Isolation, Purification, and Preparation of Taxinine-Loaded Liposomes for Improved Anti-Hepatocarcinogenic Activity

Abstract

Liver cancer is the fourth most deadly cancer worldwide, but existing treatment options are insufficient, thus highlighting the urgent need for new therapeutic agents. Taxanes, known for their anticancer properties, provide a promising avenue for intervention. In this study, a tetracyclic taxane compound with antitumor activity (taxinine) was extracted and isolated from Taxus chinensis (T. chinensis) seeds. It was then formulated into liposomes using lecithin, cholesterol, and D-α-tocopheryl polyethylene glycol succinate (TPGS) as excipients to enhance its solubility and antitumor efficacy. The isolation of taxinine was achieved through ultrasound-assisted ethanol extraction, followed by silica gel column chromatography, MTT activity screening, and recrystallization. Afterward, the structure of taxinine was confirmed using nuclear magnetic resonance and mass spectrometry. Taxinine liposomes were prepared via the thin film dispersion method, while the particle size, polydispersity index, zeta potential, and encapsulation efficiency of the nanoliposomes were discovered to be 186.76 ± 0.08 nm, 0.226 ± 0.012, −44.34 ± 0.77 mV, and 93.75 ± 1.29%, respectively. They also showed good stability with a release rate of 85.77% ± 2.43% in phosphate-buffered solution (PBS, pH 7.4). Toxicity tests conducted on zebrafish larvae indicated that taxinine liposomes were safe in vivo. Tissue distribution study showed that the concentration of taxinine liposomes increased to varying degrees in tissues (especially liver). In vitro experiments demonstrated that taxinine liposomes significantly enhanced the inhibitory effect of taxinine on HepG2 cell growth. Overall, the nanoliposomal formulation improved the anti-liver cancer activity of taxinine, thus suggesting its potential as a therapeutic agent.