Paclitaxel loaded into metformin oleate ionic liquid micelle: Preparation and synergistic antitumor

Although paclitaxel (PTX) is a broad-spectrum anticancer drug, its low water solubility, poor bioavailability, and susceptibility to drug resistance have seriously limited its application. In recent years, studies have shown that metformin has potential anti-tumor activity. This paper reports the successful loading of PTX into metformin oleate ionic liquid ([Met][Ole] IL) micelles and [Met][Ole] IL/tween 80 (T-80) micelles. The obtained PTX-IL/T-80 micelle exhibited a good particle size (5.77 nm) and stability (Zeta potential: −51.65 ± 7.73 mV) in addition to possessing in vitro and in vivo antitumor efficacy. The inhibition rate of PTX-IL/T-80 (10 ppm) on 4 T1 cells reached 93 %. Furthermore, the results of the in vivo treatment in mice revealed that the tumor inhibition rate of PTX-IL/T-80 under a small-dose treatment (0.5 mg·kg⁻¹) was 37.7 %, which was much higher than that of the PTX prodrug group (11.7 %). Consequently, PTX-IL/T-80 has a great potential for its application in cancer therapy owing to the good synergistic antitumor effect between ([Met][Ole] ionic liquid and PTX.