期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 473, 期 1-2, 页码 493-500出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2014.07.045
关键词
Heparosan; Cellular uptake; Endocytosis pathway; Nanocarrier; Cytotoxicity
资金
- National Natural Science Foundation of China [51303068]
- Natural Science Fund of Jiangsu Province [BK2012557]
- Ministry of Education of China [20110093110008]
- Key Laboratory of Biomedical Polymers, Ministry of Education, Wuhan University [20110401]
In this study, a heparosan-DOX conjugate (HDC) was designed and prepared by covalently linking heparosan with anticancer drug doxorubicin (DOX) via Schiff base. Due to the amphiphilic nature, the HDC could self-assemble into nanoparticles in aqueous solution of pH 7.4. In spite of the surface charge of HDC nanoparticles was negative, HDC could achieve intracellular delivery of DOX efficiently. Cellular uptake study revealed the endocytosis pathway of heparosan based nanocarrier includes clathrin-mediated endocytosis and macropinocytosis, and the process of endocytosis is energy dependent. This meant the HDC would reach endosomes and behave pH-sensitive DOX release profile due to the inherent property of Schiff base. The cytotoxicity assay and flow cytometry analysis demonstrated the cellular uptake of HDC was faster than that of free DOX, showing improved efficacy within short co-incubation period. Furthermore, the HDC nanoparticles were stable in culture medium containing 10% FBS, indicating promising application for drug delivery. (C) 2014 Elsevier B.V. All rights reserved.
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