Synthesis and Evaluation of Targeted Prodrugs for Cancer Treatment (häftad)

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Farmakologi

Format: Häftad (Paperback / softback)
Språk: Engelska
Antal sidor: 164
Utgivningsdatum: 2012-01-06
Förlag: LAP Lambert Academic Publishing
Illustrationer: black & white illustrations
Dimensioner: 229 x 152 x 10 mm
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Antal komponenter: 1
Komponenter: Paperback
ISBN: 9783847339373

Synthesis and Evaluation of Targeted Prodrugs for Cancer Treatment

Name: Synthesis and Evaluation of Targeted Prodrugs for Cancer Treatment
Price: 978.00 SEK
Availability: InStock
Author: Sreeja Jayant
ISBN: 9783847339373

Drug Delivery System

av Sreeja Jayant

Häftad, Engelska, 2012-01-06

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The Drug delivery system (DDS) consisted of several combination's of the anticancer drug doxorubicin (DOX), polymeric drug carrier polyethylene glycol (PEG), drug spacer citric acid (CA) and targeting moiety sialic acid (SA) which was evaluated in vitro for cytotoxicity on human ovarian carcinoma cells (A2780). The targeted prodrug conjugates with two copies of SA and DOX showed enhanced cytotoxicity when compared with non-targeted prodrugs and free DOX. Targeting of the conjugate to cancer cells by sialic acid and an increase in number of copies of targeting moiety and anticancer drug enhanced prodrug uptake by cancer cells and cytotoxicity of the prodrug. Analysis of synthesized conjugates by 1NMR, MALDI/TOF, and HPLC showed the formation of the PEG prodrugs. More than 40% of the drug was released from its conjugate in presence of esterase enzyme, whereas the conjugate was stable at pH 7.4. The data obtained suggest that PAMAM G4-SA dendrimer represents a promising vehicle for intracellular delivery of low solubility drugs such as paclitaxel. Developed dendrimer provides both cytoplasmic and nuclear delivery of therapeutics and enhances anticancer activity of paclitaxel.

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