Nanotechnology and Functional Materials, Department of Engineering Science, Uppsala University, Uppsala 751 21, Sweden.
Department of Pharmacy, Uppsala Biomedical Center, Uppsala University, Uppsala 751 23, Sweden.
Int J Pharm. 2018 Sep 5;548(1):515-521. doi: 10.1016/j.ijpharm.2018.07.021. Epub 2018 Jul 5.
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.
将活性药物成分（APIs）制成无定形状态可以提高其表观水溶性和溶解速率，从而提高其生物利用度。本研究首次证明，通过将纳米级碳酸镁粒子的固体分散体应用于 API 中，可以将 API 稳定在无定形状态。具体来说，仅使用 17wt%wt 的无定形碳酸镁纳米粒子，就能够将高达 83 倍的布洛芬比例稳定在无定形状态，并且实现了比结晶状态快 83 倍的药物释放速率。通过使用人真皮成纤维细胞在体外证明了纳米粒子的生物相容性，并且通过六个月的储存时间验证了纳米复合材料配方的稳定性。这种新型制剂的成功为提高药物的表观溶解度和增强生物利用度提供了一种有前途的方法。
