Preparation and the kinetic stability of hyaluronan radiolabeled with 111In, 125I and 14C
Autor: | R. Koppova, R. Buffa, Milos Petrik, E. Svanovsky, Alice Laznickova, D. Cozikova, L. Palek, Milan Laznicek, D. Smejkalova, V. Velebny, M. Hermannova, P. Sedova |
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Rok vydání: | 2010 |
Předmět: |
Male
Clinical Biochemistry Kinetics Pharmaceutical Science Polysaccharide Analytical Chemistry Iodine Radioisotopes chemistry.chemical_compound Drug Stability Drug Discovery Hyaluronic acid Animals Chelation Carbon Radioisotopes Hyaluronic Acid Rats Wistar Bifunctional Spectroscopy chemistry.chemical_classification Indium Radioisotopes Tyramine In vitro Rats Biochemistry chemistry Specific activity |
Zdroj: | Journal of Pharmaceutical and Biomedical Analysis. 52:517-524 |
ISSN: | 0731-7085 |
DOI: | 10.1016/j.jpba.2010.02.005 |
Popis: | Three different procedures for the labeling of hyaluronan (HA) with 111 In, 125 I and 14 C radionuclides were compared, and the kinetic stability of radiolabeled HA under different conditions (saline, artificial gastric juice and plasma) was established. Modification of HA structure with bifunctional chelating agents (DTPA) or with the prosthetic group (tyramine or tyrosine) was essential prior 111 In and 125 I labeling. These chemical labeling techniques were fast, simple and inexpensive, and labeled agents with a high specific activity were obtained. The only disadvantage of these methods was the occurrence of unknown functional groups in the HA molecule requiring further characterization of the compound. Conversely, HA labeling with 14 C by biotechnological synthesis was found to be rather expensive and time-consuming process. Although, the final product 14 C-HA was identical to natural HA its low specific activity presents certain limitation for its application in biological experiments. Stability studies showed that 14 C-HA and 125 I-Tm-HA were stable in all studied mediums. In the case of 125 I-Trs-HA, stability slightly decreased in rat plasma and in artificial gastric juice with increasing time. The least stable was 111 In-DTPA-HA, which degraded completely after 48 h in artificial gastric juice. Kinetic stability studies may provide primary information concerning the properties of radiolabeled HA in vitro , which is essential for the use and explanation of its behavior in biological experiments. |
Databáze: | OpenAIRE |
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