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两种Δ8-四氢大麻酚纳米乳液制剂在大鼠体内的药代动力学


来源: Shlomo Leibtag et al  发布日期: 2024-05-27  访问量: 38


在过去的几十年里,已经证明大麻素具有广泛的治疗益处。然而,它们的口服给药虽然可以说是最方便和最离散的,但由于提取物的强亲脂性,其生物利用度低、起效延迟和再现性差。为了克服这些障碍,大麻素可以被掺入水包油纳米乳液中:众所周知,这一过程可以通过使亲脂性生物活性物质表现得像水溶性(亲水性)化合物来增强其递送。在这份手稿中,描述了含有大麻提取物(CBDX,55%大麻二酚)的纳米乳液的配方开发和生产放大程序。通过高强度超声液体处理制备了纳米乳液样品,并根据载体油和表面活性剂的含量以及表面活性剂混合物的亲水-亲脂性平衡(HLB)对配方进行了优化
标签: Δ8-四氢大麻酚、纳米制剂、超声波萃取
 

PHARMACOKINETICS OF TWO NANOEMULSION FORMULATIONS OF Δ8‐TETRAHYDROCANNABINOL IN RATS

两种Δ8-四氢大麻酚纳米乳液制剂在大鼠体内的药代动力学

Shlomo Leibtag, Alexey S. Peshkovsky, Journal of Drug Delivery Science and Technology, Volume 60, August 2020.

Abstract

Over the past several decades, it has been demonstrated that cannabinoids offer a wide range of therapeutic benefits. Their oral administration, however, while arguably the most convenient and discrete, has been associated with low bioavailability, delayed onset of action and poor reproducibility resulting from the extracts’ strongly lipophilic character. To overcome these obstacles, cannabinoids can be incorporated into oil-in-water nanoemulsions: a process known to enhance the delivery of lipophilic bio-actives by making them behave like water-soluble (hydrophilic) compounds. In this manuscript, formulation development and production scale-up procedures for a cannabis extract (CBDX, 55% cannabidiol)-containing nanoemulsion are described. Nano-emulsion samples were prepared by high-intensity ultrasonic liquid processing, and the formulation was optimized for carrier oil and surfactant(s) contents as well as for the hydrophilic-lipophilic balance (HLB) of the surfactant mixture. Translucent CBDX-containing nanoemulsions with median droplet sizes well below 100 nm were possible to form with synthetic surfactants (Tween 80/Span 80 mixture), but not with a natural surfactant (Q-naturale®). By utilizing Barbell Horn® Ultrasonic Technology (BHUT), the nano-emulsification process was successfully scaled up, achieving a commercial-level processing rate equivalent to one million nanoemulsified 10 mg CBDX doses made per month with a single bench-scale ultrasonic liquid processor (BSP-1200).

在过去的几十年里,已经证明大麻素具有广泛的治疗益处。然而,它们的口服给药虽然可以说是最方便和最离散的,但由于提取物的强亲脂性,其生物利用度低、起效延迟和再现性差。为了克服这些障碍,大麻素可以被掺入水包油纳米乳液中:众所周知,这一过程可以通过使亲脂性生物活性物质表现得像水溶性(亲水性)化合物来增强其递送。在这份手稿中,描述了含有大麻提取物(CBDX,55%大麻二酚)的纳米乳液的配方开发和生产放大程序。通过高强度超声液体处理制备了纳米乳液样品,并根据载体油和表面活性剂的含量以及表面活性剂混合物的亲水-亲脂性平衡(HLB)对配方进行了优化。使用合成表面活性剂(Tween 80/Span 80混合物)可以形成中值液滴尺寸远低于100 nm的含半透明CBDX的纳米乳液,但使用天然表面活性剂不能形成(Q-naturale®)。通过利用Barbell Horn®超声波技术(BHUT),成功地扩大了纳米乳化工艺的规模,实现了相当于每月用单个台式超声波液体处理器(BSP-1200)生产100万剂纳米乳化10 mg CBDX的商业级加工率。

 

 


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