The predrug (prodrug) term involves chemically modified inert
compound which upon an administration releases the active parent
drug to elicit its pharmacological response within the body. For many
years, the predrug strategy has been extensively developed to solve
many unwanted drug properties. This approach has several advantages
over conventional drug administration and it has the potential to be
quite effective method for the treatment of diseases in the future. In
this mini-review we describe a number of antibacterial agents‘
predrugs, and the ways by which predrug strategy was exploited to
overcome many pharmaceutical and pharmacokinetic problems that the
parent active antibacterial drugs suffer from such as, low
bioavailability by increasing or decreasing lipophilicity, site selectivity for higher absorption
and less toxicity, short duration of action to increase patient compliance, rapid metabolism to
increase oral bioavailability and masking bitter sensation which is crucial for geriatric and
pediatric patient compliance
