In-vitro/in-vivo studies of the biodegradable XXXX microspheres of a novel @entity4396 antagonist for @entity263 treatment.

@entity4396 @entity251 @entity263 @entity10970 @entity5 @entity7050 @entity72931 @entity74 @entity968
The introduction of @entity4396 ( @entity4396 ) analogs and their antagonists is revolutionizing the treatment of @entity263 . In this study, @entity7050 ( @entity7050 ) microspheres containing a highly potent @entity4396 antagonist ( @entity72931 ) of interest in the indication of @entity263 were evaluated on release mechanisms in vitro and biological performance in vivo. @entity72931 microspheres were prepared by the water/oil/water double emulsion method and the solid/oil/oil method. The results showed that the mechanism of @entity72931 releasing from @entity7050 14,000 microspheres was the cooperation of drug diffusion and polymer degradation. This clarified the relationship between the microsphere characterization and hormone level in vivo. The larger microspheres (33  m) could inhibit the @entity251 level to castration for a longer time (35 days) than the smaller microspheres (15  m, 14 days). The formulation containing the hydrophilic additive ( @entity968 ) could suppress the @entity251 level to castration for a longer time (> 35 days) than the formulation without @entity968 (14 days). The appearance of testis, @entity10970 , and prostates changed after treatment. The weights of sexual organs decreased significantly. The in-vivo release of the @entity72931 @entity7050 14,000 microspheres curve showed that in-vivo release started immediately after day 1 (22.7%) and was rapid during the first 5 days (40.2% release). The @entity72931 microspheres could be a promising drug delivery system candidate to treat sex hormone-dependent @entity5 and other @entity74 .
