Abstract
Background: In intra-articular drug delivery, there are number of shortcomings such as lymphatic drainage from the synovial cavity, frequent dosing, adverse side effects and patient discomfort in the management of osteoarthritis (OA).Purpose: This research work reports the development and characterization of aceclofenac-loaded chondroitin sulfate (CS) conjugated (CS-SLN) and unconjugated solid lipid nanoparticles (SLN) for the effective management of OA.Methods: The SLNs were prepared using modified solvent injection method and coupled with CS. They were further characterized for size and size distribution, zeta potential, surface morphology, % entrapment efficiency and in vitro drug release profile. Anti-inflammatory activity and in vivo performance was also predicted.Results: The particle size of the SLN and CS-SLN was found to be 143.4 ± 0.9 nm and 154.2 ± 1.1 nm, respectively. SLNs exhibited sustained drug release (SLN, 64.25 ± 0.75%; CS-SLN, 57.82 ± 0.62%) in vitro for more than 24 h. In vivo performance studies revealed the highest uptake of SLNs by the knee joint.Discussion: SLNs enhanced accumulation at the knee joint due to specific interactions with CD44, annexin and leptin receptors attributed to CS coupling.Conclusion: CS-SLN could be potentially effective vector for the treatment or management of OA.
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