As the pharmaceutical industry shifts from small molecule drugs in favor of biologics, new, unique formulation needs emerge. Issues relating to shelf-stability of biologic formulations remain a key challenge to new drug development for both the developed and developing world. We have recently developed a new series of surfactant excipients for liquid thermal stabilization of biologic drugs. The surfactants were synthesized by stepwise amidation of myristoyl chloride with an amino acid and then the amino acid with a monofunctional Jeffamine™. In initial studies, a three-fold drop in IgG aggregation rate was observed by DLS for IgG formulated with these novel surfactants compared to control surfactant formulations. Isothermal circular dichroism (CD) further indicated improved structure retention for formulations containing the novel surfactant. Next, a commercial drug was reformulated with the novel excipient and significantly more protein monomer retention was observed during accelerated aging studies compared to the commercial formulation. This talk will discuss the development of the excipients and the assessment of their performance in several protein models using a variety of analytical tools.

Novel excipients for liquid stabilization of protein pharmaceuticals

252nd National Meeting (2016)

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