Min Xu1,2, Chong Yao3, Wei Zhang1, Shen Gao1, Hao Zou1, Jing Gao1,4. 1. School of Pharmacy, Second Military Medical University, Shanghai, 200433, People's Republic of China. 2. Department of Pharmacy, Changzheng Hospital, Shanghai, 200003, People's Republic of China. 3. Clinical Pharmacy Center, Department of Pharmacy, Chinese PLA General Hospital, Beijing, 100850, People's Republic of China. 4. State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, Beijing, 100850, People's Republic of China.
Abstract
PURPOSE: Nanocarriers, with a high drug loading content and good safety, to achieve desirable therapeutic effect are always the goals for industry and research. METHODS AND RESULTS: In the present study, we developed a docetaxel loaded poly-2-oxazoline polymer micellar system which employed poly-2-butyl-2 oxazoline and poly-2-methyl-2 oxazoline as the hydrophobic chain and hydrophilic chain, respectively. This micellar system achieves a high load up to 25% against the docetaxel, and further demonstrates an IC50 as low as 40% of the commercialized docetaxel injection in vitro and a double maximum tolerated dose in MCF-7 cells in vivo. CONCLUSION: The high drug loading content, superior safety, and considerable anti-cancer activity make this newly developed docetaxel loaded poly(2-oxazoline) micelle go further in future clinical research.
PURPOSE: Nanocarriers, with a high drug loading content and good safety, to achieve desirable therapeutic effect are always the goals for industry and research. METHODS AND RESULTS: In the present study, we developed a docetaxel loaded poly-2-oxazoline polymer micellar system which employed poly-2-butyl-2 oxazoline and poly-2-methyl-2 oxazoline as the hydrophobic chain and hydrophilic chain, respectively. This micellar system achieves a high load up to 25% against the docetaxel, and further demonstrates an IC50 as low as 40% of the commercialized docetaxel injection in vitro and a double maximum tolerated dose in MCF-7 cells in vivo. CONCLUSION: The high drug loading content, superior safety, and considerable anti-cancer activity make this newly developed docetaxel loaded poly(2-oxazoline) micelle go further in future clinical research.
Authors: Zhijian He; Xiaomeng Wan; Anita Schulz; Herdis Bludau; Marina A Dobrovolskaia; Stephan T Stern; Stephanie A Montgomery; Hong Yuan; Zibo Li; Daria Alakhova; Marina Sokolsky; David B Darr; Charles M Perou; Rainer Jordan; Robert Luxenhofer; Alexander V Kabanov Journal: Biomaterials Date: 2016-06-04 Impact factor: 12.479