Prophylactic and therapeutic intranasal administration with an immunomodulator, Hiltonol® (Poly IC:LC), in a lethal SARS-CoV-infected BALB/c mouse model

Antiviral Res. 2017 Mar:139:1-12. doi: 10.1016/j.antiviral.2016.12.007. Epub 2016 Dec 9.

Abstract

Hiltonol®, (Poly IC:LC), a potent immunomodulator, is a synthetic, double-stranded polyriboinosinic-polyribocytidylic acid (poly IC) stabilized with Poly-L-lysine and carboxymethyl cellulose (LC). Hiltonol® was tested for efficacy in a lethal SARS-CoV-infected BALB/c mouse model. Hiltonol® at 5, 1, 0.5 or 0.25 mg/kg/day by intranasal (i.n.) route resulted in significant survival benefit when administered at selected times 24 h prior to challenge with a lethal dose of mouse-adapted severe acute respiratory syndrome coronavirus (SARS-CoV). The infected BALB/c mice receiving the Hiltonol® treatments were also significantly effective in protecting mice against weight loss due to infection (p < 0.001). Groups of 20 mice were dosed with Hiltonol® at 2.5 or 0.75 mg/kg by intranasal instillation 7, 14, and 21 days before virus exposure and a second dose was given 24 h later, prophylactic Hiltonol® treatments (2.5 mg/kg/day) were completely protective in preventing death, and in causing significant reduction in lung hemorrhage scores, lung weights and lung virus titers. Hiltonol® was also effective as a therapeutic when give up to 8 h post virus exposure; 100% of the-infected mice were protected against death when Hiltonol® was administered at 5 mg/kg/day 8 h after infection. Our data suggest that Hiltonol® treatment of SARS-CoV infection in mice leads to substantial prophylactic and therapeutic effects and could be used for treatment of other virus disease such as those caused by MERS-CoV a related coronavirus. These properties might be therapeutically advantageous if Hiltonol® is considered for possible clinical use.

Keywords: BALB/c mouse; Hiltonol(®); MERS-CoV; SARS-CoV.

MeSH terms

  • Adjuvants, Immunologic
  • Administration, Intranasal
  • Animals
  • Carboxymethylcellulose Sodium / administration & dosage
  • Carboxymethylcellulose Sodium / analogs & derivatives*
  • Carboxymethylcellulose Sodium / therapeutic use
  • Disease Models, Animal
  • Immunomodulation*
  • Interferon Inducers / administration & dosage
  • Interferon Inducers / therapeutic use*
  • Lung / drug effects
  • Lung / pathology
  • Lung / virology
  • Mice
  • Mice, Inbred BALB C
  • Poly I-C / administration & dosage
  • Poly I-C / therapeutic use*
  • Polylysine / administration & dosage
  • Polylysine / analogs & derivatives*
  • Polylysine / therapeutic use
  • Severe Acute Respiratory Syndrome / drug therapy*
  • Severe Acute Respiratory Syndrome / mortality
  • Severe Acute Respiratory Syndrome / prevention & control*
  • Severe Acute Respiratory Syndrome / virology
  • Severe acute respiratory syndrome-related coronavirus / drug effects
  • Survival Analysis

Substances

  • Adjuvants, Immunologic
  • Interferon Inducers
  • Polylysine
  • poly ICLC
  • Carboxymethylcellulose Sodium
  • Poly I-C