Bioavailability (BA) is of course of paramount importance when a new drug candidate is selected. BA is dependent on the complex interplay of numerous physiologic and physico-chemical factors in vivo.

There are multiple formulation approaches or alternate routes of administration that PDDC can exploit to modulate the bioavailability of drugs. There are pros and cons to deviating from standard (i.e. tablet) formulations. Typically the cost per dosage unit will rise sharply with a more sophisticated manufacturing process.  However, if your candidate has very low BA initially and it improves significantly with an alternative delivery method, you may reduce the dosage needed, using less drug per dose, and ultimately lowering cost. In addition, for early stage efficacy/proof of concept studies (non-GLP), it can be advantageous to use an enhanced formulation to achieve proof-of-concept, validate animal models, or elucidate toxicities.

PDDC scientists have a great depth of experience employing various formulation approaches to optimize bioavailability and exposure. Solubilization (cosolvents, surfactants, polymers, cyclodextrins, and so forth), particle size reduction (micronization, milling, nanocrystals, etc), lipids (e.g. emulsions, liposomes) and amorphous dispersions are all formulation techniques utilized to enhance exposure. These types of formulations are optimized to the desired route of administration.