Biodegradable Nanoparticles Containing Benzopsoralens: An Attractive Strategy for Modifying Vascular Function in Pathological Skin Disorders

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Chorismate synthase: An attractive target for drug development against orphan diseases

The increase in incidence of infectious diseases worldwide, particularly in developing countries, is worrying. Each year, 14 million people are killed by infectious diseases, mainly HIV/AIDS, respiratory infections, malaria and tuberculosis. Despite the great burden in the poor countries, drug discovery to treat tropical diseases has come to a standstill. There is no interest by the pharmaceutical industry in drug development against the major diseases of the poor countries, since the financial return cannot be guaranteed. This has created an urgent need for new therapeutics to neglected diseases. A possible approach has been the exploitation of the inhibition of unique targets, vital to the pathogen such as the shikimate pathway enzymes, which are present in bacteria, fungi and apicomplexan parasites but are absent in mammals. The chorismate synthase (CS) catalyses the seventh step in this pathway, the conversion of 5-enolpyruvylshikimate-3-phosphate to chorismate. The strict requirement for a reduced flavin mononucleotide and the anti 1,4 elimination are both unusual aspects which make CS reaction unique among flavin-dependent enzymes, representing an important target for the chemotherapeutic agents development. In this review we present the main biochemical features of CS from bacterial and fungal sources and their difference from the apicomplexan CS. The CS mechanisms proposed are discussed and compared with structural data. The CS structures of some organisms are compared and their distinct features analyzed. Some known CS inhibitors are presented and the main characteristics are discussed. The structural and kinetics data reviewed here can be useful for the design of inhibitors. © 2007 Bentham Science Publishers Ltd.

A polymeric europium complex with the ligand thiophene-2-carboxylic acid: Synthesis, structural and spectroscopic characterization

A polymeric complex [Eu(α-tpc)3(α-Htpc) 2]n and its characterization by single crystal X-ray and thermal analysis, infrared and photoluminescence spectroscopies are described. The compound crystallizes in the monoclinic Cc space group. The asymmetric unit is formed from a europium ion bonded to one carboxyl oxygen of five different thiophene carboxylic moieties. Three of these moieties are deprotonated and bridge between neighboring europium ions giving rise to an infinite polymer along the c axis. Besides the europium characteristic emission lines, the emission spectra show unambiguously the crystal size effect on the 5D0 → 7F0 transition. The complex thermal decomposition at 220 C leads to a stable luminescent complex in which the 5D0 → 7F4 transition reveals a monomeric characteristic. The Judd-Ofelt intensity parameters to the polymeric and the monomeric compound with the same ligand and coordination number were compared. © 2013 Published by Elsevier Ltd.

Ciprofloxacino encapsulado em lipossomas revestidos com ácido poli láctico co-glicólico ou veiculado em gel de copolímero de bloco Pluronic R F127

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Micropartículas biodegradáveis para liberação prolongada intraocular de cetorolaco de trometamina obtidas po Spray Drying

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Fine-tuning of a nanostructure, swelling, and drug delivery profile by blending ureasil-PEO and ureasil-PPO hybrids

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Relationship between composition and organizational levels of nanostructured systems formed by Oleth 10 and PPG-5-Ceteth-20 for potential drug delivery

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

Desenvolvimento e avaliação de um sistema de liberação sustentada de gentamicina em biomembranas de látex natural

Pós-graduação em Biociências - FCLAS

Effect of steeping conditions (sulfur dioxide, lactic acid, and temperature) on starch yield, starch quality, and germ quality from the Intermittent Milling and Dynamic Steeping process (IMDS) for a Brazilian corn hybrid

Effect of lactic acid, SO2, temperature, and their interactions were assessed on the dynamic steeping of a Brazilian dent corn (hybrid XL 606) to determine the ideal relationship among these variables to improve the wet-milling process for starch and corn by-products production. A 2x2x3 factorial experimental design was used with SO2 levels of 0.05 and 0.1% (w/v), lactic acid levels of 0 and 0.5% (v/v), and temperatures of 52, 60, and 68degreesC. Starch yield was used as deciding factor to choose the best treatment. Lactic acid added in the steep solution improved the starch yield by an average of 5.6 percentage points. SO2 was more available to break down the structural protein network at 0.1% than at the 0.05% level. Starch-gluten separation was difficult at 68degreesC. The lactic acid and SO2 concentrations and steeping temperatures for better starch recovery were 0.5, 0.1, and 52degreesC, respectively. The Intermittent Milling and Dynamic Steeping (IMDS) process produced, on average, 1.4% more starch than the conventional 36- hr steeping process. Protein in starch, oil content in germ, and germ damage were used as quality factors. Total steep time can be reduced from 36 hr for conventional wet-milling to 8 hr for the IMDS process.

Growth and antimicrobial activity of lactic acid bacteria from rumen fluid according to energy or nitrogen source

Objetivou-se avaliar os efeitos da suplementação com diferentes fontes de energia e de compostos nitrogenados sobre o crescimento e produção de bacteriocinas de bactérias ácido-láticas in vitro. As incubações foram conduzidas utilizando-se fluido ruminal originado de um novilho Holandês-Zebu fistulado no rúmen. O animal foi mantido em pastagem de Brachiaria decumbens recebendo 200 g/dia de proteína bruta suplementar. Os substratos e o inóculo foram acondicionados em frascos de vidro considerando-se oito tratamentos: celulose, celulose e caseína, celulose e peptona de soja, celulose e ureia, amido, amido e caseína, amido e peptona de soja e amido e ureia. Incubações sucessivas foram conduzidas para seleção dos microrganismos em função das fontes energéticas e de compostos nitrogenados. O amido favoreceu o crescimento de bactérias ácido-láticas em comparação à celulose. A suplementação com proteína verdadeira (peptona de soja e caseína) estimulou o crescimento dessas bactérias em comparação ao controle (sem suplementação com compostos nitrogenados). A adição de ureia não estimulou o crescimento de bactérias ácido-láticas. Nenhuma atividade antimicrobiana foi detectada a partir das colônias de bactérias ácido-láticas isoladas. Fontes de proteína verdadeira incrementam a competição entre bactérias fermentadoras de carboidratos estruturais e não-estruturais.

Susceptibility of Saccharomyces cerevisiae and lactic acid bacteria from the alcohol industry to several antimicrobial compounds

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Xylan from corn cobs, a promising polymer for drug delivery: Production and characterization

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

Modeling a system of phosphated cross-linked high amylose for controlled drug release. Part 2: Physical parameters, cross-linking degrees and drug delivery relationships

High amylose cross-linked to different degrees with sodium trimetaphosphate by varying base strength (2% or 4%) and contact time (0.5-4 h) was evaluated as non-compacted systems for sodium diclophenac controlled release. The physical properties and the performance of these products for sodium diclophenac controlled release from non-compacted systems were related to the structures generated at each cross-linking degree. For samples at 2% until 2 h the swelling ability, G' and eta* values increased with the cross-linking degree, because the longer polymer chains became progressively more entangled and linked. This increases water uptake and holding, favoring the swelling and resulting in systems with higher viscosities. Additionally, the increase of cross-linking degree should contribute for a more elastic structure. The shorter chains with more inter-linkages formed at higher cross-linking degrees (2%4h and 4%) make water caption and holding difficult, decreasing the swelling, viscosity and elasticity. For 2% samples, the longer drug release time exhibited for 2%4h sample indicates that the increase of swelling and viscosity contribute for a more sustained drug release, but the mesh size of the polymeric network seems to be determinant for the attachment of drug molecules. For the 4% samples, smaller meshes size should determine less sustained release of drug. (C) 2008 Elsevier B.V. All rights reserved.

In vitro characterization of coevaporates containing chitosan for colonic drug delivery

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Controlled transscleral drug delivery formulations to the eye: establishing new concepts and paradigms in ocular anti-inflammatory therapeutics and antibacterial prophylaxis

Importance of the field: The use of topical agents poses unique and challenging hurdles for drug delivery. Topical steroids effectively control ocular inflammation, but are associated with the well-recognized dilemma of patient compliance. Although administration of topical antimicrobials as prophylaxis is acceptable among ophthalmologists, this common practice has no sound evidence base Developing a new antimicrobial agent or delivery strategy with enhanced penetration by considering the anatomical and physiological constraints exerted by the barriers of the eye is not a commonly perceived strategy. Exploiting the permeability of the sclera, subconjunctival routes may offer a promising alternative for enhanced drug delivery and tissue targeting.Area covered in this review: Ocular drug delivery strategies were reviewed for ocular inflammation and infections clinically adopted for newer class of antimicrobials, which use a multipronged approach to limit risks of endophthalmitis.What the reader will gain: The analysis substantiates a new transscleral drug delivery therapeutic approach for cataract surgery.Take home message: A new anti-inflammatory and anti-infective paradigm that frees the patient from the nuisance of topical therapeutics is introduced, opening a large investigative avenue for future improved therapies.