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Multifunctional Core/Shell Nanoparticles Self-Assembled from pH-Induced Thermosensitive Polymers for Targeted Intracellular Anticancer Drug Delivery†

  1. K. S. Soppimath1,
  2. L.-H. Liu1,
  3. W. Y. Seow2,
  4. S.-Q. Liu1,
  5. R. Powell1,
  6. P. Chan1,
  7. Y. Y. Yang1

Article first published online: 9 JAN 2007

DOI: 10.1002/adfm.200500611

Issue

Advanced Functional Materials

Advanced Functional Materials

Volume 17, Issue 3, pages 355–362, February, 2007

Additional Information

How to Cite

Soppimath, K. S., Liu, L.-H., Seow, W. Y., Liu, S.-Q., Powell, R., Chan, P. and Yang, Y. Y. (2007), Multifunctional Core/Shell Nanoparticles Self-Assembled from pH-Induced Thermosensitive Polymers for Targeted Intracellular Anticancer Drug Delivery. Adv. Funct. Mater., 17: 355–362. doi: 10.1002/adfm.200500611

Author Information

  1. 1

    Institute of Bioengineering and Nanotechnology, 31 Biopolis Way, The Nanos, 04-01, 138669, Singapore

  2. 2

    Department of Materials Science and Engineering, National University of Singapore, Blk EA, 07-40, 9 Engineering Drive 1, 117576, Singapore

  1. †

    This work was funded by the Institute of Bioengineering and Nanotechnology, Agency for Science, Technology and Research, Singapore. We thank Prof. P. S. Low (Purdue University, USA) for valuable discussions on cancer cells that over express folate receptors. We also acknowledge the technical assistance and contribution of Cherng-wen Tan (Institute of Bioengineering and Nanotechnology). Supporting Information is available online from Wiley InterScience or from the author.

Publication History

  1. Issue published online: 1 FEB 2007
  2. Article first published online: 9 JAN 2007
  3. Manuscript Revised: 2 MAR 2006
  4. Manuscript Received: 3 SEP 2005

Funded by

  • Institute of Bioengineering and Nanotechnology, Agency for Science, Technology and Research, Singapore

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Keywords:

  • Biomedical applications;
  • Core/shell nanoparticles;
  • Drug delivery;
  • Nanoparticles, functionalized;
  • Stimuli-responsive materials;
  • Thermoresponsive materials

Abstract

Core/shell nanoparticles that display a pH-sensitive thermal response, self-assembled from the amphiphilic tercopolymer, poly(N-isopropylacrylamide-co-N,N-dimethylacrylamide-co-10-undecenoic acid) (P(NIPAAm-co-DMAAm-co-UA)), have recently been reported. In this study, folic acid is conjugated to the hydrophilic segment of the polymer through the free amine group (for targeting cancer cells that overexpress folate receptors) and cholesterol is grafted to the hydrophobic segment of the polymer. This polymer also self-assembles into core/shell nanoparticles that exhibit pH-induced temperature sensitivity, but they possess a more stable hydrophobic core than the original polymer P(NIPAAm-co-DMAAm-co-UA) and a shell containing folate molecules. An anticancer drug, doxorubicin (DOX), is encapsulated into the nanoparticles. DOX release is also pH-dependent. DOX molecules delivered by P(NIPAAm-co-DMAAm-co-UA) and folate-conjugated P(NIPAAm-co-DMAAm-co-UA)-g-cholesterol nanoparticles enter the nucleus more rapidly than those transported by P(NIPAAm-co-DMAAm)-b-poly(lactide-co-glycolide) nanoparticles, which are not pH sensitive. More importantly, these nanoparticles can recognize folate-receptor-expressing cancer cells. Compared to the nanoparticles without folate, the DOX-loaded nanoparticles with folate yield a greater cellular uptake because of the folate-receptor-mediated endocytosis process, and, thus, higher cytotoxicity results. These multifunctional polymer core/shell nanoparticles may make a promising carrier to target drugs to cancer cells and release the drug molecules to the cytoplasm inside the cells.

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