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使用阳离子融合脂质体作为纳米载体递呈放射性核素 I。

Delivery of the Radionuclide I Using Cationic Fusogenic Liposomes as Nanocarriers.

机构信息

Institute of Biological Information Processing: Mechanobiology (IBI-2) Forschungszentrum Jülich GmbH, 52428 Jülich, Germany.

Institute of Neurosciences and Medicine: Nuclear Chemistry (INM-5) Forschungszentrum Jülich GmbH, 52428 Jülich, Germany.

出版信息

Int J Mol Sci. 2021 Jan 5;22(1):457. doi: 10.3390/ijms22010457.

Abstract

Liposomes are highly biocompatible and versatile drug carriers with an increasing number of applications in the field of nuclear medicine and diagnostics. So far, only negatively charged liposomes with intercalated radiometals, e.g., Cu, Tc, have been reported. However, the process of cellular uptake of liposomes by endocytosis is rather slow. Cellular uptake can be accelerated by recently developed cationic liposomes, which exhibit extraordinarily high membrane fusion ability. The aim of the present study was the development of the formulation and the characterization of such cationic fusogenic liposomes with intercalated radioactive [I]I for potential use in therapeutic applications. The epithelial human breast cancer cell line MDA-MB-231 was used as a model for invasive cancer cells and cellular uptake of [I]I was monitored in vitro. Delivery efficiencies of cationic and neutral liposomes were compared with uptake of free iodide. The best cargo delivery efficiency (~10%) was achieved using cationic fusogenic liposomes due to their special delivery pathway of membrane fusion. Additionally, human blood cells were also incubated with cationic control liposomes and free [I]I. In these cases, iodide delivery efficiencies remained below 3%.

摘要

脂质体具有高度的生物相容性和多功能性,在核医学和诊断领域的应用越来越多。到目前为止,只有带嵌入放射性金属(如 Cu、Tc)的带负电荷的脂质体被报道过。然而,脂质体通过内吞作用被细胞摄取的过程相当缓慢。最近开发的阳离子脂质体可以加速细胞摄取,其具有非凡的膜融合能力。本研究的目的是开发具有嵌入放射性碘 [I] 的这种阳离子融合脂质体的配方和特性,以用于治疗应用。上皮人乳腺癌细胞系 MDA-MB-231 被用作侵袭性癌细胞的模型,并在体外监测 [I] 的摄取。阳离子和中性脂质体的递药效率与游离碘化物的摄取进行了比较。由于其特殊的膜融合递药途径,阳离子融合脂质体实现了最佳的载药效率(约 10%)。此外,还用人血红细胞孵育阳离子对照脂质体和游离 [I]。在这些情况下,碘化物的递药效率仍低于 3%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/94e1/7796481/deead48e82fe/ijms-22-00457-g001.jpg

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