later stages of clinical trials due to lack of efficacy or narrow therapeutic window. These have been documented to act in the central nervous system and produce a wide range of pharmacological effects, including memory enhancing and analgesic actions, antianxiety, antidepressant and muscle coordination. Taking cognizance of the wide pharmacological profile of nicotine and its ligands, it was decided to evaluate some novel isoxazolidine analogues of nicotine for their potential as analgesics, using animal models like Eddy’s hot plate and Tail immersion method. The compounds showed marked decrease in hyperalgesic response as compared to pentazocine at a wide range of doses. They were well tolerated as none of the compounds was found to have any seizure potential or mortality even at the highest doses. Thus, these compounds can be developed as potent antinociceptives with better safety profile than nicotine and other currently available pain therapeutics.
  • K. Mahnam, B. Saffar, M. Mobini, Dehkordi, A. Fassihi, A. Mohammadi Pages 69-82
    Heavy metal toxicity has serious adverse effects on the environment. The metal sequestering characteristics of a novel metal binding peptide (Glu-Cys)11 Gly+linker+hexahistidine (EC11:His6) was investigated to determine if it can absorb Cu2+ or Zn2+ cations. Molecular dynamics simulations were carried out using a model of 6 Cu2+ or Zn2+ and other ions enclosed in a fully hydrated simulation box with the designed peptide. Totally, 240 nano second (ns) simulations were done in three phases. Results showed that the selected linker is able to separate two domains of this peptide and that the carboxyl oxygens of Glu residues of EC11 in the designed peptide can absorb these ions. Sequestration of Cu2+ or Zn2+ ions by the designed peptide does not change overall tertiary and secondary structures of peptide.