Nanoemulgel, an Innovative Carrier for Diflunisal Topical Delivery with Profound Anti-Inflammatory Effect: in vitro and in vivo Evaluation

Abstract

Purpose Rheumatoid arthritis is an autoimmune disorder that directly affects joints. However, other body organs including heart, eyes, skin, blood vessels and lungs may also be affected. The purpose of this study was to design and evaluate a nanoemulgel formulation of diflunisal (DIF) and solubility enhanced diflunisal (DIF-IC) for enhanced topical anti-inflammatory activity. Methodology Nanoemulsion formulations of both DIF and DIF-IC were prepared and incorporated in three different gelling agents, namely carboxymethylcellulose sodium (CMC-Na), sodium alginate (Na-ALG) and xanthan gum (XG). All the formulations were evaluated in term of particle size, pH, conductivity, viscosity, zeta potential and in vitro drug release. The formulation 2 (NE2) of both DIF and DIF-IC which expressed optimum release and satisfactory physicochemical properties was incorporated with gelling agents to produce final nanoemulgel formulations. The optimized nanoemulgel formulation was subjected to three different in vivo anti-inflammatory models including carrageenan-induced paw edema model, histamine-induced paw edema model and formalin-induced paw edema model. Results DIF-IC-loaded nanoemulgel formulations yielded significantly enhanced in vitro skin permeation than DIF-loaded nanoemulgel. The nanoemulgel formulation of DIF-IC formulated with XG produced improved in vivo anti-inflammatory activity. Conclusion It was recommended that DIF-IC-based nanoemulgel formulation prepared with XG could be a better option for effective topical treatment of inflammatory conditions.

Tamoxifen Citrate Containing Topical Nanoemulgel Prepared by Ultrasonication Technique: Formulation Design and In Vitro Evaluation

“…This indicates a non-Newtonian, pseudoplastic property with thixotropic behaviour for developed TAM-NEGs [ 42 , 43 ]. This is appropriate behaviour for pharmaceutical formulations designed for topical skin treatment [ 34 , 44 , 45 ].…”

Coriander (Coriandrum sativum L.) essential oil and oil-loaded nano-formulations as an anti-aging potentiality via TGFβ/SMAD pathway

“…CEONLC formulations were gelled using xanthan gum as a gelling agent according to the method described by 47 . For the preparation of the gel base of xanthan gum, 3 mg of the gum was added to 100 ml of deionized water and stirred continuously to form a gel base, followed by pH adjustment with triethanolamine.…”

Microemulsion Based Nanostructures for Drug Delivery

“…Also, a xanthan gum-based nanogel was designed and formulated as DDS for diflunisal (DIF) for topical antiinflammatory activity to treat rheumatoid arthritis. This nanogel showed an increased drug bioavailability and high drug release profile, ensured a modulate and localized drug effect by maintaining a higher degree of retention of payload, therefore providing a prolonged effect (Bashir et al, 2021). Hence, this approach can be an attractive alternative compared with conventional topical formulation or even a promising substitute to oral DDS.…”