Improvement of lidocaine skin permeation by using passive and active enhancer methods

Lidocaine is generally recognized and preferred for local anaesthesia, but in addition, studies have described additional benefits of lidocaine in cancer therapy, inflammation reduction, and wound healing. These properties contribute to its increasing importance in dermatological applications, and not only in pain relief but also in other potential therapeutic outcomes. Therefore, the purpose of our study was to enhance lidocaine delivery through the skin.

A stable nanostructured lipid carrier (NLC), as a passive permeation enhancer, was developed using a 2³ full factorial design. The nanosystems were characterized by crystallinity behaviour, particle size, zeta potential, encapsulation efficiency measurements, and one of them was selected for further investigation. Then, NLC gel was formulated for dermal application and compared to a traditional dermal ointment in terms of physicochemical (rheological behaviour) and biopharmaceutical (qualitative Franz diffusion and quantitative Raman investigations) properties.

The study also examined the use of 3D printed solid microneedles as active permeation enhancers for these systems, offering a minimally invasive approach to enhance transdermal drug delivery. By actively facilitating drug permeation through the skin, microneedles can complement the passive transport achieved by NLCs, thereby providing an innovative and synergistic approach to improving lidocaine delivery.

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Materials

Lidocaine and macrogol 400 were obtained from Hungaropharma Ltd. Apifil ® (PEG-8 Beeswax) was provided by Gattefossé (St. Priest Cedex, France). Miglyol® 812 (caprylic/capric triglyceride) was from Sasol GmbH (Hamburg, Germany). Kolliphor® RH40 (PEG-40 hydrogenated castor oil) was kindly supplied by BASF SE Chemtrade GmbH (Ludwigshafen, Germany). Acetonitrile (high-performance liquid chromatography [HPLC] grade), and H3PO4 (85 %) (analytical grade) were purchased from VWR Int Ltd (Radnor, PA, USA). Carbopol 971P NF was supplied by Azelis Ltd (Budapest, Hungary). Purified water (HPLC grade) produced with a TKA Smart2Pure system (TKA GmbH, Niederelbert, Germany) was used to prepare all the formulations. Purified and deionized water was used (Milli-Q system, Millipore, Milford, MA, USA). High Temp V2 resin (Formlabs, Somerville, Massachusetts, USA) was obtained from Dental Plus Kft. (Sopron, Hungary). Isopropyl alcohol (IPA) was acquired from Molar Chemicals (Halásztelek, Hungary). Human skin was acquired from a Caucasian female patient who underwent an abdominal plastic surgery procedure at the University of Szeged, Department of Dermatology and Allergology. The investigations were performed with the approval of the Hungarian Medical Research Council (ETT-TUKEB, registration number: BMEÜ/2339–3/2022/EKU).

Feria Hasanpour, Mária Budai-Szűcs, Anita Kovács, Rita Ambrus, Orsolya Jójárt-Laczkovich, Martin Cseh, Zsolt Geretovszky, Ferhan Ayaydin, Szilvia Berkó, Improvement of lidocaine skin permeation by using passive and active enhancer methods, International Journal of Pharmaceutics, Volume 660, 2024, 124377, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2024.124377.

Improvement of lidocaine skin permeation by using passive and active enhancer methods

Materials

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