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Novel two-chain fatty acid-based lipids for development of vancomycin pH-responsive liposomes against Staphylococcus

Sifiso S Makhathini1, Rahul S Kalhapure1,2, Mahantesh Jadhav1

  • 1Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal , Durban , South Africa.

Journal of Drug Targeting
|March 23, 2019
PubMed

Insights

Novel pH-responsive liposomes using fatty acid-based lipids (FAL) effectively deliver vancomycin (VAN) to infection sites. These liposomes enhance antibacterial activity against MRSA, improving targeted antibiotic delivery and combating resistance.

Area of Science:

  • Biotechnology
  • Materials Science
  • Pharmaceutical Sciences

Background:

  • Antibiotic resistance is a growing threat, exacerbated by poor drug localization at infection sites.
  • Targeted drug delivery systems are crucial for enhancing antibiotic efficacy and overcoming resistance.

Purpose of the Study:

  • To synthesize and evaluate novel pH-responsive liposomes for targeted vancomycin delivery.
  • To investigate the potential of fatty acid-based lipids (FAL) with amino acid head groups in liposome formulation.

Main Methods:

  • Formulation and characterization of pH-responsive liposomes containing vancomycin (VAN).
  • Assessment of drug loading, release kinetics, and stability.
  • In vitro evaluation of antibacterial activity against S. aureus and MRSA.
  • In vivo efficacy studies in a mouse model.

Main Results:

  • Liposomes exhibited sustained VAN release and prolonged in vitro antibacterial activity over 72 hours.
  • Enhanced efficacy at pH 6.0 was observed for specific liposome formulations (DOAPA-VAN-Lipo, DLAPA-VAN-Lipo).
  • High MRSA killing rates (71.98% and 73.32%) and significant reduction in bacterial load in vivo were achieved.

Conclusions:

  • Novel pH-responsive liposomes based on FAL show promise for targeted vancomycin delivery.
  • These formulations can improve antibiotic localization and efficacy, addressing bacterial resistance.
  • The study highlights the potential of tailored liposomal systems in combating challenging infections.
Keywords:
MRSAVancomycinfatty acid-based lipidspH-responsive liposometargeted drug delivery

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