Optimization Performance and Physical Stability of Ciprofloxacin HCL-Ca Alginate Microspheres: Effect of Different Concentration of Alginate and CaCl2

Abstract

Inhalation treatment using antibiotics is an alternative for lung delivery. However, the therapeutic efficacy of inhaled drugs is limited by their rapid clearance in the lungs. Sustained release systems in the lungs can improve therapeutic outcomes of drugs because they can retain the drug load within the lungs and progressively release the drug locally at therapeutic levels. This study presents the formulation strategies to control drug release in the lungs using an alginate polymer-based microspheres system. The microsphere’s composition can be adjusted to modulate release and can encapsulate compounds with high loading. The pulmonary route is commonly used and has been well accepted as a portal for non-invasive drug delivery for many lung diseases. It is explored for decades as an alternative for systemic as well as local drug delivery. The present study explored the in vitro benefits of ciprofloxacin encapsulated in alginate microspheres. The studies included size, morphology, yield, drug loading, and encapsulation efficiency as well as stability. Current results showed small, smooth, and spherical ciprofloxacin-alginate microspheres were produced using aerosolization techniques. Small particles of less than 5μm were formed, which suitable for inhalation particles for lung delivery. High entrapment efficiency up to 95%, loadings of 80%, and a yield of 89% were also showed from microspheres. It was confirmed that all microspheres were stably indicated by no significant changes in morphology, organoleptic, and drug content after 30 days of storage. The recent promising characteristics of microspheres for pulmonary delivery will need further evaluation of the potency against microorganisms in lung disease.