A dendrimer facilitates resonance energy transfer between hydrophobic aromatic guest molecules in water

A water soluble third generation poly(alkyl aryl ether) dendrimer was examined for its ability to solubilize hydrophobic polyaromatic molecules in water and facilitate non-radiative resonance energy transfer between them. One to two orders of magnitude higher aqueous solubilities of pyrene (PY), perylene (PE), acridine yellow (AY) and acridine orange (AO) were observed in presence of a defined concentration of the dendrimer. A reduction in the quantum yield of the donor PY* emission and a partial decrease in lifetime of the donor excited state revealed the occurrence of energy transfer from dendrimer solubilized excited PY to ground state PE molecules, both present within a dendrimer. The energy transfer efficiency was estimated to be similar to 61%. A cascade resonance energy transfer in a three component system, PY*-to-PE-to-AY and PY*-to-PE-to-AO, was demonstrated through incorporation of AY or AO in the two component PY-PE system. In the three-component system, excitation of PY resulted in emission from AY or AO via a cascade energy transfer process. Careful choice of dye molecules with good spectral overlap and the employment of dendrimer as the medium enabled us to expand absorption-emission wavelengths, from similar to 330 nm to similar to 600 nm in aqueous solution. (C) 2015 Elsevier B.V. All rights reserved.

Differenzierung von Pangasius (Pangasius hypophthalmus) und Asiatischem Rotflossenwels (Hemibagrus wyckioides) durch Protein- und DNA-Analyse

In the last years farmed Pangasius (Tra-Pangasius, Pangasius hypophthalmus) from Vietnam has reached a considerable market share, whereas aquaculture of Asian Redtail Catfish (Hemibagrus wyckioides) is in its infancy. Recently it has been detected by food control authorities in Hamburg, that Pangasius fillets have been mislabelled and sold as fillets produced from Asian Redtail catfish. The necessity to improve the analytical methods for differentiation of Pangasius and Redtail Catfish prompted us to evaluate the suitability of isoelectric focusing (IEF) and DNA-analysis for identification of the two species. IEF of water soluble proteins was found to be a fast, reliable and economical method for differentiation of raw fillets of Pangasius and Redtail Catfish, as long as reference material is available. PCR-based DNA analysis was performed as follows: (i) amplification of a 464 bp segment of the cytochrome b gene; (ii) sequencing of the PCR product; (iii) comparison of the sequence with entries in GenBank using BLAST. The sequences of both species differed considerably, allowing the unequivocal differentiation between P. hypophthalmus and H. wyckioides. Kurzfassung Pangasius (Schlankwels, Tra-Pangasius, Pangasius hypophthalmus) hat sich innerhalb weniger Jahre zu einem bedeutenden Zuchtfisch entwickelt, während die Aquakultur des Asiatischen Rotflossenwelses (Hemibagrus wyckioides) in Vietnam noch in einem relativ kleinen Maßstab stattfindet. Kürzlich wurde von der Lebensmittelüberwachung in Hamburg nachgewiesen, dass im Handel erhältliche Filets mit der Deklaration „Rotflossenwels“ aus Pangasius hergestellt worden waren. Vor diesem Hintergrund wurden zwei Methoden auf ihre Eignung zur Differenzierung von Pangasius und Rotflossenwels geprüft. Es zeigte sich, dass sowohl die isoelektrische Fokussierung (IEF) wasserlöslicher Proteine als auch die PCR-basierte DNA-Analyse zur Unterscheidung beider Arten gut geeignet ist. Die IEF stellt eine schnelle und kostengünstige Untersuchungsmethode dar, die allerdings Referenzmaterial benötigt. Mit Hilfe der PCR (Polymerase-Kettenreaktion) wurde ein Abschnitt des Cytochrom b-Gens vervielfältigt und sequenziert. Die Sequenzen von P. hypophthalmus und H. wyckioides wiesen beträchtliche Unterschiede auf. Es wird diskutiert, wie sich durch Vergleich dieser Sequenzen mit Einträgen in Gendatenbanken unbekannte Proben beider Arten sicher zuordnen lassen.

An assessment of chemical contaminants detected in passive water samplers deployed in the St. Thomas East End Reserves (STEER)

This report is the second in a series from a project to assess land-based sources of pollution (LBSP) and effects in the St. Thomas East End Reserves (STEER) in St. Thomas, USVI, and is the result of a collaborative effort between NOAA’s National Centers for Coastal Ocean Science, the USVI Department of Planning and Natural Resources, the University of the Virgin Islands, and The Nature Conservancy. Passive water samplers (POCIS) were deployed in the STEER in February 2012. Developed by the US Geological Survey (USGS) as a tool to detect the presence of water soluble contaminants in the environment, POCIS samplers were deployed in the STEER at five locations. In addition to the February 2012 deployment, the results from an earlier POCIS deployment in May 2010 in Turpentine Gut, a perennial freshwater stream which drains to the STEER, are also reported. A total of 26 stormwater contaminants were detected at least once during the February 2012 deployment in the STEER. Detections were high enough to estimate ambient water concentrations for nine contaminants using USGS sampling rate values. From the May 2010 deployment in Turpentine Gut, 31 stormwater contaminants were detected, and ambient water concentrations could be estimated for 17 compounds. Ambient water concentrations were estimated for a number of contaminants including the detergent/surfactant metabolite 4-tert-octylphenol, phthalate ester plasticizers DEHP and DEP, bromoform, personal care products including menthol, indole, n,n-diethyltoluamide (DEET), along with the animal/plant sterol cholesterol, and the plant sterol beta-sitosterol. Only DEHP appeared to have exceeded a water quality guideline for the protection of aquatic organisms.

The influence of water-miscible solvents on the permeability of clay

Centrifuge tests were carried out to determine the effect of 5 different water-soluble chemicals on a thin consolidated disc of clay. The evolution of changes in the clay permeability with time was investigated and other structural changes due to chemical attack were monitored. The findings presented here demonstrate that the permeability of the clay appear to be generally related to the polarity of the chemicals and the dielectric constant, with the exception of Butanol. In the case of Butanol at low flow rate and low stress level, the action of the chemical caused the clay to crack, with a consequent large increase in flow.

Soluble protein isolated from low cost fish and fish wastes

The method of preparation, composition, amino acid content, protein efficiency ratio and areas of possible application of water soluble protein isolates from low cost fish and fish wastes are discussed in detail in this communication.

Effect of water washing on biochemical and gel characteristics of minced meat from croaker fish (Johnius gangeticus)

Quality of analog fishery products invariably depends on the gel characteristics and nutritional status of minced meat. With an objective to find out the effect of water washing on kamaboko gel, the minced meat from Croaker fish was washed for four times (5 minutes each) using chilled water at a temperature of 8-10°C. Results reflected noticeable improvement in folding test and SSN% of kamaboko with essential decrease in fat content, water soluble proteins, expressible water and quality parameters like NPN, VBN, TMA, FFA and PV denoting superior gel quality than control sample after repeated washing. The results indicated that there was a definite improvement in functional properties such as gel forming ability, expressible water content of the croaker minced meat essential decrease in fat content, water soluble proteins, expressible water and quality parameters after each wash, but two washes of 5 minutes duration each was necessary to achieve satisfactory results.

Gas permeability of a novel cellulose membrane

A novel cellulose membrane was prepared by using amine oxides as the solvent and its mechanical performance was measured. Steady-state permeation rates of carbon dioxide, hydrogen, methane, nitrogen, oxygen, argon and helium in the homogeneous dense cellulose membrane were measured in the temperature range of 298-353 K and under gas pressures up to 1 MPa. The effect of swelling on hydrophilic membrane permeability was studied in some detail on the cellulose membrane. The difference in gas permeability between the "dry" cellulose membrane and the "water-swollen" cellulose membrane was investigated, and the gas permeability between the cellulose membrane and the Cellophane was compared. In this paper, the separation performance Of CO2 over H-2 in a "water-swollen" cellulose membrane is reported for the first time and the separation factor Of CO2/H-2 can be up to 15. (C) 2002 Elsevier Science B.V. All rights reserved.

Successful establishment of MEKC with electrochemiluminescence detection based on one functionalized ionic liquid

Herein, one water-soluble functionalized ionic liquid, 1-butyl-3-methylimidazolium dodecyl sulfate ([BMIm(+)][C12H25SO4-]), was designed and its superiorities either used as supporting electrolytes or as additives for successful establishment of MEKC with electrochemiluminescence (ECL) detection (MEKC-ECL) method were investigated. Compared with the common supporting electrolytes such as phosphate solution, 1-butyl-3-methylimidazolium dodecyl sulfate solution used as running buffers led to greatly enhanced ECL intensities and column efficiencies for negative targets, a little increase for neutral-charge ones while maintained nearly unchanged for positive ones due to the electrostatic forces between the large cation BMIm(+) and the solutes and the hydrophobic interactions resulting from the large anion C12H25SO4.

Preparation and properties of water-based conducting polyaniline

A convenient way to make water-soluble or water-dispersible conducting polyaniline was given by employing protonic acid dopants containing hydrophilic ethyleneoxide oligomer as counter-anion. The conducting polyaniline possessed electrical conductivity in the range of 10(-3) to 10(-2) S/cm, depending on the dopant, and it displayed excellent electrochemical redox reversibility in non-aqueous system.

Preparation and properties of water-based conducting polyaniline

A convenient way to prepare water-soluble or water-dispersible conducting polyaniline was developed by employing protonic acid dopants containing hydrophilic ethyleneoxide oligomer as counter-ion. The conducting polyaniline possesses electrical conductivity in the range of 10(-3) to 10(-2) S/cm depending on the chosen dopant, and it displays an excellent electrochemical redox reversibility in non-aqueous systems.

Polysaccharides from Ulva pertusa (Chlorophyta) and preliminary studies on their antihyperlipidemia activity

Polysaccharides from Ulva pertusa were isolated and prepared by extraction in hot water and precipitation by ethanol. The water-soluble polysaccharides were chemically well defined, containing 47.0% total carbohydrate, 23.2% uronic acids, 17.1% sulfate groups, 1.0% N and 29.9% ash. Gas chromatography analysis demonstrated that the neutral sugars were mainly composed of rhamnose, xylose and glucose and smaller amounts of mannose, galactose and arabinose. The FTIR and C-13-NMR spectra indicated that basic repeating units of the polysaccharides were (beta-D-GlcpA-(1->4)-alpha-L-Rhap 3S) and (alpha-L-IdopA-(1->4)-alpha-L-Rhap 3S). Fifty ICR mice were used to study the effect of water-soluble polysaccharides from Ulva pertusa on the level of plasma lipids, with inositol niacinate as positive control. The results indicated that the polysaccharides significantly lowered the contents of plasma total cholesterol, low-density lipoprotein cholesterol, triglyceride and markedly increased the contents of serum high-density lipoprotein cholesterol, compared with the hyperlipidemia control group (p<0.01). Moreover, administration of polysaccharides significantly decreased the atherogenic index. The present results suggest that the polysaccharides from Ulva pertusa have great potential for preventing ischemic cardiovascular and cerebrovascular diseases.

东天山红山高硫型浅成低温铜-金矿床氧化带的形成机理和硫酸盐矿物的系列发现及意义

Located in the Paleozoic uplift along the southern margin of Tu-Ha basin in eastern Xinjiang, the newly discovered Hongshan Cu-Au deposit occurs in the superimposed Mesozoic volcanic basin upon the north section of later Paleozoic Dananhu-Tousuquan accretionary arc. Kalatage Cu-Au orebelt is controlled by NWW-trend faults, and includes Hongshan and Meiling Cu-Au deposits. The host rocks of Hongshan ore district are mainly rhyolitic-dacitic ignimbrites, whereas Cu-Au mineralization is closely related to quartz porphyry, rhyolitic porphyry and granitic porphyry. Mineralization styles are dominantly veinlet-disseminated and veinlet, occasionally stockwork. The mineral association is chalcopyrite, pyrite, bornite, chalcocite and sphalerite. The hydrothermal alteration consists of silicfication, sericitization, alunitization, pyrophylitization, illitization, hydromuscovitization, and chloritization. Hongshan Cu-Au deposit, on the edge of the desert, is one of the driest areas in eastrn Tianshan. Moreover， the highest temperature has been up to 60℃, and the average rainfall receives only 34.1mm/y. The light rainfall and rapid evaporation in the vicinity of this deposit have allowed the formation of a great variety of water-soluble sulfates. Oxidization zone of this deposit lies on the upper part of primary sulfide orebodies appearing with a depth of 50-60m, which is dominant in sulfate minerals. 1. Based on the field observation, the volcanic and sub-volcanic rock composition, hydrothermal alteration, ore structure and mineralization characteristics, this paper proposed that the Hongshan Cu-Au deposit belongs to a transitional type from high-sulfide epithermal to porphyry Cu-Au deposit, which corresponds with the typical HS-epithermal deposit such as Zijinshan Au-Cu deposit in Fujian Province, SE-China. 2. The Hongshan copper-gold deposit was controlled by the tectonic, stratum, magma activity and volcanic apparatus, whereas Au mineralization is closely related to quartz porphyry, rhyolitic porphyry and fine grained pyritization in hydrothermal activity, and Cu mineralization is closely related to quartz porphyry and hydrothermal explosive breccia. 3. Oxidation zone of Hongshan Cu-Au deposit lies on the upper part of primary sulfide orebodies deposit. 23 sulfate minerals were identified in this work. The results of samples XRD and chemical analysis were furthermore confirmed through thermal, infrared spectrum and mössbauer spectrum analysis. Among those, nine minerals as Ferricopiapite, Cuprocopiapite, Rhomboclase, Parabutlerite, Krausite, Yavapaiite, Metasideronatrite Kroehnkite and Paracoquimbite were founded in China for the first time. And Paracoquimbite was secondly reported in the world (first case reported at 1938 in Chile). 4. EPMA analysis shows that Al impurity in crystal lattice is important to polytype formation of paracoquimbite and coquimbite besides stack fault. 5. Compared with Meiling Cu-Au deposit in the same Kalatage ore belt from the characteristics of δ34S of barite, lithofacies, hydrothermal alteration and homogeneous temperature, Hongshan Cu-Au deposit belongs to the same metallogenic system of HS-epithermal type as Meiling Cu-Au deposit. But Hongshan Cu-Au deposit has less extensive alteration and shallower denudation. 6. Sulfur isotope analyses show that δ34S values of pyrites vary in the range of +1.86‰~+5.69‰, with an average of 3.70‰, mostly in the range of +1.86‰~+3.20‰, and δ34Scp<δ34Spy. Therefore ore-forming fluid of porphyry comes from mantle and was contaminated by the earth’s crust. Sulfur isotope has reached balance in ore-forming process. 7. Sulfur isotope analyses show that δ34S values of sulfates vary in the range of +2.15‰~+6.73‰, with an average of +3.74‰, mostly equals as δ34S values of primary sulfides in Hongshan Cu-Au deposit. So supergene sulfates inherit sulfur of primary sulfide. δ34S values are mostly same in different sulfates. As well as pyrite and chalcopyrite, volcanic hot spring and associated native sulfur underground also provide water medium and sulfur during the formation process of sulfate. 8. According to the EPMA of sample chalcopyrite and pyrite in Hongshan Cu-Au, the value of Cu/Ni is 0.98-34.72, mostly close to the value of 5, which shows that Hongshan deposit is a typical volcanogenic magmaic hypothermal deposit. Au and Ag, Zn, Te and Bi are positive correlation, Cu and Hg, Se, Sb are positive correlation, indicates Au and Cu don’t locate in the factor of mineralization of same mineralization groups. The reasons of gold concentration in the oxidation zone are: 1). Change of redox potential (Eh) makes gold to deposit from the liquid of mineralization zone; 2). PH is one of the most factors of gold’s deposition; 3). Soluble complex and colloid of gold can be adsorbed easily. 9. The biotite and hornblende K-Ar isotopic ages from the wall rock－quartz diorite, biotite granite and monzonite granite are 231.99±3.45Ma, 237.97±2.36Ma and 296.53±6.69Ma respectively. The ore-bearing rhyolitic breccia lava contains breccia of the biotite granite which indicates the volcanism and related Cu-Au mineralization occurred later than the granite, possibly in Mesozoic. K-Ar ages of granitoids in Sanya, Baishiquan and Hongliugou area and Molybdenite Re-Os age of Baishan Mo deposit all are in Triassic. Besides late Paleozoic magmatism, igneous magmatic event of Mesozoic was widespread in eastern Tianshan. 10. The K-Ar age dating indicates that the K-Ar age of Voltaite occurred below surface 1m is 56.02±3.98Ma, K-Ar age of Ferricopiapite occurred below surface 1.5m is 8.62±1.12Ma, K-Ar age of Yavapaiite occurred below surface 14 m is 4.07±0.39Ma, and K-Ar age of Voltaite occurred below surface 10 m is 14.73±1.73Ma. So the age interval of oxidation zone of Hongshan copper-golden bed is between 60 -3.38Ma. Oxidization occurred at Caenozoic era (from 65Ma), which can be identified through comparing with different deposits oxidation zone in other countries. The coupling between global tectonic event and climatic change event which occur from Caenozoic era has some effect on epigeosphere system, which can act on the surface of bed oxidation zone similarly. It induces that the age mentioned above coincide with collision of India-Asia and multistage uplifting of Qinhai-Tibet Plateau happened subsequently. Bed oxidation zone is the effect and record of collision and uplifting of Tibet Plateau. The strong chemical weathering of surface accumulation to which was leaded by PETM event occurred Paleocene and Eocene is the reason of Voltaite sharply rises. On the contrary, Ferricopiapite formed due to the global cold weather. The predecessor did much research through biota, isotopes, susceptibility, but this paper try to use different sulfate mineral instead of climatic change. So the research of sulfate minerals not only indicates a great deal of oxidized zone feature, but also the intergrowth of sulfate minerals may be used to trace paleoenviroment and paleoclimate of oxidation zone. 11. Analysis of the information of alteration and mineralization features of four bore cores, induced activity polarization well logging and Eh-4 geophysical section, deep mineralization anomaly objects of Hongshan ore districts shows low resistance, middle and high polarization, measurements of Eh-4 consecutive conductance section show the existing of concealed porphyry ore body deeper than 450m, on the top of and around rock body there are low resistance body ranged from 100-300Ω•m, this area may be the ore-bearing part. In a word, Hongshan Cu-Au deposit deposit is a combine of upper HS-style epithermal Au deposit and deeper porphyry mineralization system. It has great potential to find large HS-style epithermal-porphyry Au-Cu deposits. This paper consists of seven chapters and twenty seven sections. The geological character of deposit is basic condition in this work. Constitute of oxidation zone, research of sulfate mineral, relation between oxidation and primary zone, K-Ar ages of potassic sulfate are key parts of thesis. Genesis of ore deposit is the further expansion of this research. Analysis of ore-controlling factors is the penetration above basic. Analysis of potential is application of exploration.

东南极格罗夫山地区的土壤特征及其环境研究

The Grove Mountains, including 64 nunataks, is situated on an area about 3200km2 in the inland ice cap of east Antarctica in Princess Elizabeth land (72o20'-73°101S, 73°50'-75o40'E), between Zhongshan station and Dome A, about 450km away from Zhongshan station (69°22'S, 76°22'E). Many workers thought there was no pedogenesis in the areas because of the less precipitation and extreme lower temperature. However, during the austral summer in 1999-2000, the Chinaer 16 Antarctic expedition teams entered the inland East Antarctica and found three soil spots in the Southern Mount Harding, Grove Mountains, East Antarctica. It is the first case that soils are discovered in the inland in East Antarctica. Interestingly, the soils in this area show clay fraction migration, which is different from other cold desert soils. In addition, several moraine banks are discovered around the Mount Harding. The soil properties are discussed as below. Desert pavement commonly occurs on the three soil site surfaces, which is composed of pebbles and fragments formed slowly in typical desert zone. Many pebbles are subround and variegated. These pebbles are formed by abrasion caused by not only wind and wind selective transportation, but also salt weathering and thaw-freezing action on rocks. The wind blows the boulders and bedrocks with snow grains and small sands. This results in rock disintegration, paved on the soil surface, forming desert pavement, which protects the underground soil from wind-blow. The desert pavement is the typical feature in ice free zone in Antarctica. There developed desert varnish and ventifacts in this area. Rubification is a dominant process in cold desert Antarctic soils. In cold desert soils, rubification results in relatively high concentrations of Fed in soil profile. Stained depth increases progressively with time. The content of Fed is increasing up to surface in each profile. The reddish thin film is observed around the margin of mafic minerals such as biotite, hornblende, and magnetite in parent materials with the microscope analyzing on some soil profiles. So the Fed originates from the weathering of mafic minerals in soils. Accumulations of water-soluble salts, either as discrete horizons or dispersed within the soil, occur in the soil profiles, and the salt encrustations accumulate just beneath surface stones in this area. The results of X-ray diffraction analyses show that the crystalline salts consist of pentahydrite (MgSO4-5H2O), hexahydrite (MgSO4-6H2O), hurlbutite (CaBe2(PO4)2), bloedite (Na2Mg(S04)2-4H2O), et al., being mainly sulfate. The dominant cations in 1:5 soil-water extracts are Mg2+ and Na+, as well as Ca2+ and K+, while the dominant anion is SO42-, then NO3-, Cl- and HCO3-. There are white and yellowish sponge materials covered the stone underside surface, of which the main compounds are quartz (SiO2, 40.75%), rozenite (FeSOKkO, 37.39%), guyanaite (Cr2O3-1.5H2O, 9.30%), and starkeyite (MgSO4-4H2O, 12.56%). 4) The distribution of the clay fraction is related to the maximum content of moisture and salts. Clay fraction migration occurs in the soils, which is different from that of other cold desert soils. X-ray diffraction analyses show that the main clay minerals are illite, smectite, then illite-smectite, little kaolinite and veirniculite. Mica was changed to illite, even to vermiculite by hydration. Illite formed in the initial stage of weathering. The appearance of smectite suggests that it enriched in magnesium, but no strong eluviation, which belongs to cold and arid acid environment. 5) Three soil sites have different moisture. The effect moisture is in the form of little ice in site 1. There is no ice in site 2, and ice-cement horizon is 12 cm below the soil surface in site 3. Salt horizon is 5-10 cm up to the surface in Site 1 and Site 2, while about 26cm in site 3. The differentiation of the active layer and the permafrost are not distinct because of arid climate. The depth of active layer is about 10 cm in this area. Soils and Environment: On the basis of the characteristics of surface rocks, soil colors, horizon differentiation, salt in soils and soil depth, the soils age of the Grove Mountains is 0.5-3.5Ma. No remnants of glaciations are found on the soil sites of Mount Harding, which suggests that the Antarctic glaciations have not reached the soil sites since at least 0.5Ma, and the ice cap was not much higher than present, even during the Last Glacial Maximum. The average altitude of the contact line of level of blue ice and outcrop is 2050m, and the altitude of soil area is 2160m. The relative height deviation is about 110m, so the soils have developed and preserved until today. The parental material of the soils originated from alluvial sedimentary of baserocks nearby. Sporepollen were extracted from the soils, arbor pollen grains are dominant by Pinus and Betula, as well as a small amount Quercus, Juglans, Tilia and Artemisia etc. Judging from the shape and colour, the sporepollen group is likely attributed to Neogene or Pliocene in age. This indicates that there had been a warm period during the Neogene in the Grove Mountains, East Antarctica.

Aqueous solutions of HEC and hmHEC: effects of molecular mass versus hydrophobic associations on hydrodynamic and thermodynamic parameters.

Aqueous solutions of amphiphilic polymers usually comprise of inter- and intramolecular associations of hydrophobic groups often leading to a formation of a rheologically significant reversible network at low concentrations that can be identified using techniques such as static light scattering and rheometry. However, in most studies published till date comparing water soluble polymers with their respective amphiphilic derivatives, it has been very difficult to distinguish between the effects of molecular mass versus hydrophobic associations on hydrodynamic (intrinsic viscosity [g]) and thermodynamic parameters (second virial coefficient A2), owing to the differences between their degrees of polymerization. This study focuses on the dilute and semi-dilute solutions of hydroxyethyl cellulose (HEC) and its amphiphilic derivatives (hmHEC) of the same molecular mass, along with other samples having a different molecular mass using capillary viscometry, rheometry and static light scattering. The weight average molecular masses (MW) and their distributions for the nonassociative HEC were determined using size exclusion chromatography. Various empirical approaches developed by past authors to determine [g] from dilute solution viscometry data have been discussed. hmHEC with a sufficiently high degree of hydrophobic modification was found to be forming a rheologically significant network in dilute solutions at very low concentrations as opposed to the hmHEC with a much lower degree of hydrophobic modification which also enveloped the hydrophobic groups inside the supramolecular cluster as shown by their [g] and A2. The ratio A2MW/[g], which takes into account hydrodynamic as well as thermodynamic parameters, was observed to be less for associative polymers compared to that of the non-associative polymers.

Non-aqueous silicone elastomer gels as a vaginal microbicide delivery system for the HIV-1 entry inhibitor maraviroc

Aqueous semi-solid polymeric gels, such as those based on hydroxyethylcellulose (HEC) and polyacrylic acid (e.g. Carbopol®), have a long history of use in vaginal drug delivery. However, despite their ubiquity, they often provide sub-optimal clinical performance, due to poor mucosal retention and limited solubility for poorly water-soluble actives. These issues are particularly pertinent for vaginal HIV microbicides, since many lead candidates are poorly water-soluble and where a major goal is the development of a coitally independent, once daily gel product. In this study, we report the use of a non-aqueous silicone elastomer gel for vaginal delivery of the HIV-1 entry inhibitor maraviroc. In vitro rheological, syringeability and retention studies demonstrated enhanced performance for silicone gels compared with a conventional aqueous HEC gel, while testing of the gels in the slug model confirmed a lack of mucosal irritancy. Pharmacokinetic studies following single dose vaginal administration of a maraviroc silicone gel in rhesus macaques showed higher and sustained MVC levels in vaginal fluid, vaginal tissue and plasma compared with a HEC gel containing the same maraviroc loading. The results demonstrate that non-aqueous silicone gels have potential as a formulation platform for coitally independent vaginal HIV microbicides.