title: Chitosan-tripolyphosphate nanoparticles as Arrabidaea chica standardized extract carrier: synthesis, characterization, biocompatibility, and antiulcerogenic activity.
abstract: Natural products using plants have received considerable attention because of their potential to treat various diseases. Arrabidaea chica (Humb. & Bonpl.) B. Verlot is a native tropical American vine with healing properties employed in folk medicine for wound healing, inflammation, and gastrointestinal colic. Applying nanotechnology to plant extracts has revealed an advantageous strategy for herbal drugs considering the numerous features that nanostructured systems offer, including solubility, bioavailability, and pharmacological activity enhancement. The present study reports the preparation and characterization of chitosan-sodium tripolyphosphate nanoparticles (NPs) charged with A. chica standardized extract (AcE). Particle size and zeta potential were measured using a Zetasizer Nano ZS. The NP morphological characteristics were observed using scanning electron microscopy. Our studies indicated that the chitosan/sodium tripolyphosphate mass ratio of 5 and volume ratio of 10 were found to be the best condition to achieve the lowest NP sizes, with an average hydrodynamic diameter of 150±13 nm and a zeta potential of +45±2 mV. Particle size decreased with AcE addition (60±10.2 nm), suggesting an interaction between the extract's composition and polymers. The NP biocompatibility was evaluated using human skin fibroblasts. AcE-NP demonstrated capability of maintaining cell viability at the lowest concentrations tested, stimulating cell proliferation at higher concentrations. Antiulcerogenic activity of AcE-NP was also evaluated with an acute gastric ulcer experimental model induced by ethanol and indomethacin. NPs loaded with A. chica extract reduced the ulcerative lesion index using lower doses compared with the free extract, suggesting that extract encapsulation in chitosan NPs allowed for a dose reduction for a gastroprotective effect. The AcE encapsulation offers an approach for further application of the A. chica extract that could be considered a potential candidate for ulcer-healing pharmaceutical systems.
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil ; Biomaterials Group, Polymer Science and Technology Institute-Spanish National Research Council (ICTP-CSIC), Madrid, Spain.
authors.forename: Leila
authors.initials: L
authors.lastname: Servat-Medina
authors.affiliation: Biomaterials Group, Polymer Science and Technology Institute-Spanish National Research Council (ICTP-CSIC), Madrid, Spain ; CIBER-BBN, Centro de Investigación Biomédica en Red, Madrid, Spain.
authors.forename: Alvaro
authors.initials: A
authors.lastname: González-Gómez
authors.affiliation: Biomaterials Group, Polymer Science and Technology Institute-Spanish National Research Council (ICTP-CSIC), Madrid, Spain.
authors.forename: Felisa
authors.initials: F
authors.lastname: Reyes-Ortega
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: Ilza Maria Oliveira
authors.initials: IM
authors.lastname: Sousa
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: Nubia de Cássia Almeida
authors.initials: Nde C
authors.lastname: Queiroz
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: Patricia Maria Wiziack
authors.initials: PM
authors.lastname: Zago
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: Michelle Pedrosa
authors.initials: MP
authors.lastname: Jorge
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil ; Department of Medical Clinics, Faculty of Medical Sciences, University of Campinas, Campinas-SP, Brazil.
authors.forename: Karin Maia
authors.initials: KM
authors.lastname: Monteiro
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: João Ernesto
authors.initials: JE
authors.lastname: de Carvalho
authors.affiliation: Biomaterials Group, Polymer Science and Technology Institute-Spanish National Research Council (ICTP-CSIC), Madrid, Spain ; CIBER-BBN, Centro de Investigación Biomédica en Red, Madrid, Spain.
authors.forename: Julio
authors.initials: J
authors.lastname: San Román
authors.affiliation: Chemical, Biological and Agricultural Pluridisciplinary Research Center-State University of Campinas (CPQBA-UNICAMP), Campinas-SP, Brazil.
authors.forename: Mary Ann
authors.initials: MA
authors.lastname: Foglio
mesh_terms: D000818:Animals; D029402:Bignoniaceae / Q000737:chemistry*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D048271:Chitosan / Q000737:chemistry*; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry*; D000431:Ethanol / Q000009:adverse effects; D005347:Fibroblasts / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007213:Indomethacin / Q000009:adverse effects; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D064209:Phytochemicals; D010936:Plant Extracts / Q000494:pharmacology*; D011122:Polyphosphates / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy
chemical_list: D004337:Drug Carriers; D064209:Phytochemicals; D010936:Plant Extracts; D011122:Polyphosphates; D000431:Ethanol; D048271:Chitosan; C005692:triphosphoric acid; D007213:Indomethacin
keywords: Arrabidaea chica; chitosan; herbal drug; nanoparticle; natural product; plant extract; ulcer healing