| Title | "Clickable" Polymer-Caged Nanobins as a Modular Drug Delivery Platform. | | Author(s) | Lee SM, Chen H, O'Halloran TV, Nguyen ST | | Institution | Department of Chemistry, Department of Biochemistry, Molecular Biology and Cell Biology, and the Center of Cancer Nanotechnology Excellence, Northwestern University, 2145 Sheridan Road, Evanston, Illinois 60208-3113. | | Source | J Am Chem Soc 2009 Jun 15. | | Abstract | Modularly clickable polymer-caged nanobins (PCNs) were prepared from liposome templates using a drop-in cholesterol-modified poly(acrylic acid) reagent followed by cross-linking with alkyne-functionalized diamine linker that allows for the conjugation of azide-modified targeting ligands via click ligation. These PCNs possess pH-responsive characteristics that can be used to trigger the release of encapsulated doxorubicin (DXR) payload inside the liposomal core under mild acidic conditions. After click-conjugation with azide-modified folate as an active targeting ligand, the resulting folate-conjugated, DXR-loaded PCNs (f-PCN(DXR)) demonstrated enhanced potency to folate receptor (FR)-positive tumor cells such as KB and OvCa432 over FR-negative MCF7 cells. f-PCN(DXR) can readily discriminate FR-positive tumor cells as a function of the level of cellular FR-expression, showing different degrees of potentiation in each cell. With both targeting functionalities and pH-sensitive drug-releasing triggers, f-PCN(DXR) was fifty-times more potent than the untargeted agent toward cancer cells that overexpress the folate target receptors. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19527027 |
|
