24 resultados para glycolic) acid (PLGA

em Repositório Institucional UNESP - Universidade Estadual Paulista "Julio de Mesquita Filho"


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With the purpose of enhancing the efficacy of microparticle-encapsulated therapeutic agents, in this study we evaluated the phagocytic ability of rat peritoneal exudate cells and the preferential location of poly(D,L-lactide-co-glycolic ) () microparticles inside these cells. The microparticles used were produced by a solvent evaporation method and were characterized by dynamic light scattering (DLS), transmission electron microscopy (TEM), and scanning electron microscopy (SEM). Size distribution analysis using DLS and SEM showed that the particles were spherical, with diameters falling between 0.5 and 1.5 mu m. Results from cell adhesion by SEM assay, indicated that the microparticles are not toxic to cells and do not cause any distinct damage to them as confirmed by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay. Among the large variety of cell populations found in the peritoneal exudates (neutrophils, eosinophils, monocytes, and macrophages), TEM showed that only the latter phagocytosed microparticles, in a time-dependent manner. The results obtained indicate that the microparticles studied show merits as possible carriers of drugs for intracellular delivery.

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Here we describe the application of microparticles (MPs) for the delivery and release of the drug a benzopsoralen. We also evaluated the intracellular distribution and cellular uptake of the drug by using an encapsulation technique for therapeutic optimization. MPs containing the compound 3-ethoxycarbonyl-2H-benzofuro[3,2-f]-1-benzopyran-2-one (psoralen A) were prepared by the solvent evaporation technique, and parameters such as particle size, drug encapsulation efficiency, effect of the encapsulation process on the drug's photochemistry, zeta potential, external morphology, and < i > in vitro release behavior were evaluated. The intracellular distribution of MPs as well as their uptake by tissues were monitored. Size distribution studies using dynamic ligh scattering and scanning electron microscopy revealed that the MPs are spherical in shape with a diameter of 1.4 mu m. They present low tendency toward aggregation, as confirmed by their zeta potential (+10.6 mV). The loading efficiency obtained was 75%. As a consequence of the extremely low diffusivity of the drug in aqueous medium, the drug release profile of the MPs in saline phosphate buffer (pH 7.4) was much slower than that obtained in the biological environment. Among the population of peritoneal phagocytic cells, only macrophages were able to phagocytose poly-d,l-lactic-co-glycolic () MP. The use of psoralen A in association with ultraviolet light (360 nm) revealed morphological characteristics of cell damage such as cytoplasmic vesiculation, mitochondria condensation, and swelling of both the granular endoplasmatic reticulum and the nuclear membrane. These results indicate that MP could be a promising delivery system for psoralen in connection with ultraviolet irradiation therapy (PUVA).

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

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

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

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A simple, rapid, selective and specific high performance liquid chromatographic (HPLC) method for quantitative analysis of the triamcinolone in polylactide-co-glycolide () microparticles was developed. The chromatographic parameters were reversed-phase C18 column, 250mm x 4.6mm, with particle size 5 μm. The column oven was thermostated at 35°C ± 2°C. The mobile phase was methanol/water 45:55 (v/v) and elution was isocratic at a flow-rate of 1 mL.mL-1. The determinations were performed using a UV-Vis detector at 239 nm. The injected sample volume was 10 μL. The standard curve was linear (r2 > 0.999) in the concentration range 100-2500 ng.mL-1. The method showed adequate precision, with a relative standard deviation (RSD) was smaller than 3%. The accuracy was analyzed by adding a standard drug and good recovery values were obtained for all drug concentrations used. The method showed specificity and selectivity with linearity in the working range and good precision and accuracy, making it very suitable for quantitation of triamcinolone in microparticles.

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

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Biomateriais poliméricos são desenvolvidos para uso como substitutos de tecidos danificados e/ou estimular sua regeneração. Uma classe de biomateriais poliméricos são os biorreabsorvíveis, compostos que se decompõem tanto in vitro quanto in vivo. São empregados em tecidos que necessitam de um suporte temporário para sua recomposição tecidual. Dentre os vários polímeros biorreabsorvíveis, destacam-se os alfa-hidróxi ácidos, entre eles, diferentes composições do poli(ácido lático) (PLA), como o poli(L-ácido lático) (PLLA), poli(D-ácido lático) (PDLA), poli(DL-ácido lático) (PDLLA), além do poli(ácido glicólico) (PGA) e da policaprolactona (PCL). Estes polímeros são considerados biorreabsorvíveis por apresentarem boa biocompatibilidade e os produtos de sua decomposição serem eliminados do corpo por vias metabólicas. Diversas linhas de pesquisa mostram que os diferentes substratos à base de PLA estudados não apresentam toxicidade, uma vez que as células são capazes de crescer e proliferar sobre eles. Além disso, diversos tipos de células cultivadas sobre diferentes formas de PLA são capazes de se diferenciarem sobre os diferentes polímeros e passar a produzir componentes de matriz extracelular. Neste trabalho, é revisada a utilização de substratos à base de alfa-hidróxi ácidos, com destaque para diferentes formas de PLA, utilizados como substratos para cultura de células, bem como suas aplicações.

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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

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The skin pigmentation caused by ultraviolet light irradiation as a defense against the carcinogenic action of solar light may lead to early skin aging and to hyperchromia, which treatment requires the use of photo-protective, depigmenting and rejuvenating agents. Recently, there have been used many substances for the prevention and/or treatment of skin aging as well as to lowering the skin pigmentation. Glycolic is the alpha-hydroxy most commonly used in cosmetic and dermatological prepatations. This use is due to its depigmentating and rejuvenating properties and its efficacy at different concentrations, when incorporated to different kind of excipients.

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Dimorphandra mollis Benth., Compositae, false barbatimão, has been used topically as a healing, astringent and antibacterial. In this study, antibacterial activity was verified on liquid soap containing glycolic extract of D. mollis (DGE) at different concentrations (8, 15 and 20%) and at different pH levels (6 and 8). Five soap formulations (F) were prepared: F1 - tryclosan (0.1%), F2 - DGE (8%), F3 - DGE (15%), F4 - DGE (20%) and F5 - without preservatives. Bark of D. mollis were dried in a circulating air oven and ground. The rude extracts were prepared by turbo extraction with ethanol. After screening, the extract were concentrated in rotating evaporator, lyophilized and resuspended in propileneglycol to obtain the glycolic extract. The antimicrobial activity was verified by diffusion in agar method, using cylinder in plate. Plates containing Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli were incubated at 37°C for 24 hours. After incubation, the results were analysed with a pachymeter, observing the bacterial grouth inhibition halo diameter. It was verified that the liquid soap containing tryclosan caused on inhibition of bacterial growth at both pH levels; the soaps without preservatives and containing DGE, independently of the concentration and pH levels used, did not present antibacterial activity.