Multidrug Idebenone/Naproxen Co-loaded Aspasomes for Significant in vivo Anti-inflammatory Activity

The use of proper nanocarriers for dermal and transdermal delivery of anti-inflammatory drugs recently gained several attentions in the scientific community because they pass intact and accumulate payloads in the deepest layers of skin tissue. Ascorbyl palmitate-based vesicles (aspasomes) can be considered a promising nanocarrier for dermal and transdermal delivery due to their skin whitening properties and suitable delivery of payloads through the skin. The aim of this study was the synthesis of multidrug Idebenone/naproxen co-loaded aspasomes for the development of an effective anti-inflammatory nanomedicine. Aspasomes had suitable physicochemical properties and were safe in vivo if topically applied on human healthy volunteers. Idebenone/naproxen co-loaded aspasomes demonstrated an increased therapeutic efficacy of payloads compared to the commercially available Naprosyn® gel, with a rapid decrease of chemical-induced erythema on human volunteers. These promising results strongly suggested a potential application of Idebenone/naproxen multidrug aspasomes for the development of an effective skin anti-inflammatory therapy.     

Characterization of pili nut (Canarium ovatum) oil: Fatty acid and triacylglycerol composition and physicochemical properties

The fatty acid and triacylglycerol composition of pili nut (Canarium ovatum) oil and fractions were analyzed by gas chromatography and reversed-phase high-performance liquid chromatography, respectively. The oil obtained by solvent extraction was low in polyunsaturated fatty acids and high in saturates. The polyunsaturated fatty acid (18∶2 and 18∶3) contents were less than 11%, whereas palmitic (16∶0) and stearic acid (18∶0) were 33.3 and 10.9%, respectively. The saturated fatty acid level of the low-melting fraction oil was reduced from 44.4 to 35.5% and the total unsaturated fatty acid levels were increased from 55.6 to 65% by fractional crystallization. Triacylglycerol analysis showed that the high-melting fraction (HM) from pili nut oil consisted of POP, POS, and SOS+SSO (P=palmitic acid, O=oleic acid, and S=stearic acid) in the proportion of 48.6, 38.8, and 8.7%, respectively. The physicochemical properties of the HM fraction were studied using differential scanning calorimetry and pulsed nuclear magnetic resonance. The results showed that the melting range and solid fat content of the HM fraction were very similar to those isolated from cocoa butter and olive oil. The content of POP played an important role in determining the melting range of the HM fraction. It is suggested that this HM fraction may have applications as a cocoa butter substitute in confectionery products.     

ON THE RETRIEVAL OF URBAN AEROSOL MASS CONCENTRATION BY A 532 AND 1064 nm LIDAR

Based on the hypothesis of a monomodal, lognormal size distribution, the uncertainty affecting the humid-mass retrieval from LIDAR data was estimated by considering our ignorance of the distribution width to be a source of error. The mass to backscatter ratio and its uncertainty were computed for six accumulation-mode aerosol models as a function of the backscatter angstrom coefficient (α) and of the relative humidity (RH). A mass to backscatter uncertainty of less than ±30% was obtained for all six models. We computed the mass and simulated the expected LIDAR backscatter at 532 and 1064 nm for a test data set of 14 “real-world” multimodal size distributions obtained from the literature. The possible presence of 0–20%–50% water-insoluble compounds in each aerosol mode was assumed. An urban-type accumulation mode and 10 different coarse mode compositions were considered, including dust-like aerosols. The aerosol mass concentration was derived by fitting the simulated LIDAR data at 532 and 1064 nm with a monomodal distribution of urban aerosols of “unknown” width. The relative over- or underestimation of the mass with respect to the real aerosol mass was expressed in terms of α and RH for the 10 coarse aerosol types. The LIDAR-derived mass turned out to be underestimated by 0 – 15% in the case of (NH₄)₂SO₄, NaCl, maritime, and H₂SO₄ coarse aerosols. In the case coarse dust aerosols, the range of underestimation was wider (0–30%). Absorbing aerosols showed a maximum underestimation of 40–50%.     

Protein Expression Changes in Maize Roots in Response to Humic Substances

Humic substances are known to affect plant metabolism at different levels. We characterized humic substances extracted from earthworm feces by diffuse reflectance infrared Fourier transform (DRIFT) spectroscopy and used them to treat corn, Zea mays L., seedlings to investigate changes in patterns of root protein expression. After root plasma membrane extraction and purification, proteins were separated by two-dimensional gel electrophoresis, and differential spot intensities were evaluated by image analysis. Finally, 42 differentially expressed proteins were identified by liquid chromatography-tandem mass spectrometry (LC-MS/MS). The majority of them were downregulated by the treatment with humic substances. The proteins identified included malate dehydrogenase, ATPases, cytoskeleton proteins, and different enzymes belonging to the glycolytic/gluconeogenic pathways and sucrose metabolism. The identification of factors involved in plant responses to humic substances may improve our understanding of plant-soil cross-talk, and enable a better management of soil resources.     

Modulatory Effects of Polyphenols on Apoptosis Induction: Relevance for Cancer Prevention

Polyphenols, occurring in fruit and vegetables, wine, tea, extra virgin olive oil, chocolate and other cocoa products, have been demonstrated to have clear antioxidant properties in vitro, and many of their biological actions have been attributed to their intrinsic reducing capabilities. However, it has become clear that, in complex biological systems, polyphenols exhibit several additional properties which are yet poorly understood. Apoptosis is a genetically controlled and evolutionarily conserved form of cell death of critical importance for the normal embryonic development and for the maintenance of tissue homeostasis in the adult organism. The malfunction of the death machinery may play a primary role in various pathological processes, since too little or too much apoptosis can lead to proliferative or degenerative diseases, respectively. Cancer cells are characterized by a deregulated proliferation, and/or an inability to undergo programmed cell death. A large body of evidence indicates that polyphenols can exert chemopreventive effects towards different organ specific cancers, affecting the overall process of carcinogenesis by several mechanisms: inhibition of DNA synthesis, modulation of ROS production, regulation of cell cycle arrest, modulation of survival/proliferation pathways. In addition, polyphenols can directly influence different points of the apoptotic process, and/or the expression of regulatory proteins. Although the bulk of data has been obtained in in vitro systems, a number of clinical studies suggesting a preventive and therapeutic effectiveness of polyphenols in vivo is available. However, a deeper knowledge of the underlying mechanisms responsible for the modulation of apoptosis by polyphenols, and their real effectiveness, is necessary in order to propose them as potential chemopreventive and chemotherapeutic candidates for cancer treatment.     

A potent integrin antagonist from a small library of cyclic RGD pentapeptide mimics including benzyl-substituted azabicycloalkane amino acids

A small library of cyclic RGD pentapeptide mimics, including benzyl-substituted azabicycloalkane amino acids, was synthesized with the aim of developing active and selective integrin antagonists. In vitro binding assays established one particular compound with affinity for both the alpha(v)beta(3) and the alpha(v)beta(5) integrins. The synthesis in solution and the in vitro screening of these RGD derivatives, as well as the determination of the conformational properties of the integrin ligands by spectroscopic and computational methods are described.     

Swelling Deswelling Behavior of PS‐PNIPAAM Copolymer Particles and PNIPAAM Brushes Grafted from Polystyrene Particles & Monoliths

Two sets of emulsion particles have been synthesized. In the first set, surfactant free emulsion was used to directly synthesize PS‐PNIPAAM copolymer particles. In the second set, polystyrene particles with an ATRP initiator shell were first synthesized and subsequently grafted with PNIPAAM brushes. Swelling/deswelling behavior of both sets of particles was studied with respect to temperature and time. Monoliths with two different porosities were also formed by grafting and crosslinking of PNIPAAM chains on the aggregated particles and characterized. In all cases, swelling kinetics is sufficiently fast to use these supports for separation driven by temperature changes only. However, hindrance and cross‐linking is sensibly reducing the material performance.

     

High‐density polyethylene reinforced with submicron titania particles

Submicron titania particles were prepared by means of two different synthetic procedures in order to obtain different particle size (diameter ranging from 20 to 350 nm), shapes, and morphologies (amorphous or crystalline). Titania particles were surface modified with octadecylsilane in order to improve their compatibility with respect to polymeric matrices. High‐density polyethylene (HDPE)–titania composites were prepared by melt blending by using an internal mixer. The obtained composites were mechanically characterized in quasi static and creep tensile conditions. The presence of submicron titania particles (1 %vol) led to a significant increase of elastic modulus (20–25%) with respect to the unreinforced HDPE together with a slight increase of yield stress and a decrease of ultimate elongation. An interesting reduction for both elastic and viscoelastic creep compliance components was also evidenced. POLYM. ENG. SCI., 2008. © 2008 Society of Plastics Engineers