Abstract Amyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disorder with limited treatment options, including riluzole, which is characterized by rapid clearance and low bioavailability. The objective of this investigation was to design, optimize, and characterize polymeric micelles (PMs) for riluzole delivery as a preliminary step toward enhanced brain targeting in ALS therapy. In order to optimize the polymer quantity and polymer/drug ratio, a central composite design was implemented, which assessed encapsulation efficiency (EE%), particle size, and drug loading (DL%). The results indicated that EE% was enhanced by lesser polymer concentrations, whereas EE% was initially reduced but subsequently increased by higher polymer/drug ratios. The optimized formulation (266.20 mg polymer, polymer/drug ratio of 5) achieved a particle size of 15.83 nm, EE% of 94.55%, and DL% of 16.89%. Field Emission Scanning Electron Microscope confirmed spherical micelles with a uniform size, and in vitro release studies showed sustained riluzole release. These findings showed PMs as a promising strategy to improve the riluzole delivery in ALS therapy.
Ghorbankhani et al. (Fri,) studied this question.