不同浓度和温度时无机盐和尿素对抗抑郁剂药物丙咪嗪盐酸盐的胶束化行为的影响

In the present study we report the micellization behavior of imipramine hydrochloride(IMP)in absence and presence of different concentrations of inorganic salts(LiCl,NaF,NaCl,NaBr,and KCl)and ureas(urea and thiourea)over the temperature range from 288.15 to 303.15 K.The critical micellization concentrations(cmc)of drug and drug+additive systems were determined by conductometric technique. With increasing temperature the cmc first increases then decreases.Maximum cmc values were obtained at 293.15 K with or without additives.In presence of inorganic salts the cmc value decreases which is explained on the basis of nature and ion size of the added ion.Urea and thiourea also decrease the cmc at low concentrations(0.2 mmo·lL -1 urea and 0.1 mmo·lL -1 thiourea),but,at higher concentrations,increase in cmc is observed.The related thermodynamic parameters are also evaluated and discussed.     

Synthesis of Copper Oxide-Based Nanoformulations of Etoricoxib and Montelukast and Their Evaluation through Analgesic,Anti-Inflammatory,Anti-Pyretic,and Acute Toxicity Activities

Copper oxide nanoparticles (CuO NPs) were synthesized through the coprecipitation method and used as nanocarriers for etoricoxib (selective COX-2 inhibitor drug) and montelukast (leukotriene product inhibitor drug) in combination therapy. The CuO NPs, free drugs, and nanoformulations were investigated through UV/Vis spectroscopy, FTIR spectroscopy, XRD, SEM, and DLS. SEM imaging showed agglomerated nanorods of CuO NPs of about 87 nm size. The CE1, CE2, and CE6 nanoformulations were investigated through DLS, and their particle sizes were 271, 258, and 254 nm, respectively. The nanoformulations were evaluated through in vitro anti-inflammatory activity, in vivo anti-inflammatory activity, in vivo analgesic activity, in vivo anti-pyretic activity, and in vivo acute toxicity activity. In vivo activities were performed on albino mice. BSA denaturation was highly inhibited by CE1, CE2, and CE6 as compared to other nanoformulations in the in vitro anti-inflammatory activity. The in vivo bioactivities showed that low doses (5 mg/kg) of nanoformulations were more potent than high doses (10 and 20 mg/kg) of free drugs in the inhibition of pain, fever, and inflammation. Lastly, CE2 was more potent than that of other nanoformulations.     

Influence of organic additives on the clouding phenomena of promethazine hydrochloride solutions

This paper reports the influence of organic additives (alcohols, amino acids, sugars) on the micellization and cloud point (CP) of a phenothiazine drug, promethazine hydrochloride (PMT). The critical micelle concentration (CMC) of the drug, determined by surface tension measurements in the presence of a representative of each additive class (i.e., butanol, leucine, arabinose), are used to evaluate the maximum surface excess concentration (Γ _max) and the minimum area per surfactant molecule (A _min) at the air/water interface. Γ _max increases and CMC/A _min decreases with increasing concentration of the additives, which indicate mixed micelle formation. The intermicellar interaction coefficients in the mixed micelles (β ^m and β ^σ are also calculated, and their negative values imply attractive interactions. Effect of pH revealed CP decrease with increasing pH due to deprotonation of PMT molecules. Effect of amino acids depended upon their nature and polarity, whereas sugars caused a CP decreasing effect. Aliphatic alcohols as well as cycloalkanols and diols decreased the CP. In the presence of arabinose, increase in drug concentration resulted in the CP increase, while increase in pH showed an opposite trend. Results are interpreted on the basis of mixed micelle formation, hydrophobic interactions, and change in solvent structure.     

Nonelectrolyte-Induced CP Variation of TX-114+TBAB System

The effects of nonelectrolytes (ureas, amino acids, sugars) on the cloud point (CP) of nonionic surfactant Triton X-114 (TX-114) and tetra-n-butylammonium bromide (TBAB) system were studied. Ureas as well as thioureas increased the CP. Behaviors of amino acids depended upon their nature. Nonpolar and uncharged polar amino acids were less effective in changing the CP. However, tryptophan and phenylalanine increased the CP sharply. Acidic amino acid (aspartic acid) and sugars decreased the CP. The results were explained in terms of their effect on water structure. Amino acids got solubilized either in the micellar interior or in the bulk phase.     

Study of the cloud point variation of amitriptyline hydrochloride solutions in presence of amines and amino acids

In this paper clouding phenomenon in aqueous solutions of an amphiphilic drug amitriptyline hydrochloride is reported. The effect of adding ethylamine, butylamine, hexylamine, heptylamine, octylamine, ethylenediamine, diethylenetriamine, tetraethylenepentramine, aniline, and benzylamine on the cloud point of solutions containing a fixed drug concentration (50 mM) was seen. All the amines decrease the cloud point by intercalating between the head groups with protonated amine groups at the micellar surface. The amino acids used (lysine, arginine, histidine) also behave similarly. The results are discussed in the light of a particular additive’s ability to remove water from the head group region of the drug micelles.     

A novel 2D vanadium(V)-isonicotinohydrazide coordination polymer, C15H16AgN4O8V: Synthesis, structure, catalytic activity and DFT calculation

A novel two-dimensional 3d-4d transition metal-based coordination polymer [VO(OCH₃)(OHCH₃)(L)Ag(NO₃)]_∞ (1) has been synthesized and characterized by single crystal X-ray diffraction and fluorescence spectroscopy (H₂L = (E)-N′-(2-hydroxybenzylidene)isonicotinohydrazide). The coordination sphere of each V center is octahedral and chelates to a tridentate ligand L, while the tetrahedral conformation of Ag center consists of two O and two N atoms. Infinite zigzag chains of Ag-tetrahedrals are formed. The hydrazinide L²⁻ ligands of octahedral-V centers link adjacent chains to form an undulated heterometal based 2D layer. DFT calculations on 1 reproduced the geometric parameters and the electronic absorptions were predicted. The coordination polymer 1 showed very selective heterogeneous catalytic activity with 77-89% conversion in oxidation of alkenes, cyclooctane and benzyl alcohol by H₂O₂.     

Form Factor and rms Radius of Proton Predicted Using Differential Cross-Section Data of $${p\bar{p}}$$ Elastic Scattering at $${\sqrt{s}=31}$$ , 53, 62 and 1960 GeV

Physics of Atomic Nuclei - Using differential cross-section data on $$p\bar{p}$$ elastic scattering at $$\sqrt{s}=31$$ , 53, 62, and 1960 GeV, for low momentum transfer square (...     

Bioactive Heteroleptic Bismuth(V) Complexes: Synthesis,Structural Analysis and Binding Pattern Validation

Heteroleptic triorganobismuth (V) complexes of general formula, R₃Bi(OOCR')₂ ( 1 – 7 ), where R = C₆H₅ ( 1 – 3 ), p‐CH₃C₆H₄ ( 4 – 7 ) and R' = 3,5‐Cl₂C₆H₃ ( 1 , 5 ); 3,4,5‐(OCH₃)₃C₆H₂ ( 2 , 6 ); 3‐CH₃C₆H₄ ( 3 , 7 ); 2‐OH‐3‐OCH₃C₆H₃ ( 4 ) have been synthesized and fully characterized by FT‐IR, ¹H &¹³C NMR spectroscopy, single crystal X‐ray crystallography and elemental analysis. The molecular geometry observed for the compounds is predominantly distorted trigonal bipyramidal, the fact which was subsequently authenticated through X‐ray analyses for ( 1 – 4 ). All the synthesized compounds have been bio‐assayed for antileishmanial (Leishmania tropica KWH23) and Jack beans urease inhibitory activity, and human Lymphocytes were used to measure the general toxicity. Of these, ( 4 ) proved to be highly effective against the target species (Leishmania tropica KWH23), while being non‐toxic towards the mammalian cells at levels below 0.74 μgmL^?1, making it highly promising drug candidate. The high activities for ( 2 , 4 , and 6 ) against Jack beans Urease as compared to the reference standard demonstrate their significance in searching of therapeutic agents in future programs. The significant binding score of ( 2 & 4 ) against H. pylori in molecular docking studies further revealed their importance in future drug discovery processes.     

混合胶束中Gemini阳离子表面活性剂14-s-14与常规表面活性剂的协同作用:连接臂及反离子效应(英文)

The mixed micelle formation of binary cationic 14-s-14 gemini with conventional single chain surfactants was studied by conductivity measurements.The critical micelle concentration(cmc) and the degree of counterion binding values(g) of the binary systems were determined.The results were analyzed by applying regular solution theory(RST) to calculate micellar compositions(X),activity coefficients(f1,f2),and the interaction parameters(β).The synergistic interactions of all the investigated cationic gemini+conventional surfactant combinations were found to be dependent upon the length of hydrophobic spacer of the gemini surfactant.The excess Gibbs free energy of mixing was evaluated,and it indicated relatively more stable mixed micelles for the binary combinations.