Development of a Stable Micelle for Drug Delivery in Oncology

K. Sill
Intezyne, US

Keywords: Micelle, Drug Delivery, Oncology

Summary:

Due to their ability to encapsulate hydrophobic drugs and their unique size dimensions, polymer micelles offer a promising approach in the world of drug delivery. Unfortunately, only a handful micelle based therapies have entered of clinical trials after 30 years of research by a wide range of research groups. This lack of clinical success can likely be attributed to the rapid dissolution and disruption of the drug loaded micelle shortly after administration to the patient. When the drug is prematurely released outside of the target tissue, all the beneficial properties of the micelle (e.g. long circulation lifetime and preferential tumor uptake) are lost and the biodistribution of the drug reverts to its native state. To address these challenges, we have developed a polymer micelle that is stable to dilution within biological media. Encapsulation of daunorubicin within the stabilized polymer micelle has resulted in a 100-fold increase in plasma drug exposure and a 70-fold increase in tumor accumulation when compared to the free drug. The development of the stabilized micelle, as well as in vitro and in vivo characterization will be discussed.