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Novel Chloroquine Drug Delivery

Chloroquine and hydroxychloroquine possess excellent antiviral properties against Coronavirus (SARS-CoV-2)[1] but have largely been discredited in the media because of mixed or poor results in treating the pulmonary complications of CoVID-19. Some reasons for this include...

  • It is most often given to the sickest patients admitted to hospital [2]
  • It is usually given to the patients with more advanced infection [2]
  • It is often given to patients who have other serious medical conditions [2]
  • It is often avoided early in the infection because of concern for side effects
Coronavirus rendered image provided by the CDC.

Pharmacokinetics: the Key to the Problem

Hydroxychloroquine is the active ingredient in Plaquenil (Sanofi-Synthelabo Inc.) an anti-malarial drug that is also indicated for the treatment of  lupus erythematosis and rheumatoid arthritis. It is well recognized that response of these autoimmune diseases is very slow and researchers discovered the reason for this in a study that sheds considerable light on why the drug may not be living up to its promise in the current pandemic. The secret lies in the pharmacokinetics, which is a description of how easily a drug gets absorbed, the blood levels and tissues it reaches (and in what time period) as well as how long it lasts in the body before it gets changed or excreted. Here are some facts from a study of how the drug performs in healthy adults. [3]

the Xeragenx Solution - Nebulized Chloroquine Inhalation

By delivering chloroquine to the lungs directly, via inhalation will circumvent the problem of oral or intravenous hydroxychloroquine from being trapped in the the blood cell compartment and not reaching the lungs in time. We are not just talking about blowing chloroquine into the lungs, but will be loading it onto a drug delivery system that may be successful at directing the drug to the cells that are in the front line of the battle with CoVID-19 - the M2 macrophages. These are the 'sentry cells protecting the pulmonary alveoli (air sacs) that express a specialized protein on their cell membrane, called the multi-ligand mannose receptor (or CD206) that is intimately involved in the complex inflammatory process . [4] CD206 is responsible for pathogen recognition, antigen presentation and clearance of foreign material (phagocytosis) in the alveoli. In other words, these ‘sentry cells’ are at the center of  this ‘cytokine storm’ and Xeragenx's drug delivery platform may facilitate docking of chloroquine to the M2 macrophage surface receptor to fight the virus. How do we do this? In collaboration with Prof. Robert Doyle at Syracuse University...