Micronization and Agglomeration: Understanding the Impact of API Particle Properties on Dissolution and Permeability Using Solid State and Biopharmaceutical “Toolbox”

The study aims to investigate the effect of agglomeration on micronized model active pharmaceutical ingredient (API) and to unravel the influence of API agglomerate strength on dissolution and permeation.

Methods
Model API (micronized and unmicronized) were characterized using X-ray powder diffractometry (XRPD), differential scanning calorimetry (DSC), Raman imaging, optical profilometry, and miniaturized dissolution apparatuses. Two-way ANOVA with replication was used to interpret results with statistical significance.

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Results
The API used in this study is most stable, non-solvated/non-hydrated, non-ionizable, and neutral in nature and belongs to BCS class III. The morphology of the API was needle or rod shaped, and to achieve desired manufacturability, API was micronized; however, the micronized API showed slower dissolution. Micronization resulted in high surface energy which led to the formation of agglomerates.

Conclusions
The most significant conclusion is the integration, as well as implementation, of material science tetrahedron during early stages of formulation development (micronization) which would help to understand raw material variability. This would circumvent the undesired effects of API agglomeration and accelerate the transformation from R&D prototyping to commercialization. More on micronization and agglomeration

excipients