Preparation and physicochemical characterization of the azithromycin-Eudragit RS100 nanobeads and nanofibers using electrospinning method

摘要

Azithromycin, a macrolide antibiotic, is used to eradicate the infections of the ears, lungs, sinuses, throat, skin, and reproductive organs. So therefore, taking into consideration that the nanomedicines, may confer capability for prolonged and effective delivery of the drugs into the infected tissues and organs, the aim of the present study was to prepare azithromycin-Eudragit RS100 nanoparticles. The azithromycin-Eudragit RS100 nanobeads and nanofibers with the different drug:polymer ratios and the various solution concentrations were prepared using electrospinning technique. The physicochemical characteristics of the nanoparticles and nanofibers were evaluated using scanning electron microscopy (SEM), differential scanning calorimetty (DSC), X-ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FT-IR). Drug release profiles were also compared by the use of three model-independent parameters i.e., t(50%) (the time at which 50 % of drug released), Q(15min) and Q(30min) (percent drug dissolved within 15 and 30 min. respectively). Increasing the dropped solution concentration resulted in more nanofibers and less nanobeads production with the particles size ranged from 100-500 um. DSC and XRPD studies indicated that the drug crystallinity was notably reduced. FI-IR analysis revealed no chemical interaction during the preparation process. Nanoformulations exhibited biphasic release profiles with higher release rates than pure drug. According of these findings, AZI-Eudragit RS100 nanofibers and nanobeads with improved physicochemical characteristics is possible to be formulated through optimizing the preparation parameters. Simplicity of the process on the other hand makes it an excellent choice for being scaled up.