Ursolic acid rich Ocimum sanctum L leaf extract loaded nanostructured lipid carriers ameliorate adjuvant induced arthritis in rats by inhibition of COX-1, COX-2, TNF-α and IL-1: Pharmacological and docking studies

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.

Nanostructured lipid carriers (NLCs) as drug delivery platform: Advances in formulation and delivery strategies

“…Pharmacokinetic study revealed that elimination rate constant of intravenous lansoprazole solution was higher than NLC hydrogel indicating prolonged plasma residence and hence extended inhibition of gastric acid secretion. Recently, Ocimum sanctum L. leaf extract (rich in ursolic acid) loaded NLCs were prepared and evaluated for anti-inflammatory effect after topical application ( Ahmad et al 2018 ). NLCs showed excellent anti-arthritic activity when compared to standard marketed diclofenac gel.…”

Effects of solvent—solvent fractionation on the total terpenoid content and in vitro anti‐inflammatory activity of Serevenia buxifolia bark extract

“…Terpenoids of plant extracts have potent anti‐inflammatory activity (Prakash, 2017). Moreover, studies have suggested that ursolic acid (UA) is used as a promising molecule with anti‐inflammatory, analgesic, and potential anti‐arthritic activity and diabetes (Ahmad et al., 2018; Bacanlı, 2020). Ursolic acid, found in Citrus plants, is one of the important natural pentacyclic triterpenoid carboxylic acids (Ahmad et al., 2018; Mahlo & Eloff, 2014).…”

β-Sitosterol-loaded solid lipid nanoparticles ameliorate complete Freund’s adjuvant-induced arthritis in rats: involvement of NF-кB and HO-1/Nrf-2 pathway

“…Solid lipid nanoparticles (SLNs) are the most promising oral drug delivery carriers due to their long term stability, high drug-loading capacity, excellent biocompatibility, largescale production viability and long-term stability. Furthermore, previous researcher suggests that the SLN increased the intracellular drug delivery for anti-arthritic drugs (Arora et al, 2015;Ahmad et al, 2018). SLNs are a colloidal system primarily formulated of solid lipids.…”