Sistemas para liberação colônica: Uma alternativa para a veiculação de fármacos para efeito local ou sistêmico

Problems related to the systemic administration of drugs, such as biodistribution, difficulty of targeting, necessity of high doses to achieve adequate levels of the drug in specific sites, toxicity, and undesirable side effects have lead to the development of systems able to direct the drug to specific sites in the body. Among the possible organs to the targeting of drugs, the colon can be used for local and systemic therapies. By developing such systems some models have been tested, using pH dependent release, release controlled by enzymatic degradation, time controlled release systems and pressure controlled release systems. This review presents an overview of the colonic release of drugs and the strategies used to achieve such targeting.

Ethylcelullose microspheres containing sodium diclofenac: Development and characterization

The objective of the present study was the development and characterization of ethylcellulose microspheres containing diclofenac and the determination of the in vitro drug release profile. Microspheres were prepared by emulsification/solvent evaporation method using ethyl acetate as solvent for the polymer and water as non solvent. The microspheres were characterized by morphologic and granulometric analyses. The amount of encapsulated drug as well as its release profile in vitro were also determined. The product obtained was microparticles with smooth surface and narrow size distribution, about 50% of the particles being smaller than 5 μm. The methodology used allowed drug encapsulation with a good yield and the system provided a controlled release of diclofenac.

Estratégias biotecnológicas para a liberação controlada de antígenos e adjuvantes em vacinas através de lipossomas

Liposomes (LP) are colloidal systems with ability to compartmentalize therapeutic molecules in order to improve biological activity, decreases the potential toxicity, and to obtain prolonged effect. In this work it was discussed the role of the various liposomes types to encapsulate drug molecules able to provoke some immunological response (drugs, antigens and DNA). The effect of the liposomes and the parameters about the formation of the structures are also analyzed. Detailed literature review shows that, depending on the molecules polarity and the superficial charge of the liposome structures, the system may be efficiently used to optimize the therapeutic effects by means of the release control or through a drug delivery mechanism.

Magnetic multiparticulate colonic delivery systems evaluated by AC Biosusceptometry

The biomagnetic technique called Alternate Current Biosusceptometry (ACB) is a proposal to evaluate a multiparticulate drug delivery system in the human gastrointestinal tract. Results show that ACB was able to quantify the gastrointestinal transit and spreading of the magnetic material and is an attractive tool for pharmaceutical research. © 2007.

Non-conventional applications of computerized tomography: Analysis of solid dosage forms produced by pharmaceutical industry

X-ray computed tomography (CT) refers to the cross-sectional imaging of an object measuring the transmitted radiation at different directions. In this work, we describe a non-conventional application of computerized tomography: visualization and improvements in the understanding of some internal structural features of solid dosage forms. A micro-CT X-ray scanner, with a minimum resolution of 30 μm was used to characterize some pharmaceutical tablets, granules, controlled-release osmotic tablet and liquid-filled soft-gelatin capsules. The analysis presented in this work are essentially qualitative, but quantitative parameters, such as porosity, density distribution, tablets dimensions, etc. could also be obtained using the related CT techniques. © 2010 American Institute of Physics.

Preparation and characterization of poly(ε-caprolactone) nanospheres containing the local anesthetic lidocaine

The objective of this work was to develop a modified release system for the local anesthetic lidocaine (LDC), using poly(ε-caprolactone) (PCL) nanospheres (NSs), to improve the pharmacological properties of the drug when administered by the infiltration route. In vitro experiments were used to characterize the system and investigate the release mechanism. The NSs presented a polydispersion index of 0.072, an average diameter of 449.6nm, a zeta potential of -20.1mV, and an association efficiency of 93.3%. The release profiles showed that the release of associated LDC was slower than that of the free drug. Atomic force microscopy analyses showed that the spherical structure of the particles was preserved as a function of time, as well as after the release experiments. Cytotoxicity and pharmacological tests confirmed that association with the NSs reduced the toxicity of LDC, and prolonged its anesthetic action. This new formulation could potentially be used in applications requiring gradual anesthetic release, especially dental procedures. © 2012 Wiley Periodicals, Inc.

Qualidade de mudas seminais de eucalipto em função dos substratos e fertilização de liberação controlada

For the production of quality seedlings, depending on the physical characteristics of each substrate, more rational nutritional managements, from the of economic-environmental point of view, should be sought. This study aimed to evaluate the development and quality of Eucalyptus grandis × E. urophylla seedlings in terms of substrates and doses of controlledrelease Osmocote® fertilizer. The experiment was conducted with a completely randomized, factorial design, using as substrates: vermiculite+carbonized rice chaff+coconut fiber (1:1:1); vermiculite+coconut fiber (1:1) and vermiculite+coconut fiber (2:1) and doses of 2, 4, 6 and 8kg·m -3 of substrate. The substrates with higher water holding capacity allow seedlings to reach their maximum development in most parameters using lower doses of controlled-release fertilizer. We recommend the application of the controlled-release fertilizer at a dose of 6.0kg·m-3 in vermiculite+carbonized rice chaff+coconut fiber (1:1:1) and vermiculite+coconut fiber (2:1) substrates, and in substrate vermiculite+coconut fiber (1:1) at a dose of 7.0kg·m-3. In each substrate there is a dose range that promotes a greater formation of suitable root systems for planting in the field, which consequently results in seedlings with greater morphological development at nursery.

Cloreto de potássio revestido em efeito residual no feijoeiro de inverno irrigado na região de cerrado

In order to maintain the nutrients available to plants have been studied controlled release fertilizers. In this context, the objective was to evaluate the residual effect of doses of potassium chloride, coated or not, applied in the corn crop, regarding the crop components and grains yield of irrigated winter common bean, cultivated in followed, in Cerrado region. The experiment was conducted in Selvíria - MS, Brazil, 51°22- west longitude and 20°22- south latitude, in a clayey Oxisol, in 2009 and 2010. A randomized block design with four repetitions was used, disposed in a factorial scheme 4 x 2, being: four K2O doses (0, 40, 80 and 120 kg ha-1) and two potassium sources (potassium chloride and coated potassium chloride by polymers) applied at sowing in the corn crop. The coated potassium chloride by polymers have the same residual effect as conventional KCl, because it provides results similar for the K and chlorophyll leaf contents, crop components and grains yield of winter common bean irrigated. The increment of potassium doses in the previous crop (corn) have residual effect, because it influenced positively the number of grains per plant in 2009 and increased linearly the chlorophyll leaf content and the grains yield of winter common bean irrigated in 2010, regardless of the source used for K.

Nanostructured materials based on mesoporous silica and mesoporous silica/apatite as osteogenic growth peptide carriers

The aim of this work was the preparation of inorganic mesoporous materials from silica, calcium phosphate and a nonionic surfactant and to evaluate the incorporation and release of different concentrations of osteogenic growth peptide (OGP) for application in bone regeneration. The adsorption and release of the labeled peptide with 5,6-carboxyfluorescein (OGP-CF) from the mesoporous matrix was monitored by fluorescence spectroscopy. The specific surface area was 880 and 484 m2 g- 1 for pure silica (SiO) and silica/apatite (SiCaP), respectively; the area influenced the percentage of incorporation of the peptide. The release of OGP-CF from the materials in simulated body fluid (SBF) was dependent on the composition of the particles, the amount of incorporated peptide and the degradation of the material. The release of 50% of the peptide content occurred at around 4 and 30 h for SiCaP and SiO, respectively. In conclusion, the materials based on SiO and SiCaP showed in vitro bioactivity and degradation; thus, these materials should be considered as alternative biomaterials for bone regeneration. © 2013 Elsevier B.V.

Obtenção de micro/nanopartículas poliméricas para o encapsulamento do fármaco bromidrato de galantamina

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Formadores de filmes híbridos orgânicos inorgânicos do tipo ureasil-poliéter para liberação controlada de fármacos

Pós-graduação em Ciências Farmacêuticas - FCFAR

Correlação entre estrutura e propriedades de sistemas líquidos cristalinos para a liberação prolongada de fármacos

Pós-graduação em Ciências Farmacêuticas - FCFAR

Desenvolvimento de sistemas líquido-cristalinos multifuncionais contendo nanopartículas de TiO2 para proteção solar e liberação controlada de terpinem-4-ol

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

Utilização de sistemas poliméricos híbridos orgânicos-inorgânicos no desenvolvimento de sistemas formadores de filme

Pós-graduação em Ciências Farmacêuticas - FCFAR

Sistemas de liberação controlada de óxido nítrico baseados em ditiocarbamatos

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