Tracking In Vivo Lipolysis of Lipid Nanocarriers Using NIR-II Polarity-Sensitive Fluorescent Probes.

IF 10.7 2区 材料科学 Q1 CHEMISTRY, PHYSICAL
Yanlei Zhan, Zhichao Chang, Chang Liu, Ziyu Zhang, Runtong Zhang, Yi Lu, Jianping Qi, Wei Wu, Haisheng He
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引用次数: 0

Abstract

Elucidating in vivo lipolysis is crucial for clarifying the underlying mechanisms and in vivo fates of lipid-based nanocarriers, which are essential oral drug delivery carriers. Current mainstream methodologies use various in vitro digestion models to predict the in vivo performance of lipid formulations; however, their accuracy is often impeded by the complicated environment of the gastrointestinal tract. Although fluorescence labeling with conventional probes partly reveals the in vivo translocation of lipid nanocarriers, it fails to elucidate the lipolysis process because of poor signal discrimination among nanocarriers, free probes, and mixed micelles (lipolysis end-products). Here, a polarity-sensitive probe (PN-C18) with aggregation-caused quenching properties for labeling lipid nanocarriers is developed and optimized. PN-C18 successfully eliminates interference from both free probes and mixed micelles during lipolysis. In a representative in vitro lipolysis model, PN-C18 labeling shows stronger correlation between fluorescence intensity and lipolysis progression than those of previous methods. In vivo, the translocation and lipolysis of lipid nanoparticles are clearly visualized and effectively monitored, owing to the high tissue-penetrating capability of PN-C18 NIR-II photons. This study provides practical means for elucidating the in vivo fate of lipid-based drug delivery systems and offers valuable insights and reference for further studies in this domain.

利用NIR-II极性敏感荧光探针跟踪脂质纳米载体的体内脂质分解。
阐明体内脂肪分解对于阐明基于脂质纳米载体的潜在机制和体内命运至关重要,脂质纳米载体是必不可少的口服药物递送载体。目前的主流方法使用各种体外消化模型来预测脂质制剂的体内性能;然而,其准确性往往受到胃肠道复杂环境的阻碍。尽管传统探针的荧光标记部分揭示了脂质纳米载体在体内的转运,但由于纳米载体、自由探针和混合胶束(脂解最终产物)之间的信号识别能力差,它无法阐明脂解过程。本研究开发并优化了一种具有聚合猝灭特性的极性敏感探针(PN-C18),用于标记脂质纳米载体。PN-C18成功地消除了脂肪分解过程中来自自由探针和混合胶束的干扰。在具有代表性的体外脂肪分解模型中,PN-C18标记的荧光强度与脂肪分解过程的相关性比以往的方法更强。在体内,由于PN-C18 NIR-II光子的高组织穿透能力,脂质纳米颗粒的转运和脂质分解可以清晰地可视化和有效地监测。本研究为阐明脂质给药系统的体内命运提供了实用手段,并为该领域的进一步研究提供了有价值的见解和参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Small Methods
Small Methods Materials Science-General Materials Science
CiteScore
17.40
自引率
1.60%
发文量
347
期刊介绍: Small Methods is a multidisciplinary journal that publishes groundbreaking research on methods relevant to nano- and microscale research. It welcomes contributions from the fields of materials science, biomedical science, chemistry, and physics, showcasing the latest advancements in experimental techniques. With a notable 2022 Impact Factor of 12.4 (Journal Citation Reports, Clarivate Analytics, 2023), Small Methods is recognized for its significant impact on the scientific community. The online ISSN for Small Methods is 2366-9608.
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