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12. Why lysine ester of oestrone instead of oestrone is used for oral administration?

12. Why lysine ester of oestrone instead of oestrone is used for oral administration?

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The lysine ester of oestrone is preferred over oestrone for oral administration because the lysine side chain increases the solubility of the drug (oestrone) in aqueous medium and is easily absorbed. Moreover, since the lysine ester of oestrone is more soluble in water (due to the presence of the polar lysine group), it does not form fat globules in the gut; rather it remains soluble. The prodrug (lysine ester of oestrone) is easily hydrolyzed in blood to release oestrone and lysine, a non-toxic amino acid which can be easily excreted out of the body with water.

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