Curcumin - Topical/Inj - Homebrew Help

Grayson

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Looking around and it seems that we can benefit most from curcumin by applying it topically or injecting it subcutaneously (obviously this administration method would be painful due to the reports of post-injection-pain).

There are some pre-made topical preparations available, and simply looking at the ingredient label, it seems that we can homebrew our own preparations and since homebrew has pretty much died on these forums, I'd like to create a revival.

Perusing google, I found this: Lyme Disease: NeuroBiologix Curcumin 4 oz Topical Cream, TOPICAL CREAMS

Ingredients: Deionized water, medium chain triglycerides, shea butter, curcumin extract, cetyl alcohol, stearic acide, lecithin, sodium hydroxymethylglycinate, potassium sorbate, xanthum gum. 1

So what if we acquired some bulk curcumin powder, MCTs, shea butter, coconut oil and (maybe?) DMSO?

I've never homebrewed before and would like some assistance. Thanks
 
HIT4ME

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I've made some homebrews, and DMSO can be difficult to work with ....not preparing the formula, but in using the formula. If you put too much DMSO in, you WILL smell. Even small amounts make me smell and my gf complains.

Also, Curcumin stains everything yellow. I haven't tried mixing it directly in MCTs to see how it dissolves, maybe that would eliminate this, since it is fat soluble.

An easy homebrew is to get some hand sanitizer, some DMSO and a few other ingredients and mix your ingredients in. I've done this with 7-oxo and had decent results.

I have some curcumin and some MCT oil...maybe I'll give this a shot....
 
Grayson

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I've made some homebrews, and DMSO can be difficult to work with ....not preparing the formula, but in using the formula. If you put too much DMSO in, you WILL smell. Even small amounts make me smell and my gf complains.

Also, Curcumin stains everything yellow. I haven't tried mixing it directly in MCTs to see how it dissolves, maybe that would eliminate this, since it is fat soluble.

An easy homebrew is to get some hand sanitizer, some DMSO and a few other ingredients and mix your ingredients in. I've done this with 7-oxo and had decent results.

I have some curcumin and some MCT oil...maybe I'll give this a shot....
Literally :p

From what I've read inj preparations can also just be dissolved in grape seed oil. I might just get some curcumin and do this and see. Apparently it hurts like a bitch, but the effects are very pronounced.
 
fightbackhxc

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Interesting
 
Touey

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Looking around and it seems that we can benefit most from curcumin by applying it topically or injecting it subcutaneously (obviously this administration method would be painful due to the reports of post-injection-pain).

There are some pre-made topical preparations available, and simply looking at the ingredient label, it seems that we can homebrew our own preparations and since homebrew has pretty much died on these forums, I'd like to create a revival.

Perusing google, I found this: Lyme Disease: NeuroBiologix Curcumin 4 oz Topical Cream, TOPICAL CREAMS

Ingredients: Deionized water, medium chain triglycerides, shea butter, curcumin extract, cetyl alcohol, stearic acide, lecithin, sodium hydroxymethylglycinate, potassium sorbate, xanthum gum. 1

So what if we acquired some bulk curcumin powder, MCTs, shea butter, coconut oil and (maybe?) DMSO?

I've never homebrewed before and would like some assistance. Thanks
have you looked into Longvida?

"Longvida Optimized Curcumin, which in studies exhibits up to 65 times the bioavailability of free curcuminoids compared with generic curcumin. Longvida is absorbed by the GI tract and delivered to the rest of the body as free curcumin, the active form in the body."

I've been pleased with the results from it. Topical is intriguing & I've experimented with DMSO as a carrier oil for other compounds but it's a hassle
 
Grayson

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have you looked into Longvida?

"Longvida Optimized Curcumin, which in studies exhibits up to 65 times the bioavailability of free curcuminoids compared with generic curcumin. Longvida is absorbed by the GI tract and delivered to the rest of the body as free curcumin, the active form in the body."

I've been pleased with the results from it. Topical is intriguing & I've experimented with DMSO as a carrier oil for other compounds but it's a hassle
What has your testing shown?
 
Grayson

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Preparation and in vitro evaluation of novel poly(anhydride-ester)-based amphiphilic copolymer curcumin-loaded micelles.

http://www.ncbi.nlm.nih.gov/pubmed/24738340

Novel poly(anhydride-ester)-b-poly(ethylene glycol) copolymers (PAE-b-PEGs) were synthesized by esterization of methyl poly(ethylene glycol) and poly(anhydride-ester), which were obtained by the melt polycondensation of alpha,omega-acetic anhydride-terminated poly(L-lactic acid), and characterized by 1H-NMR and gel permeation chromatography. The two poly(anhydride-ester)-b-poly(ethylene glycols) (denoted as PAE-b-PEG2k and PAE-b-PEG5k) thus obtained can self-assemble in water to form micelles with hydrodynamic diameters of 92.5 and 97.5 nm above their critical micelle concentrations of 3.78 and 2.36 microg/mL, respectively. The curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles were prepared by the solid dispersion method, and they could encapsulate approximately 7% (w/w) curcumin. The diameters of the micelles were stable for 5 days. Curcumin is released faster from the micelles at pH 5.0 than at pH 7.4. Curcumin is released from the micelles at a fast rate during the initial 12 h, followed by a zero-order release during the subsequent 200 h, both at pH 5.0 and 7.4. The IC50 values of the curcumin-loaded PAE-b-PEG2k and PAE-b-PEG5k micelles against HeLa cells are 12.41 and 15.31 microg/mL, respectively, which is lower than that of free curcumin (25.90 microg/mL). The PAE-b-PEG2k micelles are taken up faster than the PAE-b-PEG5k micelles by HeLa cells. Curcumin-loaded micelles can induce G2/M phase cell cycle arrest and apoptosis of HeLa cells.

Found this while searching for Curcumin esters. Even though it isn't a fatty acid or cholesterol based, maybe there's something out there...
 
Grayson

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4-Hydroxy-3-methoxybenzoic acid methyl ester: a curcumin derivative targets Akt/NF kappa B cell survival signaling pathway: potential for prostate cancer management.

http://www.ncbi.nlm.nih.gov/pubmed/12869308

Transcription factor NFkappaB and the serine/threonine kinase Akt play critical roles in mammalian cell survival signaling and have been shown to be activated in various malignancies including prostate cancer (PCA). We have developed an analogue of curcumin called 4-hydroxy-3-methoxybenzoic acid methyl ester (HMBME) that targets the Akt/NFkappaB signaling pathway. Here, we demonstrate the ability of this novel compound to inhibit the proliferation of human and mouse PCA cells. HMBME-induced apoptosis in these cells was tested by using multiple biochemical approaches, in addition to morphologic analysis. Overexpression of constitutively active Akt reversed the HMBME-induced growth inhibition and apoptosis, illustrating the direct role of Akt signaling in HMBME-mediated growth inhibition and apoptosis. Further, investigation of the molecular events associated with its action in LNCaP cells shows that: 1) HMBME reduces the level of activated form of Akt (phosphorylated Akt); and 2) inhibits the Akt kinase activity. Further, the transcriptional activity of NFkappaB, the DNA-binding activity of NFkappaB, and levels of p65 were all significantly reduced following treatment with HMBME. Overexpression of constitutively active Akt, but not the kinase dead mutant of Akt, activated the basal NFkappaB transcriptional activity. HMBME treatment had no influence on this constitutively active Akt-augmented NFkappaB transcriptional activity. These data indicate that HMBME-mediated inhibition of Akt kinase activity may have a potential in suppressing/decreasing the activity of major survival/antiapoptotic pathways. The potential use of HMBME as an agent that targets survival mechanisms in PCA cells is discussed.

So now we have a metabolite that effects glucose metabolism, apoptosis, cell proliferation, transcription and cell migration. Yes, yes, please go on...
 
Grayson

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Caffeic acid phenethyl ester and curcumin: a novel class of heme oxygenase-1 inducers.

http://www.ncbi.nlm.nih.gov/pubmed/11854435

Heme oxygenase-1 (HO-1) is a redox-sensitive inducible protein that provides efficient cytoprotection against oxidative stress. Curcumin, a polyphenolic natural compound that possesses anti-tumor and anti-inflammatory properties, has been reported recently to induce potently HO-1 expression in vascular endothelial cells (Free Rad Biol Med 28:1303-1312, 2000). Here, we extend our previous findings by showing that caffeic acid phenethyl ester (CAPE), another plant-derived phenolic agent, markedly increases heme oxygenase activity and HO-1 protein in astrocytes. The effect seems to be related to the peculiar chemical structures of curcumin and CAPE, because analogous antioxidants containing only portions of these two molecules were totally ineffective. At a final concentration of 30 microM, both curcumin and CAPE maximally up-regulated heme oxygenase activity while promoting marked cytotoxicity at higher concentrations (50-100 microM). Similar results were obtained with Curcumin-95, a mixture of curcuminoids commonly used as a dietary supplement. Incubation of astrocytes with curcumin or CAPE at concentrations that promoted maximal heme oxygenase activity resulted in an early increase in reduced glutathione followed by a significant elevation in oxidized glutathione contents. A curcumin-mediated increase in heme oxygenase activity was not affected by the glutathione precursor and thiol donor N-acetyl-L-cysteine. These data suggest that regulation of HO-1 expression by polyphenolic compounds is evoked by a distinctive mechanism which is not necessarily linked to changes in glutathione but might depend on redox signals sustained by specific and targeted sulfydryl groups. This study identifies a novel class of natural substances that could be used for therapeutic purposes as potent inducers of HO-1 in the protection of tissues against inflammatory and neurodegenerative conditions.

So curcum + caffeic acid = extreme reduction in oxidative stress. Awesome.

We know this of curcumin already, but caffeic acid increases these effects.
 
Grayson

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From Google Patents...

http://www.google.com/patents/US20080076821

Applying curcumin ester prodrugs to the nasal cavity; nasal administration enhances the effectiveness of curcumin in the brain and reduce side effects associated with liver metabolism

ABSTRACT
Intranasally administering curcumin prodrugs and curcumin analog prodrugs to the brain to treat Alzheimer's Disease


Here's some goodies:

SUMMARY OF THE INVENTION
Despite the beneficial effects of curcumin, the present inventors have noted that there are many bioavailability problems associated with the oral delivery of curcumin.

First, because curcumin does not easily penetrate the human digestive tract and is subject to intestine-based metabolism and rejection, less than 1% of oral curcumin enters the plasma. Second, the small amount of curcumin that enters the bloodstream is rapidly metabolized by the liver and kidney. Therefore, although curcumin is highly lipophilic (and so easily crosses the blood brain barrier), only very small amounts of orally administered curcumin are registered in the serum and in the brain tissue. One study found that ingesting up to 3.6 g of curcumin per day produced a plasma curcumin level in the range of only about 10 nM. Sharma, Clin. Cancer Res., 2004, Oct. 15, 10(20) 6847-54. A second study found that ingesting up to 6-8 g of curcumin per day produced a peak serum level in the range of about 0.51-1.77 μM. Third, it has been reported that high oral doses of curcumin in the range of 4,000-8,000 mg/day cause problems such as headache, rash and diarrhea, likely produced by metabolites of curcumin. Accordingly, it appears that the above cited plasma curcumin concentrations (10 nM-1.77 μM) represent the practical upper limit of oral dosing of curcumin. Yang, supra, concludes that higher >(5 μM) concentrations of curcumin are not likely to occur in the brain with oral dosing. In fact, Wang reports that injection of 30 mg/kg of curcumin results in a peak curcumin concentration in brain tissue of only about 0.15 ng/mg, which is about 0.40 uM.


....


The objective of the present invention is to improve curcumin brain bioavailability by administering curcumin via the nasal route in order to deliver curcumin through the olfactory mucosa and to the brain, and to reduce the dose required for its beneficial effect. As curcumin is highly lipophilic, it will easily pass through the olfactory mucosa located high in the nasal cavity, and enter olfactory neurons and thereby the brain. This mode of delivery will also pass less curcumin into the circulation, and so will result in lower plasma concentrations of metabolites of curcumin, and therefore fewer side effects. Intranasal delivery will improve drug bioavailability to the brain by passive diffusion through the olfactory mucosa, thereby avoiding extensive hepatic first-pass metabolism which significantly lowers the plasma and brain concentrations of curcumin administered orally. Therefore, small doses of curcumin can be administered which will result in fewer side effects, and the drug will be more tolerable and more effective. Lipophilic drugs such as curcumin generally achieve higher brain levels after intranasal administration than after oral or intravenous administration. Therefore, the nasal route of administration of curcumin may help to enhance the effectiveness of curcumin in the brain (the site of action). Additionally, as curcumin is heavily metabolized by the liver, administration by the nasal route may help to reduce drug interactions with other drugs that are also extensively metabolized by the liver. Lastly, because intranasally administered curcumin will passively diffuse through the olfactory mucosa and into the olfactory bulb, which is connected to the hippocampus and amygdala through the limbic system, it is believed that intranasal administration of curcumin will preferentially deposit in the hippocampus and amygdala portions of the brain. These regions are believed to be origination sites of Alzheimer's Disease.
 

FireRescue

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I wonder if Curcumin would be a good candidate for liposomal delivery?
 
Grayson

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I wonder if Curcumin would be a good candidate for liposomal delivery?
Ask and you shall receive...

Efficacy of liposomal curcumin in a human pancreatic tumor xenograft model: inhibition of tumor growth and angiogenesis.

http://www.ncbi.nlm.nih.gov/pubmed/24023285

Abstract
BACKGROUND:
Liposome-based drug delivery has been successful in the past decade, with some formulations being Food and Drug Administration (FDA)-approved and others in clinical trials around the world. The major disadvantage associated with curcumin, a potent anticancer agent, is its poor aqueous solubility and hence low systemic bioavailability. However, curcumin can be encapsulated into liposomes to improve systemic bioavailability.
MATERIALS AND METHODS:
We determined the antitumor effects of a liposomal curcumin formulation against human MiaPaCa pancreatic cancer cells both in vitro and in xenograft studies. Histological sections were isolated from murine xenografts and immunohistochemistry was performed.
RESULTS:
The in vitro (IC50) liposomal curcumin proliferation-inhibiting concentration was 17.5 μM. In xenograft tumors in nude mice, liposomal curcumin at 20 mg/kg i.p. three-times a week for four weeks induced 42% suppression of tumor growth compared to untreated controls. A potent antiangiogenic effect characterized by a reduced number of blood vessels and reduced expression of vascular endothelial growth factor and annexin A2 proteins, as determined by immunohistochemistry was observed in treated tumors.
CONCLUSION:
These data clearly establish the efficacy of liposomal curcumin in reducing human pancreatic cancer growth in the examined model. The therapeutic curcumin-based effects, with no limiting side-effects, suggest that liposomal curcumin may be beneficial in patients with pancreatic cancer.
 
Grayson

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The basic trend we're seeing is:
1) metabolites do X -> have affect on Y
2) bound to A -> increases concentration
3) special delivery -> delivers to specific area

So my thinking is... if injected either subcutaneously or intramuscularly we'll have a systemic affect in which Curcumin will not be broken down by the liver, or obliterated by stomach acids.
 
Grayson

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Interesting.
I think I'm just going to buy raw curcumin (not turmeric), mix it with grapeseed oil and inject it.

If this works well, once I'm done with TNT, I'm going to make an injectable homebrew log of compounds with awful bioavailability (I.e. curcumin, resveratrol)
 
fightbackhxc

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I think I'm just going to buy raw curcumin (not turmeric), mix it with grapeseed oil and inject it.

If this works well, once I'm done with TNT, I'm going to make an injectable homebrew log of compounds with awful bioavailability (I.e. curcumin, resveratrol)
Braver than I am
 

kissdadookie

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Topical sounds like a dumb idea tbh. Who wants to walk around looking like a Oompah Loompah?
 
koi1214

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I think I'm just going to buy raw curcumin (not turmeric), mix it with grapeseed oil and inject it.

If this works well, once I'm done with TNT, I'm going to make an injectable homebrew log of compounds with awful bioavailability (I.e. curcumin, resveratrol)
Good luck.I think it's going to give you a bad burning sensation.

Braver than I am
Agreed
 
Grayson

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Good luck.I think it's going to give you a bad burning sensation.



Agreed
Oh it most definitely will. The PIP is just as bad as some long esters. According to some users on PM that is....

But they're batchit wannabe Frankensteins.
 
brundel

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I think I'm just going to buy raw curcumin (not turmeric), mix it with grapeseed oil and inject it.

If this works well, once I'm done with TNT, I'm going to make an injectable homebrew log of compounds with awful bioavailability (I.e. curcumin, resveratrol)
Im just going to assume you know you cant just mix it and inject.
Unless you want a limb amputated.
This isnt the proper place to talk about home brewing injectables so Im not going to give you any advice here. If you want you can PM me and Ill tell you how to do it properly.
 

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I just ordered the link above, lymehub, got a conformation pretty quick. Ill update when I get the product
 

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One thing to keep in mind too if no one has mentioned it, this stuff is extremely staining so be sure to use gloves and cheap clothes when preparing it. It is a fantastic ingredient but man is it hard to work with if you get it on your fingers. People will think you are jaundiced for a week :).
 
brundel

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Yah its not really good for a transdermal.
I think a better option is research how its metabolized or what breaks it down then work to inhibit this process orally.
 

Team Six

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Yah its not really good for a transdermal.
I think a better option is research how its metabolized or what breaks it down then work to inhibit this process orally.
It is conjugation which unfortunately is very hard to overcome. Glucoronidation is a high capacity, low affinity process but sulfation takes the place of that as a high affinity low capacity metabolic process and it is susceptible to both. Really the only other option would be to load it up with other substrates in an effort to overload it but its not extremely effective. Still seems to work rather well regardless in the right dosages.
 
brundel

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It does seem to work well anyways. Great overall supplement.
 

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