Francke Nadine Monika, Schneider Frederic, Baumann Knut, Bunjes Heike
Institute of Pharmaceutical Technology and Biopharmaceutics, Technische Universität Braunschweig, Mendelssohnstraße 1, 38106 Braunschweig, Germany.
Institute of Medicinal and Pharmaceutical Chemistry, Technische Universität Braunschweig, Beethovenstraße 55, 38106 Braunschweig, Germany.
Molecules. 2021 Mar 8;26(5):1469. doi: 10.3390/molecules26051469.
In this study, the general processability of cannabidiol (CBD) in colloidal lipid carriers was investigated. Due to its many pharmacological effects, the pharmaceutical use of this poorly water-soluble drug is currently under intensive research and colloidal lipid emulsions are a well-established formulation option for such lipophilic substances. To obtain a better understanding of the formulability of CBD in lipid emulsions, different aspects of CBD loading and its interaction with the emulsion droplets were investigated. Very high drug loads (>40% related to lipid content) could be achieved in emulsions of medium chain triglycerides, rapeseed oil, soybean oil and trimyristin. The maximum CBD load depended on the type of lipid matrix. CBD loading increased the particle size and the density of the lipid matrix. The loading capacity of a trimyristin emulsion for CBD was superior to that of a suspension of solid lipid nanoparticles based on trimyristin (69% vs. 30% related to the lipid matrix). In addition to its localization within the lipid core of the emulsion droplets, cannabidiol was associated with the droplet interface to a remarkable extent. According to a stress test, CBD destabilized the emulsions, with phospholipid-stabilized emulsions being more stable than poloxamer-stabilized ones. Furthermore, it was possible to produce emulsions with pure CBD as the dispersed phase, since CBD demonstrated such a pronounced supercooling tendency that it did not recrystallize, even if cooled to -60 °C.
在本研究中,对大麻二酚(CBD)在胶体脂质载体中的一般可加工性进行了研究。由于其多种药理作用,这种水溶性差的药物的药用目前正在深入研究中,而胶体脂质乳剂是这类亲脂性物质成熟的制剂选择。为了更好地了解CBD在脂质乳剂中的可形成性,研究了CBD负载的不同方面及其与乳剂液滴的相互作用。在中链甘油三酯、菜籽油、大豆油和肉豆蔻酸甘油酯的乳剂中可实现非常高的药物负载量(>40%与脂质含量相关)。最大CBD负载量取决于脂质基质的类型。CBD负载增加了脂质基质的粒径和密度。肉豆蔻酸甘油酯乳剂对CBD的负载能力优于基于肉豆蔻酸甘油酯的固体脂质纳米颗粒悬浮液(与脂质基质相关分别为69%和30%)。除了其在乳剂液滴脂质核心内的定位外,大麻二酚在很大程度上还与液滴界面相关。根据一项应力测试,CBD使乳剂不稳定,磷脂稳定的乳剂比泊洛沙姆稳定的乳剂更稳定。此外,有可能制备以纯CBD为分散相的乳剂,因为CBD表现出如此明显的过冷趋势,即使冷却至-60°C也不会重结晶。