Synthesis, Physicochemical Characterization, and Evaluation of Antibacterial and Antitumor Activity of a New Drug Delivery System of Pefloxacin Antibiotic

Objectives The objectives of this novel study were formulation and characterization of the new drug delivery system pefloxacin (PFM) methylate antibiotic loaded on inert clay biodegradable biocompatible natural polymer carrier and evaluation performance. Material and Methods Materials were clay montmorillonite, PFM and buffer solutions. The drug was loaded on clay at optimum pH, initial concentration and contact time. Results At 25°C, the maximum adsorption capacity 93.73 mg g -1 was achieved by ion exchange mechanism at 20 min., pH 7.5, 120 mg g -1 . Intercalated antibiotic-clay nanocomposite (NC) was confirmed using Fourier Transformer Infrared spectra, transmission electron microscopy, and powder X-ray diffraction. Particle size was at range 2.06-2.61nm. The high-performance liquid chromatography (HPLC) chromatogram showed that clay was an inert drug effective carrier. Adsorption data were fitted some thermodynamic and kinetic models. In vitro rate of drug release in aqueous solutions simulating biological fluids followed the order pH: 1.2 > 6.8 >7.4. Release mechanism was controlled by diffusion and ion exchange. At pH 1.2, H + replaced drug form clay layers. At pH: 6.8, both proton and hydroxyl ion replaced drug. At pH 7.4, hydroxyl ion difficulty replaced drug molecules. Release data fitted pseudo 2 o order kinetic model. Clay controlled and targeted drug release. The NC was thermally stable and a potent anti-bacterial (inhibition zone range 28-33mm and anti-proliferated various cancer cell lines. The best anti-proliferation activity for hepatic cancer (lowest IC 50 210.401 μg L -1 versus IC 50 of standard antitumor Doxorubicin) 153.4 µg L -1 . Conclusion Biological activity of the antibiotic was improved after loading on the clay carrier as pure doxorubicin used and 210.401 μg L -1 included both PFM and clay.