Pilocarpic acid esters as novel sequentially labile pilocarpine prodrugs for improved ocular delivery

Article abstract of DOI:10.1021/jm00146a001

Pilocarpic acid esters are shown to be potentially useful prodrugs of pilocarpine with the aim of improving its ocular delivery characteristics. The diesters are of particular interest since they combine an enhanced bioavailability and greatly prolonged duration of activity with a high stability in eye-drop formulation. The proprodrug or sequential cascade concept utilized in the design of these derivatives, involving and enzymatic cleavage mechanisms prior to the occurrence of a chemical (nonenzymatic) reaction, may also be of more general interest in prodrug design.