Potentiometric study of polyaniline film synthesized with various dopants and composite-dopant: A comparative study

The potentiometric study of polyaniline (PANI) film synthesized with dopants viz. polyvinyl sulfonic acid (PVS),p-toluene sulfonic acid (p TS), dodecyl benzene sulfonic acid (DBS) and composite-dopants viz. PVS-p TS and PVS-DBS, has been carried out. The synthesized PANI films were characterized by electrochemical technique, UV-visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and conductivity measurement. It was found that the PANI doped with PVS gives good electrochemical properties, conductivity as well as surface morphology as compared to p TS and DBS, whereas in composite dopants the PANI doped with PVS-pTS gives good polymer matrix as compared to PVS-DBS.     

Sensor Network Localization,Euclidean Distance Matrix completions,and graph realization

We study Semidefinite Programming, SDP, relaxations for Sensor Network Localization, SNL, with anchors and with noisy distance information. The main point of the paper is to view SNL as a (nearest) Euclidean Distance Matrix, EDM, completion problem that does not distinguish between the anchors and the sensors. We show that there are advantages for using the well studied EDM model. In fact, the set of anchors simply corresponds to a given fixed clique for the graph of the EDM problem.     

Environmentally benign novel green pigments: Pr1-xCaxPO4 (x = 0-0.4)

Rare earth based materials have recently attracted considerable attention as potential ecofriendly colourants for low temperature as well as high temperature applications. In the present study, we have synthesized a series of Ca-doped PrPO₄ compounds with the general formula, Pr_1-xCa_xPO₄ (x = 0-0.4 in steps of 0.1) and characterized the compounds by powder X-ray diffraction. All the compositions show a monoclinic monazite structure. The optical properties of the brilliantly coloured pigments [ L (brightness),a* (+ red- green),b* (+ yellow - blue) have been examined. These materials can find application as potential green colourants.     

Development and optimization of a novel drug free nanolipid vesicular system for treatment of osteoarthritis

Objective: The goal of this study is to improve the transdermal delivery of phosphatidylcholine (PC) via constructing a novel nanolipid vesicular system (NLVS) with high level of permeability through the stratum corneum (SC).

Significance: In our study, a novel drug free NLVS was developed. The system depends on PC boundary cartilage lubrication to relieve osteoarthritic pain without developing gastrointestinal problems associated with anti-inflammatory drug.

Materials and methods: A full two-level (2³) factorial design is applied to optimize the quality of the prepared NLVS. The selected independent variables are the concentration of PC, the concentration of edge activator (EA), and EA type. The developed NLVS was evaluated for in-vitro, ex-vivo as well as in-vivo efficacy in rat animal model.

Results: Based on the factorial design, the selected formulation variables significantly affect the tested responses. The prepared NLV formulations have a particle size (PS)in the range of 10.34 to 496.3?nm, polydispersity index (PdI) values less than one, and negative zeta potential (ZP) range of ?1.42 to ?32.01?mV. In-vitro and ex-vivo study results reveal that the designed NLVS is effective in sustaining PC release and enhancing its transdermal permeation over 24?h. The optimal permeation flux through ex-vivo study is 0.415?mg/cm²/h following zero-order kinetics. Moreover, in-vivo study of the optimized formulations demonstrated remarkable reduction in inflammatory mediators associated with osteoarthritis (OA).

Conclusion: The results indicate that the optimized drug free NLVS significantly augment transdermal delivery of PC and have a potential role in treatment of OA without the risk of systemic side effects.     

Synthesis and transdermal permeation of novel N4-methoxypoly(ethylene glycol) carbamates of cytarabine

Background: Cytarabine is a deoxycytidine analogue commonly used in the treatment of hematological malignant diseases. Its clinical utility, however, is severely limited by its short plasma half-life because of the catabolic action of nucleoside deaminases. Method: In this study, N⁴-carbamate derivatives of cytarabine (1) were synthesized and evaluated for transdermal penetration because this mode of administration may circumvent its limitations. The synthesis of these compounds was achieved in a two-step process. First, the methoxypoly(ethylene glycol) was activated by p-nitrophenyl chloroformate. Second, the activated intermediates were reacted with cytarabine in the presence of N-hydroxysuccinamide to give the N⁴-methoxypoly(ethylene glycol) carbamate derivatives. The transdermal flux values of the N⁴-carbamates of cytarabine were determined in vitro by Franz diffusion cell methodology. Aqueous solubility and log D (pH 7.4) values were determined and assessed for correlation with transdermal flux values. Results: The synthesized carbamates, particularly, (9)–(13), showed increased solubility in both aqueous and lipid media. Log D values decreased as the oxyethylene chain lengthened. Conclusion: Although none of the derivatives showed significantly higher transdermal penetration than cytarabine (1), it should be mentioned that the mean for cytarabine N⁴-methoxyethyleneoxycarbamate (8) was 10 times higher and the median was 2 times higher.     

Synthesis and photovoltaic properties of conjugated copolymers bearing planar acenaphtho[1,2-b]quinoxaline moiety with deep HOMO level

A series of alternating copolymers (PC-AQx, PT-DTAQx, PC-DTAQx, PF-DTAQx, and PBDT-DTAQx) bearing novel planar acenaphtho[1,2-b]quinoxaline (AQx) or 8,11-di(thiophen- 2-yl)acenaphtho[1,2-b]quinoxaline (DTAQx)-acceptor cores have been synthesized via Suzuki or Stille coupling reactions. UV–vis absorption and GIXRD characterization results indicated that the presence of planar DTAQx unit is favorable for the promotion of well-ordered interchain packing in the solid state, and the incorporation of planar electron-donating benzo[1,2-b: 4,5-b′]-dithiophene (BDT) moiety would be propitious to the molecular self-organization. Electrochemical measurement results suggested that four copolymers possess deep HOMO energy level of −5.5 ~ −5.6 eV. The polymer solar cell with structure of ITO/PEDOT:PSS(30 nm)/polymer:PCBM (60 nm)/Bphen(10 nm)/Ag(100 nm) exhibited the highest V _oc of 0.84 V with PF-DTAQx as p-type polymer, while the best power conversion efficiency (PCE) of 0.9 % was obtained using a blend of PBDT-DTAQx and PCBM (1:4) as active layer.     

X-ray and magnetic studies of Zn2+ substituted Ni-Pb ferrites

Seven samples of the polycrystalline, Ni_1.25-xZn_xPb_0.25Fe_1.5O₄ (x = 0.0, 0.1, 0.2, 0.3, 0.4, 0.5 and 0.6) ferrites, were prepared by usual double sintering ceramic method. X-ray diffraction patterns of the samples revealed single-phase cubic spinel structure. The magnetic properties were investigated by means of magnetization and a.c. susceptibility (χ) measurements. A.C. susceptibility was measured from room temperature to the Curie temperatureT _C) of the samples. Variation of a.c. susceptibility (χ) with temperature showed that the samples withx = 0.3 and 0.5 contain single-domain (SD) particles whereas the samples with x = 0.4 and 0.6 showed multi-domain (MD) nature. Values of Curie temperature ( T _C)as obtained from the study of variation of a.c. susceptibility with temperature were found to decrease with increase in the Zn ²⁺ concentration (x bd. Magnetic measurements showed increase in magnetization as Zn²⁺ content was increased from 00 to 0.5. Further increase in Zn²⁺ contentx bd reduces the magnetization.     

Bilateral bounds for the shear and torsion factors: comments on elementary derivations

This paper proposes a new simple derivation of bilateral bounds for the strain energy–based shear and torsion factors, χ _i , of an elastic beam together with some comments about the coherence of the current formulations. A rearrangement of the definition as a mean over the cross-section and an original decomposition of the shear stress in two parts—τ _eqv that is equivalent to the external force and a residual Δτ—allow (i) to interpret (χ − 1) as the mean quadratic deviation of the shear field with respect to the distribution τ _eqv and (ii) to easily evaluate an upper bound, using minimal information about the stress field. In this formulation, the lower bound becomes trivial. Several numerical examples illustrate the accuracy and suitability of the results obtained.     

Influence ofβ-cyclodextrin as an encapsule and as an inclusion complex dopant on conducting polyaniline

An investigation on the effect ofβ-cyclodextrin (CD) in both free and inclusion-complexed forms with a guest anionic metal complex, dioxalatodiaquochromate(III) (DDC), on the characteristics of conducting polyaniline (PANI) is carried out. Four materials, PANI (i.e. PANI-SO ₄ ²⁻ ), PANI-DDC, PANI-CD and PANI-CD + DDC were prepared byin situ chemical oxidative polymerization in aqueous H ₂SO₄ at pH 1 and subjected to electrical conductivity and spectral (IR and UV-vis bd measurements. DDC and CD when separately incorporated, reduce the conductivity of PANI by about half whilst their inclusion complex CD + DDC enhances it. Spectral characterization reveals that DDC as a dopant and CD as an encapsule exhibit their effects through adverse interaction with imine-amine N centres and benzenoid moiety of PANI. The inclusion complex CD + DDC, on the contrary, functions as a dopant by lying in between the chains and seems to promote the extended conformation of PANI chain and hence theπ -electron delocalization. Exposure of the material to methanol vapour causes a decrease in conductivity in PANI and PANI-CD while an increase in PANI-CD + DDC. This study makes explicit the distinct role of CD as an encapsule and CD + DDC inclusion complex as a dopant in altering the electrical property of PANI.     

Nanoethosomes for transdermal delivery of tropisetron HCl: multi-factorial predictive modeling,characterization, and ex vivo skin permeation

Objective: The aim of the present work is to exclusively optimize and model the effect of phospholipid type either egg phosphatidylcholine (EPC) or soybean phosphatidylcholine (SPC), together with other formulation variables, on the development of nano-ethosomal systems for transdermal delivery of a water-soluble antiemetic drug. Tropisetron HCl (TRO) is available as hard gelatin capsules and IV injections. The transdermal delivery of TRO is considered as a novel alternative route supposing to improve BAV as well as patient convenience.

Methods: TRO-loaded ethanolic vesicular systems were prepared by hot technique. The effect of formulation variables were optimized through a response surface methodology using 3?×?2²-level full factorial design. The concentrations of both PC (A) and ethanol (B) and PC type (C) were the factors, while entrapment efficiency (Y₁), vesicle size (Y₂), polydispersity index (Y₃), and zeta potential (Y₄) were the responses. The drug permeation across rat skin from selected formulae was studied. Particle morphology, drug–excipient interactions, and vesicle stability were also investigated.

Results: The results proved the critical role of all formulation variables on ethosomal characteristics. The suggested models for all responses showed good predictability. Only the concentration of phospholipid, irrespective to PC type, had a significant effect on the transdermal flux (p?Conclusion: The study suggests the applicability of statistical modeling as a promising tool for prediction of ethosomal characteristics. The ethanolic vesicles were considered as novel potential nanocarriers for accentuated transdermal TRO delivery.     

Self-assembly of coordination polymers constructed from CuCN and unidentate pyridine bases

The self-assembly of K₃[Cu(CN)₄] and unidentate pyridine bases (L): pyridine (py), 3-methyl pyridine (3-mpy), and 2,4,6-trimethyl pyridine (tmpy) in the presence of Me₃SnCl affords new coordination polymers (CPs) CuCN·0.5(py)] (1), [CuCN·0.5(3-mpy)] (2), and [CuCN·0.5(tmpy)] (3). The syntheses are achieved in H₂O/acetonitrile media at room temperature. The structure of the CP 3 was characterized by X-ray single crystal analysis. It is crystallized as orthorhombic in the space group Pnma, a = 9.1065 (3) ?, b = 8.6669 (3) ?, and c = 12.1998 (5) ? and Z = 8. The CPs 1, 2 were investigated by IR, mass, Uv–visible, and ¹H-NMR spectra, as well as TGA. The CPs 1–3 are 2D-polymers consisting of 1D-(CuCN) _n chain structure while the ligands alternate on both sides of the chain with associated copper atom coordination number of three. Hydrogen bonds play an essential role for developing 2D-network structure. These CPs exhibit strong fluorescent emissions in the solid state.     

Systematic hardness measurements on mixed and doped crystals of rubidium halides

Efforts are made to improve the hardness of rubidium halide crystals by (i) solid solution hardening and (ii) impurity hardening. Systematic microhardness measurements have been made on rubidium halide mixed crystals (RbBr-RbI and KI-RbI) and rubidium halide crystals doped with Sr²⁺ ions. The composition dependence of the hardness of mixed crystals follows the law ΔH _v =K x (1− x),where ΔH _v is the enhancement in hardness,K a constant andx and (1 −x) the concentrations of the first and second component of the mixed crystals, respectively. The hardness of doped crystals increases with the concentrationC of the dopant according to the law, ΔH _v+6 =k C ^m ,wherek andm are constants. The relative efficacy of the two methods of hardening is discussed.     

Temperature dependence of the electromagnetic response function for strong-coupling amorphous Bi films

The temperature dependence of the electromagnetic response functionI(0, 0,T) has been inferred from the temperature dependence of the kinetic inductance of thin, amorphous Bi films. For normalization purposesI(0, 0, 0) has been calculated from tunneling data with the microscopic strong-coupling theory. The results are not consistent with scaled weak-coupling theory, but instead exhibit strong-coupling effects. The calculated value ofI(0, 0, 0) is approximately 40% below the BCS value for a weak-coupling superconductor, qualtiatively in agreement with determinations ofI(0, 0, 0) for Pb by Kerchner and Ginsberg. The temperature dependence ofI(0, 0,T) differs in the opposite direction from the BCS dependence as that observed for Pb.Research supported by the Robert A. Welch Foundation, Houston, Texas.     

Gelation theory for solutions of polymers with loci of strong interaction

This paper presents a statistical mechanical analysis of gelation in certain solutions ofA/B copolymers. Repeat unitsA, the major units, must constitute about 90 mole% or more of the copolymer, and are compatible with the solvent. Repeat unitsB, the minor units, must be totally incompatible with the solvent and represent loci of strong interaction between the macromolecular chains. If these interactions are sufficiently strong they can lead to gelation of the mixture. The following simplifications of the model afford results that can be expressed in simple, closed form: (1) TheB units are uniformly distributed along the chain backbone. (2) Polymer concentration must be greater then that for chain overlap. (3)B–B interactions lead to dimerization ofB units only. Examples include: (1) Any aqueous polymer solution where theA repeat units are hydrophilic and theB repeat units are hydrophobic;B–B interactions are thus by hydrophobic bonding. (2) Neutralized acrylic acid/acrylamide copolymers where theB are acrylamide repeat units which associate by hydrogen bonds. (3) Ionomer solutions whereB–B bonding is by dipole-dipole interaction. The results show that there is a critical copolymer concentration for gel formation, C _c . It turns out that C _c decreases withB content for low dimerization energies and increases withB content for higher dimerization energies. At intermediate dimerization energies, C _c is insensitive to theB content. The two extreme regimes of behavior are similar to contradictory predictions of previously published theories. Received: 18 September 2000 / Reviewed and accepted: 20 September 2000     

Cryocornea – toward enhancing the capacity and throughput of ex vivo corneal model

Abstract

Objective: The objective of this study was to investigate the effects of the concentration of two intracellular (i.e. propylene glycol and glycerol) and four extracellular (i.e. dextran, hydroxypropyl methylcellulose, polyvinylpyrolidone, trehalose) cryoprotective agents as well as the effects of freeze-thawing procedures on the corneal cryoprotection.

Significance: The corneal cryopreservation may possibly become the long-term storage technique of choice for collection of animal corneas suitable for ex vivo drug testing.

Methods: The integrity of corneal barrier was evaluated by measurements of transepithelial electrical resistance.

Results: Under the investigated experimental conditions the best result was obtained for slow freezing (2?h at ?20?°C followed by 46?h at ?70?°C) and rapid thawing (0.25?h at 34?°C) procedure where 20% (w/V) trehalose in Krebs Ringer buffer solution was used as extracellular cryoprotective agent.

Conclusions: The selection of corneal freeze-thawing protocol as well as the optimal type and concentration of a cryoprotective agent allows the cryostorage of porcine corneal tissues with suitable TEER properties (cryocornea).     

In vitro and in vivo investigation of taste-masking effectiveness of Eudragit E PO as drug particle coating agent in orally disintegrating tablets

Abstract

Context: Considering that bitter taste of drugs incorporated in orally disintegrating tablets (ODTs) can be the main reason for avoiding drug therapy, it is of the utmost importance to achieve successful taste-masking. The evaluation of taste-masking effectiveness is still a major challenge.

Objective: The objective of this study was to mask bitter taste of the selected model drugs by drug particle coating with Eudragit^® E PO, as well as to evaluate taste-masking effectiveness of prepared ODTs using compendial dissolution testing, dissolution in the small-volume shake-flask assembly and trained human taste panel.

Materials and methods: Model drugs were coated in fluidized bed. Disintequik? ODT was used as a novel co-processed excipient for ODT preparation. Selected formulations were investigated in vitro and in vivo using techniques for taste-masking assessment.

Results and discussion: Significantly slower drug dissolution was observed from tablets with coated drug particles during the first 3?min of investigation. Results of in vivo taste-masking assessment demonstrated significant improvement in drug bitterness suppression in formulations with coated drug. Strong correlation between the results of drug dissolution in the small-volume shake-flask assembly and in vivo evaluation data was established (R?≥?0.970).

Conclusion: Drug particle coating with Eudragit^® E PO can be a suitable approach for bitter taste-masking. Strong correlation between in vivo and in vitro results implicate that small-volume dissolution method may be used as surrogate for human panel taste-masking assessment, in the case of physical taste-masking approach application.     

Process monitoring research with various estimator-based MEWMA control charts

Multivariate exponentially weighted moving average (MEWMA) control chart with five different estimators as population covariance matrix is rarely applied to monitor small fluctuations in the statistical process control. In this article, mathematical models of the five estimators (S₁, S₂, S₃, S₄, S₅) are established, with which the relevant MEWMA control charts are obtained, respectively. Thereafter, the process monitoring performance of the five control charts is simulated. And the simulation results show that the S₄ estimator-based MEWMA control chart is of the best performance both in step offset failure mode and ramp offset failure mode. Since the inline process monitoring of photovoltaic manufacturing is intended to be a problem of multivariate statistics process analysis, the feasibility and effectiveness of the proposed model are elaborated in the case study during the cell testing and sorting process control for the fabrication of multicrystalline silicon solar cells.     

Preparation of Sm-Ru bimetallic alloy films on Ru(0001) surface by vapour-deposition and annealing

Sm-Ru intermetallic surface alloy films were prepared by vacuum deposition and annealing of rare earth Sm on single crystal Ru(0001) surface. The Ru 3 d and Sm 3 d core level spectra clearly show the formation of surface alloy layers. XPS measurements on surface alloy film revealed an induced peak in the Ru 3 d region at lower binding energy by 1 eV compared to the bulk Ru (elemental) suggesting an electronic effect of alloying and Sm-Ru bond formation. The Sm 3 d _5/2 photoemission peak of Sm film consists of strong features characteristic of Sm(II) with electron configuration 4 f ⁶ (5 d 6 s ) ² and Sm(III) with electron configuration 4 f ⁵ (5 d 6 s ) ³ .It is observed that the Sm(II) feature decreases in intensity upon alloy formation with surface Ru atoms. Oxidation of these films with carbon monoxide indicates alloy breakdown due to the oxidation of Sm atoms selectively. Alloy oxidation also shows a clear shift of Sm 3 d _5/2 feature.     

Synthesis and pharmaceutical properties of N-acyloxymethyl prodrugs of Allop with potential anti-trypanosomal activity

Abstract

We report herein the synthesis, and the physicochemical and pharmacokinetic properties of N-acyloxymethyl prodrugs of allopurinol (Allop) (2a–f). Allop is a compound with activity against Trypanosoma cruzi, a causative agent of Chagas disease. Its pathology leads to a huge number of infections and deaths per year, because in addition to many sufferers only having limited access to health services only an inefficient chemotherapy is available. Relevant pharmaceutical properties (pK_a, stability, solubility, lipophilicity, in vitro permeability, binding protein, xanthine oxidase binding) were also determined. The results obtained showed that derivatives behave as prodrugs of Allop, since they exhibit improved physicochemical and pharmacokinetic properties relative to their precursor. This behavior turns these compounds into active reservoirs of Allop, and reduces its unfavorable characteristics, so 2a–f compounds are excellent candidates for the treatment of Chagas disease. This work is therefore an important contribution leading to the suppression of Chagas disease.     

Formulation and ex vivo–in vivo evaluation of pH-triggered brimonidine tartrate in situ gel for the glaucoma treatment using application of 32 factorial design

Context: Short residence time, poor bioavailability and poor permeability are the major problems for conventional eye drops treatment.

Objective: The aim of this article is to develop, optimize and ex vivo–in vivo investigation of brimonidine tartrate in situ gel as compared to marketed eye drops for the treatment of glaucoma.

Materials and methods: The effect of independent variables, namely concentrations of polymers, on various dependent variables like viscosity at physiological pH and in vitro drug release were studied by using 3² factorial design. Further the optimized formulation was characterized for ex vivo and in vivo study.

Results and discussion: Experimental data demonstrated that optimized in situ gel formulation (F8) showed in vitro–ex vivo sustained release profile with polymer composites carbopol 974P and HPMC K4M. After 5?h of ex vivo transcorneal permeation study, the amount recovered from the corneal surface on the donor chamber 12.40% (124 ug) and the amount collected from the receptor chamber 76.8% (760 ug) of the initial dose 1?mg. The total amount recovered from the permeation experiment was 89.2%. Bioadhesive carbopol 974P and viscosity HPMC K4M composites optimized formulation (F 8) produce greater influence on the duration of drug action and improved intraocular pressure reduction activity as compared to marketed eye drop solution in in vivo study.

Conclusion: The developed in situ gelling system as a promising ophthalmic formulation to prolong the drug lowering effect on the intraocular pressure.