Physicochemical investigation of the influence of saccharide-based parenteral formulation excipients on L-p-boronphenylalanine solubilisation for boron neutron capture therapy.

This paper investigates the physicochemical properties of possible pharmaceutical alternatives to L-p-boronphenylalanine (BPA)-fructose intravenous formulation currently employed in boron neutron capture therapy. The physicochemical properties of BPA in the absence and presence of fructose, mannitol, trehalose and hydroxypropyl-β-cyclodextrin (HPCD) was investigated by determination of pKa values, solubility, precipitation and dissolution using a Sirius T3 instrument. Complex formation was also assessed using (10) B-Nuclear magnetic resonance (NMR).

Boron phenylalanine and related impurities: HPLC analysis, stability profile and degradation pathways.

Boron phenylalanine is one of the lead drug candidates in the field of Boron Neutron Capture Therapy. Its inherent low toxicity allows large doses to be administered, but this makes it important to identify, rationalise and quantify impurities. Here we report a chromatographic assay method, the conditions under which the parent compound is unstable, and the suggested degradation mechanisms.