Sterically stabilized liposomes as a carrier for alpha-emitting radium and actinium radionuclides.
The alpha-particle emitting radionuclides (223)Ra (t(1/2) = 11.4 d), (224)Ra (t(1/2) = 3.6 d), and (225)Ac(t(1/2) = 10.0 d) may have a broad application in targeted radiotherapy provided that they could be linked to vehicles with tumor affinity. The potential usefulness of liposomes as carriers was studied in the present work. Radium and actinium radionuclides could be loaded in good yields into sterically stabilized liposomes. Subsequent coating of the liposomes with a folate-F(ab')(2) construct yielded a product with affinity towards tumor cells expressing folate receptors. Radionuclide loaded liposomes showed excellent stability in serum in vitro.
Henriksen
Gjermund
G
University of Oslo, Blindern, Norway.
Schoultz
B W
BW
Michaelsen
T E
TE
Bruland
Ø S
ØS
Larsen
R H
RH
D000186:Actinium / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D000512:Alpha Particles / Q000627:therapeutic use; D002352:Carrier Proteins / Q000378:metabolism; D045744:Cell Line, Tumor; D020099:Coated Materials, Biocompatible / Q000138:chemical synthesis; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D004355:Drug Stability; D005260:Female; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D007140:Immunoglobulin Fab Fragments / Q000276:immunology; D008081:Liposomes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D008657:Metabolic Clearance Rate; D010051:Ovarian Neoplasms / Q000378:metabolism*; D016499:Radioimmunotherapy / Q000379:methods*; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D011883:Radium / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D011956:Receptors, Cell Surface / Q000378:metabolism; D013237:Stereoisomerism
D002352:Carrier Proteins; D020099:Coated Materials, Biocompatible; D004337:Drug Carriers; D058973:Folate Receptors, GPI-Anchored; D007140:Immunoglobulin Fab Fragments; D008081:Liposomes; D019275:Radiopharmaceuticals; D011956:Receptors, Cell Surface; D005492:Folic Acid; D000186:Actinium; D011883:Radium