Journal
CHEMMEDCHEM
Volume 7, Issue 2, Pages 281-291Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201100456
Keywords
camptothecins; drug delivery; polymer-drug conjugates; polymers; RAFT polymerization
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Funding
- CSIRO Future Manufacturing Flagship
- Max Planck Society
- German Federal Ministry of Education and Research (BMBF)
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A series of well-defined polymerdrug conjugates were prepared in order to modify the physical properties of a known cytotoxic drug, 7-ethyl-10-hydroxycamptothecin (SN-38), the active metabolite of irinotecan (CPT-11). Reversible additionfragmentation chain transfer (RAFT) polymerisation was used to covalently and site-specifically append a defined N-(2-hydroxypropyl)methacrylamide (HPMA) polymer to SN-38 using a graft-from process. These poly-HPMASN-38 conjugates displayed excellent aqueous solubility and stability, whilst retaining the cytotoxic activity of the parent SN-38. In vitro co-culture assays containing both cancer and noncancer cell lines demonstrated the specificity of RAFT-derived poly-HPMASN-38 conjugates for cancerous cells. The concept of post-optimisation modification of small-molecule drugs through a graft-from polymer conjugation method is introduced.
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