Oral bioavailability enhancement through supersaturation: an update and meta-analysis

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery
• Biopharmaceutics

Background:

• Poorly water-soluble compounds pose challenges in drug discovery.
• Supersaturating drug delivery systems (SDDS) are increasingly explored for bioavailability enhancement.
• A systematic, quantitative review of SDDS performance is lacking.

Purpose of the Study:

• To quantitatively assess the promise of SDDS for bioavailability enhancement.
• To compare the performance of different types of SDDS.
• To identify promising drug candidates for SDDS development.

Main Methods:

• Systematic literature search of Medline and Embase (2010-2015).
• Meta-analysis, box-plots, and correlation plots of retrieved data.
• Comparison of four SDDS types: amorphous solid dispersions, nano-drug systems, supersaturable lipid-based formulations, and silica-based systems.

Main Results:

• SDDS formulations show promise for enabling drug development.
• Performance varied across different SDDS types.
• Predicting in vivo performance from in vitro testing remains a challenge.

Conclusions:

• SDDS are a promising approach for improving bioavailability of poorly soluble drugs.
• Further research is needed to develop predictive tools for SDDS performance.
• A shift towards mechanistic insight-guided development is recommended.