The novel positively charged pro-drugs of beta-lactam antibiotics in the general 'Structure 4' were designed. The positively charged amino group of the pro-drug not only makes the drugs soluble in water, but also bonds to the negative charge on the phosphate head group of membranes. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the prodrug. The prodrugs can be used medicinally in treating beta-lactam antibiotics-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments. Controlled transdermal administration systems of the prodrug enables beta-lactam antibiotics to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of beta-lactam antibiotics.