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纳米制剂作为克服大麻素传递限制的策略。

Nanoformulations as a strategy to overcome the delivery limitations of cannabinoids.

机构信息

The Pangenomics Group, Biosciences and Food Technology, School of Science, RMIT University, Melbourne, Victoria, Australia.

MGC Pharmaceuticals Limited, West Perth, Western Australia, Australia.

出版信息

Phytother Res. 2023 Apr;37(4):1526-1538. doi: 10.1002/ptr.7742. Epub 2023 Feb 7.

Abstract

Medical cannabis has received significant interest in recent years due to its promising benefits in the management of pain, anxiety, depression and neurological and movement disorders. Specifically, the major phytocannabinoids derived from the cannabis plant such as (-) trans-Δ -tetrahydrocannabinol (THC) and cannabidiol (CBD), have been shown to be responsible for the pharmacological and therapeutic properties. Recently, these phytocannabinoids have also attracted special attention in cancer treatment due to their well-known palliative benefits in chemotherapy-induced nausea, vomiting, pain and loss of appetite along with their anticancer activities. Despite the enormous pharmacological benefits, the low aqueous solubility, high instability (susceptibility to extensive first pass metabolism) and poor systemic bioavailability restrict their utilization at clinical perspective. Therefore, drug delivery strategies based on nanotechnology are emerging to improve pharmacokinetic profile and bioavailability of cannabinoids as well as enhance their targeted delivery. Here, we critically review the nano-formulation systems engineered for overcoming the delivery limitations of native phytocannabinoids including polymeric and lipid-based nanoparticles (lipid nano capsules (LNCs), nanostructured lipid carriers (NLCs), nanoemulsions (NE) and self-emulsifying drug delivery systems (SEDDS)), ethosomes and cyclodextrins as well as their therapeutic applications.

摘要

近年来,由于医用大麻在治疗疼痛、焦虑、抑郁以及神经和运动障碍方面具有很大的潜力,因此引起了广泛关注。具体来说,从大麻植物中提取的主要植物大麻素,如(-)反式-Δ-四氢大麻酚(THC)和大麻二酚(CBD),已被证明具有药理学和治疗特性。最近,由于这些植物大麻素在化疗引起的恶心、呕吐、疼痛和食欲不振方面具有众所周知的缓解作用,以及其抗癌作用,它们在癌症治疗中也引起了特别关注。尽管具有巨大的药理学益处,但低水溶解度、高不稳定性(易受广泛的首过代谢影响)和差的全身生物利用度限制了它们在临床方面的应用。因此,基于纳米技术的药物输送策略正在兴起,以改善大麻素的药代动力学特性和生物利用度,并增强其靶向输送。在这里,我们批判性地回顾了为克服天然植物大麻素的输送限制而设计的纳米制剂系统,包括聚合物和基于脂质的纳米粒(脂质纳米囊(LNCs)、纳米结构脂质载体(NLCs)、纳米乳液(NE)和自乳化药物传递系统(SEDDS))、醇质体和环糊精以及它们的治疗应用。

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