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Antimicrobial molecular nanocarrier-drug conjugates
Andrzej S Skwarecki1, Sławomir Milewski2, Marta Schielmann2
1Department of Organic Chemistry, Faculty of Chemistry, Gdańsk University of Technology, Gdańsk, Poland.
Abstract:
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.
Insights
Antimicrobial drug efficacy is limited by poor activity against intracellular pathogens and insufficient cell penetration. Conjugating drugs with molecular organic nanocarriers enhances membrane crossing for improved antimicrobial treatment.
Area of Science:
- Pharmaceutical Science
- Microbiology
- Nanotechnology
Background:
- Many antimicrobial drugs struggle against intracellular pathogens like Mycobacterium tuberculosis and Plasmodium falciparum.
- Limited cellular penetration hinders the effectiveness of existing antimicrobial agents.
- The inability of drugs to cross biological membranes is a key challenge in treating intracellular infections.
Purpose of the Study:
- To review the application of molecular organic nanocarriers in drug conjugation for enhanced antimicrobial therapy.
- To explore the potential of nanocarrier-drug conjugates in overcoming challenges of cellular penetration and intracellular targeting.
- To present the current status and future perspectives of nanocarrier-based antimicrobials.
Main Methods:
- Review of scientific literature on molecular organic nanocarriers and drug conjugation.
- Analysis of various nanocarrier types, including oligopeptides, carbon nanotubes, siderophores, dendrimers, terpenoids, and molecular umbrellas.
- Evaluation of the mechanism of action for nanocarrier-drug conjugates in penetrating cell membranes and delivering active agents.
Main Results:
- Molecular organic nanocarriers offer a promising strategy to improve drug delivery across biological membranes.
- Conjugation enables active agents to reach intracellular targets, either released or intact.
- Various nanocarriers demonstrate potential for developing novel antimicrobial agents.
Conclusions:
- Drug conjugation with molecular organic nanocarriers is a viable approach to enhance antimicrobial efficacy against intracellular pathogens.
- Nanocarrier-drug conjugates can overcome limitations of poor cellular penetration, improving treatment outcomes.
- Further research into nanocarrier design and drug conjugation holds significant promise for future antimicrobial therapies.
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