This work is financially supported by a Grant-in-Aid for Scientific Research from the Ministry of Education, Culture, Sports, Science and Technology (MEXT), Japan, and by Core Research for Evolutional Science and Technology (CREST), Japan Science and Technology Corporation (JST). The authors acknowledge the National Cancer Center Research Institute, Japan, for supplying a human small cell lung cancer cell line SBC-3. Y.B. acknowledges financial support from the Japanese Monbusho's scholarship program.
Design of Environment-Sensitive Supramolecular Assemblies for Intracellular Drug Delivery: Polymeric Micelles that are Responsive to Intracellular pH Change†
Article first published online: 1 OCT 2003
Copyright © 2003 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 42, Issue 38, pages 4640–4643, October 6, 2003
How to Cite
Bae, Y., Fukushima, S., Harada, A. and Kataoka, K. (2003), Design of Environment-Sensitive Supramolecular Assemblies for Intracellular Drug Delivery: Polymeric Micelles that are Responsive to Intracellular pH Change. Angew. Chem. Int. Ed., 42: 4640–4643. doi: 10.1002/anie.200250653
- Issue published online: 1 OCT 2003
- Article first published online: 1 OCT 2003
- Manuscript Revised: 25 APR 2003
- Manuscript Received: 28 NOV 2002
- anticancer agents;
- supramolecular chemistry
Drug smuggling: Micelles made up of block copolymers and the anticancer drug adriamycin (ADR), which is linked to the polymer by a pH-sensitive linker, have been prepared (see picture). Treatment of cancer cells with the micelles shows that the micelles are transported into the cell by endocytosis, thus bypassing the cell-membrane transporters. In the cell, the decrease in pH value triggers the release of the ADR, which retains its cytotoxic effect. The released ADR fluoresces which allows its localization within the cells to be detected.