This study considered the design and process development of nanomized products in two product forms: nanoemulsion and nanodispersible solids. The effect of product formulation and processing conditions on product attributes such as particle size and appearance were studied using orange oil and Oil Red 0 as model compounds. The relationship between particle size and product quality in terms of bioactivity and bioavailability was illustrated using schisandrin B, a strong antioxidant, as a model drug. The bioactivity as measured by in vivo glutathione regeneration capacity assay of schisandrin B with an average size of 45 nm was nearly double that of the original coarse schisandrin B; the corresponding bioavailability as measured by the plasma schisandrin B level in an animal study was 14.5-fold higher.