Rutin and Scopoletin Co-Loaded Niosomes for Intranasal Brain Delivery: Formulation Optimization and Ex Vivo...

Area of Science:

• Pharmacology and Drug Delivery
• Natural Product Chemistry
• Nanotechnology

Background:

• Rutin (R) and scopoletin (S) are natural flavonols with potential health benefits, including cardiovascular protection and anti-inflammatory effects.
• Poor solubility and low oral bioavailability limit the therapeutic efficacy of R and S.
• Niosomes are lipid-based drug delivery systems that can enhance the solubility and bioavailability of poorly soluble compounds.

Purpose of the Study:

• To develop and optimize niosomes encapsulating rutin and scopoletin (RS-Ns-Opt).
• To evaluate the physicochemical properties, drug release, antioxidant activity, and in vitro permeation of RS-Ns-Opt.
• To assess the potential of RS-Ns-Opt for improving the bioavailability of R and S.

Main Methods:

• RS-Ns-Opt were prepared using the thin-film hydration method.
• Characterization included vesicle size, polydispersity index (PDI), entrapment efficiency, drug release studies, DPPH assay for antioxidant activity, and confocal laser scanning microscopy (CLSM).
• Ex vivo nasal mucosa permeation studies were conducted to assess drug penetration.

Main Results:

• Optimized niosomes (RS-Ns-Opt) exhibited nanosize vesicles (55.22 nm) with good uniformity (PDI=0.234).
• High entrapment efficiency for both rutin (72.64%) and scopoletin (72.44%) was achieved.
• RS-Ns-Opt demonstrated significantly improved drug release (79.96%) and antioxidant activity (70.11%) compared to the rutin-scopoletin suspension.

Conclusions:

• The developed RS-Ns-Opt formulation effectively improved the solubility and bioavailability of rutin and scopoletin.
• CLSM studies confirmed superior penetration of RS-Ns-Opt compared to the control.
• RS-Ns-Opt holds promise for enhanced therapeutic applications in healthcare due to improved drug delivery.