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ACS Chem Biol. 2019 Jul 19;14(7):1507-1514. doi: 10.1021/acschembio.9b00247. Epub 2019 Jun 25.

Triggered Release Enhances the Cytotoxicity of Stable Colloidal Drug Aggregates.

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Department of Chemical Engineering & Applied Chemistry , University of Toronto , 200 College Street , Toronto , Ontario M5S 3E5 , Canada.
Institute of Biomaterials and Biomedical Engineering , University of Toronto , 164 College Street , Toronto , Ontario M5S 3G9 , Canada.
Department of Pharmaceutical Chemistry , University of California, San Francisco , 1700 Fourth Street , Mail Box 2550, San Francisco , California 94143 , United States.
Department of Chemistry , University of Toronto , 80 St. George Street , Toronto , Ontario M5S 3H6 , Canada.


Chemotherapeutics that self-assemble into colloids have limited efficacy above their critical aggregation concentration due to their inability to penetrate intact plasma membranes. Even when colloid uptake is promoted, issues with colloid escape from the endolysosomal pathway persist. By stabilizing acid-responsive lapatinib colloids through coaggregation with fulvestrant, and inclusion of transferrin, we demonstrate colloid internalization by cancer cells, where subsequent lapatinib ionization leads to endosomal leakage and increased cytotoxicity. These results demonstrate a strategy for triggered drug release from stable colloidal aggregates.


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