Solution properties of amitriptyline and its partitioning into lipid bilayers

Solution properties of a drug and its partitioning into lipid bilayers were studied for drug extraction using several different techniques, such as surface tension, zeta potential, ultra filtration and UV-Vis spectroscopy. From the surface tension study it was found that the presence of salt makes the drug molecules more surface-active. Zeta potential revealed the adsorption of the drug into the liposome bilayers to be governed mostly by electrostatic forces. The drug retention volume was expressed as a capacity factor, K, and that was normalized with respect to the amount of the immobilized phospholipids. The K-values for the positively charged drug on the liposomes decreased in the presence of phosphate buffer due to the presence of the oppositely charged ions. The above methods can thus be used to understand the mechanism of drug-membrane interaction and quantification of drug absorption into liposomes.     

Conformational changes of pyrene-labeled polyelectrolytes with pH: effect of hydrophobic modifications

Structural changes of pyrene-labeled and unlabeled poly(maleic acid/octyl vinyl ether) (PMAOVE) and poly(maleic acid/methyl vinyl ether) (PMAMVE) with changes in pH have been investigated in this study. The changes in the photophysical properties of pyrene are interpreted to investigate uncoiling or swelling of the polymeric chains with pH. The vibrational fine structure of the pyrene fluorescence (I(3)/I(1)) and the ratio between excimer and monomer fluorescence (I(e)/I(m)) of both pyrene-labeled and unlabeled PMAMVE and PMAOVE suggest that, at pH 4, the polymers are in the coiled form and PMAOVE forms hydrophobic nanodomains. An increase in pH ionizes a number of COOH groups on both PMAMVE and PMAOVE, which leads to the stretching or swelling of the polymers.     

In situ assembled ZIF superstructures via an emulsion-free soft-templating approach

Assembling well-defined MOF superstructures remains challenging as it requires easily removable hard templates or readily available immiscible solutions for an emulsion-based soft-template approach. In this work, a single-step emulsion-free soft templating approach is reported to spontaneously prepare hollow ZIF-8 and ZIF-67 colloidosomes with no further purification. These superstructures can load different enzymes regardless of the size and charge with a high encapsulation efficiency of 99%. We envisage that this work will expand the repertoires of MOF superstructures by the judicious selection of precursors and the reaction medium.

An emulsion-free approach for the preparation of hollow ZIF-8 superstructures in a single step is established based on metal sulfate hydrates in methanol.     

Extracellular pH influences the mode of cell death in human colon adenocarcinoma cells subjected to photodynamic treatment with chlorin p6

Effect of varying extracellular pH on mode of cell death induced by photodynamic action of chlorin p6 was investigated in human colon carcinoma (Colo-205) cells. At an extracellular pH of 7.4, compared to cells treated with chlorin p6 in dark, the photodynamically treated cells showed reduction in mitochondrial membrane potential, an increase in ADP/ATP ratio (1:2) and a large percentage of cells with chromatin condensation. In contrast, when photodynamic treatment and post irradiation incubation was carried out in acidic medium (pH 6.5), total loss of mitochondrial membrane potential, a marked increase in ADP/ATP ratio (1:33) and increased damage to plasma membrane were observed. Further, cells subjected to photodynamic treatment in a medium of pH 7.4 showed twofold increase in caspase-3 activity as compared to photodynamic treatment at pH 6.5. These results suggest that chlorin p6 mediated photodynamic action induces apoptotic cell death when extracellular pH is 7.4 whereas necrosis is more predominant under condition when extracellular pH is 6.5.     

Evaluation of contributions to the uncertainty of cholesterol determination in human serum by means of gas chromatography/(quadrupole-) mass spectrometry

 The uncertainty budget of the determination of cholesterol in a reference material (freeze-dried human serum) by isotope dilution mass spectrometry (IDMS) was evaluated. Measurements were run on a GC/quadrupole MS. A nested experimental design combined with a corresponding model for the analysis of variance (ANOVA) revealed the components making up the total uncertainty of the determinations. The coefficient of variation (CV) of the sole GC/MS-step was 0.47%, while that of the sample preparation including hydrolyzation, extraction and derivatization was 0.84%. This made the in-laboratory (overall) CV 0.96%. In addition, there was a vial-to-vial effect of 1.00% probably due to both inhomogeneity of the pooled material and lack of reproducibility of the filling procedure (including freeze drying) of the supplier as well as the reconstitution prior to use in the laboratory. These contributions sum up to an overall CV of a single determination of about 1.4%. Received: 17 October 1996/Revised: 14 November 1996/Accepted: 18 November 1996     

Inorganic-Organic Hybrid Polymers from the Polymerisation of Methacrylate-Substituted Oxotantalum Clusters with Methylmethacrylate: A Thermomechanical and Spectroscopic Study

New inorganic-organic hybrid materials were prepared by free-radical polymerization of methyl methacrylate (MMA) with methacrylate-substituted oxotantalum cluster [Ta₄O₄(OEt)₈(OMc)₄] and their properties evaluated. The cluster was prepared by the reaction of the parent alkoxide with methacrylic acid. Samples of the hybrid materials were produced with Ta-cluster to methyl methacrylate in the ratios of 1:50 and 1:100 and were characterized by thermal and spectroscopic techniques. The glass transition temperatures of the hybrid materials are shifted to higher temperatures than pure PMMA as a result of cross-linking of the polymer by the oxotantalum clusters. The increase in T_g is also observed from the dynamic mechanical analysis (DMA). Evidence of crosslinking between the Ta-cluster and PMMA is obtained from infrared spectroscopic study. Surface studies performed by X-ray photoelectron spectroscopy (XPS) provide information about the atomic concentrations of the surface and indicate tantalum bonded to oxygen.     

Ni(II) and Cu(II) complexes of bidentate thiosemicarbazone ligand: Synthesis,structural, theoretical,biological studies and molecular modeling

The conventional condensation and refluxing process was employed to synthesize Ni(II) and Cu(II) complexes of Methylcarbamatethiosemicarbazone ligand. Reactions were carried out at the pH of 7. The molar ratio of the ligand and metal salt was 2:1. The structures of the synthesized metal complexes were suggested by different analytical techniques such as magnetic susceptibility, molar conductance, IR, EPR and UV spectroscopy. Experimental studies confirmed the octahedral geometry for all the complexes. The geometry of the ligand and complexes were also confirmed by theoretical studies. The complexes were investigated for biological action against pathogenic fungi (C. krusei, C. albican) and bacteria (S. aureus, E. coli). The antimicrobial results confirmed superior inhibition potential of the metal complexes as compared with the parent ligand. The enhanced antimicrobial activities might be due to the chelation. Molecular-docking assays confirmed the strong interaction of ligand with target antimicrobial protein DNA gyrase-B.     

Green Enzymatic Synthesis of L-Ascorbyl Fatty Acid Ester: An Antioxidant

In green chemistry, biocatalysis using microwaves is a very attractive tool for various regioselective syntheses. L-Ascorbyl fatty acid esters were synthesized by an immobilized lipase from Bulkholderia multivorans using microwaves, with a dynamically enhanced rate of reaction and appreciable yield of around 80%. Microwave radiation had no effect on enzymic inactivation, however, synergism between microwaves and biocatalyst was observed.     

Effects of Dielectric Barrier Discharge Plasma on Physicochemical Characteristics,Mechanical Properties and Biocompatibility of Silk/PVA Nanofibers

Plasma Chemistry and Plasma Processing - This work reports an investigation of the discharge characteristics of atmospheric dielectric barrier discharge (DBD) plasma in terms of I-V curves and...     

Hybrid Curdlan Poly(γ ‐Glutamic Acid) Nanoassembly for Immune Modulation in Macrophage

A nanoformulation composed of curdlan, a linear polysaccharide of 1,3‐β‐linked d ‐glucose units, hydrogen bonded to poly(γ ‐glutamic acid) (PGA), was developed to stimulate macrophage. Curdlan/PGA nanoparticles (C‐NP) are formulated by physically blending curdlan (0.2 mg mL^?1 in 0.4 m NaOH) with PGA (0.8 mg mL^?1). Forster resonance energy transfer (FRET) analysis demonstrates a heterospecies interpolymer complex formed between curdlan and PGA. The ¹H‐NMR spectra display significant peak broadening as well as downfield chemical shifts of the hydroxyl proton resonances of curdlan, indicating potential intermolecular hydrogen bonding interactions. In addition, the cross peaks in ¹H‐¹H 2D‐NOESY suggest intermolecular associations between the OH‐2/OH‐4 hydroxyl groups of curdlan and the carboxylic‐/amide‐groups of PGA via hydrogen bonding. Intracellular uptake of C‐NP occurs over time in human monocyte‐derived macrophage (MDM). Furthermore, C‐NP nanoparticles dose‐dependently increase gene expression for TNF‐α, IL‐6, and IL‐8 at 24 h in MDM. C‐NP nanoparticles also stimulate the release of IL‐lβ, MCP‐1, TNF‐α, IL‐8, IL‐12p70, IL‐17, IL‐18, and IL‐23 from MDM. Overall, this is the first demonstration of a simplistic nanoformulation formed by hydrogen bonding between curdlan and PGA that modulates cytokine gene expression and release of cytokines from MDM.