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Abstract
Despite being highly recognized as an antitumor candidate due to its high potency in binding to DNA topoisomerase I and inhibiting of DNA relegation, full clinical application of camptothecin is unfortunately hampered by its poor solubility in aqueous medium and by the adverse effects caused by its hydrolyzed product under physiological conditions. In an attempt to increase its effective solubility, nanomicelles formed through self-assembly of copolymers by polymer-drug conjugate or by physical envelopment have recently been established to improve the efficacy of many drugs. This review provides the most up-to-date information available relating novel nanomicelles technology to the improvement and realization of the full potential of camptothecin. In particular, physicochemical and biological properties of camptothecin and its derivatives, the controlled factors of micelle formation, the techniques of drug encapsulation, and the structure-properties of nanomicelles are elucidated and discussed. Undoubtedly, polymer nanomicelle carriers can be selectively delivered to tumors via the enhanced permeability and retention effect. Moreover, micelles with smart functions such as stimulus-responsive and specific drug targeting may enhance the activity of potent bioactive compounds, facilitating their clinical applications.
Acknowledgments
This research work was supported by the National Natural Science Foundation of China (20404014 and 50843031), 973 Projects of Chinese Ministry of Science and Technology (2009CB930300), Program of Energy Research and Development (PERD) of Canada, Agricultural Bioproducts Innovation Program (ABIP) of Canada via the Pulse Research Network (PURENET), Shanghai Municipality Commission for Special Project of Nanometer Science and Technology (0952nm05300), Shanghai Municipality Commission for Non-governmental International Corporation Project (09540709000) and International Corporation Project (10410710000), and Fundamental Research Funds for the Central Universities (Self-Determined and Innovative Research Funds of WUT 2010-II-022).