Novel polyoxazoline drug carriers for therapeutic applications

Many of the most potent drugs and drug candidates are not water-soluble. Solubilization of highly hydrophobic drugs with carriers that are non-toxic, non-immunogenic and well defined remains a major obstacle. Loading capacity of drug carriers and total amount of solubilized drug are among factors limiting success of such systems. Poly(2-oxazoline)s have recently attracted considerable attention for drug delivery. Hydrophilic polyoxazolines are of particular interest as they exhibit stealth and protein repellent effects. Present technology offers drug delivery platform utilizing well-defined amphiphilic di- and triblock copolymers based on poly(2-oxazolines). Polyoxazoline-based drug carriers were prepared and used for the solubilization of hydrophobic drugs. Extraordinary large loading capacity for one of them, anticancer drug paclitaxel of 45 wt.% active drug in the formulation as well as high water solubility of the resulting formulation was achieved. Futhermore, full activity of Paclitaxel as well as superior tumor inhibition as compared to the commercial micellar formulation was demonstrated. Physicochemical properties of the formulations, ease of preparation and stability upon lyophilization, low toxicity and immunogenicity suggest that poly(2- oxazoline)s are promising candidates for the delivery of highly challenging drugs.