Preparation of azithromycin-Eudragit® RS100 electrospuns and evaluation of their physicochemical properties

Abstract

Introduction: Azithromycin, a macrolide antibiotic, is used to eradicate the infections of the ears, lungs, sinuses, throat, skin, and reproductive organs. Taking into consideration that the nanomedicines, may confer capability for prolonged and effective delivery of drug into the infected tissues and organs; it seems promising to prepare nanoformulations of azithromycin. Aim: The aim of the present study was to prepare azithromycin–Eudragit® RS100 nanoparticles. Methods: The azithromycin–Eudragit® RS100 nanobeads and nanofibers with the different drug:polymer ratios and solution concentrations were prepared using electrospinning technique. The physicochemical characteristics of the nanoparticles and nanofibers were evaluated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Fourier transform infrared spectroscopy (FT-IR). Drug release profiles were compared by the use of three model-independent parameters i.e., t50% (the time at which 50% of drug released), Q15min and Q30min (percent drug dissolved within 15 and 30 min, respectively). Results: Increasing the dropped solution concentration resulted in more nanofibers and less nanobeads production with the particles size ranged from 100-500 nm. 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. Conclusions: According to these findings, AZI–Eudragit® RS100 nanofibers and nanobeads with improved physicochemical characteristics are possible to be formulated through optimizing the preparation parameters. Simplicity of the process makes it an excellent choice for being scaled up.