Polymeric Precipitation Inhibitor As an Effective Trigger to Convert Supersaturated Into Supersaturable State In Vivo

Abstract

The supersaturated state of the drug in vivo is thermodynamically unstable resulting in a delayed response and reduced efficacy. The use of polymeric precipitation inhibitor (PPI) has been demonstrated as an effective trigger for the conversion of supersaturated state to supersaturable state for improving solubilization, thermodynamic maintenance of drug concentration and oral absorption of poorly water-soluble compounds. PPI retards drug precipitation and provides a kinetically stabilized supersaturation state for an extended period in gastric and intestinal fluids. However, the selection of appropriate PPI and understanding its mechanism is a challenge for formulating a stable pharmaceutical formulation. The present review is aimed at understanding the intricacies of selecting PPIs and their applications in pharmaceutical formulations.

Keywords:

• bioavailability
• permeability
• polymeric precipitation inhibitors
• precipitation
• solubility
• supersaturated state
• supersaturation

Acknowledgments

The authors are highly thankful to all the scientists for critical assessment of case studies of various supersaturable formulations that helps for framing this article

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.