In Vivo Scintigraphic Imaging of Proteoglycans

Abstract

In this chapter, we present the methods developed in our lab for the scintigraphic imaging and direct quantitative evaluation of proteoglycan (PG) distribution in vivo. These methods relate to (1) the synthesis and radiolabeling of the NTP 15-5 with (99m)Tc, (2) preclinical scintigraphic imaging using laboratory animals, and (3) quantitative analysis of scintigraphic images.

99mTc-NTP 15-5 Imaging for Cartilage Involvement in Experimental Rheumatoid Arthritis: Comparison with Routinely Used Molecular Imaging Methods and Sensitivity to Chronic Nonsteroidal Antiinflammatory Drug Treatment

“…99m Tc-NTP 15-5 was previously demonstrated to be a candidate for the in vivo functional monitoring of proteoglycan remodeling associated with degenerative and tumoral pathologies of cartilage (15)(16)(17)(18)24). We evaluated, in an RA model, the relevance of 99m Tc-NTP 15-5 imaging for monitoring in vivo cartilage damage and response to nonsteroidal antiinflammatory drug therapy.…”

“…To that end, N-(triethylammonium)-3-propyl- [15]ane-N5 radiolabeled with 99m Tc was demonstrated to allow joint functional imaging in several experimental models of articular pathology and to specifically bind to human articular cartilage after ex vivo incubation (14)(15)(16)(17)(18).…”

Radiation dosimetry of [131I]ICF01012 in rabbits: Application to targeted radionuclide therapy for human melanoma treatment

“…The nonradiolabeled ICF01012, 34 is prepared as described by Chezal et al 8 while the tributylstannyl precursor N-(2diethylaminoethyl)-6-(tributylstannyl)quinoxaline-2-carboxamide is obtained following a published procedure. 35 [ 131 I]NaI (59.5-64.6 GBq/mL) is purchased from Perkin-Elmer (Boston, USA) as a no-carrier-added solution in dilute aqueous 0.1 M sodium hydroxide solution. [ 131 I]ICF01012 is then obtained as described by Viallard et al 36…”

Proteoglycans as Target for an Innovative Therapeutic Approach in Chondrosarcoma: Preclinical Proof of Concept

“…In vivo antitumor effects were also assessed by 99m Tc-NTP 15-5 scintigraphic imaging, as this radiotracer was previously demonstrated to provide suitable criteria for monitoring chondrosarcoma (14)(15)(16). As illustrated in Fig.…”

“…8-13) selectively to PG-rich tissues such as cartilage and chondrosarcoma. In particular, the suitability and high sensitivity of the radiotracer N-[triethylammonium]-3propyl-1,4,7,10,13-pentaazacyclopentadecane radiolabeled with 99m Tc ( 99m Tc-NTP 15-5) was validated for in vivo diagnosis and follow up of chondrosarcoma via scintigraphic imaging (14)(15)(16). This radiotracer is currently transferred into clinic for a first into human study.…”