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

Author:

Solís-Cruz Guadalupe Y.1ORCID,Alvarez-Roman Rocío1ORCID,Rivas-Galindo Verónica M.1ORCID,Galindo-Rodríguez Sergio Arturo2ORCID,Silva-Mares David A.1ORCID,Marino-Martínez Iván A.34ORCID,Escobar-Saucedo Magdalena1ORCID,Pérez-López Luis A.1ORCID

Affiliation:

1. Autonomous University of Nuevo Leon, Faculty of Medicine , Department of Analytical Chemistry Monterrey , Nuevo León , México

2. Autonomous University of Nuevo Leon, Faculty of Biological Sciences , Department of Chemistry San Nicolás de los Garza , Nuevo León , México

3. Autonomous University of Nuevo Leon , Center for Research and Development in Health Sciences Monterrey , Nuevo León , México

4. Autonomous University of Nuevo Leon, Faculty of Medicine , Department of Pathology , Monterrey , Nuevo León , México

Abstract

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.

Publisher

Walter de Gruyter GmbH

Subject

Pharmaceutical Science,Pharmacology,General Medicine

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