Abstract
Chloroquine diphosphate (CQ) is a hydrophilic drug with low entrapment efficiency in hydrophobic nanoparticles (NP). Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus worldwide known as a common human pathogen. This study aims to develop chloroquine-loaded poly(lactic acid) (PLA) nanoparticles (CQ-NP) to improve the chloroquine anti- HSV-1 efficacy. CQ-NP were successfully prepared using a modified emulsification-solvent evaporation method. Physicochemical properties of the NP were monitored using dynamic light scattering, atomic force microscopy, drug loading efficiency, and drug release studies. Spherical nanoparticles were produced with modal diameter of <300 nm, zeta potential of −20 mv and encapsulation efficiency of 64.1%. In vitro assays of CQ-NP performed in Vero E6 cells, using the MTT-assay, revealed different cytotoxicity levels. Blank nanoparticles (B-NP) were biocompatible. Finally, the antiviral activity tested by the plaque reduction assay revealed greater efficacy for CQ-NP compared to CQ at concentrations equal to or lower than 20 µg mL−1 (p < 0.001). On the other hand, the B-NP had no antiviral activity. The CQ-NP has shown feasible properties and great potential to improve the antiviral activity of drugs.
Highlights
Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus belonging to the Herpesviridae family
EE% levels less than 11% were identified for these samples, which decreased according to the Chloroquine diphosphate (CQ): poly(lactic acid) (PLA) ratio
We found that nanoprecipitation was not the best method to encapsulate the hydrophilic CQ drugs when compared to emulsification-solvent evaporation
Summary
Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus belonging to the Herpesviridae family. This virus, a common human pathogen, is the main cause of oral infection, affecting the mouth and lips. HSV-1 can be the infectious agent of several diseases including recurrent cold sores, keratoconjunctivitis, and life-threatening herpes encephalitis [1,2,3]. The treatment of infection caused by the HSV-1 include the use of drugs, such as acyclovir, valacyclovir, famciclovir, penciclovir, and cidofovirare [7]. Long-term of these treatments may lead to the selection of resistant HSV, being an additional concern mainly for the immunocompromised patients, which has emphasized the need for alternative strategies [8,9]
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