Supramolecular Amphiphilic Polymer-Based Micelles with Seven-Armed Polyoxazoline Coating for Drug Delivery

Abstract

Supramolecular polymer micelles composed of seven-armed poly(2-methy-2-oxazoline) as the coating and linear poly(dl-lactide) as the core were prepared through synthesizing β-cyclodextrin-terminated poly(2-methy-2-oxazoline) and adamantine-terminated linear poly(dl-lactide), followed by host-guest interaction between β-cyclodextrin and adamantine groups in two polymers and self-assembly in aqueous solution. Dynamic light-scattering measurement showed that the micelles based on supramolecular amphiphilic polymers have the size of 119 nm and were highly stable in salt solution. When the micelles were used as the carrier of cabazitaxel, an antitumor agent for drug-resistant cancers, satisfactory drug loading content and encapsulation efficacy were obtained. In vitro cellular cytotoxicity assays found that cabazitaxel-loaded micelles presented obvious cytotoxicity against taxane-sensitive and -resistant cancer cells. Further in vivo antitumor activity evaluation showed that cabazitaxel-loaded micelles have significantly superior efficacy in inhibiting tumor growth and prolonging survival in tumor-bearing mice compared to that of free paclitaxel and free cabazitaxel.