SLU-PP-332 Solution Discussion

You using something like this? Should work for intranasal too, right?
I have made some sublingual cialis/viagra in the past with success with jello. Fun time.

Intranasal I don't know, I think cyclodextrins have a burning sensation in the mucus membranes, but I might be wrong, it's been years
 
I have zero direct experience with EO and only have limited experience with DMSO. Gotta get that out of the way first.

I ran some hypotheticals based on DMSO + MCT and EO + MCT with target concentration of 200 mg/ml of SLU-PP-332 and a goal of an intramuscular injectable which is tolerable to humans.

Projection for DMSO + MCT: 150-200 mg/ml concentration feasible at 5-10% DMSO.
Projection for EO + MCT: 200-300 mg/ml concentration easily achievable ay 30-40% EO with 250 mg/ml being realistic and stable.

Both of these should be doable with magnetic mixing alone, but limited low-heat exposure (37-40 C) shouldn't negatively affect the solution. The EO + MCT would be the better of the two choices.

I also checked for other cosolvents that might meet this use case and got benzyl benzoate and glycerol formal as options for higher concentration intramuscular injectables.

I'm curious as to your thoughts on these options.
I haven't had my raws tested, but if they are what they should be, then dissolving the 500mg in 5ml of DMSO was a snap. I think it's going to be key, and I'm fine with taking 5%, but I'm much less gung-ho about pushing the DMSO above that.

Then as I understand it, one either tolerates EO well, or doesn't -- it doesn't seem to bother me, at least not through 3 injections.

My concern about any other carrier oil is the viscosity. At standard temp, the viscosity of EO is 4 mPa·s, MCT is 25, and glycerin 1480.
I have made some sublingual cialis/viagra in the past with success with jello. Fun time.

Intranasal I don't know, I think cyclodextrins have a burning sensation in the mucus membranes, but I might be wrong, it's been years
I'll let you know
 
I have zero direct experience with EO and only have limited experience with DMSO. Gotta get that out of the way first.

I ran some hypotheticals based on DMSO + MCT and EO + MCT with target concentration of 200 mg/ml of SLU-PP-332 and a goal of an intramuscular injectable which is tolerable to humans.

Projection for DMSO + MCT: 150-200 mg/ml concentration feasible at 5-10% DMSO.
Projection for EO + MCT: 200-300 mg/ml concentration easily achievable ay 30-40% EO with 250 mg/ml being realistic and stable.

Both of these should be doable with magnetic mixing alone, but limited low-heat exposure (37-40 C) shouldn't negatively affect the solution. The EO + MCT would be the better of the two choices.

I also checked for other cosolvents that might meet this use case and got benzyl benzoate and glycerol formal as options for higher concentration intramuscular injectables.

I'm curious as to your thoughts on these options.
Did you find any solubility data on BB?
 
I have made some sublingual cialis/viagra in the past with success with jello. Fun time.

Intranasal I don't know, I think cyclodextrins have a burning sensation in the mucus membranes, but I might be wrong, it's been years
And I'd meant to post a link to this: https://www.amazon.com/dp/B00HRK49G2 (Amazon.com)

Is this similar to what you're looking to use?
 
Did you find any solubility data on BB?
Long day and I just got home, so I'm just gonna dump the info from ChatGPT.

Benzyl benzoate (BB) and ethyl oleate (EO) are both powerful solvents commonly used in injectable formulations, but they have slightly different properties that affect their solubility capabilities, injectability, and tolerability for a compound like SLU-PP-332. Here’s a comparison of how they differ, especially in terms of solubility:

1.​

  • Benzyl Benzoate (BB):
    • BB is a highly effective solvent for lipophilic (non-polar) compounds and has strong solubilizing properties due to its benzene ring structure, which interacts well with non-polar drug molecules.
    • BB’s strong solvent capabilities allow it to dissolve high concentrations of lipophilic drugs, potentially achieving concentrations of 200-300 mg/mL for SLU-PP-332, especially when used in moderate proportions (e.g., 10-20%) with a carrier oil like MCT.
    • However, BB may be slightly less effective than EO for extremely high concentrations of highly lipophilic drugs, as it is not as long-chain fatty acid-based, which sometimes limits solubility for very lipophilic compounds compared to EO.
  • Ethyl Oleate (EO):
    • EO is also an excellent solvent for lipophilic compounds and may even support slightly higher concentrations for extremely lipophilic drugs like SLU-PP-332 due to its ester linkage and long fatty acid chain, which mimic the natural structure of fatty acids and interact well with highly non-polar drugs.
    • EO’s solubility characteristics allow it to work as both a solvent and a co-solvent with oils like MCT, often achieving target concentrations around 200-300 mg/mL or higher without requiring additional solvents. Its lipid structure is particularly favorable for solubilizing hydrophobic compounds and may allow for a slightly higher concentration of SLU-PP-332 compared to BB.
Summary: Both BB and EO can likely achieve high concentrations of SLU-PP-332, but EO might offer slightly better solubility potential for extremely lipophilic drugs due to its fatty acid structure, which has more favorable interactions with highly non-polar compounds.

2.​

  • BB: Has a low viscosity and remains fluid enough to ensure smooth injectability, especially in lower concentrations. However, it is slightly more viscous than EO, which could make the solution a bit thicker when used at higher concentrations.
  • EO: EO has an even lower viscosity than BB, making it very easy to inject, even at higher concentrations. This lower viscosity reduces the likelihood of clogging and allows for easier administration, especially in formulations where high concentrations of the drug are required.
Summary: EO may have a slight advantage in terms of injectability due to its lower viscosity, allowing for smoother administration at high concentrations.

3.​

  • BB: Generally well-tolerated up to 20% concentration in intramuscular injections. However, BB can cause mild irritation in some patients if used in higher concentrations (>20%), especially in sensitive tissues.
  • EO: EO is very well-tolerated in IM formulations and has a lower risk of causing irritation, even at higher concentrations up to 40%. Its natural fatty acid ester structure is generally better accepted by tissues, reducing the risk of irritation compared to BB.
Summary: EO is typically more tolerable for IM injection, especially at higher concentrations, due to its biocompatible fatty acid structure, whereas BB may be more suitable at concentrations below 20% to avoid irritation.

Conclusion​

For SLU-PP-332, EO is generally more advantageous if the goal is to maximize solubility while maintaining injectability and minimizing tissue irritation, especially for formulations requiring high drug concentrations. BB is a strong alternative and could be used effectively at concentrations around 10-20%, but EO may provide slightly better solubility and tolerability at higher levels due to its natural compatibility with the body’s fatty acid metabolism and lower viscosity.
 
Have anyone found any solvent that can hold over 200mg/ml? For SubQ/IM.
I could be wrong, but I don't think that's happening, unless you want to inject 100% DMSO or BB. I've got 5mg/ml working in 5:95 DMSO EO. I'll try BB and may be able to double that, but I don't see being able to get that concentration in anything injectable.
 
I could be wrong, but I don't think that's happening, unless you want to inject 100% DMSO or BB. I've got 5mg/ml working in 5:95 DMSO EO. I'll try BB and may be able to double that, but I don't see being able to get that concentration in anything injectable.
That’s an extremely low dose, especially considering studies have gone as high as 500-1000 mg per day (after translating mice doses to human equivalents). I wonder if brewing it at 500 mg/mL in pure BB (since DMSO is toxic and shouldn’t be injected at all) and injecting 1-2 mL could really be that unhealthy. It’s still quite a lot of BB, though.
 
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