Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs

Nanocrystals,a carrier-free colloidal delivery system in nano-sized range,is an interesting approach for poorly soluble drugs.Nanocrystals provide special features including enhancement of saturation solubility,dissolution velocity and adhesiveness to surface/cell membranes.Several strategies are applied for nanocrystals production including precipitation,milling,high pressure homogenization and combination methods such as Nano-Edge^(TM),SmartCrystal and Precipitation-lyophilization-homogenization(PLH)technology.For oral administration,many publications reported useful advantages of nanocrystals to improve in vivo performances i.e.pharmacokinetics,pharmacodynamics,safety and targeted delivery which were discussed in this review.Additionally,transformation of nanocrystals to final formulations and future trends of nanocrystals were also described.

Adverse effects of metal exposure on chemotaxis towards water-soluble attractants regulated mainly by ASE sensory neuron in nematode Caenorhabditis elegans

Chemotaxis to water-soluble attractants is mainly controlled by ASE sensory neuron whose specification is regulated by che-1 in Caenorhabditis elegans. Our data suggested that exposure to high concentrations of metals, such as Pb, Cu, Ag, and Cr, would result in severe defects of chemotaxis to water-soluble attractants of NaCl, cAMP, and biotin. Moreover, the morphology of ASE neuron structures as observed by relative fluorescent intensities and relative size of fluorescent puncta of cell bodies, relative lengths of sensory endings in ASE neurons, and the expression patterns of che-1 were obviously altered in metal exposed animals when they meanwhile exhibited obvious chemotaxis defects to water-soluble attractants. In addition, the dendrite morphology could be noticeably changed in animals exposed to 150 μmol/L of Pb, Cu, and Ag. Furthermore, we observed significant decreases of chemotaxis to water-soluble attractants in Pb exposed che-1 mutant at concentrations more than 2.5 μmol/L, and in Cu, Ag, and Cr exposed che-1 mutant at concentrations more than 50 μmol/L. Therefore, impairment of the ASE neuron structures and functions may largely contribute to the appearance of chemotaxis defects to water-soluble attractants in metal exposed nematodes.

On-line Measurement of Water-Soluble Ions in Ambient Particles

Combining the system of rapid collection of ambient particles and ion chromatography, the system of rapid collection of fine particles and ion chromatography （RCFP-IC） was established to automatically analyze on-line the concentrations of water-soluble ions in ambient particles. Here, the general scheme of RCFP-IC is described and its basic performance is tested. The detection limit of RCFP-IC for SO4^2-, NO3^-, NO2^-, Cl^- and F- is below 0.3μg m^-3. The collection efficiency of RCFP-IC increases rapidly with increasing sized particles. For particles larger than 300 nm, the collection efficiency approaches 100%. The precision of RCFP-IC is more than 90% over 28 repetitions. The response of RCFP-IC is very sensitive and no obvious cross-pollution is found during measurement. A comparison of RCFP-IC with an integrated filter measurement indicates that the measurement of RCFP-IC is comparable in both laboratory experiments and field observations. The results of the field experiment prove that RCFP-IC is an effective on-line monitoring system and is helpful in source apportionment and pollution episode monitoring.

Application of ion chromatography to the determination of water-soluble inorganic and organic ions in atmospheric aerosols

A simple, sensitive and convenient ion chromatography(IC) method was established for the simultaneous determination of twelve water-soluble inorganic anions(F -, Cl -, NO - 2, NO - 3, SO 2- 3, SO 2- 4, PO 3- 4), and fifteen water-soluble organic ions(formate, acetate, MSA, oxalate, malonate, succinate, phthalates, etc.) in atmospheric aerosols. The linear concentrations ranged from 0.005 μg/m 3 to 500 μg/m 3(r = 0.999—0.9999). The relative standard deviation(RSD) were 0.43%—2.00% and the detection limits were from 2.7 ng/m 3 to 88 ng/m 3. The proposed method was successfully applied to the simultaneous determination of those inorganic ions and organic ions in PM 2.5 of Beijing.

Effect of kaolin on tensile strength and humidity resistance of a water-soluble potassium carbonate sand core

Water soluble cores(WSCs) have been widely applied in manufacture of complex metal components with hollow configurations or internal channels. However, the WSCs without any additons have low tensile strength and low humidity resistance. The purpose of this study is to prepare a water-soluble potassium carbonate sand core with addition of kaolin by the hot-temping method. The effects of kaolin on tensile strength, humidity resistance, fracture mechanism, as well as the gas evolution and collapsibility of WSCs were investigated. Results show that both the crystal morphology and the fracture mechanism of the inorganic salt are changed under the participation of kaolin, contributing to the increase of the tensile strength and the humidity resistance of the core. With the addition of 3wt.% kaolin, the tensile strength could be increased by a factor of 2, reached 1.50 MPa and the hygroscopic rate could be decreased by 14%, achieved 0.559%(after stored for 8 h), respectively. As the addition amount of kaolin increases from 0wt.% to 3wt.%, the main fracture mechanism changes from a adhesive to a cohesive fracture mechanism. The water-soluble potassium carbonate core obtained has the low gas evolution and excellent collapsibility, which makes it suitable for casting low melting metal with complex cavities and crooked channels.

Preparation of Ultrafine Water-soluble Polymers Nanofiber Mats via Electrospinning

A series of water-soluble polymers such as poly（ethylene oxide）（PEO）, polyacrylamide（PAM） and poly（vinyl pyrrilidone）（PVP） was successfully prepared via the electrospinning of their aqueous solutions without the use of a surfactant. The effects of solution properties on the electrospinning of PEO, PAM and PVP solutions were investigated. The viscosity of the solution, charge density carried by the jet, and the surface tension of the solution are the key factors that influence the morphology and diameter size of the fibers. The viscosity of the solution was measured on a modular compact rheometer. The morphology and the diameter size distribution of the fibers were observed under an environmental scanning electron microscope（ESEM）. The results show that the diameters of the nanofibers electro spun from the solutions of these water soluble polymers were uniform and less than 300 nm.

Preparation of fructone catalyzed by water-soluble Brφnsted acid ionic liquids

Fructone （2-methyl-2-ethylacetoacetate-1, 3-dioxolane）, a flavouring material, has been synthesized from ethyl acetoacetate and glycol using five water-soluble Brφnsted acid ionic liquids as catalysts for the first time. The used Brφnsted acid ionic liquids include [Hmim]Tfa, [Hmim]Tsa, [Hmim]BF4, [Bmim]HSO4, [Bmim]H2P04, and [Hmim]BF4 showed the highest catalytic activity for the preparation of fructone. After reaction, the product could be isolated from the reaction system automatically, and the ionic liquid could be directly reused without dehydration.

Study on Dyeing Performance of Cationic Water-soluble Sulphur Black on Silk

A novel polyquaternaryammonium cationic sulphur black dye was synthesized and its dyeing behavior on silk was studied. The dye exhibited excellent dyeing fixation of up to 98.2 %, as well as excellent dyeing fastness on silk.

Alginate encapsulated mesoporous silica nanospheres as a sustained drug delivery system for the poorly water-soluble drug indomethacin

We applied a combination of inorganic mesoporous silica material,frequently used as drug carriers,and a natural organic polymer alginate(ALG),to establish a sustained drug delivery system for the poorly water-soluble drug Indomethacin(IND).Mesoporous silica nanospheres(MSNs)were synthesized using an organic template method and then functionalized with aminopropyl groups through postsynthesis.After drug loading into the pores of aninopropyl functionalized MSNs(AP-MSNs),IND loaded AP-MSNs(IND-AP-MSNs)were encapsulated by ALG through the ionic interaction.The effects of surface chemical groups and ALG layer on IND release were systematically studied using scanning electron microscopy(SEM),transmission electron microscopy(TEM),nitrogen adsorption,zetapotential analysis and TGA analysis.The surface structure and surface charge changes of the ALG encapsulated AP-MSNs(ALG-AP-MSNs)were also investigated.The results showed that sustained release of IND from the designed drug delivery system was mainly due to the blockage effect from the coated ALG.We believe that this combination will help designing oral sustained drug delivery systems for poorly water-soluble drugs.

Inquiry of Water-Soluble Polysaccharide Extraction Conditions from Grapefruit Skin

Water-soluble polysaccharide was isolated from grapefruit with the method of water-dissolving and ethanol-precipitating. By single factor test and orthogonal experimental method, the extraction conditions of the water-soluble polysaccharide were investigated, which contained liquid-solid ratio, temperature, time and pH. The results showed that pH was the most important factor of polysaccharide extraction, followed by temperature. The optimized extraction technology conditions were obtained. The liquid-solid ratio was 1:40, temperature was 90?C, time was 2.0 h, and pH was 2. The highest extraction rate of crude polysaccharide was 8.30%.

Synthesis and Cytotoxic Activity of Novel Water-soluble Prodrugs of Combretastatin A-4

Novel water-soluble prodrugs of combretastatin A-4 （5-8） were synthesized and evaluated for their in vitro cytotoxicity against lung carcinoma A549. Compound 5, bearing phosphoryl choline （PC） moiety, showed 90% inhibition at 32 ktg/mL concentration after 24 h. The findings showed the PC derivative would be a promising candidate for the development of new water-soluble prodrug of cytotoxic combretastatin A-4,

Designandconstructionof athree-dimensionalelectrodewith biomass-derived carbon current collector andwater-soluble binder for high-sulfur-loading lithium-sulfur batteries

Lithium-sulfur batteries attract lots of attention due to their high specific capacity,low cost,and environmental friendliness.However,the low sulfur utilization and short cycle life extremely hinder their application.Herein,we design and fabricate a three-dimensional electrode by a simple filtration method to achieve a high-sulfur loading.Biomass porous carbon is employed as a current collector,which not only enhances the electronic transport but also effectively limits the volume expansion of the active material.Meanwhile,an optimized carboxymethyl cellulose binder is chosen.The chemical bonding restricts the shuttle effect,leading to improved electrochemical performance.Under the ultrahigh sulfur load of 28mg/cm2,the high capacity of 18mAh/cm2 is still maintained,and stable cycling performance is obtained.This study demonstrates a viable strategy to develop promising lithium-sulfur batteries with a three-dimensional electrode,which promotes sulfur loading and electrochemical performance.

Concentrations,sources,and influential factors of water-soluble ions of atmospheric particles in Dunhuang Mogao Grottoes,a world heritage site in China

Atmospheric particle pollution is one of the major factors leading to degradation of ancient wall paintings,particularly heritage sites in arid and semi-arid regions.However,current systematic research on the changes,sources,and influential factors of atmospheric particulate matter and its water-soluble ion concentrations is not sufficient.Thus,the major water-soluble ion concentrations,sources,and influential factors of atmospheric particles PM_(2.5) and PM_(10)(particulate matter with an aerodynamic equivalent diameter≤2.5 and 10.0μm,respectively,in ambient air)were collected from Cave 16 and its ambient exterior environment in the Dunhuang Mogao Grottoes,China,between April 2015 and March 2016.Results showed that the concentrations of PM_(2.5) and PM_(10) inside and outside the cave were the highest in March 2016 and the lowest in December 2015.The higher particle concentration from March to May was related to the frequent occurrence of sand and dust events,and the lower particle concentration from June to September was associated with good diffusion conditions,increased precipitation,and an established cave shelterbelt.The concentration of particulate matter inside the cave was affected by the concentration of particles in the air outside the cave.Ca2+,NH+4,Na+,Cl-,and SO2-4were the main components of the total ions of PM_(2.5) and PM_(10) both inside and outside the cave.The total ions inside the cave were frequently affected by the disturbance of tourists'activities during the peak tourist season from May to August.Under the influence of dust,the total concentrations of Cl-,SO2-4,Na+,NH+4,and Ca2+in particles of different sizes inside and outside the cave increased,and the concentrations of Cl-,SO2-4,Na+,and Ca2+decreased during precipitation period.Backward air mass trajectory analysis suggested that the pollutants were mainly from Xinjiang,China.The pollutant sources of air particulates are straw burning,secondary pollution sources,soil dust,dry spring rivers,and tourist activities.

Phase Transfer Catalyzed Synthesis and Antibacterial Activity of Water-soluble S-Triazolo[3,4-b][1,3,4]thiadiazoles Containing Piperazine Group

6/3-（4-Chlorophenyl）-s-triazolo[3, 4-b][1, 3, 4]thiadiazoles （2,a-e） and （Sa-e） were synthesized respectively by intermolecular cyclization of 5-aryl / 4-chlorophenyl-4-amino-3- mercapto-1, 2, 4-triazoles （la-e） and （4） with 4-chlorobenzoic acid / aryl acids, which were condensed with piperazine under phase transfer catalyst TBAB to yield the corresponding free bases of monopiperazine derivatives and followed to form water-soluble salts （3a-e） and （6a-e） with hydrochloric acid in good yields. The in vitro biological results showed that piperazine group conjugated with the above fused heterocycles played an important role in antibacterial activity. The structures of novel compounds were confirmed by IR, ＇H NMR, MS and elemental analysis.

Diurnal variations of water-soluble ions in PM_(2.5)in Shanghai

Thirty-six daily time interval PM2.5 samples were collected in different seasonal dates in urban Shanghai, and the concentrations of four anions （Cl- , NO3-, SO4^2-, C2O4^2-） and five cations （NH＋, Na＋, K＋, Ca2＋, Mg2＋） were analyzed with ion chromatography. Sulfate, nitrate and ammonium were found to be the dominant species, accounting for about 80% of the total ions. The daily nitrate to sulfate mass ratio ranged from 0.31 to 0.82, indicating that coal combustion was still the main pollution source in Shanghai. The equivalent ratio of ammonium to stun of nitrate and sulfate showed fixed diurnal variation pattern in all the sampling days with higher values in the nighttime, suggesting that fine particles in the night were more neutralized. The oxalate to sulfate ratio was lower in the winter sampling days than that in hotter summer and autumn sampling days. Oxalate was significantly correlated with sulfate in winter sampling days, but not in the summer and autumn, suggesting that the formation mechanism of oxalate and sulfate was similar in winter, however different in hot days.

Anti-colon cancer activity of water-soluble polysaccharides extracted from Gloeostereum incarnatum via Wnt/β-catenin signaling pathway

The incidence rate of colon cancer ranks the third among malignant tumors worldwide.Gloeostereum incarnatum(GI),a fungus with homology of medicine and food,has multiple pharmacological activities.It was investigated in this study that the anti-colon cancer effect of polysaccharides purifi ed from GI(GIPS)in ApcMinC/Gpt mice(an in situ colon cancer mouse model).Eight-week administration with GIPS at doses of 30 or 90 mg/kg strongly inhibited tumor growth including the reduction on numbers and the suppression of the size without infl uencing the animals’body weight and organ functions.According to the proteomics performing by antibody array,among 308 detected cytokines,GIPS significantly regulated 89 of them.Compared with vehicle-treated mice,GIPS effectively reduced the levels of interleukin(IL)-1β,IL-4,IL-6,IL-17,IL-22,tumor necrosis factor(TNF)-α,matrix metalloproteinase(MMP)-2,and enhanced the levels of IL-15 and IL-18 in serum and/or colon tissues,which suggested its anti-inflammation of GIPS.GIPS suppressed nuclear aggregation of β-catenin,affected the expression of WNT1 and related proteins,thereby regulated the activation of the Wnt signaling.Altogether,GIPS can inhibit the growth of colon cancer,at least partially,via inhibiting the Wnt/β-catenin signaling pathway.

Application of Water-Soluble Polymer in Dewatering of Fine Coal

The addition of water-soluble polymer to a fine coal slurry to enhance dewatering process is considered to be one of the most effective ways of solving the problems of dewatering of fine coal. A series of tests are conducted with a vacuum dewatering apparatus to study the effects of various factors such as the species of polymer, polymer dosage and its ways of addition, and the pH of fine coal slurry on filtrating and dewatering of fine coal.

Synthesis and antitumor activity of water-soluble poly(aminoheterocyclic amine)s (I): N,N,N',N'-tetra[2-(4-amino-5-substituted-s-triazol-3-yl sulfanyl)ethyl] -1,4-benzyldiamine salts

Five water-soluble poly(aminoheterocyclic amine)s containing s-triazole ring were synthesized as respective HC1 salts (5a-5e). Biological activities in L1210 (murine leukemia) and Chinese hamster ovary (CHO) cell lines were investigated via IC50 cytotoxicity determinations. The tide compounds represented moderate cytotoxicity (low IC50 values between 15 and 68μmol/L) in L1210 but high cytotoxicity (lower IC50 values: 0.25,0.018,0.014μmol/L for Sa-5e, respectively) in CHO cell lines, while the corresponding HC1 salts of the intermediates (3a-3e) without polyamine tether and starting materials amino-s-triazoles (1a-1e) showed poor or no activities against the above cell lines.

Deposition of water-soluble inorganic ions in PM_(2.5) in a typical forestry system in Beijing,China

Background: Rapid economic development in China has resulted in an increase in severe air pollution in city groups such as the Beijing-Tianjin-Hebei Metropolitan Region. PM2.5(fine particles with an aerodynamic equivalent diameter of 2.5 μm or less) is one of the most important pollutants. The deposition process is an important way of removing particles from the air. To evaluate the effect of an urban forest on atmospheric particle removal, a concentration gradient method was used to measure the deposition velocities of water-soluble inorganics in PM2.5 in two national forest parks in Beijing, China. The following eight water-soluble inorganic ions in PM2.5 were investigated: sodium, ammonium, potassium, magnesium, calcium, chloride, nitrate, and sulfate.Methods: Samples were taken from two sites in Beijing from the 7 th to the 15 th May, 2013. The concentrations of water-soluble inorganic ions were analyzed with ion chromatography. We used the concentration gradient technique to estimate the deposition flux and velocity. To determine the relationships between leaf traits and particle accumulation, typical leaf samples from each selected species were studied using scanning electron microscopy.Results: The total deposition flux and total deposition velocity during the daytime were higher than those at night.Sulfate showed the biggest deposition flux and velocity at both study sites, whereas the other ions showed different trends at each site. Result from higher proportion of coniferous to broadleaved trees, the total deposition flux of the eight ions measured in Jiufeng National Forest Park was greater than that in Olympic Forest Park.Conclusions: The deposition velocity was affected by meteorological conditions such as wind speed, temperature,and humidity. The deposition velocity was also influenced by tree species. The surface of plants is an important factor influencing particle deposition. The results of this study may help in assessing the effects of forestry systems on particle removal and provide evidence for urban air pollution control and afforestation of urban areas.

Synthesis, Characterization and Biological Activities of Novel Water-soluble Metalloporphyrins

The synthesis, characterization, and biological activities of a series of metal porphyrins were described. The complexes 3a similar to 3e were prepared from the reaction of compound 2 with M(OAc)(2) in CHCl3, and the treatment of 3a similar to 3f with pyridine gave corresponding complexes 4a similar to 4f. These new compounds were identified by absorption spectroscopies, H-1 NMR and elemental analysis. The results of biological activity,testing revealed that 4a and 4c had stronger inhibiting action for Escherichia coli (CCTCC AB91115).