Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0082, USA.
Drug Dev Ind Pharm. 2010 Sep;36(9):1088-97. doi: 10.3109/03639041003657295.
The nonpsychoactive cannabinoid, cannabidiol (CBD), has great potential for the treatment of chronic and 'breakthrough' pain that may occur in certain conditions like cancer. To fulfill this goal, suitable noninvasive drug delivery systems need to be developed for CBD. Chronic pain relief can be best achieved through the transdermal route, whereas 'breakthrough' pain can be best alleviated with intranasal (IN) delivery. Combining IN and transdermal delivery for CBD may serve to provide patient needs-driven treatment in the form of a nonaddictive nonopioid therapy.
Herein we have evaluated the IN and transdermal delivery of CBD with and without permeation enhancers.
In vivo studies in rats and guinea pigs were carried out to assess nasal and transdermal permeation, respectively.
CBD was absorbed intranasally within 10 minutes with a bioavailability of 34-46%, except with 100% polyethylene glycol formulation in rats. Bioavailability did not improve with enhancers. The steady-state plasma concentration of CBD in guinea pigs after transdermal gel application was 6.3 +/- 2.1 ng/mL, which was attained at 15.5 +/- 11.7 hours. The achievement of a significant steady-state plasma concentration indicates that CBD is useful for chronic pain treatment through this route of administration. The steady-state concentration increased by 3.7-fold in the presence of enhancer. A good in vitro and in vivo correlation existed for transdermal studies.
The results of this study indicated that CBD could be successfully delivered through the IN and transdermal routes.
非精神活性大麻素，大麻二酚（CBD），对于治疗癌症等某些情况下可能发生的慢性和“突破性”疼痛具有巨大潜力。为了实现这一目标，需要开发合适的非侵入性药物输送系统用于 CBD。慢性疼痛缓解可以通过透皮途径实现，而“突破性”疼痛可以通过鼻内（IN）给药得到最佳缓解。IN 和透皮联合给药 CBD 可能有助于以非成瘾性非阿片类疗法的形式提供满足患者需求的治疗。
本文评估了有和没有渗透促进剂的 CBD 的 IN 和透皮给药。
在大鼠和豚鼠中进行了体内研究，分别评估鼻内和透皮渗透。
CBD 在 10 分钟内经鼻内吸收，生物利用度为 34-46%，但在大鼠中 100%的聚乙二醇制剂除外。生物利用度没有随着促进剂的增加而提高。豚鼠经透皮凝胶给药后 CBD 的稳态血浆浓度为 6.3+/-2.1ng/mL，在 15.5+/-11.7 小时达到。通过这种给药途径达到显著的稳态血浆浓度表明 CBD 可用于慢性疼痛治疗。在存在促进剂的情况下，稳态浓度增加了 3.7 倍。透皮研究存在良好的体外和体内相关性。
这项研究的结果表明 CBD 可以通过 IN 和透皮途径成功输送。
