Levofloksasinin pulmoner yolla uygulanmak üzere mikropartiküler kuru toz inhaler formülasyonlarının geliştirilmesi ve değerlendirilmesi
The aim of this work is to develop a dry powder inhaler formulations of lexofloxacin hemihydrate, which is one of the fluoroquinolones used for the treatment of respiratory tract infections. High doses of antibiotics have various undesirable side effects of systemic administration, so a need arised for treatments for targeting the lungs directly for reducing systemic side effects. The lung has some advantages in both local and systemic therapies, like large surface area, thin epithelial layer, high bioavailability, and high first-pass effect can be eliminated. Therefore, in our study, levofloxacin hemihydrate dry powder inhaler formulations had planned to be developed for pulmonary route. Microparticle formulations were prepared by multiple emulsion technique. Polymers that used for microparticle formulations are PLGA (poly (lactic-co-glycolic acid), and PCL (polycaprolactone), which were known as biocompatible and non-toxic. The effect of polymer type, ratio and amount of the organic solvent volume, external water phase volume, excipients that added to the external phase and organic phase, particle size and distribution, encapsulation efficiency, product yield, drug release profile, to microparticle properties was investigated. According to the results, F4 and F6 has been choosen as optimal formulations. In order to improve aerodynamic properties and prevent aggregation of microparticles, a physical mixture of selected formulations was prepared with Inhalac 70, Inhalac 120 and Inhalac 230. Determination of antimicrobial activity on the selected microparticle formulations was investigated. As result, the formulations have animicrobial effiency against tested microorganisms. The results obtained in our study showed that Levofloxacin hemihydrate microparticles with appropriate specifications were prepared.