[Studies on baicalin ethylcellulose microspheres for intranasal administration]

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Materials Science

Background:

• Intranasal administration offers a non-invasive route for drug delivery to the brain and systemic circulation.
• Baicalin, a natural flavonoid, possesses various pharmacological properties but faces challenges in bioavailability.
• Developing effective drug carriers is crucial for enhancing baicalin's therapeutic potential.

Purpose of the Study:

• To prepare and characterize baicalin-loaded ethylcellulose microspheres for intranasal administration.
• To evaluate the in vitro release, powder properties, and ex vivo nasal permeability of the developed microspheres.
• To provide a foundation for in vivo pharmacokinetic studies of baicalin microspheres.

Main Methods:

• Solvent evaporation method for preparing baicalin ethylcellulose microspheres.
• Characterization using X-ray diffraction (XRD) and thermogravimetric analysis (TGA).
• Evaluation of powder flowability, in vitro drug release, and ex vivo nasal permeability.

Main Results:

• Microspheres were successfully prepared with good drug loading (33.31%) and entrapment efficiency (63.34%).
• XRD and TGA confirmed baicalin's crystalline form and successful incorporation into the ethylcellulose matrix.
• In vitro release showed sustained release from microspheres compared to pure baicalin, following the Higuchi-Pappas model.
• Ex vivo studies demonstrated a 1.56-fold increase in nasal permeability for microspheres compared to pure baicalin.

Conclusions:

• Baicalin ethylcellulose microspheres are a promising formulation for intranasal delivery.
• The microspheres exhibit favorable characteristics for drug release and enhanced nasal permeability.
• This formulation provides a solid basis for future in vivo pharmacokinetic investigations.