Novel docetaxel-loaded nanoparticles based on PCL-Tween 80 copolymer for cancer treatment

Yuandong Ma^1,2*, Yi Zheng^1,2*, Xiaowei Zeng^1-3*, Liqin Jiang⁴, Hongbo Chen^1,2, Ranyi Liu⁵, Laiqiang Huang^1,2, Lin Mei^1,2
1School of Life Sciences, Tsinghua University, Beijing, ²Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, ³Materials and Environment Experimental Center, Department of Materials Science and Engineering, Qinhuangdao Branch, Northeastern University, Qinhuangdao, ⁴Insitute of Biomedical Engineering, Peking Union Medical College, Chinese Academy of Medical Sciences, Tianjin, ⁵State Key Laboratory of Oncology in South China, Sun Yat-sen University Cancer Center, Guangzhou, People’s Republic of China
^*These authors contributed equally to this work

Background: The formulation of docetaxel available for clinical use (Taxotere^®) contains a high concentration of polysorbate 80 (Tween 80). After incorporation of Tween 80 into poly-ε-caprolactone (PCL)-Tween 80 copolymer, the relative amount of Tween 80 should be decreased and the advantages of PCL and Tween 80 should be combined.
Methods: A novel PCL-Tween 80 copolymer was synthesized from ε-caprolactone and Tween 80 in the presence of stannous octoate as a catalyst via ring opening polymerization. Two types of nanoparticle formulation were made from commercial PCL and a self-synthesized PCL-Tween 80 copolymer using a modified solvent extraction/evaporation method.
Results: The nanoparticles were found by field emission scanning electron microscopy to have a spherical shape and be 200 nm in diameter. The copolymers could encapsulate 10% of the drug in the nanoparticles and release 34.9% of the encapsulated drug over 28 days. PCL-Tween 80 nanoparticles could be internalized into the cells and had higher cellular uptake than the PCL nanoparticles. The drug-loaded PCL-Tween 80 nanoparticles showed better in vitro cytotoxicity towards C6 cancer cells than commercial Taxotere at the same drug concentration.
Conclusion: Nanoparticles using PCL-Tween 80 copolymer as drug delivery vehicles may have a promising outcome for cancer patients.

Keywords: cancer chemotherapy, docetaxel, nanoparticles, PCL-Tween 80