Fluorescently labeled PLGA nanoparticles for visualization in vitro and in vivo: the importance of dye properties

  • Fluorescently labeled nanoparticles are widely used for evaluating their distribution in the biological environment. However, dye leakage can lead to misinterpretations of the nanoparticles’ biodistribution. To better understand the interactions of dyes and nanoparticles and their biological environment, we explored PLGA nanoparticles labeled with four widely used dyes encapsulated (coumarin 6, rhodamine 123, DiI) or bound covalently to the polymer (Cy5.5.). The DiI label was stable in both aqueous and lipophilic environments, whereas the quick release of coumarin 6 was observed in model media containing albumin (42%) or liposomes (62%), which could be explained by the different affinity of these dyes to the polymer and lipophilic structures and which we also confirmed by computational modeling (log PDPPC/PLGA: DiI—2.3, Cou6—0.7). The importance of these factors was demonstrated by in vivo neuroimaging (ICON) of the rat retina using double-labeled Cy5.5/Cou6-nanoparticles: encapsulated Cou6 quickly leaked into the tissue, whereas the stably bound Cy.5.5 label remained associated with the vessels. This observation is a good example of the possible misinterpretation of imaging results because the coumarin 6 distribution creates the impression that nanoparticles effectively crossed the blood–retina barrier, whereas in fact no signal from the core material was found beyond the blood vessels.

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Author:Vasilisa ZhukovaORCiD, Nadezhda Osipova, Aleksey SemyonkinORCiD, Julia Malinovskaya, Pavel Melnikov, Marat Valikhov, Yuri PorozovORCiD, Yaroslav Solovev, Pavel Kuliaev, En-chin Chang, Bernhard A. SabelORCiDGND, Vladimir Chekhonin, Maxim AbakumovORCiD, Alexander Majouga, Jörg KreuterGND, Petra Henrich-NoackORCiDGND, Svetlana GelperinaORCiD, Olga Maksimenko
Parent Title (English):Pharmaceutics
Place of publication:Basel
Document Type:Article
Date of Publication (online):2021/07/27
Date of first Publication:2021/07/27
Publishing Institution:Universitätsbibliothek Johann Christian Senckenberg
Release Date:2022/07/11
Tag:Cy5.5; DiI; PLGA nanoparticles; brightness; confocal microscopy; coumarin 6; fluorescent labeling; in vivo neuroimaging; intracellular internalization; quantum yield; rhodamine 123; stability of fluorescent label
Issue:8, art. 1145
Article Number:1145
Page Number:28
First Page:1
Last Page:28
This research was funded by Ministry of Science and Higher Education of the Russian Federation, project No 075-15-2020-792 (unique identifier RF-190220X0031). The APC was funded from the same source.
Institutes:Biochemie, Chemie und Pharmazie
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie
6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit
Licence (German):License LogoCreative Commons - Namensnennung 4.0