Calcium polyphosphate coacervates: effects of thermal treatment

The addition of calcium chloride eletrolyte to sodium polyphosphate solutions lead to Calcium polyphosphate coacervates. The effects of a thermal treatment were investigated with the objective to increase the relative stability of the obtained material. Thermogravimetry analysis indicates that coacervates became less hydrophilic and more thermally stable after the thermal treatment. Crystallization was identified through differential scanning calorimetry and X-ray diffraction. Morphological changes were observed after the thermal treatment by scanning electron microscopy. N-2 adsorption-desorption isotherms suggest that both materials, thermally treated or not, display type IV isotherms, low superficial area and mesoporous structure. Stability experiments in solutions at different pH values show that the thermally treated calcium polyphosphate is relatively more stable than the non-treated coacervate.

Production of turmeric oleoresin microcapsules by complex coacervation with gelatin-gum arabic

Turmeric oleoresin is a colorant prepared by solvent extraction of turmeric (Curcuma longa L.). Curcumin, the major pigment present in turmeric, has been described as a potent antioxidant, anti-inflammatory and anticarcinogenic agent. Turmeric pigments are lipid soluble and water insoluble and are sensitive to light, heat, oxygen and pH, which can be overcome by microencapsulation of turmeric oleoresin. The aim of this work was to investigate microencapsulation of turmeric oleoresin by complex coacervation using gelatin and gum Arabic as encapsulants and freeze-drying as the drying method. The coacervation process was studied by varying the concentration of biopolymer solution (2.5, 5.0 and 7.5%) and the core material: total encapsulant ratio (25, 50, 75 and 100%). Microcapsules were evaluated for encapsulation efficiency, morphology, solubility and stability to light. Encapsulation efficiency ranged from 49 to 73% and samples produced with 2.5% of wall material and 100% core: encapsulant ratio showed better stability to light. © 2012 Wiley Periodicals, Inc.

Alginate-chitosan systems: In vitro controlled release of triamcinolone and in vivo gastrointestinal transit

The aim of this study was to develop multiparticulate therapeutic systems of alginate (AL) and chitosan (CS) containing triamcinolone (TC) to colonic drug delivery. Multiparticulate systems of AL-CS, prepared by a complex coacervation/ionotropic gelation method, were characterized for morphological and size aspects, swelling degree, encapsulation content and efficiency, in vitro release profile in different environments simulating the gastrointestinal tract (GIT) and in vivo gastrointestinal transit. The systems showed suitable morphological characteristics with particle diameters of approximately 1.6 mm. In simulated gastric environment, at pH 1.2, the capsules presented low degree of swelling and in vitro release of drug. A higher swelling degree was observed in simulated enteric environment, pH 7.5, followed by erosion. Practically all the drug was released after 6 h of in vitro assay. The in vivo analysis of gastrointestinal transit, carried out in rats, showed that the systems passed practically intact through the stomach and did not show the same profile of swelling observed in the in vitro tests. It was possible to verify the presence of capsules in the colonic region of GIT. The results indicate that AL-CS multiparticulate systems can be used as an adjuvant for the preparation of therapeutic systems to colonic delivery of drugs. (C) 2010 Elsevier Ltd. All rights reserved.

AC Biosusceptometry as a Tool for Monitoring the Gastrointestinal Transit of Multiparticulate Drug Delivery System

Drug delivery systems based on natural polysaccharides, such as chitosan (CS) and pectin (PC), rather than on synthetic polymers, have been widely studied. Some reasons for that are low toxicity and costs and high biodegradability of the formers. A multiparticulate system based on CS and PC was developed in our laboratories, including the addition of an enteric polymer, cellulose acetate phtalate (CAP). Such improvement promoted stronger gastric and enteric resistances, as assessed in vitro, making the systems more selective to enzymatic degradation in the colon. Although in vitro dissolution tests can simulate some properties concerning the gastrointestinal transit (GT), collaborating to characterize the systems behavior in the biological fluids, frequently they do not result in satisfactory in vitro/in vivo correlations. The objective of this work was to follow in vivo the GT of the particles developed by means of AC biosusceptometry (ACB), a non-invasive and of low cost methodology. The particles containing ferrite in powder form were prepared by complex coacervation using an ideal 3:1:1 mass ratio for PC:CS:CAP. The magnetic particles were administered to healthy volunteers by oral route. The GT was monitored by using multi-sensor ACB system and the signal acquisition was performed every IS min until the colonic region was reached. By means of ACB technique, it was possible to acquiring images generated by the magnetic particles within the whole gastrointestinal tract including the colonic region. Variable particles transit times were observed among the volunteers, but without interference on the mapping of the particles until the colonic region. The particles were able to produce magnetic field strong enough to generate signals adequate for mapping the particles. The results suggest that integral particles reached the colon, after they resisted against gastric and enteric media. Studies associating transit time and in vivo drug release are in development in order to confirm the efficiency of the systems.

Spectroscopic studies on glassy Ni(II) and Co(II) polyphosphate coacervates

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Amorphous manganese polyphosphates: preparation, characterization and incorporation of azo dyes

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Influência do pH na estabilidade dos coacervatos de prata como precursores vítreos

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Microspheres of alginate-chitosan containing isoniazid

Isoniazid was encapsulated into microspheres of alginate-chitosan by means of a complex coacervation method in an emulsion system. Since the encapsulation of isoniazid tends to be limited by its hydrophilic characteristics, this study proposes its microencapsulation by adsorption. The particles were prepared in three steps: (1) preparation of a W/O emulsion; (2) phase separation; and (3) adsorption of the drug. The isolated particles were placed in a solution of the drug under stirring to allow adsorption. The morphology and particle size were analysed by scanning electron microscopy (SEM). The isoniazid content was determined by extraction in 1 m phosphate buffer pH 7.5 under stirring for 4 h. Finally, the samples were filtered and analysed in an UV/VIS spectrophotometer at 260 nm. In vitro release tests were carried out in 0.05 m phosphate buffer pH 7.5. The results showed that microspheres of alginate-chitosan obtained were of spherical shape. The emulsion used for microparticle formation allows the preparation of particles with a narrow size distribution. The adsorption observed is probably of chemical nature, i.e. there is an ionic interaction between the drug and the surface of the particles.

Spectroscopic study and local coordination of polyphosphate colloidal systems

The interaction between metaphosphate chains and the metal ions Ca2+ and Eu3+ has been studied in water by Eu3+ luminescence, infrared absorption, and P-31 NMR spectroscopy. Two main families of sites could be identified for the metal ions in the aqueous polyphosphate colloidal systems: (1) cagelike sites provided by the polyphosphate chain and (2) a family which arises following saturation of cagelike sites. Occupation of this second family leads to supramolecular interactions between polyphosphate chains and the consequent destabilization of the colloidal system. In the polyphosphate-Ca2+ system, this destabilization appears as a coacervation process. Equilibrium existing between colloidal species as a function of the compositions could be reasoned based on the spectroscopic measurements. The determination of coordination numbers and the correlation of the results with the observation of coacervates show that Eu3+ luminescence properties can be used to probe in a unique way the coacervation process.

Determination of calcium by atomic absorption spectrophotometry applied to the preparation of alginate:chitosan complexes

Polysaccharicles, as alginate and chitosan, have been used to obtain modified release dosage forms. Alginate, due to its property of building gels during the complex formation with calcium ions, allows the building of capsules containing a core constituted by calcium alginate. This work had for objective to determine the appropriate calcium concentration for the preparation of alginate-chitosan capsules, by means of calcium quantification using atomic absorption spectrophotometry. The methodology of calcium quantification was validated through analysis of the limit of detection, precision, accuracy and recovery of the method. The capsules, containing or not the drug, were prepared by the complex coacervation/ionotropic gelification method. Calcium was quantified after samples mineralization and dilution in lantanium solution. The results showed that the amount of calcium incorporated into the capsules depends on the amount of calcium added to the medium, and this ratio increases until the concentration of 1.5% of initial calcium chloride and above this concentration there is a decrease in the proportion of calcium bonded. It was observed that the proportion of calcium that links to the polymer is inversely proportional to the amount of calcium added. The calcium amount incorporated depends on the concentration of the polymeric dispersions used as well as on the ratio between the two polymers.

Studies on the formation of complex coacervates between chitosan and alginate during microparticles preparation

The formation of complex coacervates between chitosan and alginate was evaluated during microparticles formation. Mass ratio between polyelectrolytes and calcium chloride concentration were determinated by conductimetric analysis and by calcium ions quantification, respectively. Inert microparticles were prepared using a complex coacervation method in W/O emulsion and morphological analyses of microparticles were carried out. This method enabled the production of spherical particles, with slightly rough surface and narrow size distribution with maximal diameter of 10 μm.

Multiparticulate systems of pectin-chitosan: Study of swelling and drug release

The aim of this study was to prepare multiparticulate systems of pectin:chitosan (PC:CS) and to evaluate their swelling ratio and the drug release in different environments. PC:CS particles containing triamcinolone were prepared by a complex coacervation/ionotropic gelation method in aqueous environment. The polymer ratio, the calcium concentration and the contact time of the capsules with chitosan dispersion for particles formation and the structures obtained were analyzed. The systems were characterized in relation to morphology, size, swelling, and drug release behavior. The methodology used allowed the production of spherical particles with narrow range of size distribution. The entrapment efficiency for triamcinolone was 84.31 ± 439. It was observed that the particles present a relatively low swelling ratio in acidic medium and a larger swelling ratio in enteric medium. The release profile was dependent on pH and can be related with the swelling ratio.

Aplicação da equação de Paisson-Boltzmann com condição de contorno para regulação carga-potencial a sistemas polieletrolíticos

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Estudo físico-químico de nanopartículas de DNA com derivado de quitosana contendo grupos fosforilcolina

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Microencapsulação de oleoresina de cúrcuma (curcuma longa l.) em matrizes de gelatina, goma arábica e colágeno hidrolisado

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)