The Impact of the Oil Phase Selection on Physicochemical Properties, Long-Term Stability, In Vitro Performance and Injectability of Curcumin-Loaded PEGylated Nanoemulsions

A nanotechnology-based approach to drug delivery presents one of the biggest trends in biomedical science that can provide increased active concentration, bioavailability, and safety compared to conventional drug-delivery systems. Nanoemulsions stand out amongst other nanocarriers for being biodegradable, biocompatible, and relatively easy to manufacture. For improved drug-delivery properties, longer circulation for the nanoemulsion droplets should be provided, to allow the active to reach the target site. One of the strategies used for this purpose is PEGylation. The aim of this research was assessing the impact of the oil phase selection, soybean or fish oil mixtures with medium chain triglycerides, on the physicochemical characteristics and injectability of curcumin-loaded PEGylated nanoemulsions. Electron paramagnetic resonance spectroscopy demonstrated the structural impact of the oil phase on the stabilizing layer of nanoemulsions, with a more pronounced stabilizing effect of curcumin observed in the fish oil nanoemulsion compared to the soybean oil one. The design of the experiment study, employed to simultaneously assess the impact of the oil phase, different PEGylated phospholipids and their concentrations, as well as the presence of curcumin, showed that not only the investigated factors alone, but also their interactions, had a significant influence on the critical quality attributes of the PEGylated nanoemulsions. Detailed physicochemical characterization of the NEs found all formulations were appropriate for parenteral administration and remained stable during two years of storage, with the preserved antioxidant activity demonstrated by DPPH and FRAP assays. In vitro release studies showed a more pronounced release of curcumin from the fish oil NEs compared to that from the soybean oil ones. The innovative in vitro injectability assessment, designed to mimic intravenous application, proved that all formulations tested in selected experimental setting could be employed in prospective in vivo studies. Overall, the current study shows the importance of oil phase selection when formulating PEGylated nanoemulsion

Rapid detection of olive oil blends using a paper-based portable microfluidic platform

This paper presents an application of a portable microfluidic platform based on a filter paper on which multi-walled carbon nanotubes were deposited to quickly determine the quality of olive oil by measuring electrical resistance. Three different types of filter paper with different pore sizes and different filtration rates were used in the middle of the microfluidic platform, as a material for soaking a blend of olive and high-oleic sunflower oil. The rapid prototyping xurographic technique was used to fabricate the complete microfluidic platform. For testing purposes, oil blends in various proportions were deposited through the inlet on the top of the platform. The variation in electrical resistance at room temperature was measured, using the Chemical Impedance Analyzer, successfully indicating oil proportions in measured blends. We obtained the change of resistance in the range from 0.26 MΩ to 2.79 MΩ per percentage of olive oil content, for corresponding linearity index from 0.71 to 0.99, for papers labelled with 44–45, respectively. Additionally, a prototype of electronic device was developed for acquisition and displaying measured data, based on the created microfluidic platform

High amount of lecithin facilitates oral delivery of a poorly soluble pyrazoloquinolinone ligand formulated in lipid nanoparticles: Physicochemical, structural and pharmacokinetic performances

Preclinical development of deuterated pyrazoloquinolinone ligands, promising drug candidates for various neuropsychiatric disorders, was hindered by unusually low solubility in water and oils. DK-I-60-3 (7-methoxy-d3- 2-(4-methoxy-d3-phenyl)-2,5-dihydro-3Hpyrazolo[4,3-c]quinolin-3-one) is one of such pyrazoloquinolinones, and we recently reported about increased oral bioavailability of its nanocrystal formulation (NC). Lipid nano- particles (LNP) with a high concentration of lecithin, which enhances loading capacity of the lipid matrix, may give rise to further improvement. After preformulation studies by differential scanning calorimetry and polarized light microscopy, LNP were prepared by the hot high pressure homogenization, and characterized in terms of particle size, morphology, and encapsulation efficacy. The layered structure visible on atomic force micrographs was confirmed by nuclear magnetic resonance. Obtained formulations were desirably stable, with small particle size (99 %). Lecithin was partially fluid and most probably located in the outer shell of the particle, together with DK-I-60-3. While the hydrophobic part of polysorbate 80 was completely immobilized, its hydrophilic part was free in the aqueous phase. In oral neuropharmacokinetic study in rats, an around 1.5-fold increase of area under the curve with LNP compared to NC was noticed both in brain and plasma. In bioavailability study, F value of LNP (34.7 ± 12.4 %) was 1.4-fold higher than of NC (24.5 ± 7.8 %); however, this difference did not reach statistical significance. Therefore, employment of LNP platform in preclinical formulation of DK-I-60-3 imparted an incremental improvement of its physicochemical as well as pharmacokinetic behavior

Mechanism of Cu(II), Cd(II) and Pb(II) ions sorption from aqueous solutions by macroporous poly(glycidyl methacrylate-co-ethylene glycol dimethacrylate)

The mechanism of Cu(II), Cd(II) and Pb(II) ions sorption from aqueous solutions by macroporous poly(glycidyl methacrylate-co-ethylene glycol dimethacrylate) (PGME) functionalized by reaction of the pendant epoxy groups with diethylene triamine (PGME-deta) was studied using X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR) analysis. Atomic force microscopy (AFM) and scanning energy-dispersive X-ray spectroscopy (SEM-EDX) were used for the determination of surface morphology of the copolymer particles. The sorption behavior of heavy metals Cu(II), Cd(II) and Pb(II) ions sorption was investigated in batch static experiments under non-competitive conditions at room temperature (298 K). The obtained results were fitted to pseudo-first order, pseudo-second order and intraparticle diffusion kinetic model. The kinetics studies showed that Cu(II), Cd(II) and Pb(II) sorption obeys the pseudo-second-order model under all investigated operating conditions with evident influence of pore diffusion