Polyethylene glycol-stabilized cationic liposome encapsulating glucosamine sulfate: A promising nanoformulation for osteoarthritis therapy

Abstract

Osteoarthritis (OA) is a common orthopedic chronic disease, and the use of nanomaterials as carriers is an effective way to realize slow and controlled release therapy for OA drugs. In this study, we synthesized a polyethylene glycol-stabilized bilayer-decorated cationic liposome (CLis) as a drug delivery system for delivering glucosamine sulfate (GS) drug to achieve the treatment of OA in rats. The CLis encapsulated with GS drug (GS-CLis) was prepared by a reverse evaporation method, and its physical properties, encapsulation rate, and drug release performance were evaluated. The biological properties of GS-CLis were evaluated in vitro. The therapeutic effect of GS-CLis on osteoarthritis was evaluated in vivo, and the in vivo biosafety of the drug was assessed by hematology, blood biochemistry, and hematoxylin-eosin staining. GS-CLis had a particle size of (236.28 ± 4.76) nm, a potential of (27.35 ± 4.86) mv, and a spherical shape. The encapsulation rate was (96.18 ± 5.77)% and the drug-loading capacity was (9.61 ± 0.28)%, which provided a good slow drug release. GS-CLis has low cytotoxicity, low hemolysis rate, and good biocompatibility. GS-CLis can more effectively alleviate joint surface damage and inhibit the expression of inflammatory factors, and has no significant effect on the body weight of rats, with good biological safety. In this study, we successfully synthesized novel GS-CLis for the treatment of OA, which improved the retention time and therapeutic effect of GS in OA and provided a research basis for its development as an OA nanoformulation.