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Diroximel Fumarate-Loaded Solid Lipid Nanoparticles (DRF-SLNs) as Potential Carriers for the Treatment of Multiple
Debora Santonocito1,2, Giuliana Greco1,2, Maria Grazia Sarpietro1,2
1Department of Drug and Health Sciences, University of Catania, Viale Andrea Doria 6, 95125 Catania, Italy.
Abstract:
Diroximel fumarate (DRF) is an orally administered prodrug used in multiple sclerosis (MS) treatment. Although it exhibits better gastrointestinal (GI) tolerability than its analogues, many patients still discontinue therapy due to frequent GI adverse events. To overcome these limitations, alternative drug delivery systems that bypass the GI tract are needed. Direct nose-to-brain delivery represents a promising approach to circumvent the blood-brain barrier and target the central nervous system; however, limited nasal mucosal absorption and the small volume of the nasal cavity pose significant challenges. Solid lipid nanoparticles (SLNs) can potentially overcome these obstacles by enhancing drug bioavailability and protecting against enzymatic degradation. This research aimed to develop an innovative intranasal nanoformulation of DRF to improve brain targeting and patient compliance. DRF-loaded SLNs were prepared using a solvent-diffusion technique with stearic acid as the lipid phase and Poloxamer 188 as the surfactant. The obtained nanoparticles displayed favorable technological characteristics, with a mean diameter of 210 nm, a polydispersity index of 0.17, and a zeta potential of -36 mV, suggesting good long-term stability. Interactions between SLNs and biomembrane models (MLV) were also studied to elucidate their cellular uptake mechanism. Future work will focus on evaluating the in vivo efficacy of this novel nanoformulation.
Insights
This study developed novel intranasal Solid Lipid Nanoparticles (SLNs) for Diroximel fumarate (DRF) delivery to treat multiple sclerosis (MS). This approach aims to enhance brain targeting and improve patient compliance by bypassing gastrointestinal issues.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Neuroscience
Background:
- Diroximel fumarate (DRF) is an oral prodrug for multiple sclerosis (MS) treatment.
- Gastrointestinal (GI) adverse events limit patient compliance with DRF therapy.
- Alternative drug delivery systems are needed to bypass the GI tract and improve therapeutic outcomes.
Purpose of the Study:
- To develop an innovative intranasal nanoformulation of DRF.
- To enhance direct nose-to-brain delivery of DRF.
- To improve brain targeting and patient compliance for MS treatment.
Main Methods:
- Preparation of Diroximel fumarate-loaded Solid Lipid Nanoparticles (DRF-SLNs) using a solvent-diffusion technique.
- Characterization of nanoparticles for size, polydispersity index, and zeta potential.
- Investigation of SLN interactions with biomembrane models to understand cellular uptake.
Main Results:
- Successful development of DRF-loaded SLNs with a mean diameter of 210 nm.
- Nanoparticles exhibited a low polydispersity index (0.17) and a negative zeta potential (-36 mV), indicating good stability.
- Favorable characteristics suggest potential for enhanced nasal absorption and brain targeting.
Conclusions:
- Intranasal DRF-SLNs represent a promising strategy to overcome GI limitations of oral therapy.
- This nanoformulation may offer improved brain delivery and patient compliance for multiple sclerosis management.
- Further in vivo studies are warranted to confirm the efficacy of this novel nanoformulation.
