MicroS4pMDI is a research project aiming in the production of an innovative extended-release inhalation product of the active compounds Fluticasone Propionate and Salmeterol Xinafoate, for their prolonged administration for a period of 2 days, in patients suffering from Chronic Obstructive Pulmonary Disease (COPD). The program started in 4/6/2018 and was successfully completed in 3/3/2021. In the context of the present project, the production of 3 derivatives of chitosan was performed. More specifically, the macromolecular structure of chitosan was modified with trans aconitic acid, succinic anhydride and 2-hydroxyethyl acrylic ester. Microparticles of appropriate size (1-6 μm) of neat chitosan as well as of the new derivatives were prepared according to ionic gelation technique. Multiple benefits arise from the preparation of the drug-loaded polymeric microparticles. The optimum concentration of the two drugs was retained for prolonged time while owed to the innovative design of the product with the simultaneous inclusion of the two drugs in the polymeric microparticles, the formation of the crystalline structure is prevented. The two active compounds were entrapped in their amorphous phase leading to an increase of their solubility along with their bioavailability leading to a final product with optimum pharmacological characteristics, suitable for inhaled administration.
This project was co-funded 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”. The whole project was performed in collaboration with Medicair Bioscience S.A., a rapidly growing company, manufacturing and distributing generic medicines in a broad range of categories, specialized in the production of MDI inhalers.
Through this project, Bikiaris lab had the opportunity to have a strong collaboration with the industry combining academic research with its direct application in industry. Furthermore, during the present project new researchers had the opportunity to work on the field of pharmaceutical applications.
The results of the present project were published in 1 publication in an international paper (Molecules) as well as in 7 poster presentations in 5 international conferences.
Publication:
N.M. Ainali, E. Xanthopoulou, G. Michailidou, A. Zamboulis, D. Bikiaris Microencapsulation of Fluticasone Propionate and Salmeterol Xinafoate in modified chitosan nanoparticles for release optimization. Molecules (2020), DOI: 10.3390/molecules25173888.
Poster Presentations at international conferences:
G. Michailidou, S. Nanaki, D. Bikiaris Chitosan nanoparticles containing salmeterol xinafoate for respiratory use. 12th Hellenic Polymer Society International Conference (POLYCONF12), Ioannina, Greece 30 September-3 October 2018
G. Michailidou, N.M. Ainali, E. Xanthopoulou, D. Bikiaris Preparation and characterisation of modified chitosan with succinic anhydride and trans aconitic acid. 3rd Milan Polymer Days Congress (MIPOL2019), Milan, Italy 11-13 March 2019
G. Michailidou, N.M. Ainali, E. Xanthopoulou, D. Bikiaris Preparation of salmeterol xinafoate chitosan nanoparticles for chronic obstructive pulmonary disease treatment. 3rd Milan Polymer Days Congress (MIPOL2019), Milan, Italy 11-13 March 2019
G. Michailidou, N.M. Ainali, E. Xanthopoulou, D. Bikiaris Modified with trans aconitic acid chitosan nanoparticles containing fluticasone propionate. European Polymer Congress 2019 (EPF 2019), Hersonissos Heraklion Crete, Greece, 9-14 June 2019
E. Xanthopoulou, G. Michailidou, N.M. Ainali, D. Bikiaris Synthesis and characterization of modified with succinic anhydride chitosan nanoparticles containing salmeterol xinafoate. European Polymer Congress 2019 (EPF 2019), Hersonissos Heraklion Crete, Greece, 9-14 June 2019
G. Michailidou, N.M. Ainali, E. Xanthopoulou, D. Bikiaris Formulation of chitosan microparticles containing fluticasone propionate and salmeterol xinafoate as a method for COPD treatment. 7th International Conference on Biobased and Biodegragable Polymers (BIOPOL-2019), Stockholm, Sweden, 17-19 June 2019
G. Michailidou, N.M. Ainali, E. Xanthopoulou, D. Bikiaris Encapsulation of fluticasone propionate and salmeterol xinafoate in microparticles of chitosan derivative for copd treatment. The First International Conference on “Green” Polymer Materials 2020 (CGPM 2020), online, 5-25 November 2020
