Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity

Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formula...

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Main Authors: Solís-Cruz Guadalupe Y., Alvarez-Roman Rocío, Rivas-Galindo Verónica M., Galindo-Rodríguez Sergio Arturo, Silva-Mares David A., Marino-Martínez Iván A., Escobar-Saucedo Magdalena, Pérez-López Luis A.
Format: Article
Language:English
Published: Sciendo 2023-09-01
Series:Acta Pharmaceutica
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Online Access:https://doi.org/10.2478/acph-2023-0028
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author Solís-Cruz Guadalupe Y.
Alvarez-Roman Rocío
Rivas-Galindo Verónica M.
Galindo-Rodríguez Sergio Arturo
Silva-Mares David A.
Marino-Martínez Iván A.
Escobar-Saucedo Magdalena
Pérez-López Luis A.
author_facet Solís-Cruz Guadalupe Y.
Alvarez-Roman Rocío
Rivas-Galindo Verónica M.
Galindo-Rodríguez Sergio Arturo
Silva-Mares David A.
Marino-Martínez Iván A.
Escobar-Saucedo Magdalena
Pérez-López Luis A.
author_sort Solís-Cruz Guadalupe Y.
collection DOAJ
description Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize and physio-chemically characterize Eudragit® L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for in vitro antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of J. dioica, the major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index < 0.2, the zeta potential of –37 mV, and RZ encapsulation efficiency of 89 %. The NPR showed sustained release of RZ for 48 h with release percentages of 95 and 97 % at neutral and slightly acidic pH, respectively. Regarding in vitro antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.
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spelling doaj-art-70c85a2998d5483297488b6399c253d52025-02-03T03:40:23ZengSciendoActa Pharmaceutica1846-95582023-09-0173345747310.2478/acph-2023-0028Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activitySolís-Cruz Guadalupe Y.0Alvarez-Roman Rocío1Rivas-Galindo Verónica M.2Galindo-Rodríguez Sergio Arturo3Silva-Mares David A.4Marino-Martínez Iván A.5Escobar-Saucedo Magdalena6Pérez-López Luis A.7Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Biological Sciences, Department of Chemistry San Nicolás de los Garza, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Center for Research and Development in Health Sciences Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoAutonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry Monterrey66460, Nuevo León, MéxicoRiolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize and physio-chemically characterize Eudragit® L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for in vitro antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of J. dioica, the major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index < 0.2, the zeta potential of –37 mV, and RZ encapsulation efficiency of 89 %. The NPR showed sustained release of RZ for 48 h with release percentages of 95 and 97 % at neutral and slightly acidic pH, respectively. Regarding in vitro antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.https://doi.org/10.2478/acph-2023-0028riolozatrionepolymeric nanoparticlesherpes simplex virusantiviral
spellingShingle Solís-Cruz Guadalupe Y.
Alvarez-Roman Rocío
Rivas-Galindo Verónica M.
Galindo-Rodríguez Sergio Arturo
Silva-Mares David A.
Marino-Martínez Iván A.
Escobar-Saucedo Magdalena
Pérez-López Luis A.
Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
Acta Pharmaceutica
riolozatrione
polymeric nanoparticles
herpes simplex virus
antiviral
title Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
title_full Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
title_fullStr Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
title_full_unstemmed Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
title_short Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity
title_sort formulation and optimization of polymeric nanoparticles loaded with riolozatrione a promising nanoformulation with potential antiherpetic activity
topic riolozatrione
polymeric nanoparticles
herpes simplex virus
antiviral
url https://doi.org/10.2478/acph-2023-0028
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