A Novel Prednisolone-Loaded Layer-by-Layer Nanoparticles (LBL-NPs) for Rheumatoid Arthritis: Optimization and Therapeutic Evaluation

Abstract

Purpose

Rheumatoid arthritis (RA) is a chronic autoimmune disease associated with bone erosion, inflammatory joint disease, and long-term disability. In spite of traditional treatment, currently available therapies are challenged with several limitations such as systemic side effects, poor drug bioavailability, and frequent dosing, and therefore lead to reduced patient compliance.

Method

To addresses these challenges; this investigation focused on developing an optimized layer-by-layer (LBL) system of prednisolone acetate (PRD)-loaded nanoparticles (NPs) (LBL-PRD NPs) using the Box-Behnken design (BBD). The optimised LBL-PRD NPs (F18) were evaluated for mean hydrodynamic diameter (nm), zeta potential (ZP), scanning electron microscopy (SEM), atomic force microscopy (AFM), differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), in vitro drug release, collagen-induced arthritis (CIA), and radiological examinations on male Wistar rats.

Results

The outcome on entrapment efficiency (%EE) of 56.78 ± 2.52% and burst release (%BR) of 30.57 ± 1.63%. The drug had been successfully loaded into the NPs, exhibiting a spherical shape and physicochemical compatibility without any chemical interaction with the used polymers.

Conclusion

The prepared LBL-PRD NPs showed a longer residence time at the bloodstream, resulting in a prolonged therapeutic effect and inhibition of bone erosion and soft tissue swelling in the treated animals, which did not express any allergic reactions and skin alterations. This pioneered LBL-PRD NPs appears to be a promising, alternative, and effective nanodrug delivery system (NDDS) to treat effectively RA.