Sunday, 15 April 2018

Thymoquinone (Nigella sativa) inhalation

Nigella sativa is a widely used medicinal plant throughout the world. Most of the therapeutic properties of this plant are due to the presence of thymoquinone which is major bioactive component of the essential oil.
There is more information about the possible intranasal use of thymoquinone for the treatment of glioblastoma.

Therapeutic Potential of Thymoquinone in Glioblastoma Treatment: Targeting Major Gliomagenesis Signaling Pathways
2018 https://www.hindawi.com/journals/bmri/2018/4010629/
"Due to its multitargeting nature, TQ interferes in a wide range of tumorigenic processes and counteract carcinogenesis, malignant growth, invasion, migration, and angiogenesis.
Its potential to enter brain via nasal pathway due to volatile nature of TQ adds another advantage in overcoming blood-brain barrier."
"Interestingly, even the lower efficacy and poor bioavailability of TQ are the primary bottleneck of TQ, its volatile nature provides opportunity to be exploited for use in novel drug delivery strategy via intranasal pathway to brain due to unique connection provided by the olfactory and/or trigeminal nerve system present between the olfactory epithelium and the central nervous system. Such delivery system provides opportunity to bypass both the BBB and hepatic first-pass metabolism."

2012 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3497894/
"The studies suggest intranasal delivery of TQ to be a promising approach for brain targeting as well as in reducing the systemic exposure."

2016 https://www.ncbi.nlm.nih.gov/pubmed/26976069
"Present work aims to prepare nanoemulsions (Thymoquinone Mucoadhesive Nanoemulsion) in order enhance the bioavailability of drug and hence evaluate the drug targeting in brain via non-invasive nasal route administration."

The question is, how can we now do inhalations with Thymoquinone to benefit from it? In what form can we use Nigella sativa / Thymoquinone for inhalations?
- Thymoquinone, ≥98,5% (GC):
https://www.sigmaaldrich.com/catalog/product/sial/03416
- Essential oil from Nigella sativa:
https://www.amazon.com/Black-Cumin-Essential-Nigella-sativa/dp/B01G8ZTX12
- Or without inhalation, just like a drop for a nose:
https://www.etsy.com/listing/565401697/black-seed-nose-drops-nigella

 


And additionally about the effect of oral Nigella sativa oil on metabolism:
https://www.ncbi.nlm.nih.gov/pubmed/19902033
"A RCT done on 60 patients with metabolic syndrome showed that NS oil (5 mL/day) used in combination with atorvastatin and metformin could decrease fasting blood sugar (FBS), LDL, and TC significantly after six weeks of use."

6 comments:

  1. The fact that no responses were observed after doses of 75 - 2600 mg of pure thymoquinone is not exactly encouraging, though these advanced cancer patient would be expected to be more resistant to all treatments compared to newly diagnosed patients.

    Phase I safety and clinical activity study of thymoquinone in patients with advanced refractory malignant disease
    emedicalj.portal.tools/28126.pdf

    The intranasal delivery might increase uptake into the central nervous system, but there's little evidence to show that this would actually be therapeutic for brain tumors. You'd essentially be performing a phase 1 trial with an n of 1.

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    1. Also keep in mind that if black seed oil contains a thymoquinone percentage around 1.2%, you would need to take 83 grams of black seed oil just to get a gram of thymoquinone. The percentage probably varies though.

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    2. https://www.caymanchem.com/product/15039

      Quite a bit more cost effective, but I think the above points still apply. Large uncertainties as to both safety and efficacy.

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    3. Not that I'm encouraging this use of thymoquinone, but see the curious price difference between these two products from Sigma:

      https://www.sigmaaldrich.com/catalog/product/sial/03416?lang=en&region=US

      https://www.sigmaaldrich.com/catalog/product/aldrich/274666?lang=en&region=US

      The molecules are identical, with the same CAS number. The only difference that I can see is that the first is "analytical standard" while the second is guaranteed at least 98% pure. I'd guess the analytical standard is the purest form you could get.

      Using the analytical standard form would run you $500 per day for a one gram dose, or $15,000 per month, about the same monthly cost as nivolumab or pembrolizumab, not to mention that chemical suppliers would probably not be able to keep up with that kind of demand, and you'd quickly raise suspicions that it wasn't being used for normal laboratory purposes.

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    4. The primary concern should be safety though. You don't want to end up doing more harm than good.

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  2. Stephen, I just spent time and studied this question a little. Since there are no studies on humans, the only thing left is to think about adding essential oil to a solution for inhalation with perillic alcohol (or without). Everything else is not really tested and can be inefficient or dangerous (

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