Abstract
The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured lipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test the penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin penetration modeling methods. The formulations were characterized by laser diffraction, rheological measurements and microscopic examinations. Various in vitro methods were used to study drug release, diffusion and penetration. Two types of vertical Franz diffusion cells with three different membranes, including cellulose, Strat-M®, and heat separated human epidermis were used and compared to the Skin-parallel artificial membrane permeability assay (PAMPA) method. Results indicated that the nanostructured lipid carrier dispersion had to be gelified as soon as possible for proper stability. Both the Skin-PAMPA model and Strat-M® membranes correlated favorably with heat separated human epidermis in this research, with the Strat-M® membranes sharing the most similar drug permeability profile to an ex vivo human skin model. Our experimental findings suggest that even when the best available in vitro experiment is selected for modeling human skin penetration to study nanostructured lipid carrier gel systems, relevant in vitro/in vivo correlation should be made to calculate the drug release/permeation in vivo. Future investigations in this field are still needed to demonstrate the influence of membranes and equipment from other classes on other drug candidates.
Highlights
Topical and transdermal formulations are widely used for delivering drugs to the skin and underlying tissue, or through the skin for systemic action
The particle size of LID-nanostructured lipid carrier (NLC) stored at room temperature was the smallest (97 nm), and it was stable for three days (the values of d(0.5) and d(0.9) were below 200 nm)
Our results demonstrated that a novel Strat-M® synthetic membrane and the Skin-parallel artificial membrane permeability assay (PAMPA) method have the potential to be used as an early screening tool to select the best dermal lidocaine-loaded nanoformulation
Summary
Topical and transdermal formulations are widely used for delivering drugs to the skin and underlying tissue, or through the skin for systemic action. Topical formulations deliver the active pharmaceutical ingredients (APIs) into different layers of the skin, enabling several diseases to be prevented and/or cured. The beginning, duration and strength of the therapeutic effect depend on the efficacy of three consecutive processes: (1) The release of the API from the carrier system; (2) penetration/diffusion of the API into the stratum corneum or other skin layers; (3) exertion of a pharmacological effect at the target point. All these effects determine the safety-efficacy profile of a product [1,2,3]. For most skin problems or diseases, the target point is the stratum corneum, viable epidermis or dermis
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