Tailoring α/β Ratio of Pollen-Like Anhydrous Lactose as Ingredient Carriers for Controlled Dissolution Rate

Abstract

Lactose is a commonly used excipient with two isomers. Different isomers have different properties, especially in terms of solubility. This work is mainly to explore the influence of different a/β ratio lactose on drug dissolution. This work has developed novel mesoporous pollen-like lactose anhydrous with tailored α/β ratios as ingredient carriers for controlled dissolution rate. The produced lactose carriers are pollen-like with a particle size of ~15 μm and a mean pore width of ~30 nm. β-lactose anhydrous has a unique FTIR-peak at 948 cm−1, whereas α-lactose anhydrous shows a unique FTIR-peak at 855 cm−1. DSC analysis suggests that the pollen-like α/β-lactose crystals are polymorphs with unique peaks of melting points. XRD analysis suggests that (5:5)α/β-lactose polymorph has high crystalline purity. The loading efficiency (30.6–33.4% w/w) of acetamidophenol within the nanoporous lactose particles is dependent on the surface structure and pore volumes—the pore volumes were found to be 0.0209–0.0380 cm3/g. The release rates of acetamidophenol are lower for lactose with high α/β ratios. The lactose solubility and the first-order release constant can be tailored by changing the proportion of β-lactose in the pollen-like lactose carriers.

Keywords

• pollen-like anhydrous lactose
• α/β ratio
• solubility
• controlled release