High drug load and performance formulation platform for DPIs
Susana Saldanha1, Filipe Vultos2, João Pires1 & Eunice Costa1
1Inhalation and Advanced Drug Delivery, R&D, Hovione FarmaCiência SA, Lumiar, 1649-038, Portugal
2Analytical Development, R&D, Hovione FarmaCiência SA, Lumiar, 1649-038, Portugal
Summary
The work reports the development of an enhanced inhalable pharmaceutical formulation for high dose delivery to the lungs that comprises spray dried crystalline particles coated with a force control agent. Carrier-free dry powder formulations for inhalation comprise a widespread array of presentations for the delivery of active ingredients to the lungs. Composite particles manufactured by spray-drying from a solution, for high load formulations, are well established and can lead to suitable aerodynamic performance. Nevertheless, these dry powders often require more challenging storage and handling conditions to ensure their stability due to the amorphous state of the API and of stabilizing excipients. Moreover, amorphous API can result in a faster dissolution which may not be suitable for specific indications. Consequently, Spaycoat, a formulation platform for high drug load formulations comprising crystalline API and relatively low percentage of excipients (by coating the API surface) can circumvent some of these drawbacks towards more effective medicines. The results demonstrate that crystalline active ingredient particles coated with a force control agent, such as Leucine, provides a solution for delivering high drug loads to the lungs by increasing more than 4 times the fine particle fraction (FPF) from 7% to 38% when comparing with the uncoated API particles. The results show that this formulation platform can be applied in a wide range of therapeutic indications that require high drug load inhalable powders. In addition, the combination of the formulation with a high performance device such as Sunriser®, can further improve the delivered dose efficiency.