Abstract
Synthetic polymers have enabled amorphous solid dispersions (ASDs) to emerge as an oral delivery strategy for overcoming poor drug solubility in aqueous environments. Modern ASD products noninvasively treat a range of chronic diseases (for example, hepatitis C, cystic fibrosis, and HIV). In such formulations, polymeric carriers generate and maintain drug supersaturation upon dissolution, increasing the apparent drug solubility to enhance gastrointestinal barrier absorption and oral bioavailability. In this Review, we outline several approaches in designing polymeric excipients to drive interactions with active pharmaceutical ingredients (APIs) in spray-dried ASDs, highlighting polymer-drug formulation guidelines from industrial and academic perspectives. Special attention is given to new commercial and specialized polymer design strategies that can solubilize highly hydrophobic APIs and suppress the propensity for rapid drug recrystallization. These molecularly customized excipients and hierarchical excipient assemblies are promising toward informing early-stage drug-discovery development and reformulating existing API candidates into potentially lifesaving oral medicines for our growing global population.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 939-952 |
| Number of pages | 14 |
| Journal | Bioconjugate Chemistry |
| Volume | 29 |
| Issue number | 4 |
| DOIs | |
| State | Published - Apr 18 2018 |
Bibliographical note
Funding Information:J.M.T. acknowledges support from the National Science Foundation (NSF) Graduate Research Fellowship under grant no. 00006595 and the University of Minnesota Doctoral Dissertation Fellowship.
Funding Information:
We gratefully thank the numerous members of the oral drug delivery community that have advanced this exciting area of basic and applied scientific research. The examples and discussion herein were limited to only a few representative cases due to space limitations. We thank The Dow Chemical Company for financial support and a productive partnership throughout the years. J.M.T. acknowledges support from the National Science Foundation (NSF) Graduate Research Fellowship under grant no. 00006595 and the University of Minnesota Doctoral Dissertation Fellowship.
Publisher Copyright:
© 2018 American Chemical Society.
