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Paclitaxel is one of the most effective anticancer drugs for treatment of various human tumours.It introduces a new class ofmicrotubular stabilising drugs, which interfere mitosis.The low solubility of paclitaxel in aqueous media, however, constricts its direct application, and also the unspecific toxicity that not only interferes tumour cell division demands for new concepts of drug delivery.Therefore, improvement of tumour-cell selectivity and enhanced hydrophilicity of paclitaxel remains a goal of high priority.This review summarises the present knowledge about paclitaxel prodrugs based on macromolecular conjugates and their interaction with constituents of body fluids as well as the potential of tumour-targeted drug delivery by paclitaxel conjugates.