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Biocompatible Polymers for Solubilization of Hydrophobic Drugs

22.07.2010
Solubilization of hydrophobic drugs is a key issue in pharmaceutical industry. Currently, there are few non-toxic formulations available for drugs like paclitaxel (Taxol® or Abraxane®), which can only solubilize relatively small amounts of active ingredient and may even cause severe side effects in patients.

<p> Superior solubilization of hydrophobic drugs in aqueous solution can be achieved with a novel amphiphilic polymer. The invention utilizes non-toxic polymers for solubilizing hydrophobic drugs by means of defined polymeric micelles. The resulting nanoformulation increases the innate solubility in aqueous solution by 4 orders of magnitude and has a very high loading capacity of up to 40% wt that allows for solubilization of e.g. 8 mg/mL paclitaxel in water. <p> The annual worldwide sales of the few highly hydrophobic drugs that have been successfully solubilized sum up to several billion dollars. The use of this novel carrier system will enable the successful development of numerous APIs into potent drugs, which has an even higher commercial potential. <p>

The polymers can be developed into a carrier for paclitaxel and a multitude of other hydrophobic drugs for parenteral administration. The novel polymer system has been tested with several compounds like paclitaxel, cyclosporine or amphotericin and can be tailored to optimize properties for the solubilization of various other drugs and active agents.

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