Preparation and characterization of Bosentan monohydrate/ε-Polycaprolactone nanoparticles obtained by Electrospraying

NORMA R. SPERANDEO; WALTER MANUCHA; VIRNA M MARTIN GIMENEZ; SANDRA NORIEGA; SONIA N FAUDONE; DIEGO KASSUHA

BIOTECHNOLOGY PROGRESS

AMER CHEMICAL SOC

Lugar: Washington; Año: 2019 vol. 35 p. 1 - 11

8756-7938

The aim of this study was, firstly, to optimize the influent parameters of the electrospraying technique (flow velocity, polymeric concentration and voltage) for the manufacture of a Bosentan (BOS) nanoparticulate platform. Secondly, to evaluate its physicochemical properties and in vitro biopharmaceutical behavior. Nanoparticles loaded with BOS monohydrate were developed by subjecting a 0.5% w/w ε-Polycaprolactone (PCL) in acetone solution to flow conditions of 0.5 mL/h and voltage of 10 kV. Particles obtained had heterogeneous sizes (150 to 1150 nm) with predominance (>60%) of particles smaller than 550 nm. Their physicochemical properties were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), termogravimetry (TG) and Fourier transformed Infrared spectroscopy (FTIR). The nanostructures were semicrystalline to PXRD indicating a partial amorphization of BOS during the encapsulation in the polymer matrix. FT-IR and DSC showed an absence of chemical interactions between BOS and PCL, which allowed us to infer that both components behaved as a physical mixture in these particles. The drug loading was 25.98% and the encapsulation efficiency was 58.51%. Additionally, the dialysis membrane method during 24 and 72 hours showed prolonged and controlled release of BOS, in comparison to non-encapsulated BOS. The release data showed to fit with the Cubic Root kinetic dissolution. As a conclusion, we demonstrate that the manufacture of these BOS controlled release nanoplatforms would represent an interesting contribution in the development of new therapeutic alternatives for the treatment of pathologies such as pulmonary hypertension and other related diseases.