Passive Tumor Targeting of Polymer Therapeutics: In Vivo Imaging of Both the Polymer Carrier and the Enzymatically Cleavable Drug Model
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
- Keywords
- EPR effect, enzymatic release, in vivo imaging, polymer drug carriers, tumor targeting,
- MeSH
- Acrylamides * chemistry pharmacokinetics pharmacology MeSH
- Fluorescent Dyes * chemistry pharmacokinetics pharmacology MeSH
- Colorectal Neoplasms * drug therapy metabolism pathology MeSH
- Humans MeSH
- Mice, Nude MeSH
- Mice MeSH
- Drug Carriers * chemistry pharmacokinetics pharmacology MeSH
- Xenograft Model Antitumor Assays MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acrylamides * MeSH
- Fluorescent Dyes * MeSH
- N-(2-hydroxypropyl)methacrylamide MeSH Browser
- Drug Carriers * MeSH
The enzymatic release of a model drug from a polymer carrier inside a tumor using multispectral optical imaging in vivo in nude mice bearing colorectal carcinomas HT-29 and DLD-1 is demonstrated. Much higher release rate in vivo from a linear (30 kDa) (N-2-hydroxypropyl)methacrylamide-based polymer compared with a high molecular weight branched (170 kDa) polymer conjugate is observed, probably due to steric hindrance of the cleavable spacer of the latter polymer to proteolytic enzymes. There is no significant difference in the relative biodistribution of the two polymers, but the branched polymer circulates much longer. Both polymers are labeled with two different fluorophores. Dyomics-676 as a drug model is attached to the polymer via an enzymatically cleavable Gly-Phe-Leu-Gly spacer; Dyomics 782 is bound to the same polymer via a nondegradable amide bond, enabling the tracking of the polymer carrier after i.v. application to mice.
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