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增强疼痛管理中大麻素的生物利用度:环糊精的作用。

Enhancing Cannabinoid Bioavailability in Pain Management: The Role of Cyclodextrins.

机构信息

Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisbon, Portugal.

出版信息

Molecules. 2024 Nov 13;29(22):5340. doi: 10.3390/molecules29225340.

DOI:10.3390/molecules29225340
PMID:39598730
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11596380/
Abstract

Chronic pain (CP), including pain related to cancer, affects approximately 2 billion people worldwide, significantly diminishing quality of life and imposing socio-economic burdens. Current treatments often provide limited relief and may cause adverse effects, demanding more effective alternatives. Natural compounds from L., particularly cannabinoids like THC and CBD, exhibit analgesic and anti-inflammatory properties, but their therapeutic use is restricted by poor solubility and low bioavailability. Cyclodextrins (CDs) and cyclic oligosaccharides may encapsulate hydrophobic drugs in order to enhance their solubility and stability, offering a promising solution to these challenges. This study explores the formation of CD inclusion complexes with cannabinoids and specific terpenes, such as D-limonene (LIM), beta-caryophyllene (BCP), and gamma-terpinene (γ-TPN), aiming to improve pharmacokinetic profiles and therapeutic efficacy. We discuss analytical techniques for characterizing these complexes and their mechanisms of action, highlighting the potential of CDs to optimize drug formulations. The integration of CDs in cannabinoid therapies may enhance patient compliance and treatment outcomes in CP management. Future research should focus on innovative formulations and delivery systems to maximize the clinical applications of those compounds.

摘要

慢性疼痛(CP),包括与癌症相关的疼痛,影响着全球约 20 亿人,显著降低了生活质量,并造成了社会经济负担。目前的治疗方法往往提供有限的缓解,并且可能会引起不良反应,因此需要更有效的替代方法。L. 的天然化合物,特别是大麻素如 THC 和 CBD,具有镇痛和抗炎特性,但由于溶解度差和生物利用度低,其治疗用途受到限制。环糊精(CDs)和环状低聚糖可以将疏水性药物包合在内,以提高其溶解度和稳定性,为解决这些挑战提供了一个有前途的解决方案。本研究探讨了与大麻素和特定萜烯(如 D-柠檬烯(LIM)、β-石竹烯(BCP)和γ-松油烯(γ-TPN)形成 CD 包合物的情况,旨在改善药代动力学特征和治疗效果。我们讨论了用于表征这些配合物及其作用机制的分析技术,强调了 CDs 优化药物配方的潜力。将 CDs 整合到大麻素疗法中可能会提高 CP 管理中患者的依从性和治疗效果。未来的研究应侧重于创新的配方和输送系统,以最大程度地发挥这些化合物的临床应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/61d78b076aea/molecules-29-05340-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/81d8fa812728/molecules-29-05340-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/665021354b08/molecules-29-05340-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/4d5af0f0c5dd/molecules-29-05340-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/61d78b076aea/molecules-29-05340-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/81d8fa812728/molecules-29-05340-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/665021354b08/molecules-29-05340-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/4d5af0f0c5dd/molecules-29-05340-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0eaa/11596380/61d78b076aea/molecules-29-05340-g004.jpg

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