title: Encapsulation of teniposide into albumin nanoparticles with greatly lowered toxicity and enhanced antitumor activity.
abstract: 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.
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
authors.forename: Xinyi
authors.initials: X
authors.lastname: He
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
authors.forename: Nanxi
authors.initials: N
authors.lastname: Xiang
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
authors.forename: Jinjie
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Zhou
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China. Electronic address: yfu4@scu.edu.cn.
authors.forename: Yao
authors.initials: Y
authors.lastname: Fu
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China. Electronic address: gongtaoy@126.com.
authors.forename: Tao
authors.initials: T
authors.lastname: Gong
authors.affiliation: Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, No. 17. Section 3. Southern Renmin Road, Chengdu 610041, People's Republic of China.
authors.forename: Zhirong
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000418:Albumins; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D005079:Excipients; D006801:Humans; D054709:Lecithins; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D053758:Nanoparticles; D051381:Rats; D017208:Rats, Wistar; D013713:Teniposide / Q000008:administration & dosage* / Q000009:adverse effects / Q000494:pharmacology*; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D000418:Albumins; D000972:Antineoplastic Agents, Phytogenic; D005079:Excipients; D054709:Lecithins; D013713:Teniposide
keywords: Albumin; Antitumor; Egg Yolk Lecithin (PubChem CID: 6850739); Nanoparticle; Phospholipid complex; Teniposide; Teniposide (PubChem CID: 5396); Toxicity