Title : Noval transdermal nanoemulgel of oxaprozin with apricot kernel oil: A promising approach for osteoarthritis management
Abstract:
Osteoarthritis (OA) is one of the most common forms of degenerative joint disease and a major cause of pain and disability affecting the aging population. It is estimated that more than 20 million Americans and 35 to 40 million Europeans suffer from OA. Analgesics and non-steroidal anti- inflammatory drugs (NSAIDs) are the only therapeutic treatment options for OA. The aim of my work is to develop a transdermal delivery system consisting of Oxaprozin and Apricot oil nanoemulgel. The system is intended to reduce inflammation and pain caused by osteoarthritis. The Nanoemulsion was formulated by spontaneous emulsification method using Apricot kernel oil as an oil phase, and a mixture of Tween 80 and polyethylene glycol 400 as a surfactant and co-surfactant, respectively. Their combination was optimized using a three-factor Central Composite Design (CCD). The optimized Oxaprozin loaded Nanoemulsion had a globule size of 165.56 ± 5.97 nm, PDI 0.2479 ± 0.045, zeta potential -9.754 ± 0.241, respectively. The optimized Oxaprozin loaded Nanoemulsion was then incorporated in (1% w/w) Carbopol gel. The Nano-emulgel exhibited a good spreadability, extrudability and texture profile. The in-vitro release study demonstrated a sustained Oxaprozin release for 24 h from the Nanoemulgel that followed the Higuchi kinetic model (R2 = 0.9901) with a Fickian diffusion mechanism. While, conventional gel followed the first order release model (R2 = 0.9050). In ex-vivo permeability study, the drug permeation flux observed for Oxaprozin from Nano-emulgel (236.90 μg/cm2/h) was much higher compared to Conventional gel (128.73 μg/cm2/h). The confocal laser scanning microscopy studies confirmed enhanced depth of permeation (from 20 μm to 45 μm) for developed Nano-emulgel. In-vivo study performed on wistar rat, skin irritation study revealed that there was no irritation was reported upon topical application of Nanoemulgel. Immunohistochemistry Staining (IHC) of TNF-a and IL-6 of knee also demonstrated that Oxaprozin Nano-emulgel significantly decreases the TNF-a and IL-6 concentration in knee joint as compared to marketed formulation and conventional gel. Based on these findings, it was concluded that Oxaprozin Nano-emulgel is a promising combinatorial treatment approach for osteoarthritis.
