Diacerein-Loaded Hyaluosomes as a Dual-Function Platform for Osteoarthritis Management via Intra-Articular Injection:...

Area of Science:

• Biomaterials Science
• Pharmacology
• Rheumatology

Background:

• Osteoarthritis (OA) management often involves intra-articular injections.
• Developing effective drug delivery systems for OA is crucial.

Purpose of the Study:

• To develop novel intra-articular injectable hyaluronic acid gel-core vesicles (hyaluosomes) loaded with diacerein (DCN).
• To evaluate the efficacy of DCN-loaded hyaluosomes in an in vivo rat model of arthritis.

Main Methods:

• A full factorial design was used to optimize formulation parameters.
• Diacerein (DCN) was loaded into hyaluronic acid hyaluosomes.
• In vitro characterization included entrapment efficiency, particle size, and zeta potential.
• Transmission Electron Microscopy (TEM) was used for morphology analysis.
• In vivo efficacy was assessed in antigen-induced arthritis in rats, measuring cartilage damage and plasma inflammatory markers (TNF-α, IL-1β).

Main Results:

• Optimized DCN-loaded hyaluosomes achieved high entrapment efficiency (90.7%) and small particle size (310 nm).
• TEM confirmed spherical vesicles with a hyaluronic acid core.
• Intra-articular injection of DCN-loaded hyaluosomes significantly prevented cartilage deterioration and inflammation in rats.
• Treated rats showed significantly lower plasma levels of TNF-α and IL-1β compared to untreated controls.

Conclusions:

• Developed DCN-loaded hyaluosomes represent a promising novel intra-articular injection for osteoarthritis management.
• The hyaluosomes demonstrated superior in vivo efficacy in reducing inflammation and protecting cartilage.
• This formulation offers a potential advancement in OA treatment strategies.