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Tumor-Imaging Potential of Liposomes Loaded with In-111-NTA: Biodistribution in Mice

City of Hope National Medical Center, Duarte
Vestar Research, Inc., Pasadena
California Institute of Technology, Pasadena
Wilshire Oncology Medical Group, Los Angeles, California

Correspondence: For reprints contact: Richard T. Proffitt, PhD, Dept. of Med. Oncology, City of Hope National Med. Ctr., 1500 E. Duarte Rd., Duarte, CA 91010.

ABSTRACT

EMT6 tumors in BALB/c mice have been successfully imaged with small (<0.1µ), unilamellar lipid vesicles (SUVs) loaded with In-111 nitrilotriacetic acid (In-111 NTA). Neutral SUVs prepared from distearoyl phosphatidylcholine (DSPC) and cholesterol (CH) (ratio 2:1) delivered sufficient radioactivity to allow tumor visualization 24 hr after i.v. injection; so did positively and negatively charged SUVs with the ratio 4:1:1 for DSPC:CH:X, where X was stearylamine or dicetyl phosphate. Other SUVs containing a 6-aminomannose or 6-aminomannitol derivative of cholesterol did not cause significant tumor accumulation of In-111 NTA, and tumor images were not readily discernible. The maximum tumor-associated radioactivity, 18.5% of injected dose per gram of tissue, was achieved with neutral SUVs. This level of tumor-associated In-111 was over 4 times that observed when unencapsulated In-111 NTA was injected. Neutral SUVs also gave the lowest specific activities in the liver and spleen (14.6% and 18.8% of dose respectively).

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