Pharmaceutical Sciences I. Lectures
Dr. Kovács, Andrea
Gedeon Richter Plc., Formulation R&D; University Pharmacy Department of Pharmacy Administration, Semmelweis University
06302492732
kovacs.andrea92@gmail.com
Stability Tracking of pH Modifier- or Solubilizer-Containing Furosemide-Loaded Electrospun Nanofibrous Systems
Andrea Kovács1,2; Adrienn Kazsoki2; Géza Jakab3; Balázs Démuth1,4; Bernadett, Szirányi1; Romána Zelkó2*
1 Gedeon Richter Plc., Formulation R&D, Gyömrői Street 19-21, H-1103 Budapest, Hungary
2 University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Street 7-9, H-1092 Budapest
3 Semmelweis University, Department of Pharmaceutics, Hőgyes Endre Street 7, Budapest H-1092, Hungary.
4 Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Budafoki út 8. 3, H-1103 Budapest, Hungary
Pharmaceutical Sciences I. Lectures
Hungarian
Pharmaceutical Sciences
Molecular Sciences
Introduction: Electrospun nanofibrous drug delivery systems are promising alternatives for enhanced solubility formulations of drugs belonging to BCS (Biopharmaceutical Classification System) IV class, like furosemide, by keeping the drug in an amorphous state.
Aims: This study aimed to compare solubiliser (triethanolamine, TEA) or pH modifier (sodium hydroxide)-containing furosemide-loaded electrospun nanofibers from the point of their macro- and microstructural properties during storage.
Methods: Two hydroxypropyl cellulose and poly(vinylpyrrolidone)-based formulations were prepared. Triethanolamine or sodium hydroxide was used for solubility improvement of furosemide. Accelerated stability test (T=40°C, RH=70%, 4 weeks) was performed. Morphological characterisation was carried out by scanning electron microscopy (SEM). X-ray diffraction spectroscopy (XRD) and Fourier-transform infrared spectroscopy (FTIR) were applied to investigate the amorphous or crystalline nature of furosemide in the electrospun samples. Small-volume dissolution test (pH 6.8, 37°C) was worked out to distinguish any difference in the drug release between the two formulations. The furosemide content was determined with UV-vis spectrophotometry at 277 nm wavelength.
Results: The SEM measurements showed similar morphology and fiber diameter distribution in case of the unstored samples. In TEA-containing electrospun samples widened and merged individual fibers appeared from the first week of storage, and along with the time it has become even more dominant. In contrast, the NaOH-containing samples remained the fibrous structure with some slight changes. The microstructural studies confirmed that the formulations contained furosemide in amorphous salt form, and it was preserved during the one-month storage in each case. The dissolution test showed rapid and complete drug release from the fibrous samples.
Conclusion: Amorphous furosemide salt-containing nanofibrous formulations were successfully prepared, which preserved the drug in its amorphous state during the one-month storage. Since the SEM measurements revealed significant differences, the NaOH-containing formulation can be more promising.
Supervisor: Romána Zelkó
E-mail address: zelko.romana@pharma.semmelweis-univ.hu
Szóbeli
Szabad
elfogadva
szóbeli
nem rendelkezett róla
4686
10:25
10:40
Andrea Kovács1,2; Adrienn Kazsoki2; Géza Jakab3; Balázs Démuth1,4; Bernadett, Szirányi1; Romána Zelkó2*
1 Gedeon Richter Plc., Formulation R&D, Gyömrői Street 19-21, H-1103 Budapest, Hungary
2 University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Street 7-9, H-1092 Budapest
3 Semmelweis University, Department of Pharmaceutics, Hőgyes Endre Street 7, Budapest H-1092, Hungary.
4 Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, Budafoki út 8. 3, H-1103 Budapest, Hungary