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Hexosome engineering for targeting of regional lymph nodes

Lookup NU author(s): Professor Moein MoghimiORCiD


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© 2020Hexosomes are nanoparticles enveloping inverted discontinuous hexagonal (HII) liquid crystalline phases that offer exceptional physicochemical characteristics for drug encapsulation and targeted drug delivery. However, the fate of subcutaneously injected hexosomes has rarely been investigated. Here, we have followed the lymphatic fate of a technetium-99 m [99mTc]-labeled hexosome preparation on subcutaneous injection into the rat footpads with single-photon emission computed tomography (SPECT) in combination with CT. Hexosomes were composed of phytantriol and oleic acid and sterically stabilized with Pluronic F127. High tracer loading efficiency was achieved by chelating [99mTc]-pertechnetate to 1,12-diamino-3,6,9-triazadodecane-oleic acid conjugates incorporated within the ordered interior nanocompartments of hexosomes. The preparation was characterized by synchrotron small angle X-ray scattering, cryogenic transmission electron microscopy and nanoparticle tracking analysis. On footpad injection, hexosomes rapidly drained into the lymphatic microvessels and distributed not only to the sentinel (popliteal) lymph node, but also to wider lymph nodes (inguinal and iliac nodes) situated along the pathway of the lymph drainage. The observed hexosome drainage kinetics from the injection site and lymphatic distribution pattern is in line with previously established poly(ethylene oxide) configuration attributes of Pluronic F127 in minimizing nanoparticle aggregation at the injection site, and interaction with the ground substance of interstitium, without interfering with macrophage uptake. Accordingly, we discuss the potential utility of Pluronic F127-stabilized hexosomes for lymphatic targeting and future development of simple, yet effective multifunctional lymphotropic agents and theranostics.

Publication metadata

Author(s): Helvig SY, Andersen H, Antopolsky M, Airaksinen AJ, Urtti A, Yaghmur A, Moghimi SM

Publication type: Article

Publication status: Published

Journal: Materialia

Year: 2020

Volume: 11

Online publication date: 11/05/2020

Acceptance date: 21/04/2020

ISSN (electronic): 2589-1529

Publisher: Elsevier B.V.


DOI: 10.1016/j.mtla.2020.100705


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