Drug delivery technologies are developed to improve treatments for patients. Technology innovation can spring from academic and commercial innovation. However good the science is, it is only of value for the business if it can be translated into successful products.

Ferring has successfully developed drug delivery science into products to Help Patients Live Healthy Lives in the fields of Women’s Health, Reproductive Medicine, Urology and Gastroenterology. Examples will be shared of polymer controlled release PROPESS® vaginal system, long acting topical TESTAVAN® gel and bowel cleanser CLENPIQ® solution.

Ferring and other organisations continue to work on bringing new technologies closer to the market in on-going clinical trials. The international rules for clinical study publication allows these novel technology approaches to be shared with the scientific community at large. Examples will be shared of prolonged vaginal delivery, sustained release injectables and orally administered peptide. This provides global awareness of where science does meet business needs.

The modern drug delivery technology is only 60 years old. During the first 30 years many breakthrough formulations were developed helping patients deal with various diseases effectively. The progress in the last few decades, however, has been slow, and many important drug delivery problems have not been resolved. The field has been overwhelmed by nanotechnology, nanomedicine, and many nano-sized drug delivery systems. The drug delivery field is at the strategic inflection point, and it is time for us to find new ways of developing effective drug delivery systems. The future of this field depends on nurturing talented young scientists with purpose, passion, and the conviction of doing meaningful science. The progress will be accelerated, if all of us achieve enlightened mindset embracing paradoxes and diverse ideas.

In drug delivery field, bioavailability and specificity are key challenges in the establishment of advanced products. Nanoparticles have been proposed by our group as valid approaches to provide successful systems to deliver drugs to their site of action. Besides the proper control of nanoparticle matrix to provide a suitable release of drug payload, the surface of nanoparticles has a major impact on the interaction with biological barriers and cell membranes. We have studied thoroughly the interaction of nanoparticles with cells and mucus regarding their adhesive properties that modulates their mucoadhesive behaviour, ultimately related with passive targeting to mucosae. Understanding how nanosystems interact with individual mucin chains and the 3D structure of mucus is paramount, as a passive functionalization of nanoparticles may concern, exploring different biomaterials as mucus-modulators. Our active targeting approach for nanoparticles has been focused on ligand molecules attached to the surface of nanoparticles to increase the probability of binding to unregulated cell membrane receptors in key local effector sites. New and less - explored receptors are being targeted in engineered nanosystems, providing enhanced local and intracellular levels of drugs, without compromise the safety of the systems. In this talk, application of nanosystems for mucosal delivery of drugs with physiological and social impact, developed in our research group, will be presented. The surface modification of nanomaterials with targeting moieties, from biological biomacromolecules to biopolymers, has been successfully attained.

Not too far back in our evolution, man was a nomadic hunter-gatherer and warrior, and food was distinctly unprocessed and fibre rich. The gut had to work hard to extract nutrients from a diverse matrix and protect the body against the occasional poisons from the seeds of berries and fruits which might be ingested. For many nutrients, absorption is an active process since the products of digestion are small and polar and the nature of the epithelium is a lipoidal barrier. In contrast, drugs have almost no nutritional value but are more easily absorbed passively. Mechanisms that help us to protect ourselves from poisons have evolved: specifically taste and the vomiting reflex have to be intentionally bypassed by disguise in a formulation. All the formulation work then has to be undone in the gut in a timely fashion to achieve the anticipated drug concentration -time exposure. Most drugs in the pipeline belong to Class to of the BCS or Class IIa or IIb of the DCS and therefore have limited aqueous solubility. This can limit the rate and extent of absorption, but is strongly influenced by formulation. Moving towards a robust in vitro test to predict performance is therefore a key step in the optimisation of an oral medicine. The task we face therefore is how to make continuous measurements in a murky media, whose composition changes along the gastrointestinal tract. Within the darkness of the gut, phenomena such as disintegration, super-saturation, precipitation and dissolution are occurring in unidentified segments. The simulated biological fluids that are used in pharmaceutical sciences are evolving recipes and much research is directed towards in silico prediction through better in vitro tests.

Our research programme within the OrBiTo program, in collaboration with other European universities and major pharmaceutical companies, has attempted to more closely define the influence of the composition of fluids in the gut in order to be able to improve the prediction of drug and formulation behaviour. This lecture will review some of the progress in this large initiative across the three feeder work packages.