Acta Pharmaceutica, Vol. 73 No. 3, 2023.
Original scientific paper
https://doi.org/10.2478/acph-2023-0028
Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential anti-herpetic activity
GUADALUPE Y. SOLÍS-CRUZ
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
ROCÍO ALVAREZ-ROMAN
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
VERÓNICA M. RIVAS-GALINDO
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
SERGIO ARTURO GALINDO-RODRÍGUEZ
; Autonomous University of Nuevo Leon, Faculty of Biological Sciences, Department of Chemistry, San Nicolás de los Garza, Nuevo León, México
DAVID A. SILVA-MARES
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
IVÁN A. MARINO-MARTÍNEZ
; Autonomous University of Nuevo Leon, Center for Research and Development in Health Sciences, Monterrey 66460, Nuevo León, México; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Pathology, Monterrey 66460, Nuevo León, México
MAGDALENA ESCOBAR-SAUCEDO
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
LUIS A. PÉREZ-LÓPEZ
; Autonomous University of Nuevo Leon, Faculty of Medicine, Department of Analytical Chemistry, Monterrey 66460, Nuevo León, México
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 anti-herpetic 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 physiochemically characterize Eudragit® L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for in vitro anti-herpetic 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 anti-herpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.
Keywords
riolozatrione; polymeric nanoparticles; herpes simplex virus; antiviral
Hrčak ID:
303174
URI
Publication date:
30.9.2023.
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