A low-cost ultrasonic spray dryer to produce spherical microparticles from polymeric matrices

The spray-drying technique has been widely used for drying heat-sensitive foods, pharmaceuticals, and other substances, because it leads to rapid solvent evaporation from droplets. This method involves the transformation of a feed from a fluid state into a dried particulate, by spraying the feed into a hot medium. Despite being most often considered a dehydration process, spray drying can also be used as an encapsulation method. Therefore, this work proposes the use of a simple and low-cost ultrasonic spray dryer system to produce spherical microparticles. This equipment was successfully applied to the preparation of dextrin microspheres on a laboratory scale and for academic purposes.

Nanopartículas de lipídios sólidos: métodos clássicos de produção laboratorial

Solid lipid nanoparticles have been extensively investigated as drug delivery systems. These colloidal systems have major advantages compared to others more traditional. Reported advantages include sustained release, ability to solubilize lipophilic drugs, increased physical and chemical stability of labile molecules, decreased unwanted side-effects showing lower toxicity, and scale up facilities. This paper aims at reviewing the traditional methods of solid lipid nanoparticles production, such as fusion-emulsification (hot and cold), solvent evaporation-emulsification and microemulsion, dealing with the main technological parameters that influence the quality properties of solid lipid nanoparticles.

Characterization and in vitro release of cyclosporine-A from poly(D,L-lactide-co-glycolide implants obtained by solvent/extraction evaporation

Cyclosporine-A-loaded PLGA implants were developed intended for ocular route. Implants were prepared using solvent extraction/evaporation technique followed by casting of the cake into rods in a heated surface. XRD patterns showed that cyclosporine-A was completely incorporated into PLGA. FTIR and DSC results indicated alterations on drug molecular conformation aiming to reach the most stable thermodynamic conformation at polymer/drug interface. Implants provided controlled/sustained in vitro release of the drug. During the first 7 weeks, the drug release was controlled by the diffusion of the cyclosporine-A; and between 7-23 week period, the drug diffusion and degradation of PLGA controlled the drug release.

Compuestos volátiles libres y enlazados glicosídicamente en la pulpa de la uva Caimarona (Pourouma cecropiifolia Mart.)

Los componentes volátiles presentes en la pulpa de la uva Caimarona se estudiaron mediante GC-MS. Éstos se extrajeron por tres técnicas: evaporación del aroma asistida con solvente (Solvent Assisted Flavour Evaporation SAFE), extracción continua líquido-líquido (LL) y destilación por arrastre con vapor-extracción simultanea con solvente orgánico (DES). En general los componentes volátiles predominantes en la pulpa fueron alcoholes alifáticos y terpénicos. Las notas olfativas del extracto SAFE fueron descritas como floral tenue y verde herbal similares a las exhibidas por la pulpa fresca. Este extracto presentó como componentes mayoritarios linalol 1,2-propanodiol y salicilato de metilo. En contraste, el extracto LL presentó notas que recuerdan la uva pasa y el vino moscatel y sus componentes mayoritarios fueron el ácido acético, el salicilato de metilo y el 2,6-dimetil-2(Z),7-octadien-1,6-diol. El extracto DES fue descrito con notas fresca, floral, cereal y amargo y está constituido por un reducido número de componentes mostrando el efecto negativo de la temperatura en la extracción; sus componentes mayoritarios fueron 1,2-propanodiol, linalol y salicilato de metilo. Adicionalmente, los componentes volátiles mayoritarios liberados por hidrólisis enzimática (Rohapect D5L) de los glicósidos de la pulpa fueron ácido acético, ácido benzoico y vainillina. Cabe destacar que aunque el linalol no se encontró entre las agliconas volátiles, se detectaron los dioles biogenéticamente relacionados: 3,7-dimetil-1,5-octadien-3,7-diol y los isómeros E y Z del 2,6-dimetil-2,7-octadien-1,6-diol.

Envelhecimento das aguardentes

1 - Colour, by itself, does not constitute a solid ground for judging of the age of a brandy because the more or less pronounced colour it acquires through aging can also be obtained by the addition of oack essence to newly distilled brandy. 2 - Urder the same conditions, colour intensity of a brandy wiU depend upon the nature of the wood and the condition of the storage. 3 - In accordance with the experimental results obtained by the present writers it rests no doubt that fermentation facility ferment resistence, produce and quality of the brendy all are factors depending upon the variety of the sugar cane. In addition, the authors presume that the variety of sugar cane has also influence upon the alteration of composition of the brandy submitted to aging. 4 - All aging phenomena of the brandy are accompanied by volume decreasing, what happens in a slow and continuous manner depending upon storage and environment conditions 5 - During brandy aging the alcoholic degree is greatly af- fected by evaporation, increasing or decreasing in accordance to the hygrometric state of the air and the teriperature in the place where the tuns are stored. 6 - The specific weight of the brandy is inversely proportio- nal to its alcoholic degree, but directly proportional to the extracts since the latter indicates the amount of dissolved residues. 7 - Brandy which shows high specific weight together with high alcoholic degree cannot be considered as aged. It may, however, be takens for brandy artificially coloved in order to conceal its actual age. 8 - The amount of extracts increases with aging, since it is the result of the solvent action of the brandy upon the soluble extractive substances of the wood. Notwithstanding that the extract, considered alone, has no value in determining the age of a brandy, since nothing easier is ohan to nake it change artificially. 9 -During aging the brandy get acidity in physiological as well as in physical way, but never by the action of microorganisms. 10 - The estturs produced during aging by the action of acids upon alcohols are the mean factors of the savour (bouquet) of a brandy and therefore every thing shall be done tor fhr estherification of a preserved brandy being not limited. 11 - Aeration increases esther formation, reduces the aging- time and turn better the taste qualities of the brandy. 12 - Due to the great proportion of high alcohols ordinarily found in the brandy, their analytical discrimination will be greatly important. 13 - The high alcohols are not responsable for the disastrous consequences of the alcoholism, but the high percentage of uthyl alcohol present in the brandy. 14 - The aldehydes appear always in high rate in the brazilian brandys in consequence of some intermediary products of the oxydation of the alcohols being left in the brandys during aging. 15 - The age has little or no influence on the quantity of phurphurol present in a brandy whose amount varies greatly the manner in which the wines to be distilled are treated. Wines centrifugalized or filtered before distillation always give rise to brandys poorer in phurphurol as compared with those distilled without these treatments. 16 - Though greatly variable, brandys of good qualities generally show a high residues coefficient, never under 200 mmg 17 - Lusson - Rocques oxydation coefficient cannot be indis- criminately applied to any brandy class, being, on the contrary, specifically destined to cognacs.

Antibacterial potentiality of Argemone mexicana solvent extracts against some pathogenic bacteria

The sensitivity of two Gram positive (Staphylococcus aureus and Bacillus subtilis) and two Gram negative (Escherichia coli and Pseudomonas aeruginosa) pathogenic multi-drug resistant bacteria was tested against the crude extracts (cold aqueous, hot aqueous, and methanol extracts) of leaves and seeds of Argemone mexicana L. (Papaveraceae) by agar well diffusion method. Though all the extracts were found effective, yet the methanol extract showed maximum inhibition against the test microorganisms followed by hot aqueous extract and cold aqueous extract.

NMR investigation and theoretical calculations of the effect of solvent on the conformational analysis of 4',7-di-hydroxy-8-prenylflavan

The NMR conformational study of 4',7-di-hydroxy-8-prenylflavan 1 was carried out in acetone-d6, DMSO-d6 and CDCl3 which enabled the proposition of three conformations, namely 1a, 1b and 1c, differing in the position of the prenyl group. Geometry optimizations performed using AM1 method showed that 1a (deltaHf = -86.2 kcal/mol) is as stable as 1b (deltaHf = -85.1 kcal/mol) and 1c (deltaHf = -85.4 kcal/mol). When the solvent was included, the calculations showed that the solute-solvent interactions could be explained either in the light of the electronic intermolecular delocalization or the electrostatic character between solute and solvent. Theoretical calculations (HF/6-31G*, deltaFT/BLYP/6-31G*, and deltaFT/B3LYP/6-31G*) showed that the combination of these types of interactions present in each solute-solvent system, dependent on the chemical properties of the solvent, lead to different spatial arrangements of the prenyl group, which in turn determined the conformation of 1.

Estudo das propriedades e biodegradabilidade de blendas de poliéster/amido submetidas ao ataque microbiano

This work deals with the biodegradation of blends of poly(beta-hydroxybutyrate)/starch and poly(beta-hydroxybutyrate-co-hydroxyvalerate)/starch. The blends were obtained by evaporation of the solvent in the mixture of the polymers in chloroform. Tests were carried out in presence of micro-organisms which acted as biodegradation agents. The blends were consumed as carbon substrate and the production of CO2 was evaluated in the process. In addition, the polyesters' mechanical properties were reduced by the incorporation of starch in its structure. (¹H) NMR and infrared spectroscopy detected some characteristic polyester degradation groups in the polyesters' chemical structure, thus confirming the alteration suffered by it.

Singlet oxygen reactivity in water-rich solvent mixtures

The 3-methylindole (3MI) oxygenation sensitized by psoralen (PSO) has been investigated in 100%, 20% and 5% O2-saturated water/dioxane (H2O/Dx) mixtures. The lowering of the ¹O2* chemical rate when water (k chem∆3MI = 1.4 × 109 M-1 s-1) is replaced by deuterated water (k chem∆3MI = 1.9 × 108 M-1 s-1) suggests that hydrogen abstraction is involved in the rate determining step. A high dependence of the chemical rate constant on water concentration in H2O/Dx mixtures was found showing that water molecules are absolutely essential for the success of the 3MI substrate oxidation by ¹O2* in water-rich solvent mixtures.

Efficient synthesis of sulfonamide derivatives on solid supports catalyzed using solvent-free and microwave-assisted methods

In this work we report the synthesis of sulfonamide derivatives using a conventional procedure and with solid supports, such as silica gel, florisil, alumina, 4Å molecular sieves, montmorillonite KSF, and montmorillonite K10 using solvent-free and microwave-assisted methods. Our results show that solid supports have a catalytic activity in the formation of sulfonamide derivatives. We found that florisil, montmorillonite KSF, and K10 could be used as inexpensive alternative catalysts that are easily separated from the reaction media. Additionally, solvent-free and microwave-assisted methods were more efficient in reducing reaction time and in increasing yield.

Encapsulation of naproxen in nanostructured system: structural characterization and in vitro release studies

Nanoparticles were produced by solvent emulsification evaporation method with the following characteristics: nanometric size (238 ± 3 nm), narrow polydispersity index (0.11), negative zeta potential (-15.1 mV), good yield of the process (73 ± 1.5%), excellent encapsulation efficiency (81.3 ± 4.2%) and spherical shape. X-rays diffraction demonstrated the loss of drug crystallinity after encapsulation; however, the profile of the diffractograms of the poly-ε-caprolactone (PCL) nanoparticles was kept. Differential scanning calorimetry thermograms, correspondingly, exhibited the loss of drug melting peak and the increasing of the melting point of the PCL nanoparticles, evidencing an interaction drug-polymer. Naproxen release was low and sustained obeying the Higuchi´s kinetic. The results show that nanoparticles are promising sustained release system to the naproxen.

Synthesis of quinoxaline 1,4-di-N-oxide derivatives on solid support using room temperature and microwave-assisted solvent-free procedures

We describe the synthesis of 12 new ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives on solid supports with room temperature and microwave-assisted solvent-free procedures. Results show that solid supports have good catalytic activity in the formation of quinoxaline 1,4-di-N-oxide derivatives. We found that florisil and montmorillonite KSF and K10 could be used as new, easily available, inexpensive alternatives of catalysts. Additionally, room temperature and microwave-irradiation solvent-free synthesis was more efficient than a conventional procedure (Beirut reaction), reducing reaction time and increasing yield.

Optimization of solvent mixtures for extraction from bark of Schinus terebinthifolius by a statistical mixture-design technique and development of a UV-Vis spectrophotometric method for analysis of total polyphenols in the extract

A statistical mixture-design technique was used to study the effects of different solvents and their mixtures on the yield, total polyphenol content, and antioxidant capacity of the crude extracts from the bark of Schinus terebinthifolius Raddi (Anacardiaceae). The experimental results and their response-surface models showed that ternary mixtures with equal portions of all the three solvents (water, ethanol and acetone) were better than the binary mixtures in generating crude extracts with the highest yield (22.04 ± 0.48%), total polyphenol content (29.39 ± 0.39%), and antioxidant capacity (6.38 ± 0.21). An analytical method was developed and validated for the determination of total polyphenols in the extracts. Optimal conditions for the various parameters in this analytical method, namely, the time for the chromophoric reaction to stabilize, wavelength of the absorption maxima to be monitored, the reference standard and the concentration of sodium carbonate were determined to be 5 min, 780 nm, pyrogallol, and 14.06% w v-1, respectively. UV-Vis spectrophotometric monitoring of the reaction under these conditions proved the method to be linear, specific, precise, accurate, reproducible, robust, and easy to perform.

Test of a microlysimeter for measurement of soil evaporation

Quantifying soil evaporation is required on studies of soil water balance and applications aiming to improve water use efficiency by crops. The performance of a microlysimeter (ML) to measure soil evaporation under irrigation and non-irrigation was evaluated. The MLs were constructed using PVC tubes, with dimensions of 100 mm inner diameter, 150 mm depth and 2.5 mm wall thickness. Four MLs were uniformly distributed on the soil surface of two weighing lysimeters conducted under bare soil, previously installed at Iapar, in Londrina, PR, Brazil. The lysimeters had 1.4 m width, 1.9 m length and 1.3 m depth and were conducted with and without irrigation. Evaporation measurements by MLs (E ML) were compared with measurements by lysimeters (E L) during four different periods in the year. Differences between E ML and E L were small either for low or high atmospheric demand and also for either irrigated or non-irrigated conditions, which indicates that the ML tested here is suitable for measurement of soil evaporation.