Preparation and characterization of biodegradable paclitaxel loaded alginate microparticles for pulmonary delivery

In primary or metastatic lung cancer, administration of chemotherapeutic agents via inhalation could increase exposure of lung tumor to the drug, while minimizing systemic side effects. In addition, mucosal drug delivery system may reduce the toxicity and increase the site specific efficacy of drugs. Sodium alginate is a biodegradable, biocompatible and mucoadhesive polymer which is used for site specific drug delivery to mucosal tissues. At the present study alginate microparticles were fabricated by an emulsification technique and characterized. Selection of appropriate parameters enabled the preparation of microparticles with a mean volume diameter of 3 ± 0.7 μm, mass median aerodynamic diameter of 5.9 ± 0.33 μm, fine particle fraction of 13.9 ± 0.57% and encapsulation efficiency of 61 ± 4%. The in vitro release profile showed a slower release rate for microparticles compare to pure paclitaxel. Physiochemical characterization of paclitaxel via FT-IR, DSC and XRD techniques revealed information of solid state of paclitaxel loaded microparticles. The in vitro cytotoxicity activity of paclitaxel loaded microparticles was assessed using human non-small cell lung cancer cell lines (A549 and Calu-6). Results showed that exposure of cells to pure paclitaxel and paclitaxel loaded microparticles effectively inhibited the growth of A549 and Calu-6 cells similarly in a concentration- and time-dependent manner.