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Pharmacokinetics of a new radiopharmaceutical based on alubmin microspheres and palladium-103 and modified by heat and radiation

  • Molecular-Biological Problems of Drug Design and Mechanism of Drug Action
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Pharmaceutical Chemistry Journal Aims and scope

The pharmacokinetics of albumin microspheres (AMS) labeled with 103Pd (103Pd-AMS) were studied in healthy mice after intramuscular injections. It was established that increasing the denaturation temperature of albumin from 136 to 200°C reduced the rate of 103Pd elimination from muscle tissue. This effect can be explained by a decrease in the rate of 103Pd-AMS proteolysis due to more extensive protein denaturation. Preliminary gamma irradiation (60Co) of AMS prepared at 200°C produced a more significant deceleration of these processes. Increasing the irradiation dose from 0.1 to 1.0 MGy delayed AMS proteolysis and elimination of 103Pd from the protein matrix as a result of an increasing degree of ASM cross-linking. The rate of 103Pd elimination from muscle tissue was more rapid than that from tumor. This can be explained by faster AMS biodegradation in muscle tissue compared with tumor tissue.

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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 45, No. 8, pp. 3–7, August, 2011.

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Petriev, V.M., Shiryaev, V.K., Skvortsov, V.G. et al. Pharmacokinetics of a new radiopharmaceutical based on alubmin microspheres and palladium-103 and modified by heat and radiation. Pharm Chem J 45, 449–453 (2011). https://doi.org/10.1007/s11094-011-0652-5

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  • DOI: https://doi.org/10.1007/s11094-011-0652-5

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