Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies

Rosmarinic acid (RA), a caffeic acid derivative, has been loaded in polymeric nanoparticles made up of poly(lactic-<i>co</i>-glycolic acid) (PLGA) through a nano-emulsion templating process using the phase-inversion composition (PIC) method at room temperature. The obtained RA-loaded nan...

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Main Authors: Jessica García-Melero, Joan-Josep López-Mitjavila, María José García-Celma, Carlos Rodriguez-Abreu, Santiago Grijalvo
Format: Article
Language:English
Published: MDPI AG 2022-06-01
Series:Materials
Subjects:
Online Access:https://www.mdpi.com/1996-1944/15/13/4572
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author Jessica García-Melero
Joan-Josep López-Mitjavila
María José García-Celma
Carlos Rodriguez-Abreu
Santiago Grijalvo
author_facet Jessica García-Melero
Joan-Josep López-Mitjavila
María José García-Celma
Carlos Rodriguez-Abreu
Santiago Grijalvo
author_sort Jessica García-Melero
collection DOAJ
description Rosmarinic acid (RA), a caffeic acid derivative, has been loaded in polymeric nanoparticles made up of poly(lactic-<i>co</i>-glycolic acid) (PLGA) through a nano-emulsion templating process using the phase-inversion composition (PIC) method at room temperature. The obtained RA-loaded nanoparticles (NPs) were colloidally stable exhibiting average diameters in the range of 70–100 nm. RA was entrapped within the PLGA polymeric network with high encapsulation efficiencies and nanoparticles were able to release RA in a rate-controlled manner. A first-order equation model fitted our experimental data and confirmed the prevalence of diffusion mechanisms. Protein corona formation on the surface of NPs was assessed upon incubation with serum proteins. Protein adsorption induced an increase in the hydrodynamic diameter and a slight shift towards more negative surface charges of the NPs. The radical scavenging activity of RA-loaded NPs was also studied using the DPPH·assay and showed a dose–response relationship between the NPs concentration and DPPH inhibition. Finally, RA-loaded NPs did not affect the cellular proliferation of the human neuroblastoma SH-SY5Y cell line and promoted efficient cellular uptake. These results are promising for expanding the use of O/W nano-emulsions in biomedical applications.
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spelling doaj.art-3fb1932f8e854c32bd9c051e4db4311f2023-12-03T14:10:33ZengMDPI AGMaterials1996-19442022-06-011513457210.3390/ma15134572Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro StudiesJessica García-Melero0Joan-Josep López-Mitjavila1María José García-Celma2Carlos Rodriguez-Abreu3Santiago Grijalvo4Institute for Advanced Chemistry of Catalonia (CSIC-IQAC), Jordi Girona 18-26, E-08034 Barcelona, SpainInstitute for Advanced Chemistry of Catalonia (CSIC-IQAC), Jordi Girona 18-26, E-08034 Barcelona, SpainDepartment of Pharmacy, Pharmaceutical Technology, and Physical-Chemistry, R+D Associated Unit to CSIC Pharmaceutical Nanotechnology, IN2UB, University of Barcelona, Joan XXIII 27-31, E-08028 Barcelona, SpainInstitute for Advanced Chemistry of Catalonia (CSIC-IQAC), Jordi Girona 18-26, E-08034 Barcelona, SpainNetworking Centre in Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Jordi Girona 18-26, E-08034 Barcelona, SpainRosmarinic acid (RA), a caffeic acid derivative, has been loaded in polymeric nanoparticles made up of poly(lactic-<i>co</i>-glycolic acid) (PLGA) through a nano-emulsion templating process using the phase-inversion composition (PIC) method at room temperature. The obtained RA-loaded nanoparticles (NPs) were colloidally stable exhibiting average diameters in the range of 70–100 nm. RA was entrapped within the PLGA polymeric network with high encapsulation efficiencies and nanoparticles were able to release RA in a rate-controlled manner. A first-order equation model fitted our experimental data and confirmed the prevalence of diffusion mechanisms. Protein corona formation on the surface of NPs was assessed upon incubation with serum proteins. Protein adsorption induced an increase in the hydrodynamic diameter and a slight shift towards more negative surface charges of the NPs. The radical scavenging activity of RA-loaded NPs was also studied using the DPPH·assay and showed a dose–response relationship between the NPs concentration and DPPH inhibition. Finally, RA-loaded NPs did not affect the cellular proliferation of the human neuroblastoma SH-SY5Y cell line and promoted efficient cellular uptake. These results are promising for expanding the use of O/W nano-emulsions in biomedical applications.https://www.mdpi.com/1996-1944/15/13/4572antioxidant activitycellular uptakecolloidal dispersionsdrug deliverynano-emulsionsnanoparticles
spellingShingle Jessica García-Melero
Joan-Josep López-Mitjavila
María José García-Celma
Carlos Rodriguez-Abreu
Santiago Grijalvo
Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
Materials
antioxidant activity
cellular uptake
colloidal dispersions
drug delivery
nano-emulsions
nanoparticles
title Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
title_full Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
title_fullStr Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
title_full_unstemmed Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
title_short Rosmarinic Acid-Loaded Polymeric Nanoparticles Prepared by Low-Energy Nano-Emulsion Templating: Formulation, Biophysical Characterization, and In Vitro Studies
title_sort rosmarinic acid loaded polymeric nanoparticles prepared by low energy nano emulsion templating formulation biophysical characterization and in vitro studies
topic antioxidant activity
cellular uptake
colloidal dispersions
drug delivery
nano-emulsions
nanoparticles
url https://www.mdpi.com/1996-1944/15/13/4572
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