1. Oral nanoparticles based on gellan gum/pectin for colon-targeted delivery of resveratrol
- Author
-
Maria Palmira Daflon Gremião, Bruno Sarmento, Andreia Almeida, Fabíola Garavello Prezotti, Teófilo Vasconcelos, Daniella S. Silva, Beatriz Stringhetti Ferreira Cury, Natália Noronha Ferreira, Fernanda Isadora Boni, Universidade Estadual Paulista (Unesp), Universidade de São Paulo (USP), Universidade do Porto, and CESPU-Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde
- Subjects
Male ,Pectin ,Pharmaceutical Science ,Nanoparticle ,Administration, Oral ,02 engineering and technology ,Resveratrol ,030226 pharmacology & pharmacy ,chemistry.chemical_compound ,0302 clinical medicine ,colon-targeted release ,Drug Discovery ,triple co-culture model ,Food science ,Intestinal Mucosa ,Drug Carriers ,digestive, oral, and skin physiology ,Polysaccharides, Bacterial ,everted gut sac ,food and beverages ,Hydrogen-Ion Concentration ,021001 nanoscience & nanotechnology ,Gellan gum ,Drug release ,Pectins ,0210 nano-technology ,HT29 Cells ,food.ingredient ,Colon ,in vitro permeability ,Permeability ,Polymeric nanoparticles ,03 medical and health sciences ,food ,Cell Line, Tumor ,Animals ,Humans ,Particle Size ,Rats, Wistar ,Pharmacology ,caco-2 cells ,Organic Chemistry ,Rats ,Drug Liberation ,Mucus ,chemistry ,Caco-2 ,Permeability (electromagnetism) ,Nanoparticles ,Caco-2 Cells - Abstract
Made available in DSpace on 2020-12-12T02:34:00Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-02-01 Nanoparticles based on gellan gum/pectin blends were designed for colon-targeted release of resveratrol (RES). Their impact on drug release rates and permeability were evaluated using Caco-2 cell model and mucus secreting triple co-culture model. Polymeric nanoparticles (PNP) were successfully prepared by nebulization/ionotropic gelation, achieving high drug loading (>80%). PNP were spherical with a low positive charge density (+5mV) and exhibited diameters of around 330 nm. Developed PNP were able to promote effective modulation of drug release rates, so that only 3% of RES was released in acidic media over 2 h, and, in pH 6.8, the drug was released in a sustained manner, reaching 85% in 30 h. The permeability of RES-loaded PNP in the Caco-2 model was 0.15%, while in the triple co-culture model, in the presence of mucus, it reached 5.5%. The everted gut sac experiment corroborated the low permeability of RES-loaded PNP in the presence or absence of mucus and highlighted their high ability to interact with the intestinal tissue. Results indicate that the novel PNP developed in this work are safe and promising carriers for controlled delivery of RES at the colon. School of Pharmaceutical Sciences São Paulo State University (UNESP) Chemistry Institute of São Carlos São Paulo University (USP) I3S-Instituto de Investigação e Inovação em Saúde Universidade do Porto INEB-Instituto de Engenharia Biomédica Universidade do Porto CESPU-Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde School of Pharmaceutical Sciences São Paulo State University (UNESP)
- Published
- 2020