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Reverse micelle-lipid nanocapsules: a novel strategy for drug delivery of the plectasin derivate AP138 antimicrobial peptide

Authors Groo AC, Matougui N, Umerska A, Saulnier P

Received 12 July 2018

Accepted for publication 11 September 2018

Published 15 November 2018 Volume 2018:13 Pages 7565—7574

DOI https://doi.org/10.2147/IJN.S180040

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Govarthanan Muthusamy

Peer reviewer comments 5

Editor who approved publication: Dr Thomas J. Webster


Anne-Claire Groo,1 Nada Matougui,2 Anita Umerska,2,3 Patrick Saulnier2,4

1Normandie Univ, UNICAEN, CERMN - EA 4258, FR CNRS 3038 INC3M, SF 4206 ICORE, Caen, France; 2Micro & Nanomédecines Translationelles-MINT, UNIV Angers, INSERM U1066, CNRS UMR 6021, UBL Universite Bretagne Loire, Angers, France; 3Université de Lorraine, CITHEFOR, Nancy, France; 4Angers University Hospital, Angers, France

Introduction: Resistance to traditional antibiotics is an increasingly serious problem. Antimicrobial peptides (AMPs) have emerged as a new therapeutic class with great potential against infectious diseases, as they are less prone to induce resistance. Nanotechnology-based delivery strategies can improve the efficiency and stability of AMPs, particularly against proteolytic degradation. Lipid nanocapsules (LNCs) are a new generation of biomimetic nanocarriers and were used in this study to deliver peptides.
Methods: AMP-loaded reverse micelles (RM) were developed and incorpo­rated into LNCs by the phase inversion process and the antimicrobial activity of the AMPs-loaded LNC was evaluated by the minimum inhibitory concentration method. We studied the activity of AMP solutions and AMP-loaded LNCs against Gram-positive and Gram-negative bacterial strains and then evaluated the encapsulation of a new cationic AMP called AP138. Finally, we analyzed the effect of enzymatic attack on AP138 and AP138-RM-LNCs after incubation with trypsin.
Results: AP138 was efficiently encapsulated in the LNCs (encapsulation efficiency = 97.8% at a drug loading of 0.151%), resulting in protection against degradation by proteases and the preservation of antimicrobial activity against Staphylococcus aureus, including methicillin-resistant Staphylococcus aureus.
Conclusion: This study shows that RM-LNCs are an excellent candidate system to deliver AMPs.

Keywords: nanoparticles, nanomedicine, antibacterial, AMP, methicillin-resistant Staphylococcus aureus, infection

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