Drugs should be designed with delivery in mind (and vice versa)

Cory Berkland, Ph.D.
University of Houston
Basic principles have emerged for oral and intravenous drug design, but fewer efforts have
aimed to create drugs that persist at the administration site or molecular structures that
promote drainage to regional lymphatic networks. Examples are:(1) Pharmaceutical
aerosols that must transit anatomical barriers to reach the desired target, a pathogen for
example. Novel structures that persist in mucus to eradicate pathogens will be presented.
(2) We designed soluble antigen arrays (SAgAs) to promote the drainage of autoantigens to
secondary lymphoid organs to treat autoimmune diseases by inducing immune tolerance.(3)
We designed immunostimulants that persist in tumor tissue after intratumoral/perilesional
injection. Intratumoral immunotherapy is proposed to work synergistically with checkpoint
inhibitors making a nonresponsive ‘cold’ tumor ‘hot’ by recruiting and activating tumor
infiltrating lymphocytes. Systemic immune-related adverse reactions can occur if
immunostimulant escapes the site of administration. This can be prevented by electrostatic
mechanisms. These examples show the need for rational design of drug molecules or
formulations based upon the route of delivery and biological barriers encountered.