<abstract xmlns="http://www.w3.org/1999/xhtml">
<p>Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the <italic>Jatropha dioica</italic> root. This compound has been shown to possess moderate antiherpetic activity <italic>in vitro</italic>. 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<sup>®</sup> L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for <italic>in vitro</italic> antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of <italic>J. dioica</italic>, the  major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index &lt; 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 <italic>in vitro </italic>antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.</p>
</abstract>

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.

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

Autonomous University of Nuevo Leon, Faculty  of Medicine

Department of Analytical Chemistry Monterrey

Autonomous University of Nuevo Leon, Faculty  of Biological Sciences

Department of Chemistry San Nicolás de los Garza

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess...

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

Data publikacji: 14 wrz 2023

Zakres stron: 457 - 473

Przyjęty: 04 maj 2023

DOI: https://doi.org/10.2478/acph-2023-0028

Słowa kluczowe
riolozatrione, polymeric nanoparticles, herpes simplex virus, antiviral

© 2023 Guadalupe Y. Solís-Cruz et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

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

Data publikacji: 14 wrz 2023

Zakres stron: 457 - 473

Przyjęty: 04 maj 2023

DOI: https://doi.org/10.2478/acph-2023-0028

Słowa kluczoweriolozatrione, polymeric nanoparticles, herpes simplex virus, antiviral

© 2023 Guadalupe Y. Solís-Cruz et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

Słowa kluczowe
riolozatrione, polymeric nanoparticles, herpes simplex virus, antiviral