Enhanced oral bioavailability of capsaicin-loaded microencapsulation complex via electrospray technology: Preparation, in vitro and in vivo evaluation

Abstract

The purpose of this work was to fabricate the microencapsulation of capsaicin using electrospray technology and polyvinylpyrrolidone (PVP) K30 as a carrier. The morphological characteristics of capsaicin-PVP electrosprayed microencapsulation complex under different processing parameters were observed by scanning electron microscope (SEM), while the best process was determined, wherein it comprised of 10 KV (voltage), 0.8 ml·h⁻¹ (solution flow rate), 0.9 mm (the inner diameter of the needle), and 10 cm (receiving distance). The X-ray diffraction results of the electrosprayed complex showed that capsaicin was present in the carrier in an amorphous form. The drug release properties of capsaicin powder and electrosprayed complex in different media were investigated. The results showed that in vitro release rates of the capsaicin complex in different media were much higher than that of capsaicin powder, with correspondingly improved bioavailability, defined by intravenous and oral dosing in rats in vivo, for the electrosprayed complex compared to that of capsacin powder. The dose absorbed of the electrosprayed complex was 2.2-fold that of the capsaicin powder. In short, electrospray technology can be used to prepare capsaicin-loaded electrosprayed microencapsulation complex. This technique can improve the solubility and bioavailability of capsaicin, and provide a new idea for the solubilization of other insoluble drugs.