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1.
Pharmazie ; 76(2): 68-76, 2021 02 25.
Artigo em Inglês | MEDLINE | ID: mdl-33714282

RESUMO

Ocular toxoplasmosis is the major cause of infectious posterior uveitis worldwide, inducing visual field defect and/or blindness. Despite the severity of this disease, an effective treatment is still lacking. In this study, spiramycin-loaded PLGA implants were developed aiming at the treatment of ocular toxoplasmosis. Implants were manufactured by a hot-molding technique, characterized by Fourier Transform Infrared Spectroscopy, X-Ray Diffraction, Differential Scanning Calorimetry, Scanning Electron Microscopy; evaluated in terms of ocular biocompatibility by immunofluorescence, flow cytometry, cell migration, Hen's egg test-chorioallantoic membrane (HET-CAM) irritation test; and investigated in terms of in vitro efficacy against Toxoplasma gondii . Characterization techniques indicated that spiramycin was dispersed into the polymeric chains and both substances preserved their physical structures in implants. The HET-CAM test indicated that implants did not induce hemorrhage or coagulation, being non-irritant to the CAM. ARPE-19 cells showed viability by MTT assay, and normality in cell cycle kinetics and morphology, without stimulating cell death by apoptosis. Finally, they were highly effective against intracellular parasites without inducing human retinal pigment epithelial cell death. In conclusion, spiramycin-loaded PLGA implants represent a promising therapeutic alternative for the local treatment of ocular toxoplasmosis.


Assuntos
Sistemas de Liberação de Medicamentos/métodos , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Espiramicina/administração & dosagem , Toxoplasmose Ocular/tratamento farmacológico , Animais , Técnicas de Cultura de Células , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Galinhas , Membrana Corioalantoide , Células Epiteliais , Humanos , Microscopia Eletrônica de Varredura , Epitélio Pigmentado da Retina , Espiramicina/uso terapêutico , Toxoplasma/efeitos dos fármacos
2.
Pharmazie ; 74(4): 221-226, 2019 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-30940305

RESUMO

The use of sirolimus and its analogs has been evaluated in studies aimed at combating several types of cancer; however, because of the limited bioavailability of the drug, the search for new forms of administration is required. Biodegradable polymeric implants containing sirolimus were developed and assessed as an alternative method of drug administration. Implants containing 25 % (w/w) sirolimus were prepared employing the polymer matrices chitosan, polycaprolactone and poly(lactic-co-glycolic acid) (PLGA) in two proportions: PLGA 50:50 and PLGA 75:25. Thermal analysis techniques such as thermogravimetry and differential scanning calorimetry, combined with x-ray diffraction were used to characterize and evaluate the compatibility of the constituents of the formulation. No incompatibilities were found between the components, but drug amorphization was observed in all samples. Implants made from the polymers chitosan and PCL may accelerate the degradation of SRL when these polymers are dissolved in methanol at 50 °C. HPLC analysis showed that the implant prepared with PLGA 75:25 did not present degradation products and maintained its appropriate drug content, even when dissolved in methanol and heated to 50 °C. Therefore, it represents the most suitable biodegradable polymer for use in implants developed for the treatment of malignant solid tumors. However, it is still necessary to further study the drug effects after amorphization of the crystal and also to perform stability and solubility analysis.


Assuntos
Antineoplásicos/administração & dosagem , Portadores de Fármacos/química , Polímeros/química , Sirolimo/administração & dosagem , Varredura Diferencial de Calorimetria , Química Farmacêutica/métodos , Quitosana/química , Cromatografia Líquida de Alta Pressão/métodos , Implantes de Medicamento , Poliésteres/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Sirolimo/química , Temperatura , Termogravimetria , Difração de Raios X
3.
J Hazard Mater ; 324(Pt B): 406-413, 2017 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-27866760

RESUMO

The present study describes the influence of the concentration of lignin when used as a filler in polyurethane foam for crude oil sorption. The foams (lignin 0-20wt%) were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), thermogravimetric analysis, contact angle and density. The FTIR analysis confirmed urethane linkage formation, showing that the chemical structure of the polymer was preserved, despite the addition of different lignin concentrations. Thermogravimetric analysis showed that the presence of lignin has altered the onset temperature (Tonset) of the foams, decreasing as the concentration of lignin is increased. The contact angle analysis showed a decrease in the hydrophobicity of the foams with increasing lignin concentration. All modified foams showed an improvement in the oil sorption capacity in a PUF/oil/water system, and the PUF-10 showed an improvement of about 35.5% compared to the PUF-blank. The Langmuir isotherm showed a better fit to the data and predicted a maximum oil adsorption of 28.9gg-1 by the PUF-10. The ΔG° value of -4.4kJmol-1 indicated that crude oil adsorption process by PUF-10 was spontaneous. The results of reuse of the PUF-10 showed that oil removal efficiency remained greater than 95% after five consecutive cycles.

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