Preparation and characterization of cyclodextrin inclusion complex of naringenin and critical comparison with phospholipid complexation for improving solubility and dissolution

Naringenin, a flavonoid specific to citrus fruits shows a variety of therapeutic effects like anti-inflammatory, anticarcinogenic, and antitumour effects. But it is associated with some limitations like poor water solubility, poor dissolution, lower half-life, and rapid clearance from the body. With the aim of improving amorphous nature, water solubility, and dissolution profile of naringenin and its complexes were prepared with β-cyclodextrin in three different molar ratios (1:1, 1:2, and 1:3) by solvent evaporation method. These complexes were characterized for solubility, drug content, chemical interaction (using FTIR), phase transition behavior (using DSC), crystallinity (using XRPD), surface morphology (using SEM), and in vitro dissolution study. The results were also critically compared with the results obtained from naringenin-phospholipid complexes (from author’s previous study). The prepared complexes showed high drug content (ranging from 69.53 to 84.38 %) and about two fold improvement in water solubility (from 41.81 to 76.31 μg mL^?1 in the complex with 1:3 ratio). SEM of the complexes showed irregular and rough surface morphology. FTIR, DSC, and XRPD data confirmed the formation of the complex. Unlike the free naringenin which showed a total of only 48.78 % drug release at the end of 60 min, the complex showed 98.0–100 % in dissolution study. Thus it was concluded that the β-cyclodextrin of naringenin may be of potential use for improving bioavailability of poorly soluble phytoconstituents/herbal drugs. On critical comparison with the phospholipid complex of naringenin both the techniques were found almost equally effective in improving the solubility and the dissolution performance of naringenin in the complex form.     

Development and Validation of a High-Performance Thin-Layer Chromatographic Method for the Assay of Ternary Mixtures Containing Cetirizine Dihydrochloride in Pharmaceutical Dosage Forms

JPC – Journal of Planar Chromatography – Modern TLC - A highly validated and selective high-performance thin-layer chromatography (HPTLC) method was developed for the determination of...     

Selective Monofunctionalization Enabled by Reaction‐History‐Dependent Communication in Catalytic Rotaxanes

Selective monofunctionalization of substrates with distant, yet equally reactive functional groups is difficult to achieve, as it requires the second functional group to selectively modulate its reactivity once the first functional group has reacted. We now show that mechanically interlocked catalytic rings can effectively regulate the reactivity of stoppering groups in rotaxanes over a distance of about 2 nm. Our mechanism of communication is enabled by a unique interlocked design, which effectively removes the catalytic rings from the substrates by fast dethreading as soon as the first reaction has taken place. Our method not only led to a rare example of selective monofunctionalization, but also to a “molecular if function”. Overall, the study presents a way to get distant functional groups to communicate with each other in a reaction‐history‐dependent manner by creating linkers that can ultimately perform logical operations at the molecular level.     

Validation of TPEN as a Zinc Chelator in Fluorescence Probing of Calcium in Cells with the Indicator Fura-2

Fura-2 is widely used as a fluorescent probe to monitor dynamic changes in cytosolic free calcium in cells, where Ca²⁺ can enter through several types of voltage-operated or ligand-gated channels. However, Fura-2 is also sensitive to other metal ions, such as zinc, which may be involved in ionic channels and receptors. There is interest, in particular, in studying the synapses between mossy fibers and CA3 pyramidal cells which contain both calcium and high quantities of free or loosely bound zinc. We have found, through fluorescence probing, that endogenous zinc inhibits mossy fiber calcium transients. However, since these results might be explained by an effect of the zinc chelator N,N,N’,N’-tetrakis(2-pyridylmethyl)ethylenediamine (TPEN) on the spectral properties of Fura-2, we have carried out a validation of the method through fluorescence excitation spectra of the complex Fura-2/calcium, and show that TPEN does not affect these spectra. This supports the idea that the observed calcium enhancement is related to a zinc inhibition of presynaptic calcium mechanisms, and confirms the use of the chelator TPEN as a general procedure for the biophysical study of Ca(II) in the presence of Zn(II) using Fura-2.     

Purification of soybean oil with phospholipase Al

An enzymatic degumming step in the production of edible soybean oil is carried out. The phosphatides are present in free hydratable form (HP) or in nonhydratable form (NHP). The main characteristic of the discovery is the use of phospholipid A1 (Lecithin Ultra) enzyme, which catalyzes reactions at specific temperatures. The mechanism includes the conversion of nonhydratable phospholipids into water-soluble lysophospholipids, which are then removed by centrifuge, yielding degumming oil low in phosphorus. The effects of important determining factors affecting oil degumming such as enzyme dosage, temperature and pH are investigated.     

Photonic band gaps based on tetragonal lattices of slanted pores

We describe broad new classes of three-dimensional (3D) structures which, when made of silicon, exhibit robust 3D photonic band gaps of up to 25% of the gap center frequency. The proposed photonic crystals are readily amenable to very high precision microfabrication using established techniques such as x-ray lithography and template inversion. Each architecture consists of a set of oriented cylindrical pores emanating from a two-dimensional (2D) square lattice mask with a two-point basis. Large bandwidth, microcircuits for light may be incorporated within the resulting photonic band gaps using an intercalated 2D photonic crystal layer.     

Nanoscale zeeman localization of charge carriers in diluted magnetic semiconductor-permalloy hybrids

We investigate the possibility of charge carrier localization in magnetic semiconductors due to the presence of a highly inhomogeneous external magnetic field. As an example, we study in detail the properties of a magnetic semiconductor-permalloy disk hybrid system. We find that the giant Zeeman response of the magnetic semiconductor in conjunction with the highly nonuniform magnetic field created by the vortex state of a permalloy disk can lead to Zeeman localized states at the interface of the two materials. These trapped states are chiral, with chirality controlled by the orientation of the core magnetization of the permalloy disk. We calculate the energy spectrum and the eigenstates of these Zeeman localized states, and discuss their experimental signatures in spectroscopic probes.     

Synthesis and Characterization of Some New Quinoxalin-2(1H)one and 2-Methyl-3H-quinazolin-4-one Derivatives Targeting the Onset and Progression of CRC with SAR,Molecular Docking,and ADMET Analyses

The pathogenesis of colorectal cancer is a multifactorial process. Dysbiosis and the overexpression of COX-2 and LDHA are important effectors in the initiation and development of the disease through chromosomal instability, PGE2 biosynthesis, and induction of the Warburg effect, respectively. Herein, we report the in vitro testing of some new quinoxalinone and quinazolinone Schiff’s bases as: antibacterial, COX-2 and LDHA inhibitors, and anticolorectal agents on HCT-116 and LoVo cells. Moreover, molecular docking and SAR analyses were performed to identify the structural features contributing to the biological activities. Among the synthesized molecules, the most active cytotoxic agent, (6d) was also a COX-2 inhibitor. In silico ADMET studies predicted that (6d) would have high Caco-2 permeability, and %HIA (99.58%), with low BBB permeability, zero hepatotoxicity, and zero risk of sudden cardiac arrest, or mutagenicity. Further, (6d) is not a potential P-gp substrate, instead, it is a possible P-gpI and II inhibitor, therefore, it can prevent or reverse the multidrug resistance of the anticancer drugs. Collectively, (6d) can be considered as a promising lead suitable for further optimization to develop anti-CRC agents or glycoproteins inhibitors.     

The Influence of Mind Mapping on Eighth Graders’ Science Achievement

This study assessed the influence of using mind maps as a learning tool on eighth graders’ science achievement, whether such influence was mediated by students’ prior scholastic achievement, and the relationship between students’ mind maps and their conceptual understandings. Sixty‐two students enrolled in four intact sections of a grade 8 science classroom were randomly assigned to experimental and comparison conditions. Participants in the experimental group received training in, and constructed, mind maps throughout a science unit. Engagement with mind mapping was counterbalanced with involving the comparison group participants with note summarization to control for time on task as a confounding variable. Otherwise, the intervention was similar for both groups in all respects. A multiple choice test was used to measure student gains across two categories and three levels of achievement. Data analyses indicated that the experimental group participants achieved statistically significant and substantially higher gains than students in the comparison group. The gains were not mediated by participants’ prior scholastic achievement. Analyses also indicated that iconography was not as central to participants’ mind maps as often theorized. Depicting accurate links between central themes and major and minor concepts, and using colors to represent concepts were the major aspects that differentiated the mind maps built by students who achieved higher levels of conceptual understanding.