Formulation Approaches to Crystalline Status Modification for Carotenoids: Impacts on Dissolution, Stability, Bioavailability, and Bioactivities

Abstract

Carotenoids, including carotenes and xanthophylls, have been identified as bioactive ingredients in foods and are considered to possess health-promoting effects. From a biopharmaceutical perspective, several physicochemical characteristics, such as scanty water solubility, restricted dissolution, and susceptibility to oxidation may influence their oral bioavailability and eventually, their effectiveness. In this review, we have summarized various formulation approaches that deal with the modification of crystalline status for carotenoids, which may improve their physicochemical properties, oral absorption, and biological effects. The mechanisms involving crystalline alteration and the typical methods for examining crystalline states in the pharmaceutical field have been included, and representative formulation approaches are introduced to unriddle the mechanisms and effects more clearly.

A Fisetin Delivery System for Neuroprotection: A Co-Amorphous Dispersion Prepared in Supercritical Carbon Dioxide

“…CPV disrupts FIS's crystalline structure, leading to a less ordered arrangement of FIS molecules within the mixture. This reduction in crystallinity can influence the physicochemical properties of the mixture, potentially affecting dissolution behaviour, solubility, and stability [32,48]. It may also contribute to improved bioavailability and therapeutic efficacy.…”

“…At the same time, amorphization is a process that converts a crystalline compound into an amorphous form, which can significantly improve its solubility and bioavailability [31]. This is because the amorphous form lacks the ordered crystalline structure, leading to higher energy and increased molecular mobility, making it easier to dissolve in solvents and facilitating absorption by the body [32][33][34]. However, traditional methods of amorphization, such as spray-drying and ball milling, have limitations, including the use of toxic solvents, the generation of waste, and the potential degradation of the compound.…”