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

• Published in: International journal of pharmaceutics Vol. 660; p. 124377
• Main Authors: Hasanpour, Feria, Budai-Szűcs, Mária, Kovács, Anita, Ambrus, Rita, Jójárt-Laczkovich, Orsolya, Cseh, Martin, Geretovszky, Zsolt, Ayaydin, Ferhan, Berkó, Szilvia
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 20-07-2024
• Subjects: 3D printed microneedles; Administration, Cutaneous; Anesthetics, Local - administration & dosage; Anesthetics, Local - chemistry; Anesthetics, Local - pharmacokinetics; Animals; Dermal drug delivery; Drug Carriers - chemistry; Drug Delivery Systems - methods; Gels; Human skin; Lidocaine; Lidocaine - administration & dosage; Lidocaine - chemistry; Lidocaine - pharmacokinetics; Lipids - chemistry; nanostructured lipid carriers (NLCs); Nanostructures - administration & dosage; Nanostructures - chemistry; Needles; Particle Size; Permeability; Skin - metabolism; Skin Absorption - drug effects; Swine; 3D printed microneedles; Human skin; Lidocaine; Dermal drug delivery; nanostructured lipid carriers (NLCs)
• ISSN: 0378-5173; 1873-3476; 1873-3476
• DOI: 10.1016/j.ijpharm.2024.124377

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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.