In Vivo NMR Evaluation of the Pharmacokinetics of Boronated Compounds in the Rat Model

Abstract

The success of neutron capture therapy in the treatment of cancer is dependent on the development of boronated compounds that preferentially accumulate in tumor tissue and not in surrounding normal tissue. Researchers are investigating numerous new compounds for boron delivery to tumors. Evaluation of the performance of these compounds typically includes in vitro studies of drug uptake in tumor cell cultures followed by animal studies in which toxicity and tumor specificity are determined. Once toxicity issues are resolved, the drug proceeds to human clinical trials where tumor specificity and drug toxicity are again evaluated. The animal and human studies attempt to characterize the pharmacokinetic characteristics of the compounds by analyzing ex vivo tissue, blood, and urine samples. While these studies provide important information about drug accumulation and distribution in various tissues, they fail to provide an in vivo representation of the uptake and elimination of the boronated compound within a single animal or patient.