Open AccessGlibenclamide-Loaded Polyvinylpyrrolidone (PVP) Nanoparticles and Glibenclamide-Loaded Soluplus® Nanomicelles Intended for Parenteral Administration: Effect of Solvents Mixtures on the Electrosprayed Nanoparticles and In vitro Characterization
Author(s) -
Maryam Al-Ghezi,
Raghad F. Almilly,
Wedad K. Ali
Publication year - 2021
Publication title -
journal of pharmaceutical research international
Language(s) - English
Resource type - Journals
ISSN - 2456-9119
DOI - 10.9734/jpri/2021/v33i53a33657
Subject(s) - polyvinylpyrrolidone , glibenclamide , nanoparticle , bioavailability , materials science , polymer , drug delivery , drug , solvent , chemical engineering , nanotechnology , chemistry , pharmacology , organic chemistry , polymer chemistry , medicine , engineering , diabetes mellitus , endocrinology , composite material
Background and Objective: Glibenclamide (GB) is showing promising results in central nervous system (CNS) injuries treatment where intravenous administration of GB could overcome the oral limitations and assure maximum bioavailability. Dry powder of GB nanoparticles reconstituted for parenteral administration was prepared through electrospraying.
Methods: The drug was incorporated with two polymers, polyvinylpyrrolidone (PVP) and Soluplus® (SP), at ratios 1:4 and 1:2 (GB/polymer). Different solvent mixtures were used to formulate the particles. Physicochemical characteristics were investigated.
Results: The size of the GB-PVP nanoparticle ranged between (409-775) nm with a spherical, disk, fractured and, agglomerated morphology, while those of the GB-SP nanomicelles were of (447-785) nm with mostly irregular morphology, in consequence to the used solvents mixtures. The high encapsulation efficiency ≥ 98% reflects the well dispersed drug molecules within the polymer matrix, further confirmed by X-ray diffraction and infrared spectroscopy. GB-SP colloidal dispersions showed neutral zeta potentials with a cloud point of 36 ˚C, indicating prolonged circulation time and stability after parenteral administration. GB/SP nanomicelles at ratio 1:4 showed a sustained drug release reaching ≥ 94% in 36 hours.
Conclusion: The GB-SP nanomicelles with extended drug release and regarding physicochemical properties represent a remarkable drug delivery system for parenteral administration.