Encapsulation of Fluticasone Propionate and Salmeterol Xinafoate in Microparticles of Chitosan Derivative for COPD Treatment

Chronic obstructive pulmonary disease (COPD) is associated with an enhanced chronic inflammation of the airways caused by tobacco smoking, air pollution or genetic factors. Fluticasone propionate, a corticosteroid with high topi­cal activity and salmeterol xinafoate, a long-acting selective β₂-adrenoceptor agonist, are extensively used in COPD treatment. The main drawbacks of these pharmaceutical compounds are their high degree of crystallinity along with their hydrophobic nature. These problems, can be overcome through the inclusion of these compounds in polymeric microparticles aiming to their amorphization.

In the present study, chitosan was modified through a graft copolymerization with 2-hydroxyethyl acrylate. Microparticles of chitosan derivative were synthesized via ionic gelation technique and fluticasone propionate and salmeterol xinafoate were simultaneously enclosed in their interior in 10, 20 and 30% ratios. FTIR, X-ray diffraction, SEM and DLS measurements were conducted in order to characterize the microparticles while in vitro release studies were performed intending the assessment of the samples’ release behavior.

The successful formation of the microparticles was confirmed by FTIR while the absence of drugs’ crystallinity indicated their amorphization in the interior of the microparticles. SEM images depicted the spherical shaped particles while their actual size, which in any ratio was in micro scale, was measured through DLS. Finally, the enhancement of the in vitro release behavior of both active compounds was accomplished.

In conclusion, our results support the successful formulation of modified chitosan microparticles, the inclusion of both drugs in an amorphous state and the amelioration of their in vitro release behavior.

Acknowledgements:

Τhe author wishes to acknowledge co-funding of this research by European Union-European Regional Development Fund and Greek Ministry of Education, Research and Religions/EYDE-ETAK through program EPANEK 2014-2020/Action “EREVNO-DIMIOURGO-KAINOTOMO” (project Τ1ΕΔΚ-02667).