Insights on Fatty Acids in Lipophilic Prodrug Strategy

Aim: This review is dedicated to fatty acids importance in prodrugs development strategy. Various strategies of fatty acid-linked prodrugs are discussed in the article.

Summary: The increased drug lipophilicity is of great significance in both blood and lymphatic delivery, as the most desirable physical factor for the specified drug forms. Increased lipophilicity can prolong the action of the drug and enhance drug passive diffusion thorough the biological barriers like skin, gastrointestinal epithelium and blood-brain barrier.

Fatty acids as lipids are present in the human body and occur in the nature, moreover as the esters with steroid hormones also exist naturally.

Thus, the implementation of fatty acids into the prodrug research strategy seems to be the most desirable, especially for the improvement of lipophilicity of the parent drug. The drugs may be linked to the fatty acids either thorough the carboxylate group or by the ω-position.