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树状化:一种提高用于生物医学应用的分子系统性能的实用策略。

Dendronization: A practical strategy to improve the performance of molecular systems used in biomedical applications.

机构信息

Instituto de Investigaciones en Materiales, Universidad Nacional Autónoma de México, Mexico City, 04510, Mexico.

Instituto de Investigaciones en Materiales, Universidad Nacional Autónoma de México, Mexico City, 04510, Mexico.

出版信息

Eur J Med Chem. 2022 Feb 5;229:113988. doi: 10.1016/j.ejmech.2021.113988. Epub 2021 Nov 12.

DOI:10.1016/j.ejmech.2021.113988
PMID:34801269
Abstract

Nanomedicine is an emerging area that largely influences the efficacy of various therapies through the rational design of new materials exhibiting more targeted behavior. The synthetic effort, the amount of used material, and the cost are critical parameters to bear in mind if the production of the designed material is intended to be scaled for their widespread use. Even though materials science offers diverse options for different types of therapies, it is a difficult task to meet all the parameters mentioned above. The dendronization appears as an insightful approach to incorporate all the known benefits of the dendritic architecture by the attachment of dendrons to therapeutic agents, but in a much more affordable manner in terms of synthetic effort, amount of material, and cost. As will be presented, the most common dendrons used for biomedical applications are polyamide, polyester, carbosilane, polyether, and glycol-type, which are bonded to biological active molecules (BAMs), or molecular nanoplatforms (MPs) by hydrolysable bonds. Also relevant is the fact that the incorporation of dendrons not larger than third generation (G3) is sufficient to improve essential properties of these molecular systems, such as aqueous solubility, stability, and cellular internalization, among others. The type of dendron and its location on the BAMs or MPs, similar to placing a Lego piece on a model, will be decisive for obtaining the desired properties.

摘要

纳米医学是一个新兴领域,通过合理设计表现出更靶向行为的新材料,在很大程度上影响各种疗法的疗效。如果设计材料的生产旨在广泛应用,那么合成工作量、使用材料的数量和成本是需要牢记的关键参数。尽管材料科学为不同类型的治疗方法提供了多种选择,但要满足上述所有参数是一项艰巨的任务。通过将树枝状大分子附着到治疗剂上,可以将树枝状大分子架构的所有已知优势融入其中,这是一种很有见地的方法,而且在合成工作量、材料数量和成本方面也更加经济实惠。正如将要介绍的那样,用于生物医学应用的最常见的树枝状大分子是聚酰胺、聚酯、碳硅烷、聚醚和乙二醇型,它们通过可水解键与生物活性分子(BAMs)或分子纳米平台(MPs)结合。同样重要的是,引入不超过第三代(G3)的树枝状大分子足以改善这些分子系统的基本性质,例如水溶解度、稳定性和细胞内化等。树枝状大分子的类型及其在 BAMs 或 MPs 上的位置,类似于在模型上放置乐高积木,对于获得所需的性质将是决定性的。

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