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Novel polyoxazolines polymer drug delivery platform

17.05.2011
Oral and parenteral drug administration dominate the drug delivery market. The global market for oral drug delivery enhanced products was estimated to be worth around US$51 billion in 2009. Parenteral drug delivery is the second largest segment of the drug delivery market. It is presently valued at US$27 billion and is expected to reach US$51 billion by 2015 driven primarily by the launch of new biologics; the uptake of novel delivery platforms and the utilisation of controlled-release systems . Solubilization of hydrophobic drugs continues to be a key issue for drug delivery. The current invention relates to superior solubilization of hydrophobic drugs in aqueous solution through use of a novel amphiphilic polymer based on polyoxazolines with PEG-like properties (stealth effect, non-toxic, rapid renal clearance). The novel polyoxazoline polymers were used by inventors from the Technical University Munich for solubilizing several hydrophobic drugs from different compound classes like taxanes, cyclic

polypeptdes, protease inhibitors and polyene antibiotics by means of defined polymeric micelles. The resulting micelles were small (rh up to 30 nm), had a narrow size distribution (PD up to 0.12) and both a high loading capacity of up to 45% w/w and a high loading efficiency of more than 80%. Solubility was increased up to multiple thousand folds for the compounds tested. Lyophilization was possible without use of a cryo-protectant. Cytotoxicity studies showed no toxicity up to 20 mg/ml polymer. Animal studies for micelles loaded drugs showed at least similar effect with regard to tumor inhibition compared to commercial available drug products.



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