The development of albumin-based nanoparticle drug delivery systems is an area that has garnered increasing interest over the years. While an injectable formulation (Abraxane®) has already achieved success, development in terms of pulmonary drug delivery has been limited due to lack of knowledge about how albumin behaves in the lungs. Previous studies on the clearance, biocompatibility and biodistribution of albumin nanoparticles have demonstrated their ability to target drug delivery to the lungs. The next step is to examine drug loading of albumin nanoparticle formulations. This study has investigated the interactions of albumin with two novel anti-tuberculosis compounds, IR 20 and IF 274, from a class of drugs called benzothiazinones. Solubilisation studies with these model hydrophobic compounds in albumin solutions showed that an increase in drug surface area promoted additional solubilisation, e.g. from ~40% to ~70% of 1 mg of IR20. Benzothiazinone (BTZ)-loaded albumin nanoparticles were successfully manufactured (size ~100 nm) from the solutions, illustrating how compounds that interact with albumin can be incorporated into a nanoparticulate albumin system for inhaled drug delivery.