Preparation, Characterization, and Anti-Lung Cancer Activity of Tetrandrine-Loaded Stealth Liposomes

Abstract

Background

Tetrandrine (Tet), a bisbenzylisoquinoline alkaloid, is a potential candidate for cancer chemotherapy. However, Tet has poor aqueous solubility and a short half-life, which limits its bioavailability and efficacy. Liposomes have been widely utilized to enhance the bioavailability and efficacy of drugs.

Methods

In this study, Tet-loaded stealth liposomes (S-LPs@Tet) were prepared by ethanol injection method. Furthermore, physicochemical characterisation, biopharmaceutical behaviour, therapeutic efficacy, and biocompatibility of S-LPs@Tet were assessed.

Results

The prepared S-LPs@Tet had an average particle size of 65.57 ± 1.60 nm, a surface charge of −0.61 ± 0.10 mV, and an encapsulation efficiency of 87.20% ± 1.30%. The S-LPs@Tet released Tet in a sustained manner, and the results demonstrated that the formulation remained stable for one month. More importantly, S-LPs significantly enhanced the inhibitory ability of Tet on the proliferation and migration of lung cancer cells, and enabled Tet to escape phagocytosis by immune cells. Furthermore, in vivo studies confirmed the potential for long-circulation and potent tumor-suppressive effects of S-LPs@Tet. Moreover, ex vivo and in vivo safety experiments demonstrated that the carrier material S-LPs exhibited superior biocompatibility.

Conclusion

Our research suggested that S-LPs@Tet has potential applications in lung cancer treatment.

Keywords:

• tetrandrine
• S-LPs
• lung cancer
• immune escape
• in vivo imaging

Acknowledgments

This work was supported by the Huadong MedicineJoint Funds of the Zhejiang Provincial Natural Science Foundation of China under Grant No. LHDMZ22H300009, Key research projects of Hangzhou Medical College under Grant No. KYZD202106, Education of Zhejiang Province under Grant No. Y202146052, and Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province under Grant No.2019E10021.

Disclosure

The authors declare no conflicts of interest.