caa a22 4500 60615549X CHVBK 20210128100603.0 cr unu---uuuuu 210128e20150601xx s 000 0 eng 10.1007/s10096-015-2344-7 doi (NATIONALLICENCE)springer-10.1007/s10096-015-2344-7 Potential chitosan-coated alginate nanoparticles for ocular delivery of daptomycin [Elektronische Daten] [J. R. Costa, N. Silva, B. Sarmento, M. Pintado] Daptomycin may offer an antibacterial alternative for the treatment of endophthalmitis caused by methicillin-resistant Staphylococcus aureus (MRSA) and other potential agents. In the present project, mucoadhesive chitosan-coated alginate (CS-ALG) nanoparticles are proposed as an effective delivery system for daptomycin permeation across ocular epithelia, with potential for the treatment of bacterial endophthalmitis. CS-ALG nanoparticles were prepared by ionotropic pre-gelation of an alginate core followed by chitosan polyelectrolyte complexation, and characterized regarding particle size, polydispersity, and zeta potential. The encapsulation efficiency was determined and antimicrobial activity was also tested after encapsulation of the antibiotic. Also, in vitro ocular permeability of free daptomycin and encapsulation into chitosan and CS-ALG nanoparticles was evaluated using ocular epithelial cell culture models. Formulated daptomycin-loaded CS-ALG nanoparticles were negatively charged, with a size range of 380-420nm, suitable for ocular application. The encapsulation efficiency was between 79 and 92%, with decreasing alginate:daptomycin mass ratios. The antibacterial activity of daptomycin against major microorganisms responsible for bacterial endophthalmitis was not affected by encapsulation into nanoparticles. Daptomycin permeability was up to 16% (chitosan nanoparticles) and 9% (CS-ALG nanoparticles) through corneal cell monolayer, and 18% (chitosan nanoparticles) and 12% (CS-ALG nanoparticles) for retinal cell monolayer after 4h, demonstrating epithelial retention of the drug compared to free drug. The developed daptomycin-loaded CS-ALG nanoparticles seem to be an interesting and potential system for ocular daptomycin delivery and treatment of bacterial endophthalmitis. Springer-Verlag Berlin Heidelberg, 2015 Costa J. R. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut Silva N. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut Sarmento B. CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Instituto Superior de Ciências da Saúde-Norte, Rua Central de Gandra, 1317, 4585-116, Gandra, PRD, Portugal aut Pintado M. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut European Journal of Clinical Microbiology & Infectious Diseases Springer Berlin Heidelberg 34/6(2015-06-01), 1255-1262 0934-9723 34:6<1255 2015 34 10096 https://doi.org/10.1007/s10096-015-2344-7 text/html Onlinezugriff via DOI BK010053 XK010053 XK010000 Metadata rights reserved Springer special CC-BY-NC licence nationallicence 1 research-article jats NATIONALLICENCE NATIONALLICENCE NL-springer NATIONALLICENCE 856 40 https://doi.org/10.1007/s10096-015-2344-7 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Costa J. R. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut NATIONALLICENCE 700 1- Silva N. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut NATIONALLICENCE 700 1- Sarmento B. CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Instituto Superior de Ciências da Saúde-Norte, Rua Central de Gandra, 1317, 4585-116, Gandra, PRD, Portugal aut NATIONALLICENCE 700 1- Pintado M. CBQF - Centre for Biotechnology and Fine Chemistry - State Associated Laboratory, College of Biotechnology, Catholic University of Portugal/ Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4200-401, Porto, Portugal aut NATIONALLICENCE 773 0- European Journal of Clinical Microbiology & Infectious Diseases Springer Berlin Heidelberg 34/6(2015-06-01), 1255-1262 0934-9723 34:6<1255 2015 34 10096