| abstract |
Novel positively charged prodrugs of peptides represented by structure 1 and related compounds were synthesized. The compound represented by structure 1 can be synthesized by standard peptide synthesis protocols. The positively charged amino group of the peptide prodrug not only dissolves the drug in water, but also binds to a negative charge on the membrane phosphate head group, pushing the prodrug into the cytosol. Prodrugs diffuse through human skin 100 to 1000 times faster than peptides and related compounds. Prodrugs can be used to treat conditions treatable by peptides and related compounds in humans or animals. Prodrugs can be administered transdermally for any type of drug treatment and can avoid proteolysis by proteolytic enzymes in the gastrointestinal tract. A controlled transdermal administration system for prodrugs allows oxicam and related compounds to continually reach optimal therapeutic blood levels, increase efficacy and reduce their side effects. [Selection] Figure 2 |