Improving PROTAC Dissolution with Ionic Liquid API Encapsulation

Brunella Grassiri – Post Doc, Trinity College Dublin; Michael Stocker – Post Doc, University College Dublin; David Brayden – Professor, University College Dublin; Anne Marie Healy – Professor, Trinity College Dublin; Steven Ferguson – Associate Professor, University College Dublin

Introduction:

The poor aqueous solubility of PROTACs is one of the leading challenges limiting the success of these targeted protein degraders (Garcia Jiménez et al., 2022). Active Pharmaceutical Ingredient ionic liquids (API-ILs) are well positioned to address this challenge but suffer from poor handling characteristics. Recently, spray encapsulation has emerged as a means to mitigate the challenges associated with processing and formulation of these products (Stocker et al., 2020, Tsolaki et al., 2024). This encapsulation process in known as SEncIL (spray encapsulation of innovative liquids). Through SEncIL, a powder containing API-IL or API-IL/LBF encapsulated in a separate polymer phase can be formed.