Physicochemical Characterization and In Vitro Activity of Poly(ε-Caprolactone)/Mycophenolic Acid Amorphous Solid...

Area of Science:

• Materials Science
• Pharmaceutical Science
• Biotechnology

Background:

• Mycophenolic acid (MPA) is an immunosuppressive drug with potential anti-cancer properties.
• Improving the bioavailability of poorly soluble drugs like MPA is crucial for effective therapeutic outcomes.
• Amorphous solid dispersions (ASDs) offer a promising strategy for enhancing drug solubility and bioavailability.

Purpose of the Study:

• To prepare and characterize amorphous solid dispersions (ASDs) of mycophenolic acid (MPA) in poly(ε-caprolactone) (PCL).
• To investigate the miscibility and specific interactions between MPA and PCL in the ASDs.
• To evaluate the in vitro drug release profile and preliminary anti-cancer efficacy of the MPA-PCL ASDs.

Main Methods:

• Differential Scanning Calorimetry (DSC) to assess miscibility via glass transition temperature (Tg) and melting point depression.
• Fourier Transform Infrared Spectroscopy (FTIR) to analyze specific intermolecular interactions.
• In vitro drug release studies to quantify MPA release over time.
• In vitro cell culture experiments to assess anti-cancer activity.

Main Results:

• Favorable inter-association interactions between MPA and PCL were confirmed by a negative interaction parameter from DSC.
• FTIR analysis supported the presence of specific interactions within the PCL/MPA blends.
• In vitro drug release demonstrated that over 70% of MPA was released by day three across all compositions.
• Preliminary cell culture studies indicated a reduction in cancerous cells when treated with MPA-containing scaffolds.

Conclusions:

• Amorphous solid dispersions of MPA in PCL can be successfully prepared, leading to enhanced bioavailability due to favorable interactions.
• The developed ASDs exhibit good in vitro drug release characteristics.
• MPA-loaded PCL scaffolds show potential for anti-cancer applications, warranting further investigation.