Skin Permeation of Lidocaine from Crystal Suspended Oily Formulations

ABSTRACT

In vitro permeation of lidocaine (lidocaine base, LID) through excised rat skin was investigated using several LID-suspended oily formulations. The first skin permeation of LID from an LID-suspended oily solution such as liquid paraffin (LP), isopropyl myristate (IPM), polyoxyethylene (2) oleylether (BO-2), and diethyl sebacate (DES) was evaluated and compared with that from polyethylene glycol 400 (PEG400) solution, a hydrophilic base. The obtained permeation rate of LID, J_app, from PEG400, LP, IPM, BO-2, and DES was in the order of DES>BO-2 = IPM>LP>PEG400, and increased with LID solubility in the oily solvents, although LID crystals were dispersed in all solvents. Subsequently, oily formulations that consisted of different ratios of the first oily solvent (IPM, BO-2, or DES) (each 0–20%), the second oily solvent (LP) and an oily mixture of microcrystalline wax/white petrolatum/paraffin (1/5/4) were evaluated. BO-2 groups at a concentration of 5% and 10% had the highest J_app among the oily formulations, although a higher BO-2 resulted in lower skin permeation. In addition, pretreatment with BO-2 increased the skin permeation of LID. These results suggest that the penetration enhancing effect by the system may be related to the skin penetration of BO-2 itself. Finally, mathematical analysis was done to evaluate the effect of BO-2, and it was shown that BO-2 improved the LID solubility in stratum corneum lipids to efficiently enhance the LID permeation through skin.     

Influence of counter material on friction and wear performance of PTFE–metal binary coatings

The study presented in this paper concerns the influence of the counter materials on wear and friction performance of polytetrafluoroethylene (PTFE) reservoirs arranged in distinct patterns on coated surfaces. Al-bronze and Mo coatings were deposited on a mild steel substrate using an atmospheric plasma spray process. Three patterns of PTFE reservoirs were used. Pins, which served as counter surface, were made of three different materials. Wear tests were carried out in a pin-on-disc test rig at room temperature and under dry contact conditions. The tests were carried out at a constant pressure of 10 MPa. An average linear speed of the test disc was 0.036 m/s. The importance of appropriately matched hardness of two surfaces in sliding contact is emphasised. Due to inadequate hardness of the counter material, performance of Mo coating was adversely affected and expected beneficial action of PTFE reservoirs severely hindered. Al-bronze coating proved to be performing far better than Mo coating. Serious deterioration of Mo coating occurred faster than that for Al-bronze coating.     

The effect of the hydrothermal treatment with aqueous NaOH solution on the photocatalytic and photoelectrochemical properties of visible light-responsive TiO2 thin films

The effect of the hydrothermal treatment with aqueous NaOH solution on the photoelectrochemical and photocatalytic properties of visible light-responsive TiO₂ thin films prepared on Ti foil substrate (Vis-TiO₂/Ti) by a radio-frequency magnetron sputtering (RF-MS) deposition method has been investigated. The hydrothermally treated Vis-TiO₂/Ti electrodes exhibited a significant increase in their photocurrent under UV and visible light irradiation as compared to untreated Vis-TiO₂/Ti electrode. SEM investigations revealed that the surface morphology of Vis-TiO₂/Ti are drastically changed from the assembly of the TiO₂ crystallites to the stacking of nanowires with diameters of 30–50 nm with increasing hydrothermal treatment time (3–24 h), accompanying the increase in their surface area. The separate evolution of H₂ and O₂ from water under solar light irradiation was successfully achieved using the Vis-TiO₂/Ti/Pt which is hydrothermally treated for 5 h, while the H₂ evolution ratio was 15 μmol h⁻¹ in the early initial stage, corresponding to a solar energy conversion efficiency of 0.23%.     

Identification of Ustilago cynodontis as a new producer of glycolipid biosurfactants, mannosylerythritol lipids, based on ribosomal DNA sequences

Mannosylerythritol lipids (MELs) are one of the most promising glycolipid biosurfactants known because of their multifunctionality and biocompatibility. The search for novel producers of MELs was undertaken based on the analysis of ribosomal DNA sequences on basidiomycetous yeasts. The bermuda grass smut fungus Ustilago cynodontis NBRC 7530, which taxonomically relates to Pseudozyma shanxiensis known as a MEL-C producer, was found to accumulate glycolipids in the cultured medium. Under a shake flask culture with soybean oil, the amount of the glycolipids was 1.4 g/L for 7 days at 25 degrees C. As a result of the structural characterization, the main glycolipids was identified as 4-O-[(4'-O-acetyl-3'-O-alka(e)noyl-2'-O-butanoyl)-beta-D-mannopyranosyl]-D-erythritol, and the major fatty acids were C(14) and C(16) ones. The glycolipid was highly hydrophilic MEL-C, and very similar to those produced by P. shanxiensis. The fungi of the genus Ustilago are thus likely to be potential producers of MELs as well as the yeasts of the genus Pseudozyma.     

Novel synthesis of poly(methyl methacrylate) brush encapsulated silica particles

Silica (SiO₂)‐crosslinked polystyrene (PS) particles possessing photofunctional N,N‐diethyldithiocarbamate (DC) groups on their surface were prepared by the free‐radical emulsion copolymerization of a mixture of SiO₂ (diameter = 20 nm), styrene, divinyl benzene, 4‐vinylbenzyl N,N‐diethyldithiocarbamate (VBDC), and 2‐hydroxyethyl methacrylate with a radical initiator under UV irradiation. In this copolymerization, the inimer VBDC had the formation of a hyperbranched structure by a living radical mechanism. The particle sizes of such core–shell structures [number‐average particle diameter (D_n) = 35–40 nm] were controlled by the variation of the feed amounts of the monomers and surfactant, or emulsion system. The size distributions were relatively narrow (weight‐average particle diameter/D_n ≈ 1.05). These particles had DC groups on their surface. Subsequently, poly(methyl methacrylate) brush encapsulated SiO₂ particles were synthesized by the grafting from a photoinduced atom transfer radical polymerization approach of methyl methacrylate initiated by SiO₂‐crosslinked PS particles as a macroinitiator. © 2008 Wiley Periodicals, Inc. J Appl Polym Sci, 2008     

Molecular dynamics simulation of microcrystalline Si deposition processes by silane plasmas

Molecular dynamics (MD) simulations have been performed to examine enhanced surface diffusion of Si adatoms during silane(SiH₄)-based plasma enhanced chemical vapor deposition (PECVD) processes. Such high surface diffusion, if it actually takes place, has been known to account for the growth of microcrystalline silicon(μc-Si) in the PECVD process. Focused in the present study is the motion of a silicon (Si) adatom on a hydrogenated Si surface and the surface diffusion coefficient of Si adatoms on the fully hydrogenated (111) Si surface at 600 K was evaluated from MD simulations. The obtained diffusion coefficient is much larger than those of typical clean Si surfaces known in the literature. The interatomic potential functions for Si-H systems used for the simulations, which we have developed for this study based on ab initio calculations of the interatomic energies, are also presented.     

New type of pressurized cultivation method providing oxygen for piezotolerant yeast

For efficient oxygen supply to pressurized culture, we developed a method using a highly pressurized membrane reactor with an air-saturated medium circulation system. The new method increased the cell growth of aerobic yeast approximately 20 folds larger than that in the case of using a conventional method.     

Gallic acid oxidizes Met residues in peptides released from bovine β-lactoglobulin by in vitro digestion

Phenolic compounds (PCs) are frequently present in foods. However, little is known about the effect of PCs on enzymatic digestion process of food proteins and their products. In this study, the effect of gallic acid (GA) on in vitro digestion of β-lactoglobulin (β-LG) was investigated as a model system for analysis of the interaction between PCs and food proteins. GA showed no effect on the initial rate of β-LG digestion. However, after 1.5 h of digestion, the observed degree of hydrolysis of β-LG was lower in the presence than in the absence of GA. The peptides released from β-LG were characterized by LC/IT-TOF-MS and thirty peptides were identified. In particular, four new peaks were obtained following in vitro digestion of β-LG in the presence of GA. Met(7), Met(24) and Met(145) in the peptides corresponding to these peaks were oxidized to methionine sulfoxide residues.     

Microstructural degradation mechanisms during creep in strength enhanced high Cr ferritic steels and their evaluation by hardness measurement

There are two creep regions with different creep characteristics: short-term creep region “H”, where precipitates and subgrains are thermally stable, and long-term creep region “L”, where thermal coarsening of precipitates and subgrains appear. In region “H”, the normalized subgrain size (λ-λ₀)/(λ^∗-λ₀) has a linear relation with creep strain and its slope is 10ε⁻¹. But, region L is the time range in which the static recovery and the strain-induced recovery progress simultaneously. In this region, the static recovery accelerates the strain-induced recovery, and subgrain size is larger than that line which neglects the contribution of the static recovery. In region “L”, the Δλ/Δλ^∗-strain present a linear relation with a slope 35ε⁻¹. There is a linear relation between hardness and subgrain size. Hardness drop, H₀ − H, as a function of Larson-Miller parameter can be a good measure method for assessment of hardness drop and consequently degradation of microstructure. Hardness drop shows an identical slope in creep region “H”, whereas hardness drop due to thermal aging and creep in region “L” show together a similar slope. In region “H”, degradation of microstructure is mainly due to recovery of subgrains controlled by creep plastic deformation, and precipitates do not have a major role. However, in creep region “L”, there are three degradation mechanisms that accelerate creep failure; (1) strain-induced recovery of subgrains due to creep plastic deformation, (2) static-recovery of subgrains and precipitates and (3) strain-induced coarsening of precipitates due to the appearance of static-recovery.     

Beneficial Effects of Supplementation of the Rare Sugar “D‐allulose” Against Hepatic Steatosis and Severe Obesity in Lepob/Lepob Mice

A rare sugar, D‐allulose (also called D‐psicose), has recently been applied as a food supplement in view of controlling diabetes and obesity in Japan. D‐allulose has been proven to have unique effects against hyperglycemia and hyperlipidemia in a number of studies using several species of rats and mice. However, the antiobesity effects of D‐allulose have not yet been assessed in Lep^ob/Lep^ob (ob/ob) mice. Therefore, this study explored the dietary supplemental effects of this sugar in leptin‐deficient ob/ob mice. Consequently, the subchronic ingestion of D‐allulose in ob/ob mice for 15 wk significantly decreased the body and liver weights, and the loss of body weight was involved in the reduction of the total fat mass, including abdominal visceral fat, and not fat‐free body mass, including muscle. Furthermore, D‐allulose improved hepatic steatosis, as evaluated using hepatic histological studies and MRI. In the normal mice, none of these parameters were influenced by the single or long‐term ingestion of D‐allulose. These results indicate that dietary supplementation of D‐allulose especially influences postprandial hyperglycemia and obesity‐related hepatic steatosis, without exercise therapy or dietary restriction. Therefore, D‐allulose may be useful as a supplement for preventing and improving obesity and obesity‐related disorders.