Enhanced Apigenin Dissolution and Effectiveness Using Glycyrrhizin Spray-Dried Solid Dispersions Filled in 3D-Printed...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biotechnology

Background:

• Apigenin (APN) has demonstrated therapeutic potential, particularly in cancer treatment, but suffers from poor solubility and bioavailability.
• Developing advanced drug delivery systems is crucial to enhance apigenin's therapeutic efficacy.

Purpose of the Study:

• To prepare glycyrrhizin-apigenin spray-dried solid dispersions and 3D-printed tablets (printlets) to enhance apigenin's dissolution and therapeutic effects.
• To evaluate the physicochemical properties, in vitro dissolution, biological activities, and stability of the developed formulations.
• To assess the potential of these advanced formulations for colon cancer treatment.

Main Methods:

• Preparation of glycyrrhizin-apigenin solid dispersions using spray-drying technique.
• Development of PVA filament-based 3D printlets incorporating the solid dispersions.
• Physicochemical characterization including FTIR, Powder-XRD, DSC, and flow property analysis.
• In vitro dissolution studies, antioxidant, cytotoxicity, and antimicrobial assays.
• Stability studies according to ICH guidelines.

Main Results:

• Spray-dried solid dispersions (APN1-APN3) were successfully prepared with high yields and drug content.
• The amorphous transformation of apigenin was confirmed, leading to improved flow properties in the APN2 formulation.
• APN2 exhibited significantly enhanced in vitro dissolution (94.65% release), improved dissolution efficiency, and controlled release characteristics.
• Enhanced antioxidant, superior cytotoxicity against HCT-116 colon cancer cells, and increased antimicrobial activity were observed for APN2.
• The APN2 formulation demonstrated good stability over 90 days, meeting ICH requirements.

Conclusions:

• Glycyrrhizin-apigenin solid dispersions and 3D-printed printlets represent a promising approach to enhance apigenin's dissolution and bioavailability.
• The APN2 formulation displayed superior physicochemical, dissolution, and biological properties, indicating enhanced therapeutic potential.
• The developed 3D printlet technology offers a novel platform for improved drug delivery and effective colon cancer treatment.