Lodzki M, Godin B, Rakou L, Mechoulam R, Gallily R, Touitou E
Department of Pharmaceutics, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, 91120, Israel.
J Control Release. 2003 Dec 12;93(3):377-87. doi: 10.1016/j.jconrel.2003.09.001.
Cannabidiol (CBD) is a new drug candidate for treatment of rheumatic diseases. However, its oral administration is associated with a number of drawbacks. The objective of this study was to design a transdermal delivery system for CBD by using ethosomal carriers. CBD ethosomes were characterized by transmission electron microscopy, confocal laser scanning microscopy and differential scanning calorimetry. Results indicated that CBD and phosphatidylcholine form an eutectic mixture. In vivo application of ethosomal CBD to CDI nude mice produced a significant accumulation of the drug in the skin and in the underlying muscle. Upon transdermal application of the ethosomal system to the abdomen of ICR mice for 72 h, steady-state levels were reached at about 24 h and lasted at least until the end of the experiment, at 72 h. Furthermore, transdermal application of ethosomal CBD prevented the inflammation and edema induced by sub-plantar injection of carrageenan in the same animal model. In conclusion, ethosomes enable CBD's skin permeation and its accumulation in a depot at levels that demonstrate the potential of transdermal CBD to be used as an anti-inflammatory treatment.
大麻二酚（CBD）是一种用于治疗风湿性疾病的新型候选药物。然而，其口服给药存在诸多缺点。本研究的目的是利用乙醇脂质体载体设计一种CBD的透皮给药系统。通过透射电子显微镜、共聚焦激光扫描显微镜和差示扫描量热法对CBD乙醇脂质体进行了表征。结果表明，CBD与磷脂酰胆碱形成了低共熔混合物。将乙醇脂质体形式的CBD应用于严重联合免疫缺陷（SCID）裸鼠体内，药物在皮肤和皮下肌肉中显著蓄积。将乙醇脂质体系统经皮应用于ICR小鼠腹部72小时后，约24小时达到稳态水平，至少持续到实验结束时的72小时。此外，在同一动物模型中，经皮应用乙醇脂质体形式的CBD可预防足底注射角叉菜胶引起的炎症和水肿。总之，乙醇脂质体可促进CBD的皮肤渗透及其在储存库中的蓄积，其水平表明经皮应用CBD具有作为抗炎治疗手段的潜力。
