Abstract
BackgroundUrsolic acid (UA) is a promising molecule with anti-inflammatory, analgesic and potential anti-arthritic activity.MethodsThis study was undertaken to make formulation and evaluation of Ocimum sanctum L. leaf extract (OLE) loaded nano-structured lipid carriers (OLE-NLCs) for improved transdermal delivery of UA. Different surfactants, solid lipids and liquid lipids were used for the preparation of NLCs. The NLCs were developed using emulsion solvent diffusion and evaporation method. Different physicochemical properties, entrapment efficacy, in vitro release evaluation, and ex vivo permeation studies of the prepared NLCs were carried out. The in vivo anti-arthritic activity of OLE-loaded NLC gel and control gel formulation (OLE free NLC gel) against Complete Freund's Adjuvant (CFA) induced arthritis in wister albino rats was also carried out.ResultsOLE-NLCs were composed of spherical particles having a mean particle size of ~120 nm, polydispersity index of ~0.162 and zeta potential of ~ -27 mV. The high entrapment efficiency (EE) of UA ~89.56% was attained. The in vitro release study demonstrated a prolonged release of UA from the NLCs up to 12 h. The developed formulation was found to be significantly better with respect to the drug permeation amount with an enhancement ratio of 2.69 as compared with marketed formulation. The in vivo biological activity investigations, studies showed that the newly prepared NLCs formulation of OLE showed excellent anti-arthritic activity and the results were found at par with standard marketed diclofenac gel for its analgesic and anti-arthritic activities. These results were also supported by radiological analysis and molecular docking studies.ConclusionThe overall results proved that the prepared OLE-NLCs were very effective for the treatment of arthritis and the results were found at par with standard marketed the standard formulation of diclofenac gel.
Highlights
Rheumatoid arthritis (RA) is a most common chronic inflammatory disease of an autoimmune origin
Ursolic acid rich Nanostructured lipid carriers (NLCs) ameliorate adjuvant induced arthritis generation; solid lipid nanoparticles (SLNs) [26,27]
The Lamarckian genetic algorithm (LGA) search parameter was stimulated to activate the ligand-protein with one hundred simulations runs, Ursolic acid rich NLCs ameliorate adjuvant induced arthritis with three hundred population size
Summary
Rheumatoid arthritis (RA) is a most common chronic inflammatory disease of an autoimmune origin. According to the Centers for Disease Control and Prevention (CDC) data on arthritis in the United States; it has been reported that 54.4 million U.S adults (approximately 25% of the total adult population) are suffering from arthritis These figures of arthritis in adults are expected to increase up to 67 million by 2030. The total figures of doctor-diagnosed arthritis is projected to reach up to 78.4 million adults (25.9% of all adults) and the arthritis-attributable activity limitation in adults is expected to increase to 34.6 million (11.4% of all adults) by 2040 [1,2] These data indicated that arthritis is a serious disorder which might be more prevalent than other known diseases like diabetes, cancer and AIDS. It is said that RA has resulted from cardiovascular diseases In another recently conducted study in Saudi Arabia, the prevalence of hyperlipidemia in patients suffering from RA and its relationship with C-reactive protein level was investigated. Ursolic acid (UA) is a promising molecule with anti-inflammatory, analgesic and potential anti-arthritic activity
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