We report here on spherical lactose agglomerates as potential carriers for inhalation applications. Micromeritic properties of three spherical lactose agglomerates (SA-A, SA-B, SA-C) and a standard lactose inhalation grade carrier (Lactohale 100; LH100) were evaluated and compared. Ordered mixtures with micronized salbutamol sulfate as the model active pharmaceutical ingredient (API) and lactose carriers at two drug loadings (2 wt%, 5 wt%) were prepared, and in-vitro aerosolization performance was assessed. The spherical crystallization process led to particles with tailored micromeritic properties. These had larger specific surface area and greater fine fraction < 10 µm, compared to LH100, due to their coarse morphology. Their properties were reflected in the flowability parameters, where two types of spherical agglomerates of lactose showed more cohesive behavior compared to the other lactose grades. Blend uniformity showed improved homogeneous distribution of the API at higher drug load. In-vitro aerosolization tests showed that the spherical agglomerates of lactose enhanced the dose of API, compared to LH100. SA-B and SA-C showed significantly higher fine particle fractions at low drug load compared to the others, whereas overall, the largest fine particle fraction was for SA-B at high drug load. The carrier material attributes related to particle size, specific surface area, compressibility, flowability (cohesion, flow function), and air permeability were critical for aerosolization performance.
|Seiten (von - bis)||11-20|
|Fachzeitschrift||European Journal of Pharmaceutics and Biopharmaceutics|
|Publikationsstatus||Veröffentlicht - Feb. 2021|
ASJC Scopus subject areas
- Pharmazeutische Wissenschaften