In vivo oral insulin delivery via covalent organic frameworks

With diabetes being the 7th leading cause of death worldwide, overcoming issues limiting the oral administration of insulin is of global significance. The development of imine-linked-covalent organic framework (nCOF) nanoparticles for oral insulin delivery to overcome these delivery barriers is herein reported. A gastro-resistant nCOF was prepared from layered nanosheets with insulin loaded between the nanosheet layers. The insulin-loaded nCOF exhibited insulin protection in digestive fluids in vitro as well as glucose-responsive release, and this hyperglycemia-induced release was confirmed in vivo in diabetic rats without noticeable toxic effects. This is strong evidence that nCOF-based oral insulin delivery systems could replace traditional subcutaneous injections easing insulin therapy.

We report the successful use of a gastro-resistant covalent organic framework for in vivo oral delivery of insulin.     

Squarate complexes of some lanthanide ions in aqueous solution

The squarate complexes of Eu³⁺, Tb³⁺ and Tm³⁺ in aqueous solutions of 0.05M, 0.075M and 0.1M ionic strength are studied using the solvent extraction method. Effects of changes in the ionic strength on the stability constants of the complexes formed are discussed.     

Optimization of the preparation conditions of radioiodoepidepride: A dopamine D<Subscript>2</Subscript>receptor antagonist radioligand

Summary [¹²⁵I]iodepidepride, (s)-(-)-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[¹²⁵I]-iodo-2,3-dimethoxybenzamide is the iodine substituted analogue of isoremoxipride, both of which are very potent dopamine D₂-antagonists. Epidepride was radioiodinated using different oxidizing agents such as chloramine-T, iodogen, iodogen glass frit and hydrogen peroxide. Chloramine-T is a powerful oxidizing agent compared to both iodogen and hydrogen peroxide so that the side products, especially the chlorinated epidepride, decreases the radiochemical yield. This chlorinated epidepride is minimized in the case of iodogen and iodogen glass frit and are not observed in case of the non-chlorinated oxidizing agent hydrogen peroxide. TLC and HPLC were used to analyze the reaction components and to estimate both the radiochemical yield and purity. The reaction parameters such as reaction time, pH, epidepride and oxidizing agent concentrations and the stabilty of the final product were studied to optimize the radiochemical yield and purity. The optimized radiochemical yield was about 90% and the radiochemical purity of the final product was 99.9%.     

Fluorescence properties of recombinant tropomyosin containing tryptophan, 5-hydroxytryptophan and 7-azatryptophan

Tropomyosin mutants containing either tryptophan (122W), 5-hydroxytryptophan (5OH122W) or 7-azatryptophan (7N122W) have been expressed in Escherichia coli and their fluorescence properties studied. The fluorescent amino acids were located at position 122 of the tropomyosin primary sequence, corresponding to a solvent-exposed position c of the coiled-coil heptapeptide repeat. The emission spectrum of the probe in each mutant is blue-shifted slightly with respect to that of the probe in water. The fluorescence anisotropy decays are single exponential, with a time constant of 2-3 ns while the fluorescence lifetimes of the probes incorporated into the proteins, in water, are nonexponential. Because tryptophan in water has an intrinsic nonexponential fluorescence decay, it is not surprising that the fluorescence decay of 122W is well described by a triple exponential. The fluorescence decays in water of the nonnatural amino acids 5-hydroxytryptophan and 7-azatryptophan (when emission is collected from the entire band) are single exponential. Incorporation into tropomyosin induces triple-exponential fluorescence decay in 5-hydroxytryptophan and double-exponential fluorescence decay in 7-azatryptophan. The range of lifetimes observed for 5-hydroxyindole and 5-hydroxytryptophan at high pH and in the nonaqueous solvents were used as a base with which to interpret the lifetimes observed for the 5OH122W and indicate that the chromophore exists in several solvent environments in both its protonated and unprotonated forms in 5OH122W.     

Sorption behaviour of some actinides on silica gel from mineral acids and alcoholic solutions

Sorption of Th, Pa, U, Np and Pu on silica gel from HNO₃, HCl and HCl−ROH solutions was investigated. Equilibrium studies indicated sorption behaviour to vary greatly with the acid used. In mixtures of HCl with different alcohols, distribution coefficints were found to depend on alcohol percentage as well as on acidity. Results were discussed and conditions for possible separations were indicated.     

Global well-posedness and blow-up on the energy space for the inhomogeneous nonlinear Schrödinger equation

We consider the supercritical inhomogeneous nonlinear Schrödinger equation

$$i\partial_t u+\Delta u+|x|^{-b}|u|^{2\sigma}u=0,$$

where \({(2 - b)/N < \sigma < (2 - b)/(N-2)}\) and \({0 < b < \rm min\{2,N\}}\). We prove a Gagliardo–Nirenberg-type estimate and use it to establish sufficient conditions for global existence and blow-up in \({H^1(\mathbb{R}^N)}\).

     

2,2′-Dipyridyl and 1,10-phenanthroline in the synergetic extraction of Eu3+

The thermodynamics of the extraction of Eu³⁺ by thenoyltrifluoroacetone (HTTA) and by mixtures of HTTA and bidentate amine bases such as 2,2-dipyridyl (Dipy) and 1,10-phenanthroline (Phen) in benzene from an aqueous phase fixed to 0.1M ionic strength (NaClO₄), pH 3.9, has been investigated. Phenanthroline forms both the Eu(TTA)₃·Phen and Eu(TTA)₃·2Phen species, which are much stronger than the dipyridyl complexes. The diluent effect on the extraction is also studied.     

Applicability of winged bean extracts as organic corrosion inhibitors for reinforced steel in 0.5 ​M HCl electrolyte

Corrosion inhibition properties of winged bean (WB) extracts on reinforced steel in 0.5 ?M HCl solution was studied through experimental and theoretical calculation methods. The electrochemical studies suggested that inhibition efficiency increased with increasing concentration of WB extracts up to 95%. Nyquist diagrams revealed an increase in the charge transfer resistance values and a decrease in the constant phase element as the concentration of WB extracts were increased. The potentiodynamic polarization results revealed that WB extracts behave as mixed-type inhibitors, which physically adsorbed onto the reinforced steel surface. Effect of temperature study demonstrated that the corrosion resistance behaviour of WB extracts decreased with an increase in temperature, yielding a corrosion rate of 3.39 mmpy and 4.02 mmpy at 333 ?K with the incorporation of 1000 ?ppm WBW and WBE extracts, respectively. The thermodynamic study implied that the adsorption process follows the Langmuir isotherm with free energy adsorption of ΔG_ads WBW ?= ?-17.29 ?kJ ?mol^-1 and ΔG_ads WBE ?= ?-16.81 ?kJ ?mol^-1. Corresponding to the molecular modelling study, the semi-empirical method and molecular dynamics (MD) simulation investigated the correlation between the inhibitor compounds and the metal surface. One of the phenolic molecule constituents (gallic acid) was chosen to establish the structural and electronic parameters responsible for the high inhibition efficiency. A greater E_binding of 0.181 (a.u.) indicates that gallic acid in WB extracts can easily bind with the Fe surface, thus projecting a higher inhibitory performance. Surface morphology study affirmed the effective adsorption of WB extracts onto the surface of reinforced steel.