Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases

Int J Mol Sci. 2023 Apr 29;24(9):8053. doi: 10.3390/ijms24098053.


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.

Keywords: Riluzole; dermal administration; drug delivery system; lipid nanoparticles; nanostructured lipid carriers; psoriasis.

MeSH terms

  • Drug Carriers
  • Drug Liberation
  • Humans
  • Lipids / pharmacology
  • Nanoparticles*
  • Nanostructures*
  • Particle Size
  • Riluzole / pharmacology
  • Skin / metabolism
  • Skin Diseases* / metabolism


  • Riluzole
  • Drug Carriers
  • Lipids