Preparation of astaxanthin micelles self-assembled by a mechanochemical method from hydroxypropyl β-cyclodextrin and glyceryl monostearate with enhanced antioxidant activity.

This research aimed to overcome the current challenges in the application of natural carotenoid antioxidants, such as their complex preparation processes, low bioavailability and poor drug stability. Herein, a mechanochemical method was used to prepare an inclusion complex (IC) that self-assembles into micelles in aqueous solution and achieves solid-phase loading of astaxanthin (AST). The NMR analysis, thermodynamics study, particle size analysis and electron microscopy image results showed that AST, hydroxypropyl β-cyclodextrin (HPβ-CD) and glyceryl monostearate (GMS) formed self-assembled micelles and maintained good stability in aqueous solution. The antioxidant performance experiments showed that the formation of IC increases free radical scavenging activity. The pharmacokinetic studies showed that the bioavailability of the astaxanthin inclusion complex increased 4-fold. The tissue distribution experiments showed that the astaxanthin inclusion complex targets the liver to exert its antioxidant effects. The proposed method uses an innovative preparation technology to produce an efficient drug delivery system without solvents, and it exerts powerful antioxidant activity against astaxanthin.