Preparation of bufalin-loaded pluronic polyetherimide nanoparticles, cellular uptake, distribution, and effect on colorectal cancer

Abstract

Qiang Hu,1,3,* Bo Liang,2,* Ying Sun,4 Xiao-Ling Guo,2,* Yi-Jie Bao,2 Dong-Hao Xie,3 Ming Zhou,3 You-Rong Duan,4 Pei-Hao Yin,2 Zhi-Hai Peng11Department of Hepatobiliary Surgery, Qianfoshan Hospital, Shandong University, Jinan, 2Department of General Surgery, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, 3Department of General Surgery, Dahua Hospital, 4State Key Laboratory of Oncogenes and Related Genes, Shanghai Cancer Institute, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, People’s Republic of China*These authors contributed equally to this workAbstract: A large number of studies have shown that bufalin can have a significant antitumor effect in a variety of tumors. However, because of toxicity, insolubility in water, fast metabolism, short half-life, and other shortcomings, its application is limited in cancer therapy. In this study, we explored the anti-metastatic role of bufalin-loaded pluronic polyetherimide nanoparticles on HCT116 colon cancer-bearing mice. Nanoparticle size, shape, drug loading, encapsulation efficiency, and in vitro drug release were studied. Also, cellular uptake of nanoparticles, in vivo tumor targeting, and tumor metastasis were studied. The nanoparticles had a particle size of about 60 nm and an encapsulation efficiency of 75.71%, by weight. The in vitro release data showed that free bufalin was released faster than bufalin-loaded pluronic polyetherimide nanoparticles, and almost 80% of free bufalin was released after 32 hours. Nanoparticles had an even size distribution, were stable, and had a slow release and a tumor-targeting effect. Bufalin-loaded pluronic polyetherimide nanoparticles can significantly inhibit the growth and metastasis of colorectal cancer.Keywords: colon cancer, nanoparticles, tumor target, bufalin