Journal of Chinese Pharmaceutical Sciences ›› 2018, Vol. 27 ›› Issue (6): 408-414.DOI: 10.5246/jcps.2018.06.041

• Original articles • Previous Articles     Next Articles

Preparation and evaluation of liposomal clarithromycin with antimicrobial effect

Wenxi Zhang, Guanghua Peng, Maoyuan Song, Jiaxing Wang, Mengya Yin, Jiajia Li, Yajie Liu, Yuanyuan Zhang, Xinru Li*   

  1. Beijing Key Laboratory of Molecular Pharmaceutics and New Drug System; School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2018-03-16 Revised:2018-04-14 Online:2018-06-30 Published:2018-05-18
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  • Supported by:
    The National Natural Science Foundation of China (Grant No. 81202488).


In this study, we developed a novel liposomal delivery system modified by Tat peptide and wheat germ agglutinin (WGA) with antimicrobial effect. Physicochemical parameters, in vitro antimicrobial, time-kill study, cellular uptake, biofilm formation inhibition and in vivo antibacterial efficacy against Methicillin-resistant Staphylococcus aureus (MRSA) were investigated. Minimum inhibitory concentrations (MICs) and colony-forming units (CFUs) in the time-kill study for Tat-WGA-modified liposomal clarithromycin (CLA-TatWGALip) were lower than those of free and other modified liposomal CLA. Flow cytometry analysis disclosed that TatWGALip delivered more coumarin 6 into bacteria. Furthermore, Tat-WGA-modified liposomal CLA efficiently inhibited the formation of MRSA biofiom. CFU of MRSA in the abscess of mice treated with CLA-TatWGALip was significantly lower than that of any others (P<0.01). Collectively, liposomal delivery system modified by Tat and WGA could be a promising anti-resistant infection strategy.

Key words: Methicillin-resistant Staphylococcus aureus, Antimicrobial, Liposomes, Clarithromycin, Biofilm

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