Stability and In Vitro Drug Release of Flurbiprofen-Loaded Poly-ε-Caprolactone Nanospheres

The effects of temperature and two different initial pH (2.67 and 7.00) on poly-ε-caprolactone (PεCL) nanospheres loaded with flurbiprofen (FB) (aqueous suspensions) were studied to investigate their influence on the stability and physicochemical characteristics of these drug delivery systems. The drug release behavior was also studied. Release of the associated FB occurred very fast on high dilution in a buffered medium. The stability of the polymeric system depends on the temperature and the initial pH value; it is more degradable with the particles stored at 40°C with an initial pH value of 2.67.     

Celecoxib-cyclodextrin systems: characterization and evaluation of in vitro and in vivo advantage

Solid dispersions of Celecoxib were prepared with hydroxypropyl β cyclodextrin by various methods such as physical mixture, cogrinding, kneading, and coevaporation. The dispersions were characterized by differential scanning calorimetry (DSC), X-ray diffraction patterns, infrared spectroscopy, and nuclear magnetic resonance studies. The DSC thermograms of the dispersions indicated potential of heat-induced interaction between Celecoxib and cyclodextrin that could influence in vitro drug dissolution. The dispersions exhibited faster rates of dissolution compared to that of Celecoxib. The kneaded dispersion with the fastest in vitro dissolution rate when compressed into tablets showed a better release profile compared to the tablets of pure Celecoxib. In vivo studies revealed that the kneaded dispersion provided for quicker response and was more effective in inhibiting rat paw edema as compared to Celecoxib alone, thus confirming the advantage of improved pharmacological activity of Celecoxib when administered as a solid dispersion with cyclodextrin.     

Characterisation of blends between poly(ε-caprolactone) and polysaccharides for tissue engineering applications

In this work, bioartificial binary blends between poly(ε-caprolactone) (PCL) and a polysaccharide (chitosan (CS) or starch (S)) with different contents of the natural polymer (5–30 wt.%) were produced. Melt-mixing and double-precipitation were the methods used for the obtainment of PCL/S and PCL/CS blends, respectively. Tubular scaffolds were produced from bioartificial blends by melt-extrusion. Physico-chemical characterisation was performed by differential scanning calorimetry analysis (DSC), thermogravimetry (TGA), scanning electron microscopy (SEM), infrared analysis (FTIR-ATR and micro-ATR mapping), atomic force microscopy (AFM) and stress–strain tests. Blends were not miscible, phase-separated systems, showing a homogeneous composition and morphology only at low polysaccharide content (≤ 10 wt.%). The biocompatibility of bioartificial guides was investigated by culturing NIH-3T3 mouse fibroblasts. Cells response showed the following order: PCL/S > PCL > PCL/CS. For each blend type, biocompatibility increased with decreasing the polysaccharide content. In vitro cell tests using S5Y5 neuroblastoma cells, carried out on the most biocompatible blends, assessed their absence of cytotoxicity towards these model cells of the nervous tissue. Results showed that blends with a low chitosan or starch content (≤ 10 wt.%) are promising for the regeneration of tissues requiring tubular scaffolds, such as the peripheral nerves.     

Characterization and body distribution of beta-elemene solid lipid nanoparticles (SLN)

Solid lipid nanoparticles (SLN) containing β-elemene, a volatile oil used for the treatment of cancer, were prepared by the method combining probe sonication and membrane extrusion. Effects of the formulations and procedures on the characteristics of SLN were investigated. Body distribution of β-elemene SLN in rats after intravenous administration was compared with that of the commercial emulsion. The results showed that dispersing the surfactant in the melted lipid matrix could obtain smaller particles than that dispersing in the water phase. Increasing the ratio of monostearin in the lipid matrix or the concentration of surfactant reduced the mean volume size of the SLN. Optimized formulation was composed of monostearin and precirol ATO 5 at a mass ratio of 3:7, which was quite stable for 8 months at room temperature. In vitro release of β-elemene from the SLN was slow and stable without obvious burst release and was found to follow the Higuich equation. After intravenous administration, the β-elemene levels after 5 min injection of SLN formulation were 1.5, 2.9, and 1.4 times higher than those of β-elemene emulsion in liver, spleen, and kidney, respectively, while the concentrations of β-elemene were decreased 30% in heart and lung. Therefore, the SLN containing β-elemene might be an attractive candidate for the treatment of liver cancer.     

Preparation and evaluation of SEDDS and SMEDDS containing carvedilol

A new self-emulsifying drug delivery system (SEDDS) and self-microemulsifying drug delivery system (SMEDDS) have been developed to increase the solubility, dissolution rate, and, ultimately, oral bioavailability of a poorly water soluble drug, carvedilol. Ternary phase diagrams were used to evaluate the self-emulsification and self-microemulsfication domains. The self-emulsification time following introduction into an aqueous medium under gentle agitation was evaluated. The minimum self-emulsification time was found at a Tween 80 content of 40%. The particle size distribution and ζ-potential were determined. Benzoic acid had a dual function, it improved the self-emulsification performance of SEDDS and SMEDDS in 0.1 N HCl and lead to a positively charged emulsion. The in vitro dissolution rate of carvedilol from SEDDS and SMEDDS was more than two-fold faster compared with that from tablets. The developed SEDDS formulations significantly improved the oral bioavailability of carvedilol significantly, and the relative oral bioavailability of SEDDS compared with commercially available tablets was 413%.     

The physicochemical characterization and in vitro/in vivo evaluation of natural surfactants-based emulsions as vehicles for diclofenac diethylamine

Two sugar-based emulsifiers, cetearyl alcohol & cetearyl glycoside and sorbitan stearate & sucrose cocoate, known as potential promoters of lamellar liquid crystals/gel phases, were investigated in order to formulate an optimal vehicle for amphiphilic drug—diclofenac diethylamine (DDA).

Physico-chemical characterization and study of vehicle's physical stability were performed. Then, the in vitro DDA liberation profile, dependent on the mode of drug incorporation to the system, and the in vivo, short-term effects of chosen samples on skin parameters were examined.

Droplets size distribution and rheological behavior indicated satisfying physical stability of both types of vehicles. Unexpectedly, the manner of DDA incorporation to the system had no significant influence on DDA release. In vivo study pointed to emulsion's favorable potential for skin hydration and barrier improvement, particularly in cetearyl glycoside-based vehicle.     

Relationship Between Microstructure, Hardness, XRD, TGDTA Analysis, and Wear Performance of a Cast ZA Alloy

In the present article, microstructure, hardness, X-ray diffraction (XRD), thermal gravimetric and differential thermal analysis (TGDTA), and wear performance of a Cast ZA Alloy were studied by using scanning electron microscopy (SEM), XRD analysis, thermal gravimetric and differential thermal analysis and tensile strength, hardness, and wear test techniques. Wear performance of the alloy was investigated on a pin-on-disk wear tester under dry sliding conditions, rubbing against nitrided steel. The wear performance of some specimens was superior to others, for which microstructure and precipitated particulates were important. It has showed that some important phases occurred and improved the wear performance after solution-treatment.     

Development and in vitro evaluation of surface modified poly(lactide-co-glycolide) nanoparticles with chitosan-4-thiobutylamidine

The objective of this study was to develop a nanoparticulate drug delivery system based on the surface modification of poly(lactide-co-glycolide) (PLGA) nanoparticles with a thiolated chitosan. PLGA nanoparticles were prepared by the emulsification-solvent evaporation method. Immobilization of chitosan to the surface of PLGA nanoparticles via amide bonds was mediated by a carbodiimide. Thiol groups were covalently bound to the chitosan surface of particles by reaction with 2-iminothiolane. Obtained nanoparticles were characterized in vitro regarding size, zeta potential, thiol group content, stability at different pH values, mucoadhesion, and drug release. Results demonstrated that the surface modification of PLGA nanoparticles with thiolated chitosan (chitosan-TBA) leads to nanoparticles of a mean diameter of 889.5 ± 72 nm and positive zeta potential of + 24.74 mV. The modified nanoparticles contained 7.32 ± 0.24 μmol thiol groups per gram nanoparticles. The size of nanoparticles was strongly influenced by the pH of the surrounding medium, being 925.0 ± 76.3 nm at pH 2 and 577.8 ± 66.7 nm at pH 7.4. Thiolated nanoparticles showed a 3.3-fold prolonged residence time on the mucosa and an unchanged release profile in comparison to unmodified PLGA nanoparticles. These data suggest that surface modified chitosan-TBA conjugate PLGA nanoparticles have the potential to be used as mucoadhesive drug delivery system.     

Mechanical spectroscopy of thin layers of PPV polymer on Si substrates

The vibrating reed technique with electro“static” excitation and optical detection has been applied to investigate thin layers of poly-phenylene-vinylene, deposited by spin coating onto microfabricated Si cantilevers, during temperature cycling programs between 90 and 540 K at a rate of 1 K/min. From the vibration frequencies the Young’s modulus of the film can be estimated to be about 10 MPa at room temperature in the precursor phase (if prepared from a solution in toluene), which increases by conversion to the conjugate bonded polymer to about 50 MPa. The temperature dependence of internal friction reveals the processes of γ relaxations (crankshaft motion of side branches in the precursor) and β-relaxation (movements of a few monomer blocks in the polymer chain), as well as peaks indicating the structural transformations during conversion, and possibly a glass transition in the amorphous precursor phase. After conversion only the β-relaxation persists.     

Quantitative analysis of beta-blockers in pharmaceutical preparations by capillary electrophoresis

A simple capillary electrophoresis method was developed for the analysis of four β-blockers (atenolol, metoprolol, pindolol, and propranolol) in pharmaceutical preparations. The method was validated regarding accuracy, precision, linearity, and detection/quantification limits, and the obtained values were in accordance to those reported in the literature. The method was applied to the determination of the drugs in commercial tablet preparations and proved to be fast and reliable for the quantitative analysis of the β-blockers.     

Enhanced photoelectrochemical properties and photocatalytic activity of porous TiO2 films with highly dispersed small Au nanoparticles

Small Au nanoparticles (NPs) with mean diameter of 4.1 nm were highly deposited on TiO₂ films via a simple electrostatic self-assembly method. The physically separated Au NPs, with a high surface density of 6.3 × 10¹¹ NPs/cm², were mainly distributed on the top layer of porous TiO₂ films. The deposition of Au NPs induced a negative shift (~ 100 mV) of the apparent flat band potential of Au-TiO₂ electrodes. The charge separation efficiency of the TiO₂ electrode increased from 72.1% to 88.5% by dispersing Au NPs. Whatever redox species were present in the electrolyte, the Au-TiO₂ electrode had higher photovoltage than the TiO₂ electrode. The photovoltage was very sensitive to added redox species such as O₂, O₃, and methanol, and the effect of adsorbed redox species on electron accumulation was discussed. The electrochemical impedance spectroscopic measurements revealed that the charge transfer resistance (R_ct) of Au-TiO₂ films was reduced to 16% of bare TiO₂ electrode, and the decreased R_ct corresponded to the increased photocatalytic activity of Au-TiO₂ films. The beneficial role of uniformly dispersed small Au NPs on the charge separation was discussed. By modifying TiO₂ films with small Au NPs, the photocatalytic activity of TiO₂ films for formaldehyde degradation increased about 2.5 times.     

Comparison of physical, chemical and cellular responses to nano- and micro-sized calcium silicate/poly(epsilon-caprolactone) bioactive composites.

In this study, we fabricated nano-sized calcium silicate/poly(epsilon-caprolactone) composite (n-CPC) and micro-sized calcium silicate/poly(epsilon-caprolactone) composite (m-CPC). The composition, mechanical properties, hydrophilicity and degradability of both n-CPC and m-CPC were determined, and in vitro bioactivity was evaluated by investigating apatite forming on their surfaces in simulated body fluid (SBF). In addition, cell responses to the two kinds of composites were comparably investigated. The results indicated that n-CPC has superior hydrophilicity, compressive strength and elastic modulus properties compared with m-CPC. Both n-CPC and m-CPC exhibited good in vitro bioactivity, with different morphologies of apatite formation on their surfaces. The apatite layer on n-CPC was more homogeneous and compact than on m-CPC, due to the elevated levels of calcium and silicon concentrations in SBF from n-CPC throughout the 14-day soaking period. Significantly higher levels of attachment and proliferation of MG63 cells were observed on n-CPC than on m-CPC, and significantly higher levels of alkaline phosphatase activity were observed in human mesenchymal stem cells (hMSCs) on n-CPC than on m-CPC after 7 days. Scanning electron microscopy observations revealed that hMSCs were in intimate contact with both n-CPC and m-CPC surfaces, and significantly cell adhesion, spread and growth were observed on n-CPC and m-CPC. These results indicated that both n-CPC and m-CPC have the ability to support cell attachment, growth, proliferation and differentiation, and also yield good bioactivity and biocompatibility.     

络合法制备均匀γ-Fe2O3纳米颗粒@多层石墨烯复合材料研究

采用水热反应中的金属离子络合一步制备均匀超细磁性γ-Fe₂O₃纳米颗粒@多层石墨烯复合材料, 无需对石墨烯进行氧化处理。采用超声法制备多层石墨烯作为基片, 制备方法简单, 石墨烯表面的含氧官能团少。以FeCl₂为反应物, 以DMF(N, N二甲基甲酰胺)和水混合液作为溶剂, 其中DMF能起到络合金属离子的作用。实验研究了乙酸钠、反应温度及填充度对制备产物的影响。采用X射线衍射(XRD)、X射线光电子能谱(XPS)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)对复合材料进行微结构分析, 采用振动样品磁强计(VSM)测试了复合材料的磁性能。研究结果表明: 利用亚铁离子与DMF形成的络合物与碳环的π-π吸附作用可以在多层石墨烯表面生成铁氧化物。通过控制亚铁离子的氧化速度和氧化铁的生长速度, 在多层石墨烯表面获得了尺寸小于10 nm的均匀γ-Fe₂O₃纳米颗粒, 复合材料具有良好的磁性能。     

Investigation and physicochemical characterization of clarithromycin-citric acid-cyclodextrins ternary complexes

The purpose of this study was to investigate the effect of citric acid (CA) on the complexation of clarithromycin (CLM) with β-cyclodextrin (βCD) in aqueous solutions and in the solid state. A phase solubility study revealed a positive effect of CA on the drug solubility. A B_s-type solubility with an apparent stability constant (K_c) of 102.4 M^-1 was obtained for CLM in βCD solution and 161.2 M^-1 for CLM in 6 mM βCD solution. Solid ternary complexes were prepared by coevaporation and lyophilization. CLM-βCD-CA interactions were studied in the solid state by differential scanning calorimetry (DSC), infrared spectroscopy, scanning electron microscopy and X-ray diffractometry. A part of the guest molecule was located in the βCD host cavity. The results obtained suggest that the lyophilization method yields a higher degree of amorphous entity than coevaporation.     

In vitro dissolution studies of sodium diclofenac granules coated with Eudragit L-30D-55 by fluidized-bed system

The objective of this work was to study the dissolution process of sodium diclofenac granules coated with a polymeric suspension of Eudragit L-30D-55® by fluidized bed. Methacrylic acid-methylmetacrylate copolymer, also known as Eudragit, has been used as a pH sensitive coating material to protect drug substances prior to delivery to the human intestines. The sodium diclofenac granules were prepared by wet granulation technology using microcrystalline cellulose (MICROCEL), sodium diclofenac, and polivinilpirrolidone K-30. The granules coating operation was carried out in a fluidized bed with top spraying by a double-fluid nozzle. The dissolutions studies of the coated granules were performed in triplicate in a dissolution test station according to USP XXIII (1995) “in vitro testing requirements” Method A (paddle method, rotation of 100 RPM and temperature fixed at 37°C). The dissolution mediums were 0.1N HCl solution and a pH 6.8 phosphate buffer solution, following the pH change dissolution procedure specified in USP for enteric-coated articles: 2 h of exposure to 750 mL of 0.1N HCl followed by testing in 1000 mL of pH 6.8 phosphate buffer, the pH being adjusted with 250 mL of 0.2 M tribasic sodium phosphate solution. The released amount of sodium diclofenac was periodically determined by UV spectrophotometry at wavelength of 276 nm, using a spectrophotometer UV-VIS HP 8453. The coated product showed gastric resistance properties confirming the feasibility of the fluidized bed for applying enteric coating in granules and pharmaceutical powders.     

含氟体系下亲水性ZSM-5沸石分子筛膜的制备及其性能

用变温热浸渍法在廉价大孔α-Al₂O₃的载体管上涂覆大小晶种引入平整均匀的晶种层, 随后在无有机模板剂的含氟体系下通过二次水热生长法制备了亲水性ZSM-5沸石分子筛膜。实验考察了小晶种液浓度对形成晶种层及ZSM-5沸石分子筛膜形貌和性能的影响。并将制备的ZSM-5沸石分子筛膜分别用于渗透汽化异丙醇脱水和乙酸脱水体系中。结果显示, 小晶种液浓度为0.2wt%时, 制备的ZSM-5沸石分子筛膜在75℃下对10wt%水/异丙醇和10wt% 水/乙酸混合物体系均具有优良的分离性能, 其渗透通量分别为3.64 kg/(m²·h)和0.61 kg/(m²·h), 分离因子分别达3204和1321。     

Chemical Synthesis and Morphology of β-Naphthalene Sulfonic Acid-Doped Polypyrrole Micro/Nanotubes

A preliminary result of the morphology and yield of chemically synthesized polypyrrole (PPY) using β-naphthalene sulfonic acid (NSA) and ammonium peroxodisulphate (APS) in aqueous medium is presented. Various micro/nanotubes were obtained using different dopant/monomer (D/M) ratios and temperature settings. Similar but shorter and sheet-like nanostructures were obtained without the use of surfactant NSA; with a fibre-like, loose and admixed physical outlook. The percentage yield (m/v) of the doped PPY was greater than that from the undoped, being 27-44 and 18-20, respectively with higher values obtained from the low temperature synthesis. The highest percentage yield of 44 was obtained from a D/M ratio of 0.8.     

CaO-B2O3玻璃助烧的零膨胀系数β-锂霞石陶瓷的制备及性能研究

采用固相反应法制备CaO-B₂O₃玻璃（简称“CB”玻璃）助烧的零膨胀系数β-锂霞石陶瓷。通过差示扫描量热(DSC)、X射线衍射(XRD)、扫描电子显微镜(SEM)手段分别对CB玻璃的热学特性和助烧后的β-锂霞石陶瓷样品的物相与显微形貌进行表征。结果表明, CB玻璃具有良好的助烧效果, 可以显著降低β-锂霞石陶瓷的烧结温度(从1300℃降至1150℃), 并大幅提高陶瓷的相对密度(从93.3%提高到97.4%)。加入CB玻璃助烧剂, β-锂霞石陶瓷致密性显著提高, 内部无微裂纹存在。加入4wt%和6wt% CB玻璃的β-锂霞石陶瓷在室温~200℃范围内具有零膨胀系数, 分别为0.02×10^-6/K和0.4×10^-6/K。然而, 加入8wt% CB玻璃的β-锂霞石陶瓷样品中产生了具有高正膨胀系数的新物相LiAlO₂, 使样品的热膨胀系数提高至3.46×10^-6/K。     

CFD Studies of Indoor Airflow and Contaminant Particle Transportation

This article presents a numerical study of indoor airflows and contaminant particle transportation in three ventilated rooms. The realizable k - ε model is employed to model the air-phase turbulence, while the Lagrangian particle tracking model is utilized for the particle-phase simulation. The predicted air-phase velocities and contaminant particle concentrations are validated against the experimental data obtained from the literature. In the first case, the realizable k - ε model successfully captures the flow trend and reasonably predicts the airflow velocity. The realizable k - ε model under-predicts the vertical air velocities along the vertical inlet jet axis by 11% at x = 0.219 m, which is slightly better than the standard k - ε model error of 17%. In a two-zone room case, the realizable k - ε model, combined with a Lagrangian particle tracking model, predicts the particle concentration decay with the highest normalized difference being 24%. In the third case, the influence of particle size, location of particle resource, and particle-wall collision on the particle concentrations is investigated by the realizable k - ε model and the Lagrangian model. It is found that for relatively small particles (diameter ≤ 10 μm), the particle concentration may be insensitive to the particle diameter. In addition it has been observed that the particle-collision model may have considerable effect on the particle concentration prediction.