4.3 Article

99mTc-labeled porphyrin-lipid nanovesicles

Journal

JOURNAL OF LIPOSOME RESEARCH
Volume 25, Issue 2, Pages 101-106

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.3109/08982104.2014.932379

Keywords

Drug-encapsulated liposome; nanotechnology; size exclusion analysis; sustained release; Tc-99m-labeled porphyrin-lipid nanovesicles

Funding

  1. intramural research program of Clinical Center, NIH

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Porphyrin-lipid nanovesicles (PLN) have been developed with intrinsic capabilities as activatable multimodal photonic contrast agents. Radio labeling of PLN encapsulating drugs could eventually be able to provide quantitative in vivo information for diagnosing and treating diseases. In this study, we developed Tc-99m-labeled porphyrin-lipid nanovesicles (Tc-99m-PLN) as a cargo-encapsulated formulation without significant impact on liposome integrity and encapsulation stability. 50 mM calcein was encapsulated into PLN by probe sonication. The size of the PLN was about 150 nm. The PLN were then reacted with Tc-99m using SnCl2 dissolved in 1 mM HCl as a reducing agent and incubated for 10 min at 22 degrees C. The radiolabeling efficiency and stability of Tc-99m-PLN were evaluated by instant thin-layer chromatography and low-pressure liquid chromatography (LPLC). Tc-99m labeling was successful with a >92% labeling efficiency. LPLC showed that the liposomal elution peaks of the porphyrin-lipid and the calcein overlapped with the radioactivity elution peak of Tc-99m-labeled PLN. The Tc-99m-labeling procedure did not change the size of PLN. Encapsulated calcein remained inert inside PLN. Thus, this work lays out a simple and effective radiolabeling method using SnCl2 in HCI in the preparation of Tc-99m-PLN.

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