Pathogenic microorganisms are becoming more and more resistant to antimicrobial agents. So the synthesis of new antimicrobial agents is very important. In this work, new 5-fluoroisatin-chalcone conjugates 5(a–g) were synthesized based on previous research that showed the modifications of the isatin moiety led to the synthesis of many derivatives that have antimicrobial activity. 4-aminoacetophenone reacts with 5-fluoroisatin to form Schiff base (3), which in turn reacts with two different groups of aromatic (carbocyclic and heterocyclic) aldehydes 4(a–g) separately to form the final compounds 5(a–g). Proton-nuclear magnetic resonance (¹H-NMR) and Fourier-transform infrared (FT-IR) spectroscopy were used to confirm the chemical structures of the newly prepared compounds. Finally, the final compounds, 5-fluoroisatin-chalcone conjugates 5(a–g), were screened for their antimicrobial activities and compared with three different references: vancomycin, ciprofloxacin, and fluconazole. They appeared to be good candidates as antibacterial agents against E. coli and S. aureus as well as antifungal agents against C. albicans. In general and for comparison, the antifungal activity of the final compounds 5(a–g) was more potent than their antibacterial activity. Finally, for the antimicrobial activity, the most active compound of these series was compound 5e, while compound 5g was the least active one.
Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MorePolymeric microsphere devices occupy a wide range in the field of controlled drug delivery. Subcutaneous injectable preparations of Poly(Lactide-co-Glycolide) (PLGA) microsphere of Daptomycine were prepared by solvent extraction/evaporation technique using different copolymers ratio and molecular weights. Four formulations were prepared (F1-F4) and characterized in term of particle size, surface morphology, bulk density and porosity in addition to the drug content. The effects of the above parameters on the in-vitro release study were evaluated. These formulas were evaluated also for their in-vivo release profile using rat (as an animal model) and
... Show MoreThis study designed to prepare ultrafine apixaban (APX) o/w nanoemulsion (NE) based gel with droplet size below 50 nm as a good method for transdermal APX delivery without using permeation enhancer, alternatively, the formulation components itself act as permeation enhancer. APX, a potent oral anticoagulant drug that selectively and directly inhibit coagulation factor Xa, was selected as a good candidate for transdermal delivery as it displays poor water solubility (0.028 mg/mL) and low bioavailability (50%). APX-NE gel was prepared using triacetin, triton-x-100 and carbitol as oil phase, surfactant and cosurfactant respectively, while Carbopol 940 used as a gelling agent. Ex vivo permeation of APX-NE gel through human stratum c
... Show MoreOral fast dissolving films (OFDFs) are the most innovative oral solid pharmaceutical dosage form, especially for elderly and pediatric patients who may have dysphagia. Bilastine (BLA), is a second – generation antihistamine used to manage allergy symptoms; it is very slightly soluble in water. The main objective of this research was to enhance the solubility and dissolution rate of BLA by complexation technique. Ternary complex of BLA: methyl β- cyclodextrin (M-β-CD): soluplus® 5% w/w was prepared via solvent evaporation technique as a trial to enhance its solubility to be prepared as OFDF by incorporated into aqueous polymeric solution. Seven formulas of OFDFs were prepared using the solvent casting method using
... Show MoreThe present study revealed a low-cost process for utilizing desert sand for preparing nanosilica by sol-gel technique. This work required sodium hydroxide, concentrated hydrochloric acid, distillate water as raw materials, and Iraqi sand. Nanosilica sample was characterized by X-Ray Diffraction (XRD), scanning electron microscopy analysis (SEM), atomic force microscope(AFM), surface area (BET) method, and fourier transform infrared (FTIR). The XRD result of produced sample is referred to as amorphous silica, and it has a broad peak at 2Θ= 22° – 22.5 º. SEM showed spherical, agglomerated silica particles with a diameter range of 26.57–28.93 nm. In addition, the average particle size was 76.35nm, with a dimension range of 40-11
... Show MoreThe reservoir characterization and rock typing is a significant tool in performance and prediction of the reservoirs and understanding reservoir architecture, the present work is reservoir characterization and quality Analysis of Carbonate Rock-Types, Yamama carbonate reservoir within southern Iraq has been chosen. Yamama Formation has been affected by different digenesis processes, which impacted on the reservoir quality, where high positively affected were: dissolution and fractures have been improving porosity and permeability, and destructive affected were cementation and compaction, destroyed the porosity and permeability. Depositional reservoir rock types characterization has been identified de