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OBJECTIVES: the aim of the current study was to assess the effect of a ß2-adrenoceptor agonist; namely salbutamol, on hyperalgesic as well as nerve dysfunction components of diabetic peripheral neuropathy. MATERIAL AND METHODS: the present study was conducted on 60 male Wistar albino rats divided into six groups. Groups I and II were normal control rats injected by a single i.p. injection of normal saline and received 2% gum acacia (Group I) or salbutamol (Group II) for six weeks, starting one week following saline injection. Groups III-VI: rats that were rendered diabetic by a single i.p. injection of STZ and received either 2% gum acacia, salbutamol, salbutamol and propranolol or salbutamol and atenolol, respectively daily orally for six weeks, starting one week following STZ injection. RESULTS: vehicle-treated diabetic rats exhibited: significant sciatic nerve dysfunction in the form of significantly prolonged distal latency and significantly decreased maximum peak and peak to peak amplitude of compound muscular action potential, significant thermal and mechanical hyperalgesia evidenced by significant decrease in hot plate latency, tail-flick latency and vocalization threshold, respectively. Salbutamol administration improved nerve dysfunction as well as thermal and mechanical hyperalgesia. These effects of salbutamol are most likely mediated by ß2-adrenoceptors evidenced by significant abolishment of salbutamol effects after administration of the non-selective rather than the selective beta blockers; propranolol and atenolol, respectively. CONCLUSIONS: chronic administration of salbutamol could ameliorate DPN, an effect which is most likely mediated by ß2-adrenoceptors.

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Oxybenzone wax microparticles (MPs) were prepared by the hydrophobic congealable disperse phase method. The formulation of oxybenzone-loaded MPs was optimized using a 24 experimental design. Factorial analysis indicated that the main MP characteristics were influenced by initial drug loading, emulsification speed, emulsifier concentration and hydrophilic-lipophilic balance. MPs were spherical with 50.5­88.1 µm size range, 17.8­38.9 drug content in mg/100 mg MPs and 33.1­87.2% oxybenzone release in 1 h. A wide range of sunscreen delivery systems suitable for different formulation purposes were generated which may contribute to the advanced formulation of sunscreen products with improved performance.

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Competitive immunoassays for Cd(II), Co(II), Pb(II) and U(VI) were developed using identical reagents in two different assay formats, a competitive microwell format and an immunosensor format with the KinExA 3000. Four different monoclonal antibodies specific for complexes of EDTA-Cd(II), DTPA-Co(II), 2,9-dicarboxyl-1,10-phenanthroline-U(VI), or cyclohexyl-DTPA-Pb(II) were incubated with the appropriate soluble metal-chelate complex. In the microwell assay format, the immobilized version of the metal-chelate complex was present simultaneously in the assay mixture. In the KinExA format, the antibody was allowed to pre-equilibrate with the soluble metal-chelate complex, then the incubation mixture was rapidly passed through a microcolumn containing the immobilized metal-chelate complex. In all four assays, the KinExA format yielded an assay with 10-1000-fold greater sensitivity. The enhanced sensitivity of the KinExA format is most likely due to the differences in the affinity of the monoclonal antibodies for the soluble versus the immobilized metal-chelate complex. The KinExA 3000 instrument and the Cd(II)-specific antibody were used to construct a prototype assay that could correctly assess the concentration of cadmium spiked into a groundwater sample. Mean analytical recovery of added Cd(II) was 114.25+/-11.37%. The precision of the assay was satisfactory; coefficients of variation were 0.81-7.77% and 3.62-14.16% for within run and between run precision, respectively.

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A rapid, simple, and reliable competitive immunoassay was developed and validated for measurement of Cd(II) in environmental water samples. This assay employed a monoclonal antibody that recognizes Cd(II)-EDTA complexes as capture reagent and a Cd(II)-EDTA conjugate of horseradish peroxidase as an enzyme label. The assay depended on a competitive binding reaction between the enzyme conjugate and Cd(II)-EDTA complexes, derived from the environmental water sample, for the binding sites of the immobilized antibody. The concentration of Cd(II) in the sample was quantified by the ability of its EDTA complexes to inhibit the binding of the enzyme conjugate to the antibody and, subsequently, color formation in the assay. The assay was specific to Cd(II), with a limit of detection of 0.3 ppb. Ca(II), Mg(II), and Fe(III), the metal ions commonly found in ambient water at relatively high concentrations, did not interfere with the assay. Mean analytical recovery of added Cd(II) was 100.29 +/- 3.60. The precision of the assay was satisfactory; coefficients of variation were 3.6-10.9 and 4.81-10.21% for intra- and interassay precision, respectively. The assay compared favorably with graphite furnace atomic absorption spectroscopy in its ability to accurately measure Cd(II) spiked into water samples from a Louisiana bayou.

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A solvent-treatment technique aiming at manipulating the properties of powdered materials is reported. Potentials of the technique were assessed using sulphadiazine (SD). A suspension of the drug in a preselected solvent (5% aqueous ammonia solution) was stirred under controlled conditions. The solvent was subsequently removed and the material dried. The effect of experimental variables such as stirring speed and time, powder/solvent ratio and inclusion of additives (Tween 80, sodium chloride and PVP) on the properties of solvent treated SD was assessed. Data obtained were compared with those for SD recrystallized under identical conditions. Solvent treatment of SD in the absence of additives resulted in a limited change in crystal morphology as indicated by SEM. This was associated with improved flowability and a limited reduction in dissolution rate relative to untreated SD. On the other hand, recrystallized SD exhibited superior flowability but a considerably low dissolution rate. Solvent treatment of SD in the presence of 2% PVP produced a microgranular directly compressible material.

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Since 3-methoxy-4-hydroxyphenylglycol (MHPG) is a neutral metabolite from norepinephrine, it will be a diagnostic marker for mental diseases such as depression. For the development of an immunoassay, the natural enantiomer of MHPG would be required to prepare its antigen and to examine the specificity of the antibody. A natural enantiomer synthesized, however, has not been obtained so far. In this paper, we attempted to enantioseparate synthetic DL-MHPG and to assign D-enantiomer from the optical rotation of MHPG purified from human urine, because endogenous norepinephrine occurs as D-enantiomer which should metabolically generate D-MHPG. Enantioseparation conditions were tested using a Ceramospher Chiral RU-1 column (4.6 x 250 mm) at a flow rate of 0.5 ml/min. The resolution was adequate for the analysis and purification of synthetic DL- and the urinary MHPGs using methanol as a mobile phase and the column temperature at 0 degrees C, where DL-MHPG was detected as two peaks. The earlier peak (peak 1) showed (-) optical rotation, while the latter gave (+) optical rotation. After being treated with beta-glucuronidase, the normal human urine was extracted with ethyl acetate and then evaporated to dryness. The residue was suspended in water and the supernatant was analyzed and purified by a reversed phase column with a multi channel detector. A peak corresponding to MHPG was collected and concentrated to dryness. The pooled residues were dissolved in methanol and enantioseparated on the chiral HPLC. The urinary MHPG appeared as a single peak which was corresponded to the earlier peak of DL-MHPG and showing (-) optical rotation. Thus, the urinary MHPG was found to be D-(-)-MHPG. Then the absolute configuration of enantioseparated MHPGs were assigned to each optical rotation, judging from the chemical data and the metabolic pathway of the urinary D-MHPG. These enantiomers will be useful for studying on biochemistry and immunoassay.

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Siderophores selectively bind ferric iron and are involved in receptor-specific iron transport into bacteria. Several types of siderophores were synthesized, and growth-promoting or inhibitory activities when they were conjugated to carbacephalosporin, erythromycylamine, or nalidixic acid were investigated. Overall, 11 types of siderophores and 21 drug conjugates were tested against seven different bacterial species: Escherichia coli, Bordetella bronchiseptica, Pasteurella multocida, Pasteurella haemolytica, Streptococcus suis, Staphylococcus aureus, and Staphylococcus epidermidis. In some species, the inhibitory activities of the drug conjugates were associated with the ability of the bacteria to use the siderophore portion of the molecules for growth promotion in disc diffusion tests (0.04 mumol of conjugate or siderophore per disc). E. coli used catechol-based siderophore portions as well as hydroxamate-based tri-delta-OH-N-OH-delta-N-acetyl-L-ornithine ferric iron ligands for growth under iron-restricted conditions achieved by supplemental ethylenediamine di (O-hydroxyphenylacetic acid) (100 micrograms/ml) and was sensitive to carbacephalosporin conjugated to these siderophore types (up to a 34-mm-diameter inhibition zone). B. bronchiseptica used desferrioxamine B and an isocyanurate-based or trihydroxamate in addition to catechol-based siderophore portions for promotion but was not inhibited by beta-lactam conjugates partly because of the presence of beta-lactamase. P. multocida and P. haemolytica did not use any of the synthetic siderophores for growth promotion, and the inhibitory activities of some conjugates seemed partly linked to their ability to withhold iron from these bacteria, since individual siderophore portions showed some antibacterial effects. Individual siderophores did not promote S. suis growth in restrictive conditions, but the type of ferric iron ligands attached to beta-lactams affected inhibitory activities. The antibacterial activities of the intracellular-acting agents erythromycylamine and nalidixic acid were reduced or lost, even against S. aureus and S. epidermidis, when the agents were conjugated to siderophores. Conjugate-resistant E. coli mutants showed the absence of some iron-regulated outer membrane proteins in gel electrophoresis profiles and in specific phage or colicin sensitivity tests, implying that the drugs used outer membrane receptors of ferric complexes to get into cells.

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Siderophores bind ferric ions and are involved in receptor-specific iron transport into bacteria. Six types of siderophores were tested against strains representing the 12 different serotypes of Actinobacillus pleuropneumoniae. Ferrichrome and bis-catechol-based siderophores showed strong growth-promoting activities for A. pleuropneumoniae in a disk diffusion assay. Most strains of A. pleuropneumoniae tested were able to use ferrichrome (21 of 22 or 95%), ferrichrome A (20 of 22 or 90%), and lysine-based bis-catechol (20 of 22 or 90%), while growth of 36% (8 of 22) was promoted by a synthetic hydroxamate, N5-acetyl-N5-hydroxy-L-ornithine tripeptide. A. pleuropneumoniae serotype 1 (strain FMV 87-682) and serotype 5 (strain 2245) exhibited a distinct yellow halo around colonies on Chrome Azurol S agar plates, suggesting that both strains can produce an iron chelator (siderophore) in response to iron stress. The siderophore was found to be neither a phenolate nor a hydroxamate by the chemical tests of Arnow and Csaky, respectively. This is the first report demonstrating the production of an iron chelator and the use of exogenous siderophores by A. pleuropneumoniae. A spermidine-based bis-catechol siderophore conjugated to a carbacephalosporin was shown to inhibit growth of A. pleuropneumoniae. A siderophore-antibiotic-resistant strain was isolated and shown to have lost the ability to use ferrichrome, synthetic hydroxamate, or catechol-based siderophores when grown under conditions of iron restriction. This observation indicated that a common iron uptake pathway, or a common intermediate, for hydroxamate- and catechol-based siderophores may exist in A. pleuropneumoniae.

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We propose a new process for making an array illuminator that combines the Talbot effect and the principle of holography. For high diffraction efficiency we use a thick phase hologram recorded in dichromated gelatin. Special conditions for the intensity uniformity of the recorded wave are required with this type of hologram. We discuss these conditions as a function of the pixel shape.

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Etoposide, a commonly used anticancer agent, has an aqueous solubility of 0.2 mg/mL. It is formulated for intravenous use as a more concentrated solution (Vepesid; 20 mg/mL) with polysorbate 80 and with cosolvents. In this work, hydrotropic agents such as sodium benzoate, sodium o-hydroxybenzoate (sodium salicylate), sodium 2,5-dihydroxybenzoate (sodium gentisate), and the sodium salts of 2,4-dihydroxy- and 2,6-dihydroxybenzoic acid and of 2,4,6-trihydroxybenzoic acid have been used as alternative solubilizers of etoposide. The weakest and strongest interactants with etoposide were, respectively, sodium benzoate and sodium 2,4,6-trihydroxybenzoate. The effect of mono- and dihydroxybenzoates on etoposide solubility was intermediate. Although sodium 2,4,6-trihydroxybenzoate is the most efficient solubilizer, its use is limited by its own low aqueous solubility. The effect of sodium salicylate and other formulation ingredients on the in vitro protein binding and precipitation of etoposide upon dilution with normal saline and human plasma has been studied. Etoposide binds to the extent of 94% to human serum albumin (HSA) and human plasma, but only 24% to bovine serum albumin (BSA) in vitro. Sodium salicylate significantly decreased the binding of the drug to both HSA and human plasma, whereas the components of Vepesid did not. Dilution of Vepesid (1:2 and 1:3) with plasma in vitro resulted in immediate precipitation, while the corresponding dilutions of etoposide aqueous solution (20 mg/mL in 2 M sodium salicylate) produced no precipitate for the first hour.

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