Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases

Area of Science:

• Pharmaceutical Sciences
• Nanotechnology
• Dermatology

Background:

• Nanostructured lipid carriers (NLCs) are effective for topical drug delivery due to biodegradability and sustained release.
• Riluzole (RLZ), a glutamate release inhibitor for ALS, has anti-proliferative properties beneficial for conditions with excessive cell turnover.
• Riluzole exhibits poor water solubility and high light sensitivity, limiting its topical application.

Purpose of the Study:

• To develop and optimize Riluzole-loaded NLCs (RLZ-NLCs) for enhanced topical drug delivery.
• To evaluate the physicochemical properties, in vitro release, and biological activity of RLZ-NLCs.
• To assess the potential of RLZ-NLCs as a topical treatment for keratinocyte hyperproliferative conditions.

Main Methods:

• RLZ-NLCs were prepared using the hot-pressure homogenization method with essential oils as liquid lipids.
• The design of experiments approach was employed for NLC optimization.
• Physicochemical characterization included particle size, surface charge, and entrapment efficacy. In vitro release studies and anti-angiogenesis and anti-proliferation assays were performed.

Main Results:

• Optimized RLZ-NLCs exhibited desirable properties for dermal application: mean size below 200 nm, negative surface charge, and high RLZ entrapment efficacy.
• In vitro studies confirmed sustained Riluzole release from the NLCs.
• RLZ-NLCs demonstrated no angiogenic potential and effectively inhibited keratinocyte proliferation.

Conclusions:

• Optimized RLZ-NLCs provide a stable and effective system for sustained topical delivery of Riluzole.
• The combination of Riluzole and NLCs, utilizing natural essential oils, presents a promising therapeutic strategy for hyperproliferative keratinocyte conditions.
• This NLC-based delivery system addresses Riluzole's limitations and offers a novel approach for dermatological treatments.