title: Biocompatible nanocarrier fortified with a dipyridinium-based amphiphile for eradication of biofilm.
abstract: Annihilation of bacterial biofilms is challenging owing to their formidable resistance to therapeutic antibiotics and thus there is a constant demand for development of potent antibiofilm agents that can abolish established biofilms. In the present study, the activity of a dipyridinium-based cationic amphiphile (compound 1) against established bacterial biofilms and the subsequent development of a compound 1-loaded nanocarrier for potential antibiofilm therapy are highlighted. Solution-based assays and microscopic analysis revealed the antagonistic effect of compound 1 on biofilms formed by Staphylococcus aureus MTCC 96 and Pseudomonas aeruginosa MTCC 2488. In combination studies, compound 1 could efficiently potentiate the action of tobramycin and gentamicin on P. aeruginosa and S. aureus biofilm, respectively. A human serum albumin (HSA)-based nanocarrier loaded with compound 1 was generated, which exhibited sustained release of compound 1 at physiological pH. The compound 1-loaded HSA nanocarrier (C1-HNC) displayed the signature membrane-directed activity of the amphiphile on target bacteria, efficiently eliminated established bacterial biofilms, and was observed to be nontoxic to a model human cell line. Interestingly, compound 1 as well as the amphiphile-loaded HSA nanocarrier could eradicate established S. aureus biofilm from the surface of a Foley's urinary catheter. On the basis of its biocompatibility and high antibiofilm activity, it is conceived that the amphiphile-loaded nanocarrier may hold potential in antibiofilm therapy.
authors.affiliation: Department of Biotechnology, Indian Institute of Technology Guwahati , Guwahati 781039, India.
authors.forename: Sudeep
authors.initials: S
authors.lastname: Goswami
authors.forename: Durairaj
authors.initials: D
authors.lastname: Thiyagarajan
authors.forename: Gopal
authors.initials: G
authors.lastname: Das
authors.forename: Aiyagari
authors.initials: A
authors.lastname: Ramesh
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001672:Biocompatible Materials; D018441:Biofilms / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D049329:Nanostructures / Q000737:chemistry*; D011726:Pyridinium Compounds / Q000737:chemistry*; D012709:Serum Albumin
chemical_list: D000900:Anti-Bacterial Agents; D001672:Biocompatible Materials; D004337:Drug Carriers; D011726:Pyridinium Compounds; D012709:Serum Albumin
keywords: HSA nanocarrier; amphiphile; antibacterial; antibiofilm; antibiotic; catheter