Polylactide-doxorubicin nanoparticles with controlled sizes and high loadings

POLY 412

Rong Tong, rtong2@uiuc.edu and Jianjun Cheng, jianjunc@uiuc.edu. Department of Materials Science and Engineering, University of Illinois at Urbana-Champaign, 1304 West Greet Street, 201 MSEB, Urbana, IL 61801
Liposome-based delivery technology has been established and used in clinic for the treatment of breast cancer. To address formulation and stability challenges of liposomes, many other types of delivery vehicles have been developed and are under preclinical or clinical evaluations. There is growing interest in using polymeric nanoparticles for the delivery of chemotherapeutics, especially after Abraxane, a polymer-paclitaxel nanoencapsulate, was approved by the FDA for breast cancer therapy. However, since doxorubicin is hydrophilic with an aqueous solubility of 10 mg/mL in its hydrochloride salt, encapsulation of doxorubicin into hydrophobic polymeric nanoparticles is very difficult. Only limited success was achieved with drawbacks including low encapsulate efficiency, large particle size and multimodal particle distribution. Addressing these difficulties, we report the formation of polylactide-doxorubicin nanoparticles with 27% drug loading, quantitative loading efficiency and unimodal size distribution.