Aminolevulinic acid-loaded Witepsol microparticles manufactured using a spray congealing procedure: implications for topical photodynamic therapy

Objectives The aim was to enhance aminolevulinic acid (ALA) stability by incorporation into low-melting microparticles prepared using a spray congealing procedure and to evaluate temperature-triggered release, allowing topical bioavailability following melting at skin temperature.

Comparison of a novel spray congealing procedure with emulsion-based methods for the micro-encapsulation of water-soluble drugs in low melting point triglycerides

The particle size characteristics and encapsulation efficiency of microparticles prepared using triglyceride materials and loaded with two model water-soluble drugs were evaluated. Two emulsification procedures based on o/w and w/o/w methodologies were compared to a novel spray congealing procedure. After extensive modification of both emulsification methods, encapsulation efficiencies of 13.04% tetracycline HCl and 11.27% lidocaine HCl were achievable in a Witepsol (R)-based microparticle. This compares to much improved encapsulation efficiencies close to 100% for the spray congealing method, which was shown to produce spherical particles of similar to 58 mu m. Drug release studies from a Witepsol (R) formulation loaded with lidocaine HCl showed a temperature-dependent release mechanism, which displayed diffusion-controlled kinetics at temperatures similar to 25 degrees C, but exhibited almost immediate release when triggered using temperatures close to that of skin. Therefore, such a system may find application in topical semi-solid formulations, where a temperature-induced burst release is preferred.

Laser-driven quasimonoenergetic proton burst from water spray target

A narrow band proton bursts at energies of 1.6 +/- 0.08 MeV were observed when a water spray consisting of empty set(150 nm)-diameter droplets was irradiated by an ultrashort laser pulse of about 45 fs duration and at an intensity of 5 X 10(19) W/cm(2). The results are explained by a Coulomb explosion of sub-laser-wavelength droplets composed of two ion species. The laser prepulse plays an important role. By pre-evaporation of the droplets, its diameter is reduced so that the main pulse can interact with a smaller droplet, and this remaining bulk can be ionized to high states. In the case of water, the mixture of quite differently charged ions establishes an

MeV negative ion generation from ultra-intense laser interaction with a water spray

MeV negative oxygen ions are obtained from a water spray target irradiated by high intensity (5 x 10(19) W/cm(2)) and ultrashort (50 fs) laser pulses. Generation of negative ions is ascribed to electron-capture processes that the laser-accelerated high-energy positive ion experiences when it interacts with atoms in the spray. This mechanism implies the existence of a large number of MeV neutral oxygen atoms, which is consistent with indirect experimental evidence. (C) 2011 American Institute of Physics. [doi:10.1063/1.3622664]

A comprehensive aerosol spray method for the rapid photocatalytic grid area analysis of semiconductor photocatalyst thin films

Indicator inks, previously shown to be capable of rapidly assessing photocatalytic activity via a novel photo-reductive mechanism, were simply applied via an aerosol spray onto commercially available pieces of Activ (TM) self-cleaning glass. Ink layers could be applied with high evenness of spread, with as little deviation as 5% upon UV-visible spectroscopic assessment of 25 equally distributed positions over a 10 cm x 10 cm glass cut. The inks were comprised of either a resazurin (Rz) or dichloroindophenol (DCIP) redox dye with a glycerol sacrificial electron donor in an aqueous hydroxyethyl cellulose (HEC) polymer media. The photo-reduction reaction under UVA light of a single spot was monitored by UV-vis spectroscopy and digital images attained from a flat-bed scanner in tandem for both inks. The photo-reduction of Rz ink underwent a two-step kinetic process, whereby the blue redox dye was initially reduced to a pink intermediate resorufin (Rf) and subsequently reduced to a bleached form of the dye. In contrast, a simple one-step kinetic process was observed for the reduction of the light blue redox dye DCIP to its bleached intermediates. Changes in red-green-blue colour extracted from digital images of the inks were inversely proportional to the changes seen at corresponding wavelengths via UV-visible absorption spectroscopy and wholly indicative of the reaction kinetics. The photocatalytic activity areas of cuts of Activ (TM) glass, 10 cm x 10 cm in size, were assessed using both Rz and DCIP indicator inks evenly sprayed over the films: firstly using UVA lamp light to activate the underlying Activ (TM) film (1.75 mW cm(-2)) and secondly under solar conditions (2.06 +/- 0.14 mW cm(-2)). The photo-reduction reactions were monitored solely by flat-bed digital scanning. Red-green-blue values of a generated 14 x 14 grid (196 positions) that covered the entire area of each film image were extracted using a Custom-built program entitled RGB Extractor(C). A homogenous degradation over the 196 positions analysed for both Rz (Red colour deviation = 19% UVA, 8% Solar: Green colour deviation = 17% UVA, 12% Solar) and DCIP (Red colour deviation = 22% UVA, 16% Solar) inks was seen in both UVA and solar experiments, demonstrating the consistency of the self-cleaning titania layer on Activ (TM). The method presented provides a good solution for the high-throughput photocatalytic screening of a number of homogenous photocatalytically active materials simultaneously or numerous positions on a single film; both useful in assessing the homogeneity of a film or determining the best combination of reaction components to produce the optimum performance photocatalytic film. (C) 2010 Elsevier B.V. All rights reserved.

Spray Congealed Lipid Microparticles with High Protein Loading: Preparation and Solid State Characterization

The spray-congealing technique, a solvent-free drug encapsulation process, was successfully employed to obtain lipid-based particulate systems with high (10–20% w/w) protein loading. Bovine serum albumin (BSA) was utilised as model protein and three low melting lipids (glyceryl palmitostearate, trimirystin and tristearin) were employed as carriers. BSA-loaded lipid microparticles were characterised in terms of particle size, morphology and drug loading. The results showed that the microparticles exhibited a spherical shape, mean diameter in the range 150–300 µm and an encapsulation efficiency higher than 90%. Possible changes in the protein structure as a result of the manufacturing process was then investigated for the first time using UV spectrophotometry in fourth derivative mode and FT-Raman spectroscopy. The results suggested that the structural integrity of the protein was maintained within the particles. Thermal analysis indicated that the effect of protein on the thermal properties of the carriers could be detected. Spray-congealing could thus be considered a suitable technique to produce highly BSA-loaded microparticles preserving the structure of the protein.

Investigation Into The Effect of Varying L-leucine Concentration on the product characteristics of Spray-dried Liposome Powders

Spray-dried formulations offer an attractive delivery system for administration of drug encapsulated into liposomes to the lung, but can suffer from low encapsulation efficiency and poor aerodynamic properties. In this paper the effect of the concentration of the anti-adherent l-leucine was investigated in tandem with the protectants sucrose and trehalose. Two manufacturing methods were compared in terms of their ability to offer small liposomal size, low polydispersity and high encapsulation of the drug indometacin. Unexpectedly sucrose offered the best protection to the liposomes during the spray drying process, although formulations containing trehalose formed products with the best powder characteristics for pulmonary delivery; high glass transition values, fine powder fraction and yield. It was also found that l-leucine contributed positively to the characteristics of the powders, but that it should be used with care as above the optimum concentration of 0.5% (w/w) the size and polydispersity index increased significantly for both disaccharide formulations. The method of liposome preparation had no effect on the stability or encapsulation efficiency of spray-dried powders containing optimal protectant and anti-adherent. Using l-leucine at concentrations higher than the optimum level caused instability in the reconstituted liposomes.