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体外经皮吸收研究大麻二酚的方法:探讨药物浓度、化学增强剂和精油的影响。

In vitro percutaneous absorption studies of cannabidiol using human skin: Exploring the effect of drug concentration, chemical enhancers, and essential oils.

机构信息

Center for Drug Delivery Research, Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, USA.

Department of Pharmaceutical Sciences, Bill Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN 37614, USA.

出版信息

Int J Pharm. 2022 Mar 25;616:121540. doi: 10.1016/j.ijpharm.2022.121540. Epub 2022 Feb 4.

DOI:10.1016/j.ijpharm.2022.121540
PMID:35124116
Abstract

Cannabidiol, a non-psychoactive constituent of cannabis, has garnered much attention after United States Food and Drug Administration approved Epidiolex® for oral use. Although therapeutic effect of cannabidiol after systemic absorption has been investigated extensively, its therapeutic potential in treating skin disorders after local delivery still needs further exploration. Our study has investigated the effect of cannabidiol concentration, chemical enhancers, and essential oils on percutaneous absorption of cannabidiol. In vitro permeation tests were conducted on human skin. The 24 h study results suggest no significant difference in amount of drug absorbed into skin, between 5% (242.41 ± 12.17 µg/cm) and 10% (232.79 ± 20.82 cm) cannabidiol solutions. However, 1% delivered (23.02 ± 4.74 µg/cm) significantly lower amount of drug into skin than 5% and 10%. Transcutol and isopropyl myristate did not enhance delivery of cannabidiol. However, oleic acid was found to be useful as chemical enhancer. Oleic acid (43.07 ± 10.11 µg/cm) had significantly higher cannabidiol delivery into skin than the group without oleic acid (10.98 ± 3.40 µg/cm) after a 4 h in vitro permeation study. Essential oils at concentrations tested had lower total cannabidiol delivery when compared to control. This study's findings will help guide future research on the pharmacological effect of percutaneously delivered cannabidiol on inflammatory skin disorders.

摘要

大麻的非精神活性成分大麻二酚在获得美国食品和药物管理局批准用于口服后引起了广泛关注。尽管大麻二酚在全身吸收后的治疗效果已经得到了广泛的研究,但它在局部给药治疗皮肤疾病方面的治疗潜力仍需要进一步探索。我们的研究调查了大麻二酚浓度、化学增强剂和精油对大麻二酚经皮吸收的影响。在人体皮肤上进行了体外渗透试验。24 小时研究结果表明,5%(242.41±12.17μg/cm)和 10%(232.79±20.82cm)大麻二酚溶液吸收到皮肤中的药物量没有显著差异。然而,1%的给药量(23.02±4.74μg/cm)显著低于 5%和 10%的给药量。Transcutol 和肉豆蔻酸异丙酯没有增强大麻二酚的传递。然而,发现油酸可用作化学增强剂。油酸(43.07±10.11μg/cm)在 4 小时的体外渗透研究中,向皮肤输送的大麻二酚明显高于不含油酸的组(10.98±3.40μg/cm)。在测试浓度下,精油的总大麻二酚传递量低于对照。本研究的结果将有助于指导未来对经皮给予大麻二酚治疗炎症性皮肤疾病的药理作用的研究。

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