Prospecção tecnológica, desenvolvimento e caracterização in vitro de nanopartículas de PLGA contendo PJOV 56 como agente antitumoral

Abstract

Tumor chemotherapeutic treatment may have adverse effects, such as the action of the drug on healthy cells. As a measure to reduce these effects, the nanoencapsulation is an alternative to the increase of the biodisponibility of antitumor drugs. Therefore, quinoxaline PJOV 56 was chosen for encapsulation by PLGA, and the characterization of the nanoparticles was studied. In nanoparticles preparation it was used 100 mg of PLGA dissolved in 2 mL of dichloromethane, with the addition of 200 µL of PJOV 56 5mM. This oil phase was poured in the aqueous phase, composed by 9 mL of PVA. Ultrassonication was used in the solution, and it stayed 4 hours under mild agitation to the evaporation of the solvent. After that, the solution was washed three times in a centrifuge during 25 minutes at the temperature of 4ºC and under 3.220xg. The pellet was ressuspended and lyophilized after it’s freezing. The determination of then size of the particle was made through measures of DLS. The distribution of particle size is obtained by the polidispersion index. The measure of the average zeta potential were made by the technique of microelectrophoresis. To the calibration curve, a liquid chromatography – mass spectrometry was used (UPLC-QToF-MSE). The characterization showed monodispersed populations of particles of small dimensions of 231.06±5.51 nm of control samples and 511.83±4.96 por loaded particles samples, showing a PDI of 0.182±0.007 and 0.444±0.02 respectively. The zeta potential was -9.84 ± 0.26 mV for the control samples and - 30.76 ± 0.49 mV for the loaded particles samples. The results obtained in the scanning electron microscope corroborated to the previous assays to attest particle size and allowed to confirm it’s spherical shape and uniformity. The particle size obtained was in the same scale size than the biological macromolecules – nucleic acids, proteins, etc. -, allowing an integration of nanotechnology and biology, enabling advances in passive and active strategies of selectivity for drug delivering antitumor drugs. Besides, a bibliographic survey and an anteriority search about this technology were made. The survey and the anteriority search were made in national and international databases. The keywords were chosen to help to refine the searcj for technologies related to the PLGA nanoparticles. It was found that there is not a clear correlation between published articles and patents deposited, and Brazil still have na unconsistent production of articles and patents in the area.