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Updated: Aug 18, 2026
Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Neutron activation of NDDP, a liposomal platinum antitumor agent
D S MacLean1, A R Khokhar, R Perez-Soler
1Department of Thoracic/Head and Neck Medical Oncology, University of Texas M.D. Anderson Cancer Center, Houston, USA.
Unlabelled:
Cis-bis-neodecanoato-trans-R,R-1,2-diamminocyclohexane platinum (II) [NDDP] is a liposome-entrapped platinum compound currently, in phase II clinical trials, that has been shown to undergo intraliposomal activation. The objective of this study was to determine the feasibility of activating NDDP and using the induced radioactivity to monitor NDDP distribution and penetration.
Methods:
Neutron activation analysis (NAA) was done on NDDP using the nuclear reactor at Texas A & M University, College Station, Texas. After a 3-hour irradiation, the NDDP samples were analyzed using an HPGE (high purity germanium) detector to determine the activation of the radioisotopic platinum. This was followed by HPLC-UV analysis to determine the stability of NDDP after exposure to the reactor's core.
Results:
Platinum radioisotopes were produced along with potassium-40 and sodium-24. Irradiation did not result in any significant degradation of NDDP.
Conclusions:
(1) Irradiating fully synthesized NDDP is feasible for diagnostic use if a purification step is taken after the irradiation, and (2) radiation exposure is lessened by irradiating NDDP after synthesis rather than starting with high-specific-activity isotopes.
