A novel polyethylene glycol mediated lipid nanoemulsion as drug delivery carrier for paclitaxel

作者：Jing Xiaolong; Deng Li; Gao Baoan; Xiao Lin; Zhang Yingying; Ke Xingfa; Lian Jianhao; Zhao Qiang; Ma Lulu; Yao Jianzhong^*; Chen Jianming

来源：Nanomedicine: Nanotechnology, Biology and Medicine , 2014, 10(2): 371-380.

DOI：10.1016/j.nano.2013.07.018

• Lipid emulsion
• Drug carrier
• Poorly water-soluble drug
• Paclitaxel
• Tumor

A novel polyethylene glycol 400 (PEG400) mediated lipid nanoemulsion as drug-delivery carrier for paclitaxel (PTX) was successfully developed. The formulation comprised a PEG400 solution of the drug (25 mg/mL) that would be mixed with commercially 20% lipid emulsion to form PTX-loaded nanoemulsion (1 mg/mL) prior to use. This two-vial formulation of PTX-loaded lipid nanoemulsion (TPLE) could significantly reduce extraction of reticuloendothelial system (RES) organs and increase tumor uptake, and exhibited more potent antitumor efficacy on bearing A2780 or Bcap-37 tumor nude mice compared to conventional PTX-loaded lipid nanoemulsion (CPLE). TPLE did not cause haematolysis and intravenous irritation response yet, and showed the same cytotoxicity against HeLa cells as Taxol (R), and its LD50 was 2.7-fold higher than that of Taxol (R), suggesting its good safety and druggability. In addition, TPLE displayed distinctly faster release of PTX, a greater proportion of PTX in phospholipids layer and a smaller share in oil phase than CPLE. From the Clinical Editor: This study demonstrates the feasibility and potential advantage of a novel PEG400-mediated two-vial formulation of lipid nanoemulsion as drug carrier for PTX in clinical application for the cancer therapy.

• 出版日期2014-2
• 单位福建中医药大学; 上海医药工业研究院; 中国人民解放军第二军医大学