Advanced Medical Center, The Second Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan, P.R. China.
School of Life Sciences, Manipal Academy of Higher Education, Dubai, United Arab Emirates.
Biomed Pharmacother. 2022 Feb;146:112531. doi: 10.1016/j.biopha.2021.112531. Epub 2021 Dec 11.
Despite the promising medicinal properties, berberine (BBR), due to its relatively poor solubility in plasma, low bio-stability and limited bioavailability is not used broadly in clinical stages. Due to these drawbacks, drug delivery systems (DDSs) based on nanoscale natural polysaccharides, are applied to address these concerns. Natural polymers are biodegradable, non-immunogenic, biocompatible, and non-toxic agents that are capable of trapping large amounts of hydrophobic compounds in relatively small volumes. The use of nanoscale natural polysaccharide improves the stability and pharmacokinetics of the small molecules and, consequently, increases the therapeutic effects and reduces the side effects of the small molecules. Therefore, this paper presents an overview of the different methods used for increasing the BBR solubility and bioavailability. Afterwards, the pharmacodynamic and pharmacokinetic of BBR nanostructures were discussed followed by the introduction of natural polysaccharides of plant (cyclodextrines, glucomannan), the shells of crustaceans (chitosan), and the cell wall of brown marine algae (alginate)-based origins used to improve the dissolution rate of poorly soluble BBR and their anticancer and antibacterial properties. Finally, the anticancer and antibacterial mechanisms of free BBR and BBR nanostructures were surveyed. In conclusion, this review may pave the way for providing some useful data in the development of BBR-based platforms for clinical applications.
尽管小檗碱(BBR)具有很有前景的药用特性,但由于其在血浆中的溶解度相对较低、生物稳定性差和生物利用度有限,因此并未广泛应用于临床阶段。由于这些缺点,基于纳米级天然多糖的药物传递系统(DDS)被应用于解决这些问题。天然聚合物是可生物降解、非免疫原性、生物相容和无毒的物质,能够将大量疏水性化合物捕获在相对较小的体积内。纳米级天然多糖的使用提高了小分子的稳定性和药代动力学特性,从而提高了治疗效果并降低了小分子的副作用。因此,本文综述了提高 BBR 溶解度和生物利用度的不同方法。随后,讨论了 BBR 纳米结构的药效学和药代动力学,接着介绍了用于提高难溶性 BBR 溶解速率及其抗癌和抗菌特性的植物来源的天然多糖(环糊精、葡甘露聚糖)、甲壳类动物外壳(壳聚糖)和褐藻细胞壁(海藻酸盐)。最后,调查了游离 BBR 和 BBR 纳米结构的抗癌和抗菌机制。总之,本综述可能为基于 BBR 的平台在临床应用中的开发提供一些有用的数据。