title: Insights into the protective role of solid lipid nanoparticles on rosmarinic acid bioactivity during exposure to simulated gastrointestinal conditions.
abstract: The evaluation of the digestion effects on bioactive solid lipid nanoparticles (SLN) was performed. For this purpose, witepsol and carnauba SLN loaded with rosmarinic acid (RA) were exposed to the simulated gastrointestinal tract (GIT) conditions prevailing in stomach and small intestine. The simulation of intestinal epithelium was made with a dialysis bag and intestinal cell culture lines. Changes on SLN physical properties, RA release and absorption profiles were followed at each step. Combination of digestion pH and enzymes showed a significant effect upon SLN physical properties. Zeta potential values increased at stomach conditions and decreased at small intestine simulation. Also, at intestine, SLN increased their sizes and released 40-60% of RA, maintaining its initial antioxidant activity values. Sustained release of 40% of RA from SLN was also observed in dialysis tube. At CaCo-2 cell line, both types of SLN showed similar absorbed RA % (ca. 30%). Nevertheless, in CaCo-2/HT29x mix cell lines, for carnauba SLN a lower adsorption RA % was observed than for witepsol SLN. Solid lipid nanoparticles protected RA bioactivity (in terms of antioxidant activity) until reaching the intestine. A controlled release of RA from SLN was achieved and a significant absorption was observed at intestinal cells. Overall, SLN produced with witepsol showed a higher stability than carnauba SLN.
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. Electronic address: rmadureira@porto.ucp.pt.
authors.forename: Ana Raquel
authors.initials: AR
authors.lastname: Madureira
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: Débora A
authors.initials: DA
authors.lastname: Campos
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: Ana
authors.initials: A
authors.lastname: Oliveira
authors.affiliation: I3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Portugal and INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Rua do Campo Alegre, Portugal; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra 1317, 4585-116 Gandra-PRD, Portugal.
authors.forename: Bruno
authors.initials: B
authors.lastname: Sarmento
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: Maria Manuela
authors.initials: MM
authors.lastname: Pintado
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: Ana Maria
authors.initials: AM
authors.lastname: Gomes
mesh_terms: D000975:Antioxidants / Q000737:chemistry*; D040761:Biomimetic Materials / Q000737:chemistry; D018938:Caco-2 Cells; D002934:Cinnamates / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D053630:Depsides / Q000737:chemistry*; D003956:Dialysis; D004339:Drug Compounding; D065546:Drug Liberation; D005750:Gastric Juice / Q000737:chemistry; D019073:HT29 Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption / Q000502:physiology; D007421:Intestine, Small / Q000737:chemistry / Q000502:physiology; D008954:Models, Biological; D053758:Nanoparticles / Q000737:chemistry*; D010194:Pancreatin / Q000737:chemistry*; D010316:Particle Size; D010434:Pepsin A / Q000737:chemistry*; D013270:Stomach / Q000737:chemistry / Q000502:physiology; D014280:Triglycerides / Q000737:chemistry; D014885:Waxes / Q000737:chemistry; D000097123:Rosmarinic Acid
chemical_list: D000975:Antioxidants; D002934:Cinnamates; D003692:Delayed-Action Preparations; D053630:Depsides; D010194:Pancreatin; D010434:Pepsin A; D014280:Triglycerides; D014885:Waxes; D000097123:Rosmarinic Acid; C009683:witepsol; C026344:carnauba wax
keywords: Antioxidant activity; Release profiles; Rosmarinic acid; Simulated gastrointestinal tract (GIT)