Synthesis of diethylenetriaminepentaacetic acid conjugated inulin and utility for cellular uptake of liposomes
The synthesis, binding of radioactive cations, liposomal encapsulation, and biodistribution of the oxidized-inulin reaction product with ethylenediamine and diethylenetriaminepentaacetic acid (4) are described. The four-step synthesis of the inulin derivative proceeded in a good overall yield of 72%. The complex of the inulin derivative with either /sup 67/Ga3+ or /sup 111/In3+ was stable in vivo and did not readily distribute into tissues, being excreted primarily in urine after intravenous administration to mice. The liposome-entrapped inulin derivative can be loaded with radioactive heavy metal cations by mobile ionophores in high radiochemical yields of 80-91%. Following the intravenous administration of the liposomal encapsulation of the indium-111-labeled inulin derivative, the entrapped compound had a biodistribution characteristic of liposomes and allowed an estimation of the extent of the intracellular uptake of liposomes. The ability of the inulin derivative to chelate many different types of metals will allow the use of this probe for studying subtle differences in tissue distribution resulting from different drug targeting or delivery protocols in the same animal by multiple labeling techniques. Moreover, the chelate-conjugated inulin permits studies of the applications of drug delivery systems in primates or human subjects by noninvasive techniques such as gamma-scintigraphic or nuclear magnetic resonance imaging methods.
- Research Organization:
- Univ. of Southern California, Los Angeles (USA)
- OSTI ID:
- 7196016
- Journal Information:
- J. Med. Chem.; (United States), Vol. 31:5
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
LIPOSOMES
UPTAKE
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
TISSUE DISTRIBUTION
CHEMICAL REACTION YIELD
DTPA
GALLIUM 67
INDIUM 111
INTRAVENOUS INJECTION
INULIN
MICE
AMINO ACIDS
ANIMALS
BETA DECAY RADIOISOTOPES
CARBOHYDRATES
CARBOXYLIC ACIDS
CELL CONSTITUENTS
CHELATING AGENTS
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
GALLIUM ISOTOPES
INDIUM ISOTOPES
INJECTION
INTAKE
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MINUTES LIVING RADIOISOTOPES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC ACIDS
ORGANIC COMPOUNDS
ORGANOIDS
POLYSACCHARIDES
RADIOISOTOPES
RADIOPROTECTIVE SUBSTANCES
RODENTS
SACCHARIDES
SYNTHESIS
VERTEBRATES
YIELDS
550601* - Medicine- Unsealed Radionuclides in Diagnostics