Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases

• Main Authors: Agudelo, M.G (Author), Bonilla, L. (Author), Espina, M. (Author), Esteruelas, G. (Author), Filgaira, I. (Author), García, M.L (Author), Gong, R.C (Author), Llorente, X. (Author), Lopez-Ramajo, D. (Author), Manils, J. (Author), Pujol, M. (Author), Sánchez-López, E. (Author), Soler, C. (Author)
• Format: Article
• Language: English
• Published: MDPI 2023
• Subjects: dermal administration; drug delivery system; lipid nanoparticles; nanostructured lipid carriers; psoriasis; Riluzole
• Online Access: View Fulltext in Publisher; View in Scopus

 Nanocarriers, and especially nanostructured lipid carriers (NLC), represent one of the most effective systems for topical drug administration. NLCs are biodegradable, biocompatible and provide a prolonged drug release. The glutamate release inhibitor Riluzole (RLZ) is a drug currently used for amyotrophic lateral sclerosis (ALS), with anti-proliferative effects potentially beneficial for diseases with excessive cell turnover. However, RLZ possesses low water solubility and high light-sensibility. We present here optimized NLCs loaded with RLZ (RLZ-NLCs) as a potential topical treatment. RLZ-NLCs were prepared by the hot-pressure homogenization method using active essential oils as liquid lipids, and optimized using the design of experiments approach. RLZ-NLCs were developed obtaining optimal properties for dermal application (mean size below 200 nm, negative surface charge and high RLZ entrapment efficacy). In vitro release study demonstrates that RLZ-NLCs allow the successful delivery of RLZ in a sustained manner. Moreover, RLZ-NLCs are not angiogenic and are able to inhibit keratinocyte cell proliferation. Hence, a NLCs delivery system loading RLZ in combination with natural essential oils constitutes a promising strategy against keratinocyte hyperproliferative conditions. © 2023 by the authors.