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载大麻二酚固体脂质纳米粒改善体外炎症诱导细胞模型中促炎细胞因子和自由基的抑制作用。

Cannabidiol-Loaded Solid Lipid Nanoparticles Ameliorate the Inhibition of Proinflammatory Cytokines and Free Radicals in an In Vitro Inflammation-Induced Cell Model.

机构信息

Center of Excellence in Natural Products for Ageing and Chronic Diseases, Chulalongkorn University, Bangkok 10330, Thailand.

Department of Food and Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

出版信息

Int J Mol Sci. 2024 Apr 26;25(9):4744. doi: 10.3390/ijms25094744.

Abstract

Cannabidiol (CBD) is a non-psychoactive compound derived from . It has demonstrated promising effects in combating inflammation and holds potential as a treatment for the progression of chronic inflammation. However, the clinical application of CBD is limited due to its poor solubility and bioavailability. This study introduces an effective method for preparing CBD-loaded solid lipid nanoparticles (CBD-SLNs) using a combination of low-energy hot homogenization and ultrasonication. We enhanced this process by employing statistical optimization with response surface methodology (RSM). The optimized CBD-SLN formulation utilizes glyceryl monostearate as the primary lipid component of the nanocarrier. The CBD-SLN formulation is screened as a potential tool for managing chronic inflammation. Stable, uniformly dispersed spherical nanoparticles with a size of 123 nm, a surface charge of -32.1 mV, an encapsulation efficiency of 95.16%, and a drug loading of 2.36% were obtained. The CBD-SLNs exhibited sustained release properties, ensuring prolonged and controlled CBD delivery, which could potentially amplify its therapeutic effects. Additionally, we observed that CBD-SLNs significantly reduced both reactive oxygen and nitrogen species and proinflammatory cytokines in chondrocyte and macrophage cell lines, with these inhibitory effects being more pronounced than those of free CBD. In conclusion, CBD-SLNs demonstrated superiority over free CBD, highlighting its potential as an effective delivery system for CBD.

摘要

大麻二酚(CBD)是一种非精神活性化合物,来源于大麻。它在对抗炎症方面表现出了有希望的效果,并有可能成为治疗慢性炎症进展的一种方法。然而,由于 CBD 的溶解度和生物利用度差,其临床应用受到限制。本研究采用低能量热匀化和超声联合的方法,介绍了一种制备负载 CBD 的固体脂质纳米粒(CBD-SLNs)的有效方法。我们通过使用响应面法(RSM)进行统计优化来增强该过程。优化的 CBD-SLN 制剂采用单硬脂酸甘油酯作为纳米载体的主要脂质成分。筛选 CBD-SLN 制剂作为管理慢性炎症的潜在工具。得到了稳定、均匀分散的纳米粒,粒径为 123nm,表面电荷为-32.1mV,包封效率为 95.16%,载药量为 2.36%。CBD-SLNs 表现出持续释放的特性,确保了 CBD 的延长和控制释放,这可能会增强其治疗效果。此外,我们观察到 CBD-SLNs 显著降低了软骨细胞和巨噬细胞系中活性氧和氮物种以及促炎细胞因子的水平,其抑制作用比游离 CBD 更明显。总之,CBD-SLNs 优于游离 CBD,突出了其作为 CBD 有效递送系统的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14df/11083812/63e8c1a72f28/ijms-25-04744-g001.jpg

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