Miltefosine-loaded polymeric micelles for treatment of cervical cancer: characterization and in vitro evaluation

VALENZUELA-OSES, JOHANNA; GARCÍA, MÓNICA C; FEITOSA, VALKER A.; PACIONI-VASCONCELOS, JULIANA; RANGEL-YAGUI, CARLOTA

Simposio; XXI Semana Farmacêutica de CIência e Tecnologia, 47ª Semana Universitária Paulista de Farmácia e Bioquímica (XLVII SUPFAB), Simpósio Anual de Pesquisa em Ciências Farmacêuticas.; 2016

Introduction and Objectives: The effects of temperature, speed rate and speed time were investigated miltefosine encapsulation in polymeric micelles of Pluronic 127 (PM MF-F127) and evaluated the in vitro activity in HeLa cancer cells.Material and Methods: PM MF-F127 were prepared by thin-film method in a drug: polymer molar proportion of 9:7.2. The effect of temperature, speed rate and speed time on particle size (Dh) and polydispersity index (PI) of PM MF-F127 were investigated by a factorial design 2k. Dh and PI of polymeric micelles were defined by Dynamic light scattering (DLS). Differential scanning calorimetry (DSC) was used to investigate polymer: drug interaction. Dialysis method was employed to determine drug loading (%DL). Morphology was observed by transmission electron microscopy (TEM). Physical stability of the lyophilized PM MF-F127 after 3 months storage at 4°C was studied. In vitro cytotoxicity by MTT assay against HeLa cells and hemolytic potential were also evaluated.Results and Conclusions: Values of Dh and PI of 24.33 ± 0.05 and 0.112 ± 0.001, respectively were obtained at 30 °C, 550 rpm for 30 min. DSC confirmed no significant chemical interaction between F127 and miltefosine. Morphology of micelle was found to be spherical. Lyophilized micelle showed Dh and PI of 20.33 ± 0.05 and 0.259 ± 0.008, respectively. PM MF-F127 at 80 µM of miltefosine was found no hemolytic. PM MF-F127 showed higher cytotoxicity against HeLa compared with free MF.Financing: FAPESP; CAPES.