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¹⁸⁶Re-Liposome Labeling Using ¹⁸⁶Re-SNS/S Complexes: In Vitro Stability, Imaging, and Biodistribution in Rats

¹ Department of Radiology, University of Texas Health Science Center at San Antonio, San Antonio, Texas
² Department of Chemistry, University of Texas at San Antonio, San Antonio, Texas

View larger version (10K): [in a new window]   FIGURE 1. Structure of 186Re/188Re-SNS/S complexes.

View larger version (7K): [in a new window]   FIGURE 2. Structures of 186Re-BMEDA (A) and 186Re-BMEDA + BT (B).

View larger version (21K): [in a new window]   FIGURE 3. (A) In vitro labeling stability (n = 3) of 400-nm 186Re-(NH4)2SO4 liposomes labeled with 186Re-BMEDA and with 186Re-BMEDA + BT in 50% FBS-PBS buffer, pH 7.4, at 37°C. (B) In vitro labeling stability (n = 3) of 400-nm 186Re-cysteine liposomes labeled with 186Re-BMEDA and with 186Re-BMEDA + BT in 50% FBS-PBS buffer at 37°C. 186Re-(NH4)2SO4 liposomes labeled with 186Re-BMEDA had the best in vitro labeling stability of the liposomes tested. This stability could be retained for 96 h in 50% FBS-PBS buffer at 37°C (*P < 0.05).

View larger version (15K): [in a new window]   FIGURE 4. Effect of high specific activity on in vitro labeling stability of 400-nm 186Re-(NH4)2SO4 liposomes labeled with 186Re-BMEDA. With (NH4)2SO4 liposomes, specific activity of 1.85 GBq (50 mCi) of 186Re per 50 mg of DSPC (1 mL 120 mmol/L liposomes) labeled to (NH4)2SO4 liposomes also showed good in vitro labeling stability up to 96 h of incubation in 50% FBS-PBS buffer at 37°C (*P < 0.05).

View larger version (29K): [in a new window]   FIGURE 5. -Camera images of normal rats via intravenous injection method. (Top row) Images of rat at baseline and at 1, 4, 24, and 72 h after intravenous injection of 100-nm 186Re-(NH4)2SO4 liposomes labeled with 186Re-BMEDA. (Middle row) Images of rat at corresponding times after intravenous injection of 100-nm 186Re-cysteine liposomes labeled with 186Re-BMEDA. (Bottom row) Images of rat at corresponding times after intravenous injection of 186Re-BMEDA alone. 186Re-(NH4)2SO4 liposomes and 186Re-cysteine liposomes labeled with 186Re-BMEDA showed slow blood clearances and spleen accumulations, which are common features of liposome distribution after intravenous injection in rats. 186Re-BMEDA alone showed fast blood clearance, fast excretion from bowel and urine, and no spleen accumulation.