Antimicrobial molecular nanocarrier-drug conjugates

Many antimicrobial drugs are poorly active against pathogenic microbes causing intracellular infections, such as Mycobacterium tuberculosis or Plasmodium falciparum. On the other hand, several known antimicrobial agents are not effective enough because of their limited cellular penetration. A common feature of both challenges is the inability of an active agent to cross the biological membrane(s). One of the possible approaches facing these challenges is conjugation of an active substance with a molecular organic nanocarrier. The conjugate thus formed should be able to penetrate the membrane(s) and, once internalized, the active component could reach its intracellular target, either after release from the conjugate or in an intact form. Several molecular nanocarriers have been proposed: oligopeptides, including cell penetrating peptides, carbon nanotubes, siderophores, dendrimers, terpenoids and molecular umbrellas. A comprehensive review of the current status of molecular organic nanocarrier-drug conjugates and the future perspectives of their application as novel antimicrobials is presented. (C) 2016 Elsevier Inc. All rights reserved.