Formulation and optimization of nano lipid based oral delivery systems for arthritis

Abstract

Rheumatoid arthritis is an autoimmune disease characterized by chronic synovitis that leads to tissue dysfunction as well as loss of complete function. There are several synthetic NSAIDs, glucocorticoids and biological drugs that are commonly used to treat arthritis. These drugs have severe life‐threatening side effects. The use of a bioactive compound (Apigenin) could be an alternative to synthetic conventional delivery systems. It is a poorly water‐soluble drug having a wide range of pharmacological activities. It has been reported for potential anti‐inflammatory and anti-arthritic activity. In the present study, Apigenin (APG) solid lipid nanoparticles were prepared using the solid lipid (glyceryl mono stearate, GMS), surfactant (d ‐α‐Tocopheryl polyethylene glycol 1000 succinate, TPGS) and sonication time (ST). The optimized APG SLNs showed a particle size of 161.7 nm and encapsulation efficiency of 80.44 ± 4.11%. It was further coated with 0.1% w/v chitosan (APG‐CH‐SLNs) and showed the particle size, PDI and zeta potential of 185.4 nm, 0.45 + 26.7 mV, respectively. The significant (p < 0.001) enhancement in drug release, permeation and mucoadhesive study was observed after chitosan coating. The antioxidant study results depicted an increase in antioxidant property. Finally, the anti‐arthritic biochemical parameters revealed marked changes in the results in comparison to arthritic control animals. From the study, it was concluded that APG-loaded mucoadhesive lipid nanoparticles are an alternative to the synthetic oral delivery systems.