Abstract
The aim of the present study was to investigate the nanoemulgel as transdermal delivery system for poorly water soluble drug, ketoprofen, in order to overcome the troubles associated with its oral delivery. Different nanoemulsion components (oil, surfactant, and cosurfactant) were selected on the basis of solubility and emulsification ability. Pseudoternary phase diagrams were constructed using titration method to figure out the concentration range of components. Carbomer 940 was added as gel matrix to convert nanoemulsion into nanoemulgel. Drug loaded nanoemulsions and nanoemulgels were characterized for particle size, TEM, viscosity, conductivity, spreadability, rheological behavior, and permeation studies using Wistar rat skin and stability studies. Transdermal permeation of ketoprofen from nanoemulgels was determined by using Franz diffusion cell. Nanoemulgel containing 6% oleic acid as oil, 35% Tween 80, and Transcutol P as surfactant cosurfactant mixture, 56.5% water, 2.5% drug, and 0.6% carbomer was concluded as optimized formulation (NG6). The ex vivo permeation profile of optimized formulation was compared with nanoemulsion and marketed formulation (Fastum). Nanoemulgel showed significantly higher (P<0.05) cumulative amount of drug permeated and flux along with lower lag time and skin retention than marketed formulation. Thus, the study substantiated that nanoemulgel formulation can be used as a feasible alternative to conventional formulations of ketoprofen with advanced permeation characteristics for transdermal application.
Highlights
Nanoemulsion is a promising tool for transdermal drug delivery and is defined as a dispersion consisting of oil, surfactant, cosurfactant, and aqueous phase, which is a single optically isotropic and thermodynamically stable liquid solution with a droplet diameter usually in range of 10–200 nm [1]
The incorporation of nanoemulsion into gel matrix can result in nanoemulgel which may be more relevant for transdermal application as compared to nanoemulsion
To develop a nanoemulsion system of ketoprofen for transdermal delivery, it should possess good solubility in the components of system, as only solubilized drug can permeate through the skin
Summary
Nanoemulsion is a promising tool for transdermal drug delivery and is defined as a dispersion consisting of oil, surfactant, cosurfactant, and aqueous phase, which is a single optically isotropic and thermodynamically stable liquid solution with a droplet diameter usually in range of 10–200 nm [1]. The aptness of nanoemulsion to increase the concentration gradient and thermodynamic activity towards skin along with permeation enhancement activity of its components makes the system expedient for transdermal delivery. The low viscosity of nanoemulsion constrains its application in transdermal delivery due to cumbersome use. Biocompatible gels having weak interaction with surfactants have already been explored to modify the rheological behavior of nanoemulsion [3]. Variant gel matrices such as carbomer 940, xanthan gum, and carrageenan have been exploited to increase the viscosity of nanoemulsion for transdermal delivery [4]. The incorporation of nanoemulsion into gel matrix can result in nanoemulgel which may be more relevant for transdermal application as compared to nanoemulsion
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