Villate Aitor, Barreto Gastón Pablo, Nicolás Markel San, Aizpurua-Olaizola Oier, Olivares Maitane, Usobiaga Aresatz
Department of Analytical Chemistry, Faculty of Science and Technology, University of the Basque Country (UPV/EHU), 48940, Leioa, Basque, Spain.
Research Centre for Experimental Marine Biology and Biotechnology (PIE), University of the Basque Country (UPV/EHU), 48620, Plentzia, Basque, Spain.
AAPS PharmSciTech. 2024 May 30;25(5):120. doi: 10.1208/s12249-024-02836-4.
Cannabinoids, such as ∆-tetrahydrocannabinol (THC) and cannabidiol (CBD), are effective bioactive compounds that improve the quality of life of patients with certain chronic conditions. The copolymer poly(lactic-co-glycolic acid) (PLGA) has been used to encapsulate such compounds separately, providing pharmaceutical grade edible products with unique features. In this work, a variety of PLGA based nanoformulations that maintain the natural cannabinoid profile found in the plant (known as full-spectrum) are proposed and evaluated. Three different cannabis sources were used, representing the three most relevant cannabis chemotypes. PLGA nanocapsules loaded with different amounts of cannabinoids were prepared by nanoemulsion, and were then functionalized with three of the most common coating polymers: pectin, alginate and chitosan. In order to evaluate the suitability of the proposed formulations, all the synthesized nanocapsules were characterized, and their cannabinoid content, size, zeta-potential, morphology and in vitro bioaccessibility was determined. Regardless of the employed cannabis source, its load and the functionalization, high cannabinoid content PLGA nanocapsules with suitable particle size and zeta-potential were obtained. Study of nanocapsules' morphology and in vitro release assays in gastro-intestinal media suggested that high cannabis source load may compromise the structure of nanocapsules and their release properties, and hence, the use of lower content of cannabis source is recommended.
大麻素，如∆-四氢大麻酚（THC）和大麻二酚（CBD），是有效的生物活性化合物，可改善某些慢性病患者的生活质量。聚乳酸-乙醇酸共聚物（PLGA）已被用于分别封装此类化合物，从而提供具有独特特性的药用级可食用产品。在这项工作中，提出并评估了多种基于PLGA的纳米制剂，这些纳米制剂能保持植物中发现的天然大麻素特征（即全谱特征）。使用了三种不同的大麻来源，代表了三种最相关的大麻化学型。通过纳米乳液制备了负载不同量大麻素的PLGA纳米胶囊，然后用三种最常见的包衣聚合物进行功能化处理：果胶、海藻酸盐和壳聚糖。为了评估所提出制剂的适用性，对所有合成的纳米胶囊进行了表征，并测定了它们的大麻素含量、大小、zeta电位、形态和体外生物可及性。无论使用何种大麻来源、其负载量以及功能化处理如何，均获得了具有合适粒径和zeta电位的高大麻素含量PLGA纳米胶囊。对纳米胶囊形态的研究以及在胃肠道介质中的体外释放试验表明，大麻来源高负载量可能会损害纳米胶囊的结构及其释放特性，因此，建议使用较低含量的大麻来源。
