Electrospun nanofiber-based niflumic acid capsules with superior physicochemical properties

The aim of this study was to assess whether nanofibrous drug mats have potential as delivery systems for poorly water-soluble drugs. Amorphous nanofiber mats from a model poorly water-soluble active pharmaceutical ingredient (API), niflumic acid, together with the polymer excipient, polyvinyl pyrrolidine, were prepared by nozzle-free electrospinning. This technique offers a scalable way for drug formulation, and by increasing the surface area of the drug, the dissolution rate and therefore bioavailability of the API can be improved. In this study, both the amount of the dissolved active ingredient and the dissolution kinetics has been improved significantly when the nanofibrous mats were used in the drug formulation. A 15-fold increase in the dissolved amount of the produced amorphous niflumic acid nanofiber was observed compared to the dissolved amount of the raw drug within the first 15 minutes. Capsule formulation was made by mixing the electrospun nanofibers with a microcrystalline cellulose filler agent. When comparing the dissolution rate of the capsule formulation on the market with the nanofibrous capsules, a 14-fold increase was observed in the dissolved drug amount within the first 15 minutes

Anomalous codeposition of cobalt and ruthenium from chloride-sulfate baths

Codeposition of Ru and Co was studied at room temperature and at 50oC with various Ru3+ and Co2+ concentrations in the electrolyte. The codeposition of Co and Ru proved to be anomalous since no pure Ru could be obtained in the presence of Co2+ in the electrolyte, but a significant Co incorporation into the deposit was detected at potentials where the deposition of pure Co was not possible. The composition of the deposits varied monotonously with the change of the concentration ratio of Co2+ and Ru3+. The deposition of Ru was much hindered and the current efficiency was a few percent only when the molar fraction of Co in the deposit was low. Continuous deposits could be obtained only when the molar fraction of Co in the deposit was at least 40 at.%. The deposit morphology was related to the molar fraction of Co in the deposit. The X-ray diffractograms are in conformity with a hexagonal close-packed alloy and indicate the formation of nanocrystalline deposits. Two-pulse plating did not lead to a multilayer but to a Co-rich alloy. Magnetoresistance of the samples decreased with increasing Ru content

Sferična kristalizacija zdravilnih učinkovin

Spherical crystallization of drugs is the process of obtaining larger particles by agglomeration during crystallization. The most common techniques used to obtain such particles are spherical agglomeration and quasi-emulsion solvent diffusion. Ammonia diffusion systems and crystallo-co-agglomeration are extensions of these techniques. By controlling process parameters during crystallization, such as temperature, stirring rate, type and amount of solvents, or excipient selection, it is possible to control the formation of agglomerates and obtain spherical particles of the desired size, porosity, or hardness. Researchers have reported that the particles produced have improved micromeritic, physical, and mechanical properties, which make them suitable for direct compression. In some cases, when additional excipients are incorporated during spherical crystallization, biopharmaceutical parameters including the bioavailability of drugs can also be tailored.Sferična kristalizacija je postopek izdelave večjih delcev z aglomeracijo manjših med samo kristalizacijo. Najpogosteje uporabljeni tehniki za izdelavo takšnih delcev sta sferična aglomeracija in kvaziemulzija z difuzijo topila. Sistem z difuzijo amoniaka in kristalo-ko-aglomeracija sta razširitvi teh dveh metod. Z nadzorovanjem procesnih parametrov med kristalizacijo, kot sta temperatura in hitrost mešanja, z izbiro lastnosti in množine topil ter z izbiro pomožnih snovi, lahko vplivamo na nastanek aglomeratov in izdelamo sferične delce želenih velikosti, primerne poroznosti ali trdote. Raziskovalci poročajo, da imajo izdelani delci izboljšane pretočne lastnosti, izboljšane druge fizikalne in mehanske lastnosti zaradi česar so primerni za direktno tabletiranje. V nekaterih primerih lahko ob vgradnji ustreznih pomožnih snovi, ki jih dodamo med procesom sferične kristalizacije, izboljšamo tudi biofarmacevtske lastnosti zdravilnih učinkovin vključno s povečanjem biološke uporabnosti

Effect of polymers for aerolization properties of mannitol-based microcomposites containing meloxicam

The aim of this study was to develop respirable microcomposites of meloxicam and adjuvants (different polymers and amino acid) for inhalation as drug delivery systems for local lung therapy. Meloxicam was transformed into microcomposites, i.e. crystals of drug embedded in mannitol and other adjuvants. We focused on the influence of polymers concentration on the physico-chemical properties of the microparticles. The objective was to optimize the aerodynamic parameters of the particles and to achieve the fast release of meloxicam. The size of the meloxicam particles suspended in aqueous mannitol solution containing different additives was reduced by high-pressure homogenization. Dry powders were produced from the microsuspensions by a co-spray-drying technique. Morphological, structural and in vitro dissolution studies were presented. The in vitro aerosol performance was tested by using the multistage Next Generation Impactor. It was found that polyvinyl alcohol and polyvinylpyrrolidone, promoted the presence of individual microcomposites by decreasing the aggregation tendency. L-leucine improved the fine particle fraction content of the samples. The co-spray-dried mannitol-based formulations containing the additives released 90% of the meloxicam by dissolution in 5 min. Aerodynamic assessment showed the fine particle fraction was >53% and the mass median aerodynamic diameter was <3.52 lm. This study indicated that meloxicam micro composites prepared according to the described procedure are suitable for pulmonary local anti-inflammatory and antifibrotic therapy

Effect of High-Pressure Homogenization on the Formulation of Micro- and Nanocrystals Containing Poorly Watersoluble Meloxicam

Specially engineered drug particles can solve solubility and formulation problems, [...

Development of a microparticle-based dry powder inhalation formulation of ciprofloxacin hydrochloride applying the quality by design approach

Keyhaneh Karimi, Edina Pallagi, Piroska Szab&oacute;-R&eacute;v&eacute;sz, Ildik&oacute; Cs&oacute;ka, Rita Ambrus Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged, Hungary Abstract: Pulmonary drug delivery of ciprofloxacin hydrochloride offers effective local antibacterial activity and convenience of easy application. Spray drying is a trustworthy technique for the production of ciprofloxacin hydrochloride microparticles. Quality by design (QbD), an up-to-date regulatory-based quality management method, was used to predict the final quality of the product. According to the QbD-based theoretical preliminary parameter ranking and priority classification, dry powder inhalation formulation tests were successfully performed in practice. When focusing on the critical parameters, the practical development was more effective and was in correlation with our previous findings. Spray drying produced spherical microparticles. The dry powder formulations prepared were examined by particle size analysis, scanning electron microscopy, Fourier-transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry, and in vitro drug release and aerodynamic particle size analyses were also performed. These formulations showed an appropriate particle size ranging between 2 and 4 &micro;m and displayed an enhanced aerosol performance with fine particle fraction up to 80%. Keywords: antibiotic, carrier-free formulation, quality by design, aerodynamic evaluation, dry powder for inhalatio

A Model for Studying Nasal Drug Delivery: RPMI 2650 Human Nasal Epithelial Cell Line

Studies on nasal epithelial models are important to develop vehicles for systemic nasal drug delivery, and also for targeting drugs to brain via the nasal route. [...