Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Denmark.
University of Applied Sciences and Arts Northwestern Switzerland, Institute of Pharmaceutical Technology, Hofackerstr. 30, CH-4132 Muttenz, Switzerland.
Eur J Pharm Sci. 2023 Oct 1;189:106556. doi: 10.1016/j.ejps.2023.106556. Epub 2023 Aug 4.
Lipid-based formulations, in particular supersaturated lipid-based formulations, are important delivery approaches when formulating challenging compounds, as especially low water-soluble compounds profit from delivery in a pre-dissolved state. In this article, the classification of lipid-based formulation is described, followed by a detailed discussion of different supersaturated lipid-based formulations and the recent advances reported in the literature. The supersaturated lipid-based formulations discussed include both the in situ forming supersaturated systems as well as the thermally induced supersaturated lipid-based formulations. The in situ forming drug supersaturation by lipid-based formulations has been widely employed and numerous clinically available products are on the market. There are some scientific gaps in the field, but in general there is a good understanding of the mechanisms driving the success of these systems. For thermally induced supersaturation, the technology is not yet fully understood and developed, hence more research is required in this field to explore the formulations beyond preclinical studies and initial clinical trials.
脂质体制剂，特别是过饱和脂质体制剂，是在对具有挑战性的化合物进行制剂时的重要给药途径，因为特别是低水溶性的化合物可以从溶解前的状态下得到受益。本文描述了脂质体制剂的分类，然后详细讨论了不同的过饱和脂质体制剂以及文献中报道的最新进展。讨论的过饱和脂质体制剂包括原位形成的过饱和系统以及热诱导的过饱和脂质体制剂。通过脂质体制剂的药物原位形成过饱和已得到广泛应用，并且市场上有许多临床可用的产品。该领域存在一些科学空白，但总体而言，人们对这些系统成功的驱动机制有了很好的理解。对于热诱导过饱和，该技术尚未得到充分的理解和开发，因此该领域需要更多的研究来探索超越临床前研究和初步临床试验的制剂。
