Abstract
We studied the local effect of a controlled-release formulation of 17α-acetoxy-6-chloro-2-oxa-4,6-pregnadine-3, 20-dione (TZP-4238) on the inhibition of rat prostatic growth. A poly(dl-lactic acid) (PLA) with an Mn value of 1600 was synthesized by polycondensation in the presence of water at 200°C. This polymer showed a typical S-type degradation pattern in-vivo, as the specimen is undetectable after 12 weeks. TZP-4238 was incorporated into PLA microspheres in the size range 100–150 μm by the solvent evaporation process. The drug concentration contained in this microsphere was found to be approximately 27%. Ten milligrams of PLA microspheres with and without TZP-4238 was directly injected into the ventral prostates of male rats after abdominal surgery. We concluded that TZP-4238 was released gradually from PLA microspheres and prevents the prostatic growth, acting as a potent androgen receptor antagonist.
Published Version
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