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Asma Ismail Albdrawy,1 Fadilah Sfouq Aleanizy,1 Esraa Kamal Eltayb,1 Abdullah A Aldossari,2 Mohammed M Alanazi,2 Rihaf Alfaraj,1 Eram Eltahir,1 Hibah M Albasri,3 Jouri S Alanazi,4 Fulwah Yahya Alqahtani1 1Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 3Department of Biology, College of Science, Taibah University, Madinah, Saudi Arabia; 4Pharmaceutical Care Department, National Guard Health Affairs, Riyadh, Saudi ArabiaCorrespondence: Fulwah Yahya Alqahtani, Department of Pharmaceutics, College of Pharmacy, King Saud University, PO Box 22452, Riyadh, 11495, Saudi Arabia, Tel +966-11-8051478 ; +966503416440, Email fyalqahtani@ksu.edu.saIntroduction: The emergence of Neisseria gonorrhoeae-resistant strains represents one of the most urgent global threats. In this regard, C7-3 peptide is one of the anti-virulence therapies that has demonstrated promising anti-gonococcal activity. Accordingly, this research aimed to formulate C7-3 peptide and its derivatives in chitosan nanoparticles.Methods: The peptide loaded chitosan nanoparticles were prepared using ion gelation method, and their physicochemical characteristics were investigated. The anti-gonococcal and antibiofilm activity of prepared NPs was assessed, and their cytotoxicity in human ovarian cells was evaluated.Results: All prepared NPs were optimized for the smallest particle size of 136.9 to 168.3 nm. The EE% of C7-3, C7-3m1, and C7-3m2 CNPs reached 90.2, 92.5, and 91.8%, respectively. An in vitro release study demonstrated a continuous sustained-release pattern of C7-3 peptide from NPs. The SDS-PAGE assay confirmed the integrity of C7-3 peptide after the fabrication process. When comparing each peptide alone, the generated NPs demonstrated higher anti-gonococcal and anti-biofilm effectiveness against standard and resistant bacterial strains under anaerobic conditions. The cytotoxicity experiments revealed the cytocompatibility of NPs in HeLa cell lines. Given the advantages of enhanced anti-gonococcal activity of the C7-3 peptide and its derivatives when loaded with CNPs, as well as the antimicrobial properties of chitosan NPs, the reported NPs have great potential in the treatment of gonococcal infection.Keywords: N. gonorrhoeae, chitosan, nanoparticles, C7-3 peptide, biofilm |
