Next Article in Journal
A Versatile and Robust Serine Protease Inhibitor Scaffold from Actinia tenebrosa
Previous Article in Journal
Genome-Wide Identification and Characterization of SODs in Zhikong Scallop Reveals Gene Expansion and Regulation Divergence after Toxic Dinoflagellate Exposure
Previous Article in Special Issue
High-Performance Thin-Layer Chromatography Hyphenated with Microchemical and Biochemical Derivatizations in Bioactivity Profiling of Marine Species
Open AccessArticle

Pharmaceutical Development and Safety Evaluation of a GMP-Grade Fucoidan for Molecular Diagnosis of Cardiovascular Diseases

Université de Paris, UMRS1148, INSERM, F-75018 Paris, France
X. Bichat Medical School, Université de Paris, UMS34 FRIM, F-75018 Paris, France
AP-HP, Department of Nuclear Medicine, X. Bichat Hospital, F-75018 Paris, France
Algues & Mer, F-29242 Ouessant, France
Bracco Research Center, Bracco Imaging Spa, 20811 Colleretto Giacosa, Italy
Nanomedicine Research and Education Center, Semmelweis University, 1085 Budapest, Hungary
Department of Vascular Medicine, Academic Medical Center, 1105 AZ Amsterdam, The Netherlands
Author to whom correspondence should be addressed.
Mar. Drugs 2019, 17(12), 699;
Received: 15 November 2019 / Revised: 4 December 2019 / Accepted: 9 December 2019 / Published: 12 December 2019
(This article belongs to the Special Issue Vascular Bioactivities of Marine Natural Products)
The adhesion molecule P-selectin is present on the cell surface of both activated endothelium and activated platelets. The present study describes the pharmaceutical development, safety evaluation, and preclinical efficacy of a micro-dosed radiotracer. The macromolecular nanoscale assembly consisted of a natural compound made of a sulfated fucose-rich polysaccharides (fucoidan) and a radionuclide (technetium-99m) for the detection of P-selectin expression in cardiovascular diseases. After extraction and fractionation from brown seaweeds, the good manufacturing practice (GMP) production of a low molecular weight (LMW) fucoidan of 7 kDa was achieved and full physicochemical characterization was performed. The regulatory toxicology study in rats of the GMP batch of LMW fucoidan revealed no adverse effects up to 400 μg/kg (×500 higher than the expected human dose) and pseudoallergy was not seen as well. In a myocardial ischemia-reperfusion model in rats, the GMP-grade LMW fucoidan labeled with technetium-99m detected P-selectin upregulation in vivo. The present study supports the potential of using 99mTc-fucoidan as an imaging agent to detect activated endothelium in humans. View Full-Text
Keywords: GMP-grade fucoidan; regulatory toxicology; molecular diagnosis; scintigraphy GMP-grade fucoidan; regulatory toxicology; molecular diagnosis; scintigraphy
Show Figures

Graphical abstract

MDPI and ACS Style

Chauvierre, C.; Aid-Launais, R.; Aerts, J.; Chaubet, F.; Maire, M.; Chollet, L.; Rolland, L.; Bonafé, R.; Rossi, S.; Bussi, S.; Cabella, C.; Dézsi, L.; Fülöp, T.; Szebeni, J.; Chahid, Y.; Zheng, K.H.; Stroes, E.S.G.; Le Guludec, D.; Rouzet, F.; Letourneur, D. Pharmaceutical Development and Safety Evaluation of a GMP-Grade Fucoidan for Molecular Diagnosis of Cardiovascular Diseases. Mar. Drugs 2019, 17, 699.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

Back to TopTop