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By Nicole Buist

RTC FellowCoauthors: Ken Liljegren and Thiago Carvalho

I often find myself reflecting on how it’s a wonderful time to be alive. New technologies give us new degrees of freedom. If I need directions to go somewhere, I type the address in my GPS. I was fortunate to spend the summer in Africa and was able to Skype home to my family and friends, closing the distance between us. All these new technologies have emerged to make our daily lives richer and more efficient. I mention this because it’s also a wonderful time to be a pharmaceutical scientist! There is no room for boredom as the industry charges forward, exploring all these new ways to provide medicines for current unmet medical needs. Suitable biologic formulations are a tall order, and I look forward to seeing all the innovative tricks the industry comes up with to solve the problem. This is what we do best after all, and don’t you just love a challenge?

Small molecule formulations benefit from many decades of extensive formulation design research and experience with excipients. Excipients play a vital role in the transformation of bulk active pharmaceutical ingredient (API) powder into a tablet that is shelf-and transport-stable but also dissolves properly once ingested. Even though there are years and years of experience formulating small molecules, new chemical entities often still require advanced formulation design and optimization.

Lately, the pharmaceutical industry has ventured into more challenging modalities that might be pursued for a specific target. Small molecule therapies are not necessarily the treatment of choice, and a biologic may be more desirable. Within the realm of biologics a target could require a small peptide, a fusion protein, or a monoclonal antibody. Each one of these biologic classes will require different formulation approaches. One could imagine that there may be gaps in our knowledge of how excipients are going to play a role in such new formulations. How will excipients impact biophysical stability? Can excipients help impart antimicrobial preservation? Will the current set of available excipients fill the voids, or do new challenges present opportunities for innovation? In the past, most biologics were delivered parenterally, but the new frontier of therapies could be delivered via alternative routes of administration as well. Novel routes of administration will require even more advanced formulation technologies to get the job done.

The 2015 AAPS National Biotechnology Conference will have the exciting open forum, Advances in Pharmaceutical Excipients towards Optimizing Delivery and Stability of Biopharmaceutical Products, which will highlight many of the issues mentioned above. Come learn about the latest formulation strategies that aim to stabilize biologics and deliver them efficiently, no matter the route of administration. The open forum will have top researchers present on already successful strategies for selecting inert and functional excipients for biopharmaceutical products, as well as an exciting example: use of a novel excipient to allow pulmonary delivery of insulin. Several companies failed, but Mannkind has solved the puzzle.

Nicole Buist, Ph.D. is a principal scientist in the Discovery Pharmaceutical Sciences department at Merck & Co., Inc. She is also the 2015 chair of the Excipients Focus Group and a Merck Fellow for Global Health.