Amorphous solid dispersion of a binary formulation with felodipine and HPMC for 3D printed floating tablets

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery Systems

Background:

• Gastroretentive drug delivery aims to prolong drug residence time in the stomach for improved therapeutic efficacy.
• Amorphous solid dispersions (ASD) enhance the solubility and bioavailability of poorly soluble drugs.
• Three-dimensional printing (3DP) offers precise control over tablet architecture for tailored drug release profiles.

Purpose of the Study:

• To develop gastroretentive floating tablets using a combination of 3DP and ASD technologies.
• To investigate the formation of amorphous solid dispersions of felodipine in hydroxypropyl methylcellulose (HPMC) via hot melt extrusion (HME) and fused deposition modeling (FDM).
• To evaluate the drug release characteristics and buoyancy of the 3D printed tablets.

Main Methods:

• Solubility parameter estimation and molecular dynamics simulations to predict drug-polymer interactions.
• Fabrication of drug-loaded filaments using HME and 3D printed tablets using FDM.
• Physical characterization of filaments and tablets, including assessment of amorphous dispersion and density.
• In vitro drug release studies and buoyancy assessment over an 8-hour period.

Main Results:

• Successful formation of amorphous solid dispersion of felodipine within the HPMC matrix was confirmed.
• 3D printed tablets with low infill percentage exhibited low density, ensuring buoyancy throughout the drug release process.
• Sustained zero-order drug release kinetics were achieved from the gastroretentive system for over 8 hours.
• The developed 3DP tablets demonstrated effective gastroretentive properties and controlled drug release.

Conclusions:

• The combination of 3DP and ASD technologies is a promising approach for manufacturing advanced gastroretentive floating tablets.
• This study demonstrates the potential of 3DP for creating complex drug delivery systems with tailored release profiles.
• The developed formulation offers an effective strategy for improving the oral delivery of poorly soluble drugs requiring prolonged gastric residence time.