DESENVOLVIMENTO TECNOLÓGICO E CARACTERIZAÇÃO DE NANOCÁPSULAS POLIMÉRICAS CONTENDO CILOSTAZOL

Detalhes bibliográficos
Ano de defesa: 2015
Autor(a) principal: Gomes, Mona Lisa Simionatto lattes
Orientador(a): Farago, Paulo Vitor
Banca de defesa: Zanin, Sandra Maria Warumby lattes, Ferrari, Priscileila Colerato lattes
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: UNIVERSIDADE ESTADUAL DE PONTA GROSSA
Programa de Pós-Graduação: Programa de Pós Graduação Ciências Farmacêuticas
Departamento: Farmacos, Medicamentos e Biociências Aplicadas à Farmácia
País: BR
Palavras-chave em Português:
Palavras-chave em Inglês:
Área do conhecimento CNPq:
Link de acesso: http://tede2.uepg.br/jspui/handle/prefix/88
Resumo: Cilostazol is a selective inhibitor of phosphodiesterase III. It acts as a vasodilator and antiplatelet agent. It is the main drug for the treatment of intermittent claudication related to peripheral arterial occlusive disease. This drug belongs to the class II of the Biopharmaceutical Classification System (BCS) and shows low solubility and high permeability in gastrointestinal tract. The usual oral dose is 100 mg twice a day, which represents a disadvantage in treatment compliance. Cilostazol is a lipophilic drug and the development of controlled drug delivery systems can improve its bioavailability. The aim this study was to obtain and characterize nanocapsules suspensions prepared from poly(caprolactone) (PCL), poly(D,L-lactic-co-glycolic acid) (PLGA) and blends using polyethylene glycol (PEG), PCL/PEG and PLGA/PEG containing 0 to 3.0 mg.mL-1cilostazol. The analytical method was developed and validated for the quantification of cilostazol into the nanocápsulas by high performance liquid chromatography. All formulations had suitable encapsulation efficiencies (≥99.6%). Nanocapsules showed pH values between 6.0 and 6.4, average size lower than 137 nm, polydispersity index lower than 0.22 and average negative zeta potential of -35.34 mV. The images observed by electron transmission microscopy and scanning electron microscopy, revealed spherical shape with smooth surface. The results achieved by X-ray diffraction demonstrated no crystallinity which indicated the drug amorphization compared to the raw materials. Analyses performed by Fourier transform infrared spectroscopy showed no chemical reactions between drug and polymers. The formulations prepared from blends of PCL/PEG showed the best stability parameters after 60 days of storage. The use of nanoparticles can be a promising strategy for increasing the apparent solubility of cilostazol leading to better dissolution profiles and therapeutical effect.