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Oral Delivery of DMAB-Modified Docetaxel-Loaded PLGA-TPGS Nanoparticles for Cancer Chemotherapy

Hongbo Chen12, Yi Zheng12, Ge Tian3, Yan Tian3, Xiaowei Zeng4, Gan Liu4, Kexin Liu3, Lei Li3, Zhen Li3, Lin Mei123* and Laiqiang Huang12*

Author Affiliations

1 School of Life Sciences, Tsinghua University, 100084, Beijing, People's Republic of China

2 The Shenzhen Key Lab of Gene and Antibody Therapy, Center for Biotech and Bio-Medicine and Division of Life Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong Province 518055, China

3 College of Pharmacy, Dalian Medical University, 116027, Dalian Liaoning, People's Republic of China

4 Key Laboratory of Functional Polymer Materials, Ministry of Education; Institute of Polymer Chemistry, Nankai University, 300071, Tianjin, People's Republic of China

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Nanoscale Res Lett 2011, 6:4  doi:10.1007/s11671-010-9741-8

Published: 20 August 2010


Three types of nanoparticle formulation from biodegradable PLGA-TPGS random copolymer were developed in this research for oral administration of anticancer drugs, which include DMAB-modified PLGA nanoparticles, unmodified PLGA-TPGS nanoparticles and DMAB-modified PLGA-TPGS nanoparticles. Firstly, the PLGA-TPGS random copolymer was synthesized and characterized. DMAB was used to increase retention time at the cell surface, thus increasing the chances of particle uptake and improving oral drug bioavailability. Nanoparticles were found to be of spherical shape with an average particle diameter of around 250 nm. The surface charge of PLGA-TPGS nanoparticles was changed to positive after DMAB modification. The results also showed that the DMAB-modified PLGA-TPGS nanoparticles have significantly higher level of the cellular uptake than that of DMAB-modified PLGA nanoparticles and unmodified PLGA-TPGS nanoparticles. In vitro, cytotoxicity experiment showed advantages of the DMAB-modified PLGA-TPGS nanoparticle formulation over commercial Taxotere® in terms of cytotoxicity against MCF-7 cells. In conclusion, oral chemotherapy by DMAB-modified PLGA-TPGS nanoparticle formulation is an attractive and promising treatment option for patients.

PLGA-TPGS; DMAB; Nanoparticle; Oral Chemotherapy; Docetaxel