Microemulsion-Based Topical Hydrogels of Tenoxicam for Treatment of Arthritis

Abstract

Abstract. Tenoxicam (TNX) is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, backache and pain. However, prolonged oral use of this drug is associated with gastrointestinal adverse events like peptic ulceration, thus necessitating its development as topical formulation that could obviate the adverse effects and improve patient compliance. The present study was aimed at development of microemulsion-based formulations of TNX for topical delivery at the affected site. The pseudoternary phase diagrams were developed and microemulsion formulations were prepared using Captex 300/oleic acid as oil, Tween 80 as surfactant and n-butanol/ethanol as co-surfactant. Optimized microemulsions were characterized for drug content, droplet size, viscosity, pH and zeta potential. The ex vivo permeation studies through Laca mice skin were performed using Franz diffusion cell assembly, and the permeation profile of the microemulsion formulation was compared with aqueous suspension of drug and drug incorporated in conventional cream. Microemulsion formulations of TNX showed significantly higher (p<0.001) mean cumulative percent permeation values in comparison to conventional cream and suspension of drug. In vivo anti-arthritic and anti-inflammatory activity of the developed TNX formulations was evaluated using various inflammatory models such as air pouch model, xylene-induced ear edema, cotton pellet granuloma and carrageenaninduced inflammation. Microemulsion formulations were found to be superior in controlling inflammation as compared to conventional topical dosage forms and showed efficacy equivalent to oral formulation. Results suggest that the developed microemulsion formulations may be used for effective topical delivery of TNX to treat various inflammatory conditions.

Re-entrant DNA gels

“…The resulting material thus gels only in a limited T range centred around human body values, making it possibly promising for pre-clinical and clinical use to facilitate medical treatments and therapies. In addition, we envision applications of such gels in vaccines43 as antigen interacting adjuvant, in inflammation/arthritis44 or bone tissue restoration45 as support for cell migration and adhesion. Our results become particularly interesting for these applications in view of the fact that DNA interacts with RNA and/or proteins at specific oligonucleotides.…”

In vitro and ex-vivo evaluation of topical formulations designed to minimize transdermal absorption of Vitamin K1

“…One formulation was selected from each category. Viscosity of the vehicle is one of the factors that is speculated to affect the diffusion of the active ingredient and the release rate from the dosage form [ 18 , 19 ]. In this study we manipulated the lipid content and the lipid composition to create a wide range of viscosity among the compounded dosage forms.…”

Formulation and optimization of gentamicin hydrogel infused with tetracarpidium conophorum extract via Central composite design for topical delivery

“…2 In addition to the above characteristics, the soft and rubbery nature of hydrogels minimises irritation to surrounding tissue. Their highly porous structure which can easily be tuned by controlling the density of cross-links in the gel matrix and the affinity of the hydrogels for the aqueous environment in which they are swollen 3 is also an advantage. The porosity of hydrogels also permits loading of drugs into the gel matrix and subsequent drug release at a rate, which is dependent on the diffusion coefficient of the small molecule or macromolecule through the gel network.…”

“…The porosity of hydrogels also permits loading of drugs into the gel matrix and subsequent drug release at a rate, which is dependent on the diffusion coefficient of the small molecule or macromolecule through the gel network. 3 Tetracarpidium conophorum, commonly called the African walnut plant, whose ethanolic extract would make up the second component of the formulation of study, is a perennial climbing shrub 10 to 20 feet long, found growing wild in forest zones of sub-Sahara Africa, including Nigeria. Studies have shown that the African walnut possess some beneficial properties like antibacterial, 4 antioxidant 4,5 and immune-stimulating activities.…”