title: Chitosan-based nanoparticles for rosmarinic acid ocular delivery--In vitro tests.
abstract: In this study, chitosan nanoparticles were used to encapsulate antioxidant rosmarinic acid, Salvia officinalis (sage) and Satureja montana (savory) extracts as rosmarinic acid natural vehicles. The nanoparticles were prepared by ionic gelation using chitosan and sodium tripolyphosphate (TPP) in a mass ratio of 7:1, at pH 5.8. Particle size distribution analysis and transmission electron microscopy (TEM) confirmed the size ranging from 200 to 300 nm, while surface charge of nanoparticles ranged from 20 to 30 mV. Nanoparticles demonstrate to be safe without relevant cytotoxicity against retina pigment epithelium (ARPE-19) and human cornea cell line (HCE-T). The permeability study in HCE monolayer cell line showed an apparent permeability coefficient Papp of 3.41±0.99×10(-5) and 3.24±0.79×10(-5) cm/s for rosmarinic acid loaded chitosan nanoparticles and free in solution, respectively. In ARPE-19 monolayer cell line the Papp was 3.39±0.18×10(-5) and 3.60±0.05×10(-5) cm/s for rosmarinic acid loaded chitosan nanoparticles and free in solution, respectively. Considering the mucin interaction method, nanoparticles indicate mucoadhesive proprieties suggesting an increased retention time over the ocular mucosa after instillation. These nanoparticles may be promising drug delivery systems for ocular application in oxidative eye conditions.
authors.affiliation: Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal; CBQF-Centro de Biotecnologia e Química Fina, Laboratório Associado, Escola Superior de Biotecnologia, Universidade Católica Portuguesa/Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4202-401 Porto, Portugal. Electronic address: sara.baptistadasilva@gmail.com.
authors.forename: Sara Baptista
authors.initials: SB
authors.lastname: da Silva
authors.affiliation: Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, Rua Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal.
authors.forename: Domingos
authors.initials: D
authors.lastname: Ferreira
authors.affiliation: CBQF-Centro de Biotecnologia e Química Fina, Laboratório Associado, Escola Superior de Biotecnologia, Universidade Católica Portuguesa/Porto, Rua Arquiteto Lobão Vital, Apartado 2511, 4202-401 Porto, Portugal.
authors.forename: Manuela
authors.initials: M
authors.lastname: Pintado
authors.affiliation: CESPU, IINFACTS, Department of Pharmaceutical Sciences, Institute of Health Sciences-North, Rua Central de Gandra, 1317, 4585-116 Gandra, Portugal; INEB, Institute of Biomedical Engineering, University of Porto, Rua do Campo Alegre, 823, 4150-180 Porto, Portugal. Electronic address: bruno.sarmento@ineb.up.pt.
authors.forename: Bruno
authors.initials: B
authors.lastname: Sarmento
mesh_terms: D000818:Animals; D002460:Cell Line; D002463:Cell Membrane Permeability; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D048271:Chitosan / Q000737:chemistry*; D002934:Cinnamates / Q000008:administration & dosage* / Q000493:pharmacokinetics; D053630:Depsides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D005123:Eye / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D000097123:Rosmarinic Acid
chemical_list: D048271:Chitosan; D002934:Cinnamates; D053630:Depsides; D004337:Drug Carriers; D000097123:Rosmarinic Acid
keywords: Cell models; Chitosan; Nanoparticles; Rosmarinic acid