He Xinyi, Xiang Nanxi, Zhang Jinjie, Zhou Jing, Fu Yao, Gong Tao, Zhang Zhirong
Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
Int J Pharm. 2015 Jun 20;487(1-2):250-9. doi: 10.1016/j.ijpharm.2015.04.047. Epub 2015 Apr 18.
Teniposide (VM-26) is a semisynthetic derivative of podophyllotoxin effective for the treatment of many types of tumors. However, the poor water solubility and adverse effects restrict its clinical use. Our study aimed to develop a novel phospholipid complex albumin nanoparticle (VM-E80-AN) to reduce the systemic toxicity and enhance antitumor activity of VM-26. Egg yolk lecithin E80 and human serum albumin (HSA) were used as the main excipients to replace Cremophor EL in the commercial formulation. The physicochemical properties of VM-E80-AN were characterized to optimize the formulation. Cell and animal studies were further carried out to estimate its tumor inhibition efficacy, biodistribution, and toxicity. Comparison between VM-26 solution and VM-E80-AN showed that VM-E80-AN significantly reduced the toxicity of VM-26 and enhanced the anticancer efficacy of the drug. Thus, VM-E80-AN represents a safe and promising formulation of teniposide for clinical application.
