Rational Selection of Bio-Enabling Oral Drug Formulations – A PEARRL Commentary

Martin Kuentz*, René Holm, Christian Kronseder, Christoph Saal, Brendan T. Griffin

*Corresponding author for this work

Research output: Contribution to journalComment/debatepeer-review

Abstract

New drug candidates often require bio-enabling formation technologies such as lipid-based formulations, solid dispersions, or nanosized drug formulations. Development of such more sophisticated delivery systems generally requires higher resource investment compared to a conventional oral dosage form, which might slow down clinical development. To achieve the biopharmaceutical objectives while enabling rapid cost effective development, it is imperative to identify a suitable formulation technique for a given drug candidate as early as possible. Hence many companies have developed internal decision trees based mostly on prior organizational experience, though they also contain some arbitrary elements. As part of the EU funded PEARRL project, a number of new decision trees are here proposed that reflect both the current scientific state of the art and a consensus among the industrial project partners. This commentary presents and discusses these, while also going beyond this classical expert approach with a pilot study using emerging machine learning, where the computer suggests formulation strategy based on the physicochemical and biopharmaceutical properties of a molecule. Current limitations are discussed and an outlook is provided for likely future developments in this emerging field of pharmaceutics.

Original languageEnglish
JournalJournal of Pharmaceutical Sciences
Volume110
Issue number5
Pages (from-to)1921-1930
Number of pages10
ISSN0022-3549
DOIs
Publication statusPublished - May 2021

Keywords

  • Bioavailability
  • Dissolution
  • Formulation
  • In silico modeling
  • Lipid-based formulation(s)
  • Physicochemical properties
  • Solid dosage forms

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