Ghetto-rigging Iontophoreris Drug Delivery Systems

[nuke]

Ghetto-rigging Iontophoresis Drug Delivery Systems

Is it possible? The science behind it isn't terribly difficult to swallow. I'm mostly interested in the facilitation and titration of compounds, so that in a therapeutic environment, it would be easy to apply a small dosage of a compound, wait 5-10 minutes, see if the patient would like more and how much more, and then to increase the dosage progressively so that a compound that takes a very long time to reach peak levels in the brain like 2c-e can be effectively administered and working within 30-60 minutes. This would be a much less invasive means of administration in this fashion compared to say, progressive IV injections via the hands.

So, does anyone have any experience, or could direct me to somewhere that describes the preparation and execution of such systems?

 

[vecktor]

Is it possible? The science behind it isn't terribly difficult to swallow. I'm mostly interested in the facilitation and titration of compounds, so that in a therapeutic environment, it would be easy to apply a small dosage of a compound, wait 5-10 minutes, see if the patient would like more and how much more, and then to increase the dosage progressively so that a compound that takes a very long time to reach peak levels in the brain like 2c-e can be effectively administered and working within 30-60 minutes. This would be a much less invasive means of administration in this fashion compared to say, progressive IV injections via the hands.

So, does anyone have any experience, or could direct me to somewhere that describes the preparation and execution of such systems?

I am right in thinking it would still take the same time to reach the parts other (beers) chemicals don't reach, but is less invasive than IV?

 

[nuke]

Huh? I'm not sure how to respond to that. It's slower than IV, but should be faster or similar to the results you'd get from nasal or rectal administration, with higher bioavailabilities. There's currently a fentanyl patch (approved in the US last year) that works rapidly by this means of administration.

 

[haribo1]

There's currently a fentanyl patch (approved in the US last year) that works rapidly by this means of administration.

Aren't those SLOOWW release? It goes into the fat under the skin and then into the body? I mean, faster than the old patches, but still slow...

 

[vecktor]

I don't think that incremental dosing like this will work, because the drug will most likely end up in temporary depot somewhere in the body, where it will be released as and when, it will also take time to diffuse across the BBB. drugs that take a long time to reach peak usually do so because of distribution after absorbtion. so the theraputee will report satisfactory levels but the plasma and brain levels will continue to rise.

perhaps an intracranial catheter is the way to go?
its a bit more invasive, but it only needs to be fitted once as long as the port will fit under a hat it could be left in place

 

[nuke]

Aren't those SLOOWW release? It goes into the fat under the skin and then into the body? I mean, faster than the old patches, but still slow...

I don't think that incremental dosing like this will work, because the drug will most likely end up in temporary depot somewhere in the body, where it will be released as and when, it will also take time to diffuse across the BBB. drugs that take a long time to reach peak usually do so because of distribution after absorbtion. so the theraputee will report satisfactory levels but the plasma and brain levels will continue to rise.

Hmm, that sounds pretty problematic then.

perhaps an intracranial catheter is the way to go?
its a bit more invasive, but it only needs to be fitted once as long as the port will fit under a hat it could be left in place

Perhaps so, but it'd be a whole ton of work for anything beyond chronic therapy for perhaps a neurological problem (maybe a means to administer neuroprotectants in something like MS?).

Well, aside from that idea, DMT is a pretty ideal compound for possible use in iontophoretic delivery, since it exists as a solid in its freebase form... I like that one a lot, but I really hate smoking it.

 

[kidamnesiac]

The pharmacological availability will be very similar in time with oral, IF it follows similar profiles to macromolecules. However, the peak of availability is 25% + higher in most cases. I think you would be gaining little by this method vs. oral.
DMT is a neat idea, although I think the best way would be to move it quickly with DMSO or some other surfactant, as you may never reach high enough [] due to MAO being literally everywhere.
I like vecktors idea personally

Oh, forgot- skin is positively charged no? So, em, forget about getting an amine across there unless you are going to do it with iontophoretically a solution of pH >9 on your skin for a while. As far as I know, there are no commercial products for iontophoretic delivery, it is mostly still in the lab and for peptides (insulin)

I may be wrong about all of this

 

[nuke]

The pharmacological availability will be very similar in time with oral, IF it follows similar profiles to macromolecules. However, the peak of availability is 25% + higher in most cases. I think you would be gaining little by this method vs. oral.
DMT is a neat idea, although I think the best way would be to move it quickly with DMSO or some other surfactant, as you may never reach high enough [] due to MAO being literally everywhere.

Yeah, I'd been considering it with DMSO too for a little while but never got around to it.

Oh, forgot- skin is positively charged no? So, em, forget about getting an amine across there unless you are going to do it with iontophoretically a solution of pH >9 on your skin for a while. As far as I know, there are no commercial products for iontophoretic delivery, it is mostly still in the lab and for peptides (insulin)

Well, there is a study about a sympathomimetic amine called KM-13 that safely makes it to peak levels via iontophoresis in about 15-30 minutes in dogs. I thought that they'd work okay with a positive current, but, maybe not. And, I have absolutely no idea about where to obtain the supplies necessary for this, just musing mostly..

Oh, and thanks for putting up with my curiousities, everyone -- I'm not a biochemist or even a graduate student like a lot of people seem to be here.