The use of albumin solid dispersion to enhance the solubility of unionizable drugs.

In this study, solid dispersions of prednisolone (PRD) and bovine serum albumin (BSA) were prepared by spray drying and freeze drying methods using a PRD:BSA solution [20:1 molar ratio (MR)]. PRD-BSA dispersed mixtures were characterized by scanning electron microscopy (SEM), and powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). PRD-BSA physical and dispersed mixtures showed significantly higher solubility in water than that of unprocessed drug. Enhancement factor of six was obtained in both physical mixture and solid dispersion solubility studies. In-vitro dissolution and release studies under physiological conditions showed an immediate release of PRD from the solid dispersions, with almost 90% of the drug dissolved in the first 10 min. PRD was immediately released from BSA binding complex. This study demonstrates the potential for the use of BSA to enhance the solubility and dissolution rate, hence bioavailability, of the unionizable drugs.

Efficient removal of antibiotics from water by highly crosslinked metal-alginate particles: Preparation, isotherms, kinetics, and microbiological assay.

Traces of antibiotics reaching aquatic environment lead to the emergence of antimicrobial resistance (AMR). The efficient removal of antibiotics (ATBs) traces from wastewater is essential to tackle the AMR. In this study, a novel solid-state crosslinking method of alginate (ALG) was developed and applied to specifically remove ATBs from water. A wide range of crosslinkers (Ca2+, Zn2+, Cu2+, Ni2+, Fe3+ and Al3+) was used and the crosslinking nature, density, and distribution were evidenced by FTIR, ICP-MS, and SEM-EDS. Compared with ionotropic gelation, the novel solid-state crosslinking method proved superior in term of ease of production, high crosslinking degree, and ATBs removal capacity. Fe-ALG and Zn-ALG showed high removal capacity of ciprofloxacin (356.5 mg/g and 928.6 mg/g) and doxycycline (90 mg/g and 690 mg/g), however, they were less effective toward amoxicillin (11.5 mg/g and 6 mg/g). Removal isotherms and kinetics followed type I and pseudo-second order suggesting a chemisorption removal mechanism. Fe-ALG was successfully regenerated with no loss in ATB removal capacity. The microbiological assay showed significant reductions of antibacterial activities after ATBs removal from water. Overall, metal-ALG systems obtained by solid-state crosslinking are promising for ATBs removal from wastewater giving the ease of production, high efficiency, regenerability, and scalability potential.

The effects of some components on the electrodeposition process used for solar cell applications.

The study has described through the extrapolation method the roles of those precursors' ions as main substances accompanying the progress of electroplating processes that have been used mainly in the deposition of semiconductor thin film and in the fabrication of solar cells. The role of some materials as primary salts have been compared to each other according to their structures, and through the extrapolation method the atomic structures of the metals included in those salts have been reviewed in 3D forms, investigated and compared. The nuances, on the other hand, cannot be denied. However, the study has reached a plausible point of comparison to substantiate the pieces of evidence of these ions' role in the aqueous solitons. Definitely, the aim is to build up the ultimate steps to finally disclose the essential role of some inorganic or organic compounds in the deposition solution, claiming a step ahead for particular purposes about some elements in the periodic table. Basically, the study cannot rebuke that the available data play an innate part in this study and the next investigating steps in the future. This attempt has somehow illustrated the role of sulfate, nitrate and chloride as accompanying ions in the major salts that have been used to get the desired results in solar cells fabrications. Also, the study has confirmed the basics of mechanisms in which those ions could be compared to each other. For instance, sulfate, nitrate and chloride ions can compare the final results of some metals electrodeposition according to the positions of those metals in the periodic table when fabricating the solar cells. The thickness or the atomic composition of Cu and Zn deposits can be increased at considerably higher voltages starting from IB to IIB columns, whilst for Ga and In deposits, they can be increased starting from the top to the bottom of IIIA column.

Selective radical depolymerization of cellulose to glucose induced by high frequency ultrasound.

The depolymerization of cellulose to glucose is a challenging reaction and often constitutes a scientific obstacle in the synthesis of downstream bio-based products. Here, we show that cellulose can be selectively depolymerized to glucose by ultrasonic irradiation in water at a high frequency (525 kHz). The concept of this work is based on the generation of H˙ and ˙OH radicals, formed by homolytic dissociation of water inside the cavitation bubbles, which induce the cleavage of the glycosidic bonds. The transfer of radicals on the cellulose particle surfaces prevents the side degradation of released glucose into the bulk solution, allowing maintaining the selectivity to glucose close to 100%. This work is distinguished from previous technologies in that (i) no catalyst is needed, (ii) no external source of heating is required, and (iii) the complete depolymerization of cellulose is achieved in a selective fashion. The addition of specific radical scavengers coupled to different gaseous atmospheres and ˙OH radical dosimetry experiments suggested that H˙ radicals are more likely to be responsible for the depolymerisation of cellulose.

Potential Use of the Maillard Reaction for Pharmaceutical Applications: Gastric and Intestinal Controlled Release Alginate-Albumin Beads.

In this study, bovine serum albumin (BSA) and alginate (ALG) conjugates were synthesized by the Maillard reaction in order to evaluate their potential to develop controlled release drug delivery systems. The progress of the Maillard reaction was evidenced using ultraviolet (UV) absorbance, determination of BSA remaining free amino groups, and sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE). BSA-ALG conjugates possessed enhanced and tunable viscosity, foamability and foam stability. Foam generated from BSA-ALG conjugate solution was used to prepare floating gastroretentive calcium ALG beads. Unlike traditional ALG beads, BSA-ALG foam beads were able to float and sustain the ciprofloxacin (CIP) release in gastric medium. Interestingly, intestinal beads made of ALG, BSA-ALG physical mixture and BSA-ALG conjugate resulted in different release rates and orders of indomethacin (IND) in simulated intestinal fluids; while beads based on a physical mixture of BSA-ALG resulted in a first order sustained release profile, both systems based on ALG and BSA-ALG conjugate displayed zero order sustained release profiles with IND being released at a slower rate from the conjugate beads.

Mechanocatalytic Depolymerization of Cellulose With Perfluorinated Sulfonic Acid Ionomers.

Here, we investigated that the mechanocatalytic depolymerization of cellulose in the presence of Aquivion, a sulfonated perfluorinated ionomer. Under optimized conditions, yields of water soluble sugars of 90-97% were obtained using Aquivion PW98 and PW66, respectively, as a solid acid catalyst. The detailed characterization of the water soluble fraction revealed (i) the selective formation of oligosaccharides with a DP up to 11 and (ii) that depolymerization and reversion reactions concomitantly occurred during the mechanocatalytic process, although the first largely predominated. More importantly, we discussed on the critical role of water contained in Aquivion and cellulose on the efficiency of the mechanocatalytic process.

Selectivity enhancement of silica-supported sulfonic acid catalysts in water by coating of ionic liquid.

Coating of silica-supported sulfonic acid catalysts with hydrophobic ionic liquid leads to a significant improvement of catalyst selectivity. Many organic reactions, including Prins cyclization, cycloaddition of epoxide to aldehyde, and dehydrative etherification of secondary benzyl alcohols, proceed well in formalin or pure water. In particular, tandem dehydration/Prins cyclization reactions of tertiary and secondary alcohols with formaldehyde were developed for the first time.

Significant enhancement on selectivity in silica supported sulfonic acids catalyzed reactions.

Thanks to strong hydrophilic interactions between reaction products and the catalyst surface, mesoporous silica supported sulfonic sites were found to be much more selective than homogeneous and common solid acid catalysts.

Conversion of Cellulose into Amphiphilic Alkyl Glycosides Catalyzed by Aquivion, a Perfluorosulfonic Acid Polymer.

The perfluorosulfonic acid (PFSA) Aquivion PW98 is an amphiphilic solid superacid which is shown to catalyze the conversion of cellulose into amphiphilic alkyl glycosides (AAGs) in 85 % yield (with 97 % selectivity). The process involves a mechanocatalytic depolymerization of cellulose followed by a direct glycosylation with n-dodecanol. In comparison to H2 SO4 and solid acid catalysts commonly employed in cellulose processing, Aquivion PFSA PW98 is not only recyclable but also exhibits superior catalytic performances in terms of yield, selectivity, and reactor productivity.

Selective and Catalyst-free Oxidation of D-Glucose to D-Glucuronic acid induced by High-Frequency Ultrasound.

This systematic experimental investigation reveals that high-frequency ultrasound irradiation (550 kHz) induced oxidation of D-glucose to glucuronic acid in excellent yield without assistance of any (bio)catalyst. Oxidation is induced thanks to the in situ production of radical species in water. Experiments show that the dissolved gases play an important role in governing the nature of generated radical species and thus the selectivity for glucuronic acid. Importantly, this process yields glucuronic acid instead of glucuronate salt typically obtained via conventional (bio)catalyst routes, which is of huge interest in respect of downstream processing. Investigations using disaccharides revealed that radicals generated by high frequency ultrasound were also capable of promoting tandem hydrolysis/oxidation reactions.

Determination of optimal conditions for electrodeposition of Tin(II) in the presence of Alizarin Red S.

A detailed physicochemical properties of aqueous solutions of alizarin red S - tin (II) chloride, has been thoroughly investigated by extensively exploring the effect of pH, concentration and temperature on the optimal conditions for the formation of tin (II)-alizarin red S (ARS-Sn II) complex. UV-Vis spectra, electrical conductivity and pH method were also used to characterize the final product. The stoichiometry of the reaction complex formation was determined via different referential methods. It was observed that, the reaction complex was formed when the concentrations were smaller than a certain limit (10-5 M). Adjusting the pH of the reaction (typically from 3.7 to 6.0) also resulted in the formation of the complex. The formed complex was highly stable in dark conditions (absence of sunlight) and at ambient temperature. Without the use of additives and by employing the investigated optimal conditions (i.e. pH: 5.0, i: 6 mA/cm2, t: 5 min, C: 0.1 M, d: 1.273 × 10-4 cm), electrodeposition of tin (II) was demonstrated to be successful.

Effect of non-cross-linked calcium on characteristics, swelling behaviour, drug release and mucoadhesiveness of calcium alginate beads.

In this study, ibuprofen-loaded calcium alginate beads (CABs) with varying amounts of non-cross-linked calcium (NCL-Ca) were prepared using different washing methods. The influence of NCL-Ca on beads properties was investigated. Increasing the number or duration of washes led to significant decreases in the amount of NCL-Ca whereas the impact of the volume of washes was not significant. Approximately 70% of the initial amount of Ca(2+) was NCL-Ca which was removable by washing while only 30% was cross-linked (CL-Ca). Ca(2+) release from the CABs was bimodal; NCL-Ca was burst-released followed by a slower release of CL-Ca. Washing methods and the amount of NCL-Ca had significant influences on the encapsulation efficiency, beads weight, beads swelling, drug release profile and the mucoadhesiveness of CABs. This study highlighted the importance of washing methods and the amount of NCL-Ca to establish CABs properties and understand their behaviour in the simulated intestinal fluids (SIFs).

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin.

The aim of this study was to investigate the use of bovine serum albumin (BSA) as a solubility enhancer for indometacin (IND) as a model drug. IND-BSA solid dispersions were prepared by both spray drying and freeze drying techniques using IND:BSA solution (20:1 Molar Ratio (MR)) and IND:BSA suspension (100:1 MR). The solid state of IND in solid dispersions was characterised by SEM, DSC and XRD. The aqueous solubility of IND in the presence of increased amounts of BSA was evaluated. Additionally, IND dissolution and release profiles were evaluated. IND in solid dispersions with BSA showed significantly higher solubility in water than that of the physical mixture of both. Enhancement factors of 24,000 and 100,000 were obtained for the solid dispersion formulated in 20:1 MR and 100:1 MR, respectively. Dissolution studies in-vitro indicated a significant increase in the dissolution rate of IND from solid dispersions compared to that of the free drug, with almost 95% of the drug dissolved in the first 5min. Furthermore, an immediate release of IND from BSA solid dispersions was shown. The potential use of albumin as solubility enhancer for poorly soluble drugs, particularly, for immediate release volume-limited dosage forms is reported.

Sulfonic acid functionalized crystal-like mesoporous benzene-silica as a remarkable water-tolerant catalyst.

Here we report that sulfonated crystal-like benzene-silica is much more robust and active than conventionally used periodic mesoporous silica for catalyzing aqueous organic reactions.