在相关胃肠道条件下控制释放大麻二醇的纳米脂质体
Karol Zapata1, Stephania Rosales1, As Rios1
1Grupo de Investigación en Fenómenos de Superficie-Michael Polanyi, Departamento de Procesos y Energía, Facultad de Minas, Universidad Nacional de Colombia, Sede Medellín, Medellín 050034, Colombia.
ACS omega
|November 29, 2023
概括
这项研究开发了低成本的纳米脂质体,以提高大麻 (CBD) 的溶解度和受控释放. 纳米CBD配方证明了对结肠癌细胞的安全性和显著的抗瘤活性,提供了一种新的治疗方法.
科学领域:
- 制药科学 制药科学
- 纳米技术纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 大麻二醇 (CBD) 具有治疗潜力,但面临着诸如低生物可用性和溶解性等挑战.
- 现有的制药局限性阻碍了基于CBD的有效药物的开发.
- 需要新的药物输送系统来克服CBD固有的物理化学障碍.
研究的目的:
- 开发一种简单,低成本的纳米脂质体配方,以提高CBD水溶性.
- 为了实现控制的CBD从口腔到肠道的输送.
- 评估纳米-CBD配方的细胞毒性和抗瘤活性.
主要方法:
- 封装CBD的核心外纳米脂质体在三个步骤中合成.
- 描述包括TEM,DLS,FTIR,TGA和PZ用于结构和化学分析.
- 在模拟生理条件下 (口腔,十二指肠) 进行了体外溶解研究.
- 用Korsmeyer-Peppas和Noyes-Whitney模型建模了药理动力学模型.
- 评估了对HaCaT细胞的细胞毒性和对SW480结肠癌细胞的抗增殖作用.
主要成果:
- 成功合成了含有CBD的纳米脂质体,其核实了核心外结构,纳米尺寸和增强的水溶性.
- 观察到受控的CBD释放,由于在pH>7.2.2时的莱西外不稳定,在十二指肠条件下溶解率更高.
- 非Fickian扩散动力学控制了CBD释放,正如Korsmeyer-Peppas模型所证实的那样.
- 在高度下,纳米CBD对高达1000mg·L-1的HaCaT细胞显示出安全性,对SW480细胞具有显著的抗瘤活性.
结论:
- 开发的纳米脂质体系统有效地提高了CBD的水溶性,并使控制释放成为可能.
- 纳米CBD表现出良好的安全性和对结肠癌细胞有强大的抗增殖作用.
- 这种低成本的纳米-CBD配方为药物管理和癌症化疗提供了一个有前途的新途径.
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