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Optimized Composite Particles for API-independent Formulations with Enhanced Performance

Moura C, Neves F, Costa E.

RDD Europe 2015. Volume 1, 2015: 165-176.

Abstract:

The design of carrier-free, dry powder composite particle formulations for pulmonary administration is an emerging area of research, since these engineered particles allow improved delivery efficiency over traditional lactose-based ordered mixtures and enhanced control over powder properties. Spray drying has been the particle engineering technology most frequently used for the production of composite particles. An integrated knowledge of both formulation and process design is important for obtaining dispersible and stable formulations with the desired attributes through a scalable process. Herein, a quality by design (QbD) approach, using design of experiments (DoE), was adopted to optimize the aerodynamic performance of active pharmaceutical ingredient (API)-free composite particles through the integrated modeling of the spray drying process and formulation parameters. Composite particles with fine particle fractions as high as 75% were obtained using spray drying conditions viable for large-scale manufacturing and future scale-up. In addition, the performance of the API-free composite particles was shown to be independent of low-dose incorporated model drugs: tobramycin, salmeterol xinafoate, and iopamidol. This is an indication that development can be performed up front without the need to include the API for low-dosage formulations.