(194v) Multi-Drug Loaded PLGA Microparticles for Cancer Treatment

Current chemotherapeutic drugs approved by the United States Food & Drug Administration (FDA) for advanced stage cancer have poor aqueous solubility and require solubilization in toxic solvents such as polyethoxylated castor oil (trademark Kolliphor® EL) [1]. This leads to adverse side effects such as fatigue, hair loss, easy bruising and bleeding, infection, anemia, nausea and vomiting, and appetite changes. Additionally, patients receive combinations of these anticancer drugs along with steroids intravenously over a series of weeks by a trained professional in a clinic or hospital setting. To increase drug efficacy as well as patient compliance, a degradable polymeric particle formula for the controlled release of two or more drugs, could be beneficial.

The goal of this work was to co-encapsulate a hydrophobic chemotherapeutic (paclitaxel) and a hydrophobic anti-angiogenesis (thalidomide) drug in a degradable polymeric particle (PLGA). This was accomplished using ultrasonic atomization without the use of surfactants. Results show that the encapsulation of a single drug or co-encapsulation of both drugs did not affect particle size. The particles were evaluated for encapsulation efficiency, drug release profiles, and in vitro efficacy.

1. Gelderblom, H., et al., Cremophor EL: the drawbacks and advantages of vehicle selection for drug formulation. Eur J Cancer, 2001. 37(13): p. 1590-8.