Amorphous magnesium carbonate nanoparticles with strong stabilizing capability for amorphous ibuprofen

作者：Yang Jiaojiao; Alvebratt Caroline; Lu Xi; Bergstrom Christel A S; Stromme Maria; Welch Ken^*

来源：International Journal of Pharmaceutics, 2018, 548(1): 515-521.

DOI：10.1016/j.ijpharm.2018.07.021

• Magnesium carbonate
• Nanoparticles
• Nanocomposite
• Amorphous
• Ibuprofen
• Solubility
• Dissolution

Formulating active pharmaceutical ingredients (APIs) in the amorphous state can increase their apparent aqueous solubility and dissolution rate and consequently improve their bioavailability. This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved. Biocompatibility of the nanoparticles was demonstrated in vitro using human dermal fibroblasts and stability of the nanocomposite formulation was verified with a storage time of six months. The success of this novel formulation provides a promising approach for achieving improved apparent solubility and enhanced bioavailability of drugs.

• 出版日期2018-9