Fig. 4: Stabilization of hydrophobic payload by PPnGRAD 31P MRI agents applied to PROTAC ARV-825.

A Photograph of PROTAC-loaded PPnGRAD micelles (right vial) and a control PROTAC suspension prepared without the addition of PPnGRAD (left vial). PROTAC-loaded micelles form a clear dispersion. Conversely, in the control PROTAC (yellow) precipitated immediately after the preparation. B DLS of PROTAC-loaded PPnGRAD micelles. The micelles had a low polydispersity and were stable for at least two months. In contrast, PROTAC suspension displayed a broad size distribution. The size measurement of PROTAC-only suspension can be affected by sedimentation. C Viability of cancer cells (HeLa) was reduced upon the administration of PROTAC-loaded micelles to a comparable level as with free PROTAC. Unloaded PPnGRAD micelles were used as a control. The viability values are normalized to untreated controls. n = 3 (data presented as mean ± SD). D Flow cytometry shows that cancer cells treated with PROTAC-loaded micelles (1 µM ARV-825) start entering an early apoptosis phase.