The formation of a Schiff-base with N2O2 donor atoms derived from the hydrazine segment and its metal complexes are reported. The Schiff-base ligand; N’-((1R,2S,4R,5S,Z)-2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-ylidene)furan-2-carbohydrazide (HL) was prepared from the reaction of furan-2-carbohydrazide with (1R, 2R, 4R, 5S)-2,4-diphenyl-3-azabicyclo[3.3.1]nonan-9-one (M1) in ethanol medium. The reaction of the title ligand with selected metal ions Cr(III), Mn(II), Ni(II), Cu(II), Zn(II) and Cd(II) gave complexes with the general formula [M(L)Cl2], (where: M = Cr(III), Mn(II), Ni(II), Cu(II), Zn(II) and Cd(II)). Spectroscopic analyses Fourier transform infrared (FT-IR), Nuclear Magnetic Resonance (NMR) Carbon-13 nuclear magnetic resonance (1H- and 13C-NMR), mass and electronic spectroscopy and atomic absorption) along with elemental microanalysis (C.H.N), chloride percentage, conductivity measurements, magnetic moments and melting point were used to establish the identity of ligand and complexes. The biological activity of the synthesized compounds towards bacterial strains (G+ and G-) was investigated.
Clotrimazole (CLO) is an antimycotic imidazole derivative applied locally for the treatment of vaginal yeast infections. In this study, CLO was formulated as vaginal mucoadhesive hydrogel, using different types of mucoadhesive polymers to ensure prolonged contact between active ingredient and vaginal mucosa.
Physicochemical properties of the prepared formulas were evaluated as a visual inspection, pH, swelling index, spreadability, and mucoadhesive characteristics, in addition to an in-vitro drug release. The influence of type and concentration of polymers as CMC-Na (1.5, 2.5, and 3.5%w/w), carbopol 940( 0.25, 0.5, and 1 %w/w) and poloxamer 407 (15, 25, 30%w/w) on CLO release from the prepared gels were also invest
... Show MoreLetrozole (LZL) is a non-steroidal competitive aromatase enzyme system inhibitor. The aim of this study is to improve the permeation of LZL through the skin by preparing as nanoemulsion using various numbers of oils, surfactants and co-surfactant with deionized water. Based on solubility studies, mixtures of oleic acid oil and tween 80/ transcutol p as surfactant/co-surfactant (Smix) in different percentages were used to prepare nanoemulsions (NS). Therefore, 9 formulae of (o/w) LZL NS were formulated, then pseudo-ternary phase diagram was used as a useful tool to evaluate the NS domain at Smix ratios: 1:1, 2:1 and 3:1.
Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
... Show MoreMagnetic plaster kiln dust (MPKD) was synthesized as a unique, low-cost composite reused of byproduct plaster kiln dust (PKD), which is considered a source of air pollution. The FESEM, EDS, XRD, FTIR, VSM, and BET tests were used to characterize the MPKD. The characterization revealed that the MPKD was nanotubes non-agglomerated and super-paramagnetic with a high specific surface area (102.7 m2/g). Compared with the specific area of other materials (composites), the MPKD could be considered a promising substance in the field of water/wastewater treatment.
Background: The treatment of schizophrenia typically involves the use of olanzapine (OLZ), a typical antipsychotic drug that has poor oral bioavailability due to its low solubility and first-pass effect. Objective: To prepare and optimize OLZ as nanoparticles for transdermal delivery to avoid problems with oral administration. Methods: The nanoprecipitation technique was applied for the preparation of eight OLZ nanoparticles by using different polymers with various ratios. Nanoparticles were evaluated using different methods, including particle size, polydispersity index (PDI), entrapment efficiency (EE%), zeta potential and an in vitro release study. The morphology was evaluated by a field emission scanning electron microscope (F
... Show MoreLiquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liq
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The effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of differ
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