Alvebratt Caroline, Dening Tahnee J, Åhlén Michelle, Cheung Ocean, Strømme Maria, Gogoll Adolf, Prestidge Clive A, Bergström Christel A S
Department of Pharmacy, Uppsala Biomedical Centre P.O. Box 580, Uppsala University, SE-751 23, Uppsala, Sweden.
University of South Australia, UniSA: Clinical and Health Sciences, Adelaide SA 5000, Australia.
Pharmaceutics. 2020 May 6;12(5):426. doi: 10.3390/pharmaceutics12050426.
Lipid-based formulations can circumvent the low aqueous solubility of problematic drug compounds and increase their oral absorption. As these formulations are often physically unstable and costly to manufacture, solidification has been suggested as a way to minimize these issues. This study evaluated the physicochemical stability and in vitro performance of lipid-loaded mesoporous magnesium carbonate (MMC) particles with an average pore size of 20 nm. A medium chain lipid was loaded onto the MMC carrier via physical adsorption. A modified in vitro lipolysis setup was then used to study lipid release and digestion with H nuclear magnetic resonance spectroscopy. The lipid loading efficiency with different solidification techniques was also evaluated. The MMC, unlike more commonly used porous silicate carriers, dissolved during the lipolysis assay, providing a rapid release of encapsulated lipids into solution. The digestion of the dispersed lipid-loaded MMC therefore resembled that of a coarse dispersion of the lipid. The stability data demonstrated minor degradation of the lipid within the pores of the MMC particles, but storage for three months did not reveal extensive degradation. To conclude, lipids can be adsorbed onto MMC, creating a solid powder from which the lipid is readily released into the solution during in vitro digestion. The chemical stability of the formulation does however merit further attention.
基于脂质的制剂可以克服有问题的药物化合物的低水溶性，并增加其口服吸收。由于这些制剂通常物理稳定性差且制造成本高，因此有人提出固化是减少这些问题的一种方法。本研究评估了平均孔径为20nm的载脂介孔碳酸镁（MMC）颗粒的物理化学稳定性和体外性能。通过物理吸附将中链脂质负载到MMC载体上。然后使用改进的体外脂解装置，通过氢核磁共振光谱研究脂质释放和消化情况。还评估了不同固化技术的脂质负载效率。与更常用的多孔硅酸盐载体不同，MMC在脂解试验期间溶解，从而将包封的脂质快速释放到溶液中。因此，分散的载脂MMC的消化类似于脂质粗分散体的消化。稳定性数据表明MMC颗粒孔内的脂质有轻微降解，但储存三个月未发现广泛降解。总之，脂质可以吸附到MMC上，形成一种固体粉末，在体外消化过程中脂质很容易从该粉末释放到溶液中。然而，该制剂的化学稳定性确实值得进一步关注。
