An Eco-Friendly Approach to the Control of Pathogenic Microbes and Anopheles stephensi Malarial Vector Using Magnesium Oxide Nanoparticles (Mg-NPs) Fabricated by Penicillium chrysogenum

The discovery of eco-friendly, rapid, and cost-effective compounds to control diseases caused by microbes and insects are the main challenges. Herein, the magnesium oxide nanoparticles (MgO-NPs) are successfully fabricated by harnessing the metabolites secreted by Penicillium chrysogenum. The fabricated MgO-NPs were characterized using UV-Vis, XRD, TEM, DLS, EDX, FT-IR, and XPS analyses. Data showed the successful formation of crystallographic, spherical, well-dispersed MgO-NPs with sizes of 7–40 nm at a maximum wavelength of 250 nm. The EDX analysis confirms the presence of Mg and O ions as the main components with weight percentages of 13.62% and 7.76%, respectively. The activity of MgO-NPs as an antimicrobial agent was investigated against pathogens Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans, and exhibited zone of inhibitions of 12.0 ± 0.0, 12.7 ± 0.9, 23.3 ± 0.8, 17.7 ± 1.6, and 14.7 ± 0.6 mm respectively, at 200 µg mL⁻¹. The activity is decreased by decreasing the MgO-NPs concentration. The biogenic MgO-NPs exhibit high efficacy against different larvae instar and pupa of Anopheles stephensi, with LC50 values of 12.5–15.5 ppm for I–IV larvae instar and 16.5 ppm for the pupa. Additionally, 5 mg/cm² of MgO-NPs showed the highest protection percentages against adults of Anopheles stephensi, with values of 100% for 150 min and 67.6% ± 1.4% for 210 min.     

Niosomal encapsulation of the antitubercular drug, pyrazinamide

It is estimated that more than one-third of the world population is infected with Mycobacterium tuberculosis. Pyrazinamide (PZA) plays a unique role in shortening therapy because it kills a population of semilatent tubercle bacilli residing in an acidic environment. Niosomes are vesicles made up of non-ionic surfactant and exhibit behavior similar to liposomes in vivo. Preparation of PZA niosomes took place using different molar ratios of Span 60 and Span 85, with cholesterol (CH) i.e. Span: CH (1:1) and (4:2). Dicetyl phosphate and stearyl amine were used in preparation of negative and positively charged niosomes, respectively. Free PZA was separated by cooling centrifugation and estimated spectrophotometrically at 268.4 nm. Niosomes were characterized by electron microscopy and differential scanning calorimetry. The highest percentage PZA entrapped was obtained using Span 60 and the molar ratio (4:2:1) negatively charged niosomes. This was followed by the neutral PZA neutral (4:2) Span 60 niosomes. Biological evaluation of selected PZA niosomal formulations took place on guinea pigs infected with M. tuberculosis. The present work is an attempt to target maximum concentration of PZA to the affected site (lungs) and to exclude undesirable side effects and decrease toxicity. Macrophage targeting and overcoming drug resistance is our final goal.     

Vibrational and AFM studies of adsorption of glycine on DLC and silicon-doped DLC

A better understanding of protein adsorption onto surfaces of materials is required to control biocompatibility and bioactivity. Diamond-like carbon (DLC) is known to have excellent biocompatibility. Various samples of a-C:H and silicon-doped a-C:H thin films (Si-DLC) were deposited onto silicon substrates using plasma-enhanced chemical vapour deposition (PECVD). Subsequently, the adsorption of the simplest amino acid glycine onto the surfaces of the thin films was investigated to elucidate the mechanisms involved in protein adhesion. The physicochemical characteristics of the surfaces, before and after adsorption of glycine, were investigated using Raman spectroscopy and atomic force microscopy (AFM). The Raman study highlighted a slight decrease in the I _D/I _G ratio with increasing the silicon dopant levels. Following exposure to glycine solutions, the presence of bands at ~1735 and ~1200 cm⁻¹ indicates that the adsorption of glycine onto the surfaces has taken place. Glycine was bound to the surfaces via both deprotonated carboxyl and protonated amino groups whilst, as the silicon content in the DLC film increased the adsorption of glycine decreased. AFM analysis showed that the surface roughness increased following exposure to glycine. These results show that at low silicon doping the adsorption of the amino acid was enhanced whilst increased doping levels led to a reduced adsorption compared to undoped DLC. Therefore, doping of DLC may provide an approach to control the protein adsorption.     

Preparation and optimization of monodisperse polymeric microparticles using modified vibrating orifice aerosol generator for controlled delivery of letrozole in breast cancer therapy

Abstract

Letrozole (LTZ) is effective for the treatment of hormone-receptor-positive breast cancer in postmenopausal women. In this work, and for the first time, using vibrating orifice aerosol generator (VOAG) technology, monodisperse poly-ε-caprolactone (PCL), and poly (D, L-Lactide) (PDLLA) LTZ-loaded microparticles were prepared and found to elicit selective high cytotoxicity against cancerous breast cells with no apparent toxicity on healthy cells in vitro. Plackett–Burman experimental design was utilized to identify the most significant factors affecting particle size distribution to optimize the prepared particles. The generated microparticles were characterized in terms of microscopic morphology, size, zeta potential, drug entrapment efficiency, and release profile over one-month period. Long-term cytotoxicity of the microparticles was also investigated using MCF-7 human breast cancer cell lines in comparison with primary mammary epithelial cells (MEC). The prepared polymeric particles were monodispersed, spherical, and apparently smooth, regardless of the polymer used or the loaded LTZ concentration. Particle size varied from 15.6 to 91.6?µm and from 22.7 to 99.6?µm with size distribution (expressed as span values) ranging from 0.22 to 1.24 and from 0.29 to 1.48 for PCL and PDLLA based microparticles, respectively. Upon optimizing the manufacture parameters, span was reduced to 0.162–0.195. Drug entrapment reached as high as 96.8%, and drug release from PDLLA and PCL followed a biphasic zero-order release using 5 or 30% w/w drug loading in the formulations. Long-term in vitro cytotoxicity studies indicated that microparticles formulations significantly inhibited the growth of MCF-7 cell line over a prolonged period of time but did not have toxic effects on the normal breast epithelial cells.     

Preparation and evaluation of optimized zolmitriptan niosomal emulgel

Objective: Novel niosomal formulation may be successfully applied to treat a systemic disease such as migraine through transdermal drug delivery system (TDDS), moreover, the treatment of topical diseases such as mycotic infections by targeting and localizing the drug to the stratum corneum. The current study aims to formulate zolmitriptan (Zt) in niosomal vesicles to potentiate its transdermal effect.

Significance: The development of a promising niosomal formulation will push the scaling up of pharmaceutical industry in this field.

Methods: Design- Expert 10 was used to design twelve formulations using Box-Behnken. Zt loaded niosomes were prepared by the thin film hydration method using Span 60(S 60), Span 80(S 80) along with cholesterol(Ch) at three different levels. The optimized formulation (F11) was formulated in Emulgel (1:1 emulsion/gel ratio).

Results: The vesicles revealed vesicle size (VS) ranging from 133.1 to 851.3?nm, zeta potential (ZP) ?43.8 to ?82.8?mV, entrapment efficiency (EE%) from 66.7 to 88.7%, and Zt release after 4?h up to 67%. Optimized niosomal formulation (F11) depicted the smallest VS (133.1?nm), highest EE (88.7%), high ZP (?80.6?mV) and satisfactory release after 4?h (61.5%). There was a significant difference (p <.05) in drug permeation after 8?h for niosomal F11(460.98?ug/cm²) and niosomal F11 loaded Emulgel (336.92?ug/cm²) compared to plain Zt loaded emulgel (160.83?ug/cm²). Niosomal F11 loaded emulgel showed thixotropic behavior of rapid recovery, significant bioavailability and pharmacokinetic parameters as compared to the plain Zt-loaded Emulgel.

Conclusion: Optimized F11 represents a promising formulation for transdermal drug delivery system to treat both topical and systemic diseases.     

Immediate release three-layered chewing gum tablets of fenoprofen calcium: preparation, optimization and bioavailability studies in healthy human volunteers

A three-layered gum tablet (1800 mg), containing 200 mg of Fenoprofen Calcium (Fn) with an inner core containing the drug, and two external layers containing antiadherent lubricant, has been prepared using direct compression. A 2(3) factorial plan has been designed to evaluate the effect of formulation variables namely, Pharmagum(?) M concentration, Maltodextrin type, and Co-adjuvant type on the release characteristics of Fn from the prepared tablets. The formula consisting of 65% Pharmagum(?) M, 75% Maltodextrin DE 39 and 5% Talc comparatively exhibited the highest release (66.59% ± 2.39) in the mouth after 5 min of chewing. Binary and ternary β-cyclodextrin (β-CD) complexation was adopted to enhance the release of Fn from the selected gum tablet. The highest significant release (p < 0.05) was achieved from the lyophilized ternary complex containing 100 mg of Fn in presence of polyvinylpyrrolidone (PVP K(25)), exhibiting a release of 88.25% ± 0.93 after 5 min of chewing. The relative bioavailability of the selected gum tablet was found to be 166.06% compared to Nalfon(?) 200 mg capsules. Reduction of the dose to 100 mg exhibited faster absorption rate than Nalfon(?) capsules. The obtained results suggest the possibility of reducing the dose of Fn in chewing gum.     

Niosomes as a potential drug delivery system for increasing the efficacy and safety of nystatin

Nonionic surfactant (NIS) vesicles (niosomes) formed from self-assembly of hydrated synthetic NIS monomers are capable of entrapping a variety of drugs and have been evaluated as an alternative to liposomes. Nystatin (NYS) is a polyene antifungal drug that has been used in the treatment of cutaneous, vaginal and oral fungal infections since the 1950s. The aim of this work is to encapsulate NYS in niosomes to obtain a safe and effective formula administered parenterally for neutropenic patients. NYS niosomes were prepared by the thin-film hydration method using Span 60 or Span 40 and cholesterol (CHOL). Stearylamine and dicetyl phosphate were added as the positive and negative charge-inducing agents (CIA), respectively. Two molar ratios were used, namely NIS/CHOL/CIA (1:1:0.1 and 2:1:0.25). Neutral and positively charged niosomes gave the highest encapsulation efficiencies. NYS niosomes were characterized using transmission electron microscopy, differential scanning calorimetry and dynamic light scattering. The release of neutral and negatively charged NYS niosomes was estimated, and it showed a slow sustained release profile. A 25-kGy γ-irradiation dose was sufficient to sterilize the investigated vesicles. NYS niosomes exerted less nephrotoxicity and hepatotoxicity in vivo, showed higher level of drug in vital organs and revealed pronounced efficacy in elimination of the fungal burden in experimental animals infected with Candida albicans compared with those treated with free NYS. Niosomal encapsulation thus provided means for parenteral administration of NYS, reducing its toxicity and making it a more active antifungal agent.     

Physicochemical and Radiation Hazardous Properties of Scale TENORM Waste: Evaluation by Different Analytical Techniques

The scale material in TENORM waste from petroleum industry was characterized using nuclear and non-nuclear techniques. The scale TENORM samples were collected from the Ras Shukeir area on the west bank of the Suez Gulf in Egypt during gas and oil production. These scales represent the TENORM deposits formed in the pipelines and removed during the periodical maintenance. X-ray fluorescence analysis showed that the main elements in all investigated fractions were Si, Fe, Mg, Ca, Sr, and Ba in addition to traces of some heavy elements, e.g. Pb, Cr, and Zn. The radioactivity concentrations of natural radionuclides ²²⁶Ra, ²³²Th, and ⁴⁰K in seven particle size fractions were found to be in the range from 14.1 ± 0.4 to 28.9 ± 0.9, from 5.0 ± 0.2 to 9.5 ± 0.4, and from 0.25 ± 0.02 to 0.43 ± 0.02 kBq kg^–1, respectively. The radiation hazard parameters were calculated. The values obtained are much greater than the accepted values. The results were compared to the values reported for other countries.     

Low Resistance Polycrystalline Diamond Thin Films Deposited by Hot Filament Chemical Vapour Deposition

Polycrystalline diamond thin films with outgrowing diamond (OGD) grains were deposited onto silicon wafers using a hydrocarbon gas (CH4) highly diluted with H2 at low pressure in a hot filament chemical vapour deposition (HFCVD) reactor with a range of gas flow rates. X-ray diffraction (XRD) and SEM showed polycrystalline diamond structure with a random orientation. Polycrystalline diamond films with various textures were grown and (111) facets were dominant with sharp grain boundaries. Outgrowth was observed in flowerish character at high gas flow rates. Isolated single crystals with little openings appeared at various stages at low gas flow rates. Thus, changing gas flow rates had a beneficial influence on the grain size, growth rate and electrical resistivity. CVD diamond films gave an excellent performance for medium film thickness with relatively low electrical resistivity and making them potentially useful in many industrial applications.     

Effects of Calcination on Structural, Photocatalytic Properties of TiO2 Nanopowders Via TiCl4 Hydrolysis

Photocatalytic degradation of methyl orange (MO) in water was examined using TiO₂ nanopowders under solar irradiation. These photocatalysts were successfully synthesized by hydrolysis of titanium tetra chloride (TiCl₄) in the temperature range of 70-95 °C and calcined at higher temperatures of between 400 and 900 °C. The samples prepared were characterized using x-ray powder diffraction, scanning electron microscope (SEM) and Fourier transform infrared spectrophotometer (FTIR). UV-Vis spectrometer was used for analyzing the concentration of MO in solution at different time intervals during the photodegradation experiment. Parameters affecting the photodegradation rate such as catalyst crystallinity, concentration of the catalyst, MO concentration, and pH of the solution have been investigated. The results indicate that TiO₂ nanopowder was antase at low calcination temperatures in the range of 400-500 °C. The sample calcined at 600 °C is composed of both anatase and rutile phase. Further increase in the temperature enhanced the intensities of diffraction peaks of the rutile phase. The size of the crystallites for all the samples prepared were found to be in the 6-13 nm range and from SEM micrographs it was in the range of 19-43 nm. The mixture of both phases exhibited a higher photoactivity in comparison with pure anatase or rutile catalysts.