Farnaz Monajjemzadeh
1,2, Mahsa Bagheri
3, Seyed Hassan Montazam
4, Mitra Jelvehgari
4,5*1 Food and Drug Safety Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
2 Department of Pharmaceutical and Food Control, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
3 Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
4 Department of Microbiology, Bonab Branch, Islamic Azad University, Bonab, Iran.
5 Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
6 Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Abstract
Background: Selegiline hydrochloride (Sel) is a drug applied for
the therapy of early‐step Parkinson's disease. In usual clinical doses, it is
an elective irreversible MAO-B inhibitor.
This study intended to formulate mucoadhesive microspheres of selegiline
with the objective of improving the therapeutic efficacy, patient compliance
and bioavailability. Methods: The
microspheres were prepared by emulsion
solvent evaporation method (O1/ O2) using hydroxypropyl methylcellulose (HPMC).
In the current study, bucco‐adhesive
microspheres were prepared with different
drug to polymer ratios and characterized by encapsulation efficiency, particle
size, Differential Scanning Calorimetry (DSC), FTIR Fourier Transform Infrared Spectroscopy (FTIR), flowability, the degree of swelling and surface pH, mucoadhesive
character, retentive time, and drug release studies.
Results: The best
drug to polymer ratio in microspheres was 1:2 (as F1). The production yield
microspheres F1 showed production yield of 84.79%, mean particle size of 744.73
μm and loading efficiency of 53.33%. The DSC exhibited the property of selegiline loaded microspheres
changed to amorphous form. The FTIR spectrum proposed that the drug kept its
chemical stability during the
emulsification process. The results showed that the microspheres of F1 had
faster release than the microspheres of F2 (1:4), F3 (1:6), and commercial
tablet (p<0.05). The microspheres did not exhibit good retention time
properties (276.66‐329.66 min). The results of mucoadhesion strength (8.3‐18.3
g/cm2) and surface pH of discs (6.44‐6.97) showed the better characterization of microspheres in buccal.
Conclusion: The
formulations were found to be appropriate candidates for the improvement of
microspheres for the remedial objects.