理性设计与脂质-肽核酸纳米复合物的多组分合成：迈向定制药物输送系统组装。

Rational Design and Multicomponent Synthesis of Lipid-Peptoid Nanocomposites towards a Customized Drug Delivery System Assembly.

机构信息

Laboratório de Química Metodológica e Orgânica Sintética (LaQMOS), Instituto de Química, Universidade de Brasília, Campus Universitário Asa Norte, Brasilia 70904-970, Brazil.

Laboratório de Modelagem de Sistemas Complexos (LMSC), Instituto de Química, Universidade de Brasília, Campus Universitário Asa Norte, Brasilia 70904-970, Brazil.

出版信息

Molecules. 2023 Jul 28;28(15):5725. doi: 10.3390/molecules28155725.

DOI:10.3390/molecules28155725

PMID:37570698

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10421149/

Abstract

Nanotechnology has assumed a significant role over the last decade in the development of various technologies applied to health sciences. This becomes even more evident with its application in controlled drug delivery systems. In this context, peptoids are a promising class of compounds for application as nanocarriers in drug delivery systems. These compounds can be obtained efficiently and with highly functionalized structural diversity via the Ugi 4-component reaction (U-4CR). Herein, we report the design of the process control strategy for the future development of lipid-peptoid-based customized drug delivery system assemblies. Over 20 lipid-peptoid nanocomposites were synthesized via the U-4CR in good to excellent yields. These products were successfully submitted to the nanoparticle formation by the emulsification-evaporation process from lipophilic solution and analyzed via Dynamic Light Scattering (DLS). Several molecules generated nanoparticles with a size ≤200 nm, making them good candidates for drug delivery systems, such as in cancer treatment.

摘要

在过去的十年中，纳米技术在健康科学领域的各种技术发展中发挥了重要作用。将其应用于控释药物传递系统中，这一点更加明显。在这种情况下，类肽是作为药物传递系统中纳米载体应用的一类很有前途的化合物。通过 Ugi 四组分反应 (U-4CR)，可以有效地获得具有高度功能化结构多样性的类肽。在此，我们报告了未来基于脂质-类肽的定制药物传递系统组装的过程控制策略的设计。通过 U-4CR 合成了超过 20 种脂质-类肽纳米复合材料，产率良好至优秀。这些产物通过亲脂性溶液的乳化-蒸发过程成功提交给纳米颗粒形成，并通过动态光散射 (DLS) 进行分析。一些分子生成了尺寸≤200nm 的纳米颗粒，使它们成为药物传递系统的良好候选物，例如在癌症治疗中。