Love them or hate them, superhero films are among Hollywood’s tropiest genres. Over the years, these reoccurring storytelling elements have helped define the superhero category.
To begin with, superheroes are known for hiding in plain sight. By adopting mundane personas, they can operate unnoticed among ordinary people. One could say that pharmaceutical excipients are the mild-mannered Clark Kents of drug formulation. Often described as ‘inactive’ ingredients, it’s easy to see how their role in the final drug product could be underestimated.
But pharma manufacturers know the truth about excipients’ real identity. What appears to be an unremarkable white powder is, in fact, a critical player in enhancing a drug’s stability, bioavailability, delivery and safety. Without excipients, many of medicine’s biggest advances simply wouldn’t be possible.
And of course, you can’t have a superhero tale without superpowers — and as you’ll read in this issue’s cover story, excipients have plenty.
Excipients can be used as flavoring agents in bad-tasting chewable tablets or as coating agents in bad-smelling tablets. As binders, they hold APIs together to create solid dosage forms. They improve tablet compressibility and provide tablet hardness. As fillers and diluents, they enhance flowability during manufacturing while supporting uniform API distribution. Excipients are also enabling new drug forms, such as opioid abuse-deterrent formulations. Recently, they’ve played a key role in improving oral delivery of large molecule drugs, enhancing absorption in the stomach and protecting against degradation by gastric enzymes.
As we know, superheroes aim to save the world. In that spirit, new biodegradable excipients, such as naturally occurring polymers, are helping the pharma industry shift toward more sustainable, environmentally friendly practices.
No hero’s origin story is complete without tragedy. Lessons about the risks of irresponsible excipients were learned early on, unfortunately coming at the expense of human lives. In the 1930s, S.E. Massengill sought to convert sulfanilamide, a streptococcal infection treatment typically sold as tablets, into a liquid form. The company’s chief chemist selected diethylene glycol as a solvent — due to its sweet taste — to make the medication more palatable. What he failed to realize was that diethylene glycol was not a harmless excipient — it’s a deadly poison commonly used in antifreeze. More than 100 adults and children died after taking the liquid antibiotic.
Tragedies like this laid bare the need to safeguard drug product ingredients. Having learned the hard way, excipient manufacturers rallied around the moral obligation to use their abilities for good. Organizations such as IPEC-Americas were formed to help ensure the safe and eff ective production and use of excipients.
But as every superhero learns, challenges are always lurking around the corner. The lack of an independent regulatory approval pathway for novel excipients remains a stumbling block. But with the development of new grades of existing excipients as well as advances in excipient manufacturing processes, such as co-processing techniques, there is an overwhelming sense that this is not the end of the excipient innovation story. Stay tuned for the sequel.
Image Credit: Michael Annino | Shutterstock-AI