DESIGN OF AZITHROMYCIN LOADED EUDRAGIT RL 100 NANOPARTICLES WITH EXTENDED ANTIBACTERIAL EFFECT

Abstract

The main purpose of this study was to prepare Azithromycin (AZM) loaded Eudragit RL 100 (ERL) nanoparticles in order to increase the antibacterial activity of AZM and to compare the drug release profiles of the formulations at the stomach and intestinal pH. AZM-NP-1:5 (AZM:ERL = 1:5) and AZM-NP-1:10 (AZM:ERL = 1:10) nanoparticles were prepared using different drug-polymer ratios. Particle size and zeta potential were analysed and physicochemical characterization was performed using Scanning Electron Microscope (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy, Proton Nuclear Magnetic Resonance (1H-NMR) Spectroscopy, Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD). AZM-NP-1:10 have 554.4 ± 29.3 nm size, + 15.4 ± 3.18 mV charge with 77.06 ± 3.63% DL%. In the in vitro release tests, after the first 3 hours, 49.35 ± 1.64% of the active ingredient was released from AZM-NP-1:10 at pH 1.2 HCl medium and the release was found to fit Korsmeyer-Peppas kinetic model. A similar release profile (f2 = 71) of 51.40 ± 1.71% for the first 3 hours was also obtained for AZM-NP-1:10 in PBS at pH 6.8. The Minimum Inhibitory Concentration (MIC) of free AZM and AZM-NP-1:10 against Staphylococcus aureus was found to be 2 and 0.5 µg/mL, respectively. The activity of AZM started to decrease after 6 hours while AZM-NP-1:10 presented a continuous antibacterial activity for 24 hours. AZM-NP-1:10 exhibited an enhanced antibacterial activity and a prolonged drug release pattern compared to free AZM, allowing for more effective treatment with fewer side effects.