Design of biocompatible chitosan microgels for targeted pH-mediated intracellular release of cancer therapeutics

Hong Zhang; Sawitri Mardyani; Warren C.W. Chan; Eugenia Kumacheva

doi:10.1021/bm050912z

Design of biocompatible chitosan microgels for targeted pH-mediated intracellular release of cancer therapeutics

Hong Zhang, Sawitri Mardyani, Warren C.W. Chan^*, Eugenia Kumacheva

^*Corresponding author for this work

University of Toronto

Research output: Contribution to journal › Article › peer-review

232 Citations (Scopus)

Abstract

We report the rational design of a chitosan-based drug delivery system. The chitosan derivative N-[(2-hydroxy-3-trimethylammonium)propyl]chitosan chloride (HTCC) was ionically cross-linked by sodium tripolyphosphate (TPP) to form sub-200-nm microgels that are responsive to pH changes. When these microgels were loaded with methotrexate disodium (MTX), a cytotoxic drug for cancer treatment, and conjugated to the targeting biomolecule apo-transferrin, a protein known to enter cells via receptor-mediated endocytosis, enhanced killing of immortalized HeLa cells was observed. In this intracellular delivery method, the microgel was exposed to low-pH environments that caused the chitosan to swell and release the drug. This rational drug delivery design may be useful in enhancing cancer therapy and reducing side effects.

Original language	English
Pages (from-to)	1568-1572
Number of pages	5
Journal	Biomacromolecules
Volume	7
Issue number	5
DOIs	https://doi.org/10.1021/bm050912z
Publication status	Published - May 2006
Externally published	Yes

ASJC Scopus Subject Areas

Bioengineering
Biomaterials
Polymers and Plastics
Materials Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1021/bm050912z

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abstract = "We report the rational design of a chitosan-based drug delivery system. The chitosan derivative N-[(2-hydroxy-3-trimethylammonium)propyl]chitosan chloride (HTCC) was ionically cross-linked by sodium tripolyphosphate (TPP) to form sub-200-nm microgels that are responsive to pH changes. When these microgels were loaded with methotrexate disodium (MTX), a cytotoxic drug for cancer treatment, and conjugated to the targeting biomolecule apo-transferrin, a protein known to enter cells via receptor-mediated endocytosis, enhanced killing of immortalized HeLa cells was observed. In this intracellular delivery method, the microgel was exposed to low-pH environments that caused the chitosan to swell and release the drug. This rational drug delivery design may be useful in enhancing cancer therapy and reducing side effects.",

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Design of biocompatible chitosan microgels for targeted pH-mediated intracellular release of cancer therapeutics

Abstract

ASJC Scopus Subject Areas

UN SDGs

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