Effect of Ultrafine Powderization and Solid Dispersion Formation via Hot-Melt Extrusion on Antioxidant, Anti-Inflammatory, and the Human Kv1.3 Channel Inhibitory Activities of Angelica gigas Nakai

Abstract

Angelica gigas Nakai (AGN) was first processed by ultrafine grinding technology and hot-melt extrusion (HME). The potential antioxidant and anti-inflammatory activities of AGN with a different process were compared, and the effect on the human Kv1.3 potassium channel was detected. The process of ultrafine powderization on AGN significantly increased the total phenolic and flavonoid contents, antioxidant activity, and DNA damage protective effect. On the contrary, AGN solid dispersion (AGN-SD) based on Soluplus® showed the highest inhibitory effect on NO production and the human Kv1.3 channel. In addition, AGN-SD inhibited the production of prostaglandin E2 and intracellular reactive oxygen species and the mRNA expression of inducible nitric oxide synthase, cyclooxygenase-2, interleukin 1β, and interleukin 6. Taken together, these results suggest that ultrafine powderization and solid dispersion formation via HME can significantly improve the biological activities of AGN. The results also suggested that ultrafine powderization and HME may be developed and applied in the pharmaceutical industry.

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“…The formulation also showed greater anti-inflammatory activity by achieving edema inhibition (up to 90%) in 6 h, whereas pure drug depicted lesser edema inhibition (77%) in the same time. In another research, ultrafine grinding technology and HME technique were employed to prepare Angelica gigas Nakai solid dispersion (AGN-SD) and evaluated for the antioxidant and anti-inflammatory activities (Jiang et al., 2020 ). From the above findings, the authors concluded that AGN-SDs significantly enhanced biological activities.…”

Advancing Drug Delivery Paradigms: Polyvinyl Pyrolidone (PVP)-Based Amorphous Solid Dispersion for Enhanced Physicochemical Properties and Therapeutic Efficacy

“…The molten mixture is then forced through a die and rapidly cooled to solidify it into ASD. The resulting amorphous solid dispersion can be further characterized and evaluated for its physical properties and drug-polymer interactions [ 23 , 67 , 68 ].…”

Current Techniques of Water Solubility Improvement for Antioxidant Compounds and Their Correlation with Its Activity: Molecular Pharmaceutics

“…These results showed that AGN's biological activities can be significantly enhanced by ultrafine powderization and solid dispersion production by hot-melt extrusion (HME). Furthermore, 1e discoveries indicated that HME and ultrafine powderization can be developed and used in the pharma industry [125].…”