Development of dry powder formulations combining both a biologic therapeutic entity and a small molecule drug substance

Amy Worle & Harriet Bridgwater

An inhalation product combining a biological therapeutic entity with a small molecule drug substance is still a very novel concept in inhalation. A combination product would potentially have significant compliance and patient benefits via simplifying and reducing the time of treatment.
This study assessed the combination of an immunomodulatory protein (Omalizumab) with a co-prescribed corticosteroid (Fluticasone Propionate). The objective was to produce a biologically, chemically and physically stable powder formulation as evidenced by the stability data presented.
Small molecules and biologics are typically formulated and delivered in different ways, with biologics commonly developed as liquid formulations for injection. For this study the formulation was designed for delivery via a dry powder inhaler (DPI). Biologics can be rendered more stable in the solid state via co-formulation with specific excipients therefore a dry powder format can offer improved stability and potentially remove the necessity for refrigerated storage and transport.
The development of a combination dry powder formulation presented a number of challenges that were addressed through the combined use of spray drying and low intensity blending techniques. Excipients were identified to provide protein stability and improve aerosol performance. The physical stability (via aerosol performance testing) and biological integrity of the formulation was assessed for 6 months at 30⁰C/65% relative humidity. The study demonstrated that a small molecule and a biologic can be combined successfully to produce a novel model dry powder formulation with good homogeneity and stability.

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