Ethylcellulose microspheres containing WR 2721 were prepared by the emulsion-solvent evaporation technique. No significant loss or degradation of this phosphorothioate was noted during preparation. Oral administration of these microspheres to mice gave an important lowering of WR 2721 toxicity and an enhancement of its radioprotective activity with a D.R.F. of about 1.7-1.8 over 2-3 h. This action is explained by the protection of WR 2721 from acid hydrolysis and degradation in the gastro-intestinal tract. The adsorption of a fraction of WR 2721 onto the surface of microspheres constitutes an inconvenience. This study confirms the interest of such carriers for providing important sustained radioprotection after oral administration.
The present review describes the work carried out during the last 20 years in the field of the
radioprotective activity and toxicity of several classes of organosilicon and organogermanium
compounds (i.e. metallathiazolidines, metalladithioacetals, metallatranes and germathianes).
Silathiazolidine and metalladithioacetals (M = Si, Ge) have been prepared by the
interaction of dialkyldichloro- or bis(diethylamino)dialkylsilanes and -germanes with 3-[N-(2-
thioethyl)]amino-propanamide (WR-2529) and [1-thioethyl-2-(1-naphtylmethyl)]-2-
imidazoline. The study of these compounds in the field of chemical radioprotection has
shown a notable decrease in the toxicity and a rather large increase in the radioprotective
activity of these new derivatives in comparison with the starting organic compounds.
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