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Current Drug Discovery Technologies


ISSN (Print): 1570-1638
ISSN (Online): 1875-6220

Macromolecular and Nanotechnological Modification of Camptothecin and its Analogs to Improve the Efficacy

Author(s): Hiraku Onishi and Yoshiharu Machida

Volume 2 , Issue 3 , 2005

Page: [169 - 183] Pages: 15

DOI: 10.2174/1570163054866891

Price: $65


Camptothecin (CPT) and its analogs are some of the most potent antitumor agents known. However, their poor water-solubility and high toxicity require changes of their physicochemical and biological characteristics. Active lactone forms have provoked interest in the utility of CPT and its analogs again. Macromolecular chemical modifications and nanotechnological formulations have been used to obtain improved systems of CPT-related compounds. In these systems, one of the most important concepts is the enhanced permeability and retention (EPR) effect. The outcomes obtained by these approaches are displayed by introducing concrete examples.

Keywords: camptothecin (cpt), analog, macromolecular chemical modification, nanotechnological formulation, enhanced permeability and retention (epr) effect

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