Effect of Hypromellose Acetate Succinate and Sorbitan Monolaurate on the Properties and Bioactivity of Ternary Lycopene Amorphous Solid Dispersions

ABSTRACT

In this study, ternary lycopene amorphous solid dispersions (LYC ASDs) were successfully prepared using hypromellose acetate succinate HF (HPMCAS-HF) and sorbitan monolaurate (Span 20). Differential scanning calorimetry (DSC) thermograms showed that no typical crystalline melting endotherm of LYC was observed, whereas powder x-ray diffraction (PXRD) patterns corroborated these findings by showing complete disappearance of patterns associated with crystalline LYC. Fourier transform infrared (FT-IR) spectroscopic analysis uncovered potential intermolecular interactions, including hydrophobic interaction and hydrogen bonds, between the drug and excipients. Homogeneous morphology was displayed in the scanning electron microscopy (SEM) images of LYC ASDs with a series of nanotopographies distributed on their rough surface. LYC ASDs exhibited enhanced in vitro radical scavenging capacity, whereas their excellent cellular reactive oxygen species (ROS) scavenging capacity was proved in both LO2 and Caco-2 cells. Besides, LYC ASDs possessed superior biocompatibility as their cytotoxicity against LO2 and Caco-2 cells was negligible, and their cell adhesion and migration were not affected by LYC ASDs. Furthermore, LYC ASDs markedly alleviated metabolic dysregulation, oxidative stress, and hepatic damage in a high-fat diet-induced liver injury model. In summary, LYC ASDs exhibited enormous potential for boosting the biopharmaceutical manifestation of similar hydrophobic bioactivates in the functional food field.

Practical Application

In this study, the effect of hypromellose acetate succinate HF and sorbitan monolaurate on the physicochemical properties and bioactivity of ternary lycopene amorphous solid dispersions was investigated. Therefore, this study provides a theoretical basis for the industrial application of lycopene-containing functional food products.