Solubilised ivermectin improves drug delivery
Interview and article by Christine Clark.
Patented solubilisation technology improves the bioavailability of oral ivermectin and makes possible the formulation of an ivermectin injection for human use, according to recent work undertaken by Mountain Valley MD in Canada. IMI spoke to Dennis Hancock, President and CEO of Mountain Valley MD to find out more.
Mountain Valley MD is a public company that’s focused on biotechnology innovation – it works with existing molecules to make them more soluble or to develop formulations that deliver the drugs more effectively.
Ivermectin is of particular interest to Mountain Valley MD. It has applications both in human and animal medicine. In humans it is used as an anti-parasitic and has recently been used in many countries in the treatment of covid-19. It is also widely used in animal husbandry and for treatment of ticks and parasites in companion animals. “What people may not realise is the vast safety and efficacy in humans – to date it’s been administered over 3.8 billion times in humans with an adverse event rate of only 168 events per year. You’d be surprised to know that is safer than most vitamins!” says Mr Hancock. “It’s defined as a blockbuster drug which means it’s done at least a billion dollars in annual sales and it’s done that for 20 years”, he adds.
The number one limitation for ivermectin is its poor solubility (in water). “The body’s ability to absorb a drug is directly related to its solubility and bioavailability in turn”, explains Mr Hancock. Moreover, there is still no injectable form of the drug for human use and so ivermectin has to be taken by the oral route. “It takes about six hours for its onset and has a 40% variability which means it’s difficult to prescribe for humans”, explains Mr Hancock. Taking ivermectin with food (especially high-fat food) improves absorption and distribution is affected by body weight.1
Currently the only injectable form of ivermectin has been developed for use in large animals and contains excipients that are not approved for human use. The Mountain Valley MD product, IvectosolTM contains solubilised ivermectin. “We have a technique that is applied to the macrocyclic lactone drug class – one of which is ivermectin and another is selamectin – there are 12 or 13 of them in this class. So now we’ve taken ivermectin and made it 5000 times more soluble using two excipients that are already approved by the FDA as safe for human consumption. So it’s the only leading candidate in the world that’s safe for human injection”, says Mr Hancock. “It’s also the same solubilised form that we’ve used in a rapid-dissolve sublingual application – take something the size of a little piece of gum that dissolves under your tongue”, he adds.
Compared to existing oral forms, the sublingual presentation offers a number of advantages. “We’ve done preclinical trials – we’ve been able to use one fifth of the ivermectin, the API (active pharmaceutical ingredient) in this case, and achieve a sublingual [dosage form] – so again it does not go through digestive enzymes – it crosses directly across the [oral] mucosa and we’ve achieved a one-hour onset, with 5% variability”, explains Mr Hancock. The injectable form uses one eighth of the API and has a 15-minute onset of action.
He concludes, “So we have basically an oral form that uses less of the drug, dramatically more effect in a fraction of the time and then the same thing with the solubilised [injectable] format. You can now imagine emergency use authorisation, frontline – before you put someone on to a ventilator you can inject them with the precision the medical requirement would dictate.” This makes IvectosolTM a leading candidate as a treatment for covid.
Muñoz J et al. Safety and pharmacokinetic profile of fixed-dose ivermectin with an innovative 18mg tablet in healthy adult volunteers. PLoS Negl Trop Dis 2018; 12 e0006020. https://doi.org/10.1371/journal. pntd.0006020
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