Aspectos fundamentais no desenvolvimento de sistemas microemulsionados contendo anfotericina B para uso oftálmico

A exemplo do que ocorre com outros fármacos, a biodisponibilidade da anfotericina B (AmB) através da via ocular repreesenta um grande desafio para a pesquisa científica. Na verdade, a baixa biodisponibilidade apresentada por tal molécula é devido, principalmente, a presença das barreiras oculares que impedem a absorção deste fármaco para os tecidos internos. A toxicidade associada a este fármaco, assim como a sua baixa capacidade em permear a córnea íntegra também consiste em um problema associado ao seu uso clínico. Novos veículos seguros e eficazes para a liberação ocular da AmB são, portanto, necessários. As microemulsões (MEs) aparecem como um interessante sistema devido à sua transparência, estabilidade termodinâmica e favorável viscosidade. O conhecimento do processo de formação das MEs contendo AmB, assim como a compreensão de toda a sua caracterização físicoquímica correspondem a aspectos importantes para se determinar as condições favoráveis para que estes sistemas venham a ser empregados como colírios. Esta revisão tem como objetivo, portanto, abordar este tema enfatizando os principais aspectos relacionados com a utilização de MEs como sistemas de liberação para a AmB através da via tópica oftálmica

5CN05 partitioning in an aqueous two-phase system: A new approach to the solubilization of hydrophobic drugs

Liquid-liquid extraction for the purification of molecules has been central to many advances in the pharmaceutical industry. These processes were developed based on the property that some polymer and/or micellar solutions present to separate into a concentrated phase and a diluted phase. Based on the differences in the physical and chemical environments of the two coexisting phases, and since both phases contain approximately 60-90% of water, liquid-liquid extraction provides a powerful alternative to both extract and solubilize a molecule. This paper examines the partition behavior of the synthetic drug, 2-[(3,4-dichlorine-benzylidene)-amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carbonitrile (5CN05), in an aqueous two-phase polymer system (ATPPS) and also in an aqueous two-phase micellar system (ATPMS). The results showed that both systems are favorable for extraction the 5CN05 drug high partition coefficient values (K-5CN05 > 200) and yield (Y-5CN05 > 99.48%) in the concentrated phase were achieved with the systems. However, the ATPPS generated a partition coefficient (K-5CN05) higher than the one obtained with ATPMS. The results suggest that both processes may be used for the extraction and concentration of molecules with hydrophobic characteristics, such as 5CN05. They also provide an optimal environment for the solubilization of such molecules, allowing for greater efficiency when purifying many classes of drugs. (C) 2014 Elsevier Ltd. All rights reserved.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP

Prevalência de hemoglobinas variantes em comunidades quilombolas no estado do Piauí, Brasil

Gonçalves, Marilda de Souza. “Documento produzido em parceria ou por autor vinculado à Fiocruz, mas não consta à informação no documento”.Submitted by Ana Maria Fiscina Sampaio ([email protected]) on 2018-04-05T17:04:49Z No. of bitstreams: 1 Soares LF Prevalência de hemoglobinas variantes ....pdf: 176831 bytes, checksum: 9b26af0009ec33cf402748ffe72b5f47 (MD5)Approved for entry into archive by Ana Maria Fiscina Sampaio ([email protected]) on 2018-04-05T17:14:17Z (GMT) No. of bitstreams: 1 Soares LF Prevalência de hemoglobinas variantes ....pdf: 176831 bytes, checksum: 9b26af0009ec33cf402748ffe72b5f47 (MD5)Made available in DSpace on 2018-04-05T17:14:17Z (GMT). No. of bitstreams: 1 Soares LF Prevalência de hemoglobinas variantes ....pdf: 176831 bytes, checksum: 9b26af0009ec33cf402748ffe72b5f47 (MD5) Previous issue date: 2017Ministério da Saúde, Secretária da Saúde do Estado do Piauí, Centro de Pesquisa Gonçalo Muniz (Fiocruz-Bahia).Universidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade Estadual da Paraíba. Centro de Ciências da Saúde. Departamento de Bioquímica e Farmacologia. Teresina, PI, BrasilUniversidade do Vale do Paraíba. São José dos Campos, SP, BrasilUniversidade Federal da Bahia. Faculdade de Medicina. Salvador, BA, BrasilAs hemoglobinas variantes (Hb) decorrem de mutações nos genes da globina. As variantes estruturais mais frequentes são HbS, HbC, HbD e HbE. O gene da hemoglobina S tem frequência elevada na América, enquanto que no Brasil é maior no Sudeste e Nordeste. O presente artigo tem por objetivo investigar a presença de hemoglobinas variantes em 15 comunidades quilombolas do estado do Piauí. Foram analisadas 1.239 amostras, nas quais as hemoglobinas foram triadas pela cromatografia líquida de alta eficiência (HPLC). Aplicou-se questionário referente a gênero, etnia e consanguinidade das populações. Das 1.239 amostras, 5,4% apresentaram o traço falciforme AS, as doenças falciformes SS e SC apareceram em 0,8% do total, nas hemoglobinas AC, AD e DD. Das 1.069 pessoas negras, 84 apresentaram alteração das hemoglobinas; destas, 34 eram do sexo masculino e 53 do feminino. Ocorreu a presença de 13 casamentos consanguíneos dentre as 84 alterações das hemoglobinas. O estudo das hemoglobinas variantes em 15 comunidades remanescentes de quilombos do Piauí contribui para sua educação em saúde frente aos aspectos da herança genética destas proteínas, relevante questão de saúde pública, proporcionando subsídios para a implantação do Programa Estadual da Doença Falciforme do Piauí.Hemoglobin variants (Hb) result from mutations in globin genes, with amino acid substitution in the polypeptide chain. Among the most common structural variants are HbS, HbC, HbD and HbE. The S hemoglobin gene is a high frequency gene across America and Brazil, where it is more frequent in the Southeast and Northeast. The scope of this article is to investigate the presence of hemoglobin variants in 15 quilombos (fugitive slave communities) of Piaui. The sample was of 1,239 people and hemoglobin was screened by high-performance liquid chromatography (HPLC). A questionnaire was applied related to gender, ethnicity and consanguinity. Of the samples analyzed, 5.4% had AS sickle cell trait, while SS and SC sickle cell anemia showed a rate of 0.8%, with AC, AD and DD hemoglobin. Of the 1,069 Afro-descendants, 84 revealed hemoglobin abnormalities, 34 being male 53 being female. There were 13 consanguineous marriages among the 84 hemoglobin alterations. The study of hemoglobin variants in 15 former quilombo communities in the state of Piaui contributes to their education in health in the aspects of genetic inheritance of hemoglobin, a relevant public health issue, providing input for the implementation of the State Program of Sickle Cell Disease of Piaui

Extraction, isolation and characterization of inulin from Agave sisalana boles

Agave sisalana Perrine is a widespread species of the Brazilian Northeast region, where it is exploited only as a source of hard fiber (sisal). Although some other Agave species are sources of fructans, there is no study on this issue on A. sisalana. This paper aimed at extracting and isolating inulin from aqueous extract of A. sisalana boles. After preparation of extracts, crude inulin was precipitated with acetone at low temperature (4 \ub0C). After purification by ion-exchange chromatography, a white powder was obtained by freeze-drying and characterized by X-Ray Diffraction (XRD), thermal analysis, Circular Dichroism (CD) and Matrix-Assisted Laser Desorption/Ionization Time of Flight Mass Spectrometry (MALDI-TOF-MS). Moreover, its polysaccharide structure was confirmed by Fourier Transformed Infrared (FT-IR) spectroscopy and Nuclear Magnetic Resonance (NMR). FT-IR analysis pointed out absorption at 1420 cm 121, corresponding to deformation of CH2\u2013OH lying on fructose ring, while absorption at 1075 cm 121 was assigned to C[sbnd]O and C[sbnd]C stretching vibrations of inulin pyranose ring. NMR showed the presence of one signal in the anomeric region at \u3b4 5.4 ppm and others between 3.1 and 4.2 ppm in the 1H spectrum, besides a chemical shift at 104.4 ppm corresponding to the anomeric region of the 13C spectrum of an internal \u3b2-fructofuranose unit. XRD highlighted the amorphous state of inulin-rich powder, thermal analysis a glass transition temperature in the range between 50.0 and 55.8 \ub0C, CD a good thermal stability, and MALDI-TOF-MS a prevalence of oligosaccharides with degree of polymerization in the range 5\u201313. These techniques revealed that A. sisalana boles contain inulin with features similar to those extracted from other commercial sources such as Agave tequilana or Agave atrovirens, which extends the economic importance of this species beyond its simple use as a fiber source

Prevalence of hemoglobin variants in quilombola communities in the state of Piauí, Brazil

<p></p><p>Abstract Hemoglobin variants (Hb) result from mutations in globin genes, with amino acid substitution in the polypeptide chain. Among the most common structural variants are HbS, HbC, HbD and HbE. The S hemoglobin gene is a high frequency gene across America and Brazil, where it is more frequent in the Southeast and Northeast. The scope of this article is to investigate the presence of hemoglobin variants in 15 quilombos (fugitive slave communities) of Piaui. The sample was of 1,239 people and hemoglobin was screened by high-performance liquid chromatography (HPLC). A questionnaire was applied related to gender, ethnicity and consanguinity. Of the samples analyzed, 5.4% had AS sickle cell trait, while SS and SC sickle cell anemia showed a rate of 0.8%, with AC, AD and DD hemoglobin. Of the 1,069 Afro-descendants, 84 revealed hemoglobin abnormalities, 34 being male 53 being female. There were 13 consanguineous marriages among the 84 hemoglobin alterations. The study of hemoglobin variants in 15 former quilombo communities in the state of Piaui contributes to their education in health in the aspects of genetic inheritance of hemoglobin, a relevant public health issue, providing input for the implementation of the State Program of Sickle Cell Disease of Piaui.</p><p></p

Therapeutic potential of Melaleuca alternifolia essential oil in new drug delivery systems

Medicinal plants produce secondary metabolites with special biological activities, which may be used as new therapeutic alternatives. For instance, tea tree essential oil (TTO) was shown to exert antimicrobial, antifungal, anthelmintic, antiviral, anti-tumor and anti-inflammatory activities. Due to their thermal instability, active principles can be easily degraded by physicochemical processes; therefore, they must be protected to increase their time of action and improve their controlled release. The aim of this review is to report formulations making use of encapsulated TTO as the active ingredient. Micro and nanoencapsulated systems proved to be more thermostable than TTO and to exert better antimicrobial, antifungal, antiparasitic and larvicidal effects. Nanoencapsulation also reduced the oil toxicity. Emulsified and hybrid systems developed by various methods proved to be promising for the pharmaceutical industry, because they showed improved repellent, antibacterial, antifungal and anti-inflammatory activities. Liposomal formulations produced by hydration of lipid films exhibited constant rate of terpineol-4 release. In addition, their incorporation into biomaterials, such as sponges, nanofibers and films, showed great potential for treating infections. Mainly due to the advantages of their incorporation into new drug delivery systems over conventional formulations, there is interest in the development of systems containing TTO as a pharmaceutical ingredient of plant origin

Microemulsions containing Copaifera multijuga Hayne oil-resin: Challenges to achieve an efficient system for \uce\ub2-caryophyllene delivery

\uce\ub2-Caryophyllene (\uce\ub2-CP) is a bioactive sesquiterpene abundant in copaiba oil-resin (COR), which is widely used in Brazilian folk medicine; however, its instability due to the presence of unsaturations is an obstacle to the use of COR in its natural form. Therefore, the development of a system for \uce\ub2-CP delivery, like the one proposed herein for the first time, may protect it and preserve its therapeutic action. Pseudo-ternary phase diagrams were constructed in this study to obtain COR-containing nanocarriers. Two microemulsions (MEs) were obtained, namely a) ME-I containing (% w/w) 47.1 water, 8.5 Plurol Oleique, 33.8 Labrasol and 10.6 COR and b) ME-II containing (% w/w) 39.0 water, 18.3 Plurol Oleique, 36.6 Labrasol and 6.1 COR. Both MEs showed physicochemical properties suitable for a delivery system such as pH 5.25-5.74, conductivity of 79.5\ue2\u80\u93120.9 \uce\ubcS cm\ue2\u88\u921and slightly negative Zeta potential (-3.57/-2.63 mV). Transmission electron microscopy revealed the nanometric size of MEs droplets, differential scanning calorimetry their oil/water nature, while refractive indices clarity and isotropicity. Both systems behaved as Newtonian fluids and exhibited low viscosity (64.42 \uc2\ub1 0.667 mPa.s for ME-I and 118.78 \uc2\ub1 0.503 mPa.s for ME-II). After COR incorporation in MEs, steam distillation allowed obtaining \uce\ub2-CP contents depending on their initial COR amount. The pharmacological effectiveness of these innovating systems for \uce\ub2-CP delivery was confirmed by antimicrobial and anti-inflammatory activity tests. ME-II afforded a stronger antimicrobial effect against all target microorganisms than ME-I and a much stronger one than COR. Carrageenan-induced inflammation in rat paw was visibly inhibited by MEs