Confinement of Amorphous Lactose in Pores Formed Upon Co-Spray Drying With Nanoparticles

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• 作者：Joel Hellrup ; ^{joel.hellrup@farmaci.uu.se} ; Denny Mahlin
• 关键词：amorphous ; crystallization ; glass transition ; mobility ; physical stability ; solid state stability ; stabilization ; spray drying
• 刊名：Journal of Pharmaceutical Sciences
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：106
• 期：1
• 页码：322-330
• 全文大小：1301 K
• 卷排序：106

文摘

This study aims at investigating factors influencing humidity-induced recrystallization of amorphous lactose, produced by co-spray drying with particles of cellulose nanocrystals or sodium montmorillonite. In particular, the focus is on how the nanoparticle shape and surface properties influence the nanometer to micrometer length scale nanofiller arrangement in the nanocomposites and how the arrangements influence the mechanisms involved in the inhibition of the amorphous to crystalline transition. The nanocomposites were produced by co-spray drying. Solid-state transformations were analyzed at 60%-94% relative humidity using X-ray powder diffraction, microcalorimetry, and light microscopy. The recrystallization rate constant for the lactose/cellulose nanocrystals and lactose/sodium montmorillonite nanocomposites was lowered at nanofiller contents higher than 60% and was stable for months at 80% nanofiller. The most likely explanation to these results is spontaneous formations of mesoporous particle networks that the lactose is confined upon co-spray drying at high filler content. Compartmentalization and rigidification of the amorphous lactose proved to be less important mechanisms involved in the stabilization of lactose in the nanocomposites.