Paclitaxel, a natural occurring diterpene alkaloid, is a relatively new antineoplastic agent for clinical treatment of breast, lung, ovarian, head and neck cancers. Anti-cancer agents in the cancer therapy cause a large number of toxic side effects which require a reduced dosage of chemotherapeutic agents or occasionally interruption of the therapy itself. Thus, invention of new effective agents preventing tumor cell growth without causing non-specific side effects is clinically important. Here below, we demonstrate a strategy for the preparation of new types of biodegradable, water-soluble polyphosphoester-based paclitaxel complexes.
Object: Presentation of a new type of covalently bonded or physically immobilized paclitaxel.
Materials: Used substances: Poly(ethylene glycol) with number-average molecular weight 600 g/mol (PEG 600); Paclitaxel (99%): distilled Dimethyl H-phosphonate.
Methods: 1) Synthesis of poly(oxyethylene H-phosphonate); 2) Synthesis of poly(hydroxyoxyethylene phosphate); 3) Synthesis of Polyphosphoestes-Paclitaxel Conjugate; 4) Physical immobilization (hydrogen bonding) of paclitaxel onto of poly(hydroxyoxyethylene phosphate).
Results: After the synthesis of the polyphosphoesters, their structure was proved by 1H, 13C{H} and 31 P NMR spectroscopy. Paclitaxel was immobilized onto poly(oxyethyle H-phosphonate)s with Mn = 5117 Da and Mn = 8822 Da via covalent bond using Atherton-Todd reaction conditions. Different types of complexes were synthesized as a result of the physical immobilization of paclitaxel onto polyphosphoesters.
Conclusion: We have developed new water-soluble paclitaxel-polyphosphoesters complexes. The synthesis of covalently bonded paclitaxel onto poly (oxyethylene H-phosphonate) was conducted at room temperature. Paclitaxel was physically
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