Abstract
The aim of this study was to prepare nanostructured lipid carriers (NLC)-based topical gel of aceclofenac for the treatment of inflammation and allied conditions. Stearic acid as the solid lipid, oleic acid as the liquid lipid, pluronic F68 as the surfactant, and phospholipon 90G as the co-surfactant were used. NLCs were prepared by melt-emulsification, low-temperature solidification, and high-speed homogenization methods. Characterization of the NLC dispersion was carried out through particle size analysis, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and an in vitro release study. The anti-inflammatory effect of the NLC gel was assessed by the rat paw edema technique and compared to marketed aceclofenac gel. The NLC dispersions exhibited d90% between 233 nm and 286 nm. All of the NLC showed high entrapment efficiency ranging from 67% to 82%. The particle size of NLC was further confirmed by the SEM study. The result of DSC showed that aceclofenac was dispersed in NLC in an amorphous state. Both the entrapment and release rate were affected by the percentage of oleic acid, but the method of preparation affected only the entrapment efficiency. The nanoparticulate dispersion was suitably gelled and assessed for in vitro permeation. Finally, NLC-based gels were found to possess superior (almost double) the anti-inflammatory activity compared to the marketed product. The anti-inflammatory activity of NLC gel showed a rapid onset of action, as well as a prolonged duration of action as compared with the marketed gel.
Highlights
Nanostructure lipid carriers (NLC) are the new generation of lipid nanoparticles, attracting major attention as novel colloidal drug carriers for topical use
Stearic acid was selected as the solid lipid for the formulation of NLC because stearic acid has more potential to solubilize the aceclofenac as compared to the other two lipids
Followed by Dunnett’s t-test at p < 0.05. This present work indicates that the NLCs of aceclofenac could be successfully prepared by the melt-emulsification and high-speed homogenization methods
Summary
Nanostructure lipid carriers (NLC) are the new generation of lipid nanoparticles, attracting major attention as novel colloidal drug carriers for topical use. Observed disadvantages of SLN include limited drug-loading capacity, drug expulsion during storage, and relatively high water content in the dispersions (70–99.9%) [2, 3]. As compared to SLN, NLC have a higher drug-loading capacity for a number of active compounds, and avoid or minimize potential expulsion of active compounds during storage [2]. For a number of drugs, the solubility of liquid lipid is higher than that of solid lipid, which enhances drug-loading [4]. NLC possess numerous features that are advantageous for the topical route of application. These carriers are composed of physiological and biodegradable lipid, exhibiting low systemic toxicity and low cytotoxicity [5]. The small size of lipid particles ensure close contact to the stratum corneum and can enhance drug flux through the skin, and due to their solid lipid matrix, a controlled release from these carriers are possible [5, 6]
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