A carbohydrate polymer is a critical variable in the formulation of drug nanocrystals: a case study of idebenone.

: Stabilizers, especially carbohydrate polymers, have been shown to be necessary for the stabilization of drug nanocrystals. However, the impacts of select stabilizers on the and efficacy of therapeutics have rarely been reported. The aim of this study was to evaluate the importance of stabilizers in the formulation of drug nanocrystals.: Idebenone nanocrystals (IDBNC) stabilized by various stabilizers were formulated using a milling method. The dissolution profiles in water and absoprtion were compared. Finally, an pharmacokinetic study was performed.: The IDBNC profiles were found to have acceptable sizes and similar morphology and crystallinity. The dissolution profiles of IDBNC stabilized by different stabilizers were notably different, indicating the critical influence of stabilizers on the release rate of IDB. The Soluplus-stabilized IDBNC (IDBNC/Soluplus) achieved better absorption than HPMC stabilized IDBNC (IDBNC/HPMC). The pharmacokinetic study demonstrated that Soluplus-stabilized IDBNC had preferable kinetics, with an AUC of IDBNC/Soluplus (3.08-fold relative to IDB suspension), compared to IDBNC/HPMC (1.88-fold).: Choice of stabilizer plays an important role in the formulation of IDBNC. We anticipate that the role of stabilizers in the pharmacokinetic disposition of IDBNC has significant implications for a wide range of other drug crystal formulations.