Is UTT really necassary with liposomes?

[lozgod]

I have been researching nanocarriers and liposomes and wondered if under the tounge (sublingual) is really necessary. Most medications (primarily cancer treatments) work by oral administration. Only found one thing regarding bioavailability orally and it was very high, 80%. Couldn't find anything regarding sublingual dosage.

 

[Zero V]

Interesting, will be good to know. I kinda figured the UTT is kinda half n half. I mean not 100% of it is going ot be sucked up into your body sublingually, there will be some that end up swallowed I would imagine. So I am guessing the combo of the sublingual to rapidly raise plasma levels and what goes down orally kinda keeps it going?

It would be good to know

 

[lozgod]

Interesting, will be good to know. I kinda figured the UTT is kinda half n half. I mean not 100% of it is going ot be sucked up into your body sublingually, there will be some that end up swallowed I would imagine. So I am guessing the combo of the sublingual to rapidly raise plasma levels and what goes down orally kinda keeps it going?

It would be good to know

The administration is what helps it reach plasma levels rapidly. The blood vessels under the tongue are fairly easily accessible so it goes directly in to the bloodstream. What keeps it going is the fact it is in the nanocarrier. It acts as a cell or a better analogy is an egg. The liposome is the shell and the hormone is the yolk. The liposome protects it from being degraded by the body so it reaches target tissues intact 100%. So I guess that kind of answers my question about the UTT. That provides the rapid plasma levels. It would still be achieved orally but would take slightly longer if I am understanding it correctly. Almost all of the hormone gets used as opposed to most of it being destroyed by the filters in the body.

Now I am wondering if taking an antacid before swallowing it would help even more get absorbed when taking orally.

 

[Zero V]

The administration is what helps it reach plasma levels rapidly. The blood vessels under the tongue are fairly easily accessible so it goes directly in to the bloodstream. What keeps it going is the fact it is in the nanocarrier. It acts as a cell or a better analogy is an egg. The liposome is the shell and the hormone is the yolk. The liposome protects it from being degraded by the body so it reaches target tissues intact 100%. So I guess that kind of answers my question about the UTT. That provides the rapid plasma levels. It would still be achieved orally but would take slightly longer if I am understanding it correctly. Almost all of the hormone gets used as opposed to most of it being destroyed by the filters in the body.

Now I am wondering if taking an antacid before swallowing it would help even more get absorbed when taking orally.

Pretty nice bit of info there. Thanks for the explanation. I am not sure if he acid in your stomach is the real enemy, isn't it the kidney/liver?

 

[lozgod]

Pretty nice bit of info there. Thanks for the explanation. I am not sure if he acid in your stomach is the real enemy, isn't it the kidney/liver?

Yeah it is the kidneys and liver but I am sure acid does cause some loss as well. That might be the reason for the 80% number. Might be able to increase it.

 

[quigs]

I have been researching nanocarriers and liposomes and wondered if under the tounge (sublingual) is really necessary. Most medications (primarily cancer treatments) work by oral administration. Only found one thing regarding bioavailability orally and it was very high, 80%. Couldn't find anything regarding sublingual dosage.

The point of sublingual or UTT delivery is to avoid 1st pass hepatic metabolism. This is a huge problem with many oral non-methylated hormones. The majority of the drug does not survive the first pass degradation by the liver and is inactivated before it can reach the target tissues. By sublingual administration, it is directed directly to the lymphatic/blood supply and will be able to reach target tissues unaltered and create the desired effect.

 

[quigs]

Yeah it is the kidneys and liver but I am sure acid does cause some loss as well. That might be the reason for the 80% number. Might be able to increase it.

No, the decreased bioavailability is due to hepatic degradation. You see, every time you eat something and the nutrients are absorbed by the GI it is transferred to the associated portal veins. These portal veins direct the new material (which includes drugs) directly to the liver prior to entering the normal circulation. Here the liver is able to "filter out" (for lack of a better term) toxins, drugs, vitamins, etc. This is good if you have harmful things, but bad if you're trying to get a drug into the normal circulation. Once the blood has been "filtered" through the liver it is allowed to enter the normal circulation.

Other types of drug administration, or "parenteral" administration (not oral) are meant to bypass this portal system. These include, but aren't limited to, intravenous, IM injection, Sub-q injection, transdermal, intranasal, and sublinqual administration.

 

[lozgod]

The point of sublingual or UTT delivery is to avoid 1st pass hepatic metabolism. This is a huge problem with many oral non-methylated hormones. The majority of the drug does not survive the first pass degradation by the liver and is inactivated before it can reach the target tissues. By sublingual administration, it is directed directly to the lymphatic/blood supply and will be able to reach target tissues unaltered and create the desired effect.

I am really new to all this but I thought the liposome protects it from the liver.

 

[quigs]

I am really new to all this but I thought the liposome protects it from the liver.

This is not really a concern with the UTT method as it avoids the first pass metabolism by the liver. The liposomes create a lipophillic carrier for the hormone.

 

[lozgod]

This is not really a concern with the UTT method as it avoids the first pass metabolism by the liver. The liposomes create a lipophillic carrier for the hormone.

Back to my original question though. With the liposome carrier is it necessary to do UTT. That is what I was asking. Or maybe a better question is does the liposome carrier protect the hormone from the liver.

 

[quigs]

Back to my original question though. With the liposome carrier is it necessary to do UTT. That is what I was asking. Or maybe a better question is does the liposome carrier protect the hormone from the liver.

In order to be effective at the dosage in the UTT products, yes it needs to be sublingual. If you want to take the products orally, the capsules are a much better option as they're dosed in order to account for decreased bioavailability through the GI.

The liposome will not sufficiently protect the compound from hepatic first pass degradation for the product to be taken orally like the capsules and still be effective.