| Lipotropin Supplement Science.
(Fred Hatfield, Ph. D. interviews Sam Bernal, M.D.) Dr. Hatfield:
...I have seen the clinical data on a scientific study known as the Lipotropin Project and you were the major research force involved. I understand the delivery base is liposomes. What directed you to the study of liposomes for this innovative research and formula? Dr. Bernal:
...We have been doing research on liposomes for more than 10 years, mostly on liposomes as they relate to the delivery of anti-cancer drugs. We have found an advantage in terms of lower toxicity and greater absorption of these drugs with liposomes. We saw the same enhanced delivery when we used nutritional supplements including growth hormone, so we then applied the same type of pharmaceutical technology to the nutritional supplement area. Dr. Hatfield:
...But why the interest in nutritional supplements? Dr. Bernal:
...From a commercial point of view, it was fairly recent because when we were still in Boston, our group of scientists had formed a collaboration between several faculty members from Harvard and MIT. And one of the things we were guided by was that a lot of our research remained in the laboratory. Very often we were directed to research that really took 10 to 15 years sometimes to really come to clinical application. Going through the FDA process is a lengthy process. So even though most of us continued to do the FDA process, we felt that many of the research findings we had in the laboratory could be applied to commercial products more quickly if we went into the nutritional area.
...Many of my colleagues who are also working with us in the research and in the commercial development, had backgrounds that were often in nutritional biochemistry, in protein biochemistry, in drug delivery, in pharmaco-kinetics. So it was a natural progression for us to apply these technologies to the nutritional scene. We have people in our group with Ph.D.'s in nutritional biochemistry. Dr. Hatfield:
...I am familiar with liposomal delivery, but please explain more to Planet Muscle readers. Dr. Bernal:
...The key to successful ingestion and use of very large molecular substances like human growth hormone is stability. Liposomes provide an advantage in keeping the structure of a molecule in its native form. There is a tendency for large molecules, in particular, to become de-natured by the gut and hepatic system. They are left without any protection. They must be made to stay stable. Another principal is cellular interaction. We know from studies done on other ingredients that the presence of the liposome increases the interaction with the target cell. Stability and biological activity are critical. Dr. Hatfield:
...So the liposomes are crucial in keeping the three dimensional structure of the HgH molecule in solution? Dr. Bernal:
...Yes. Human growth hormone, just like other polypeptide hormones, is linear in structure, a linear three dimensional chain. In order for it to act biologically, it has to maintain its three-dimensional structure. This allows the molecule to interact with the cell receptor and to be able to perform its biological action on the cell. Keeping the three-dimensional structure of the molecule in solution by itself is very difficult. However, the more concentrated you keep it, the more likely it is to keep its native three-dimensional structure and do its work. Liposome is able to trap molecules inside a fat carrier. Once inside the carrier, it is kept in a concentrated form and 3-dimensional structure, instead of jettisoning into solution. Dr. Hatfield:
...Assuming this Lipotropin formula has efficacy, is it safer than injecting pharmaceutical, recombinant growth hormone? Dr. Bernal:
...Well, it certainly is less likely to cause local problems at the site of injection and is much more convenient and less expensive by some hundred-fold. You don't have to worry about sterile technique and are less likely to overdose. Because you are able to administer it several times during the day, it is easier to achieve a stable level. As you know with many injections, you get a big infusion of dose and a spike all of a sudden, but the rest of the time, there is not much remaining to affect an outcome. Dr. Hatfield:
...Clinically, why did you use kidney cells to measure an effect? Dr. Bernal:
...Kidney cells are important targets for the action of growth hormones. In fact, the three major targets of a growth hormone are liver, muscle, and kidney. Kidney cells are important for another reason. It's that for many of our drug studies particularly involving anti-cancer drugs or in nutritional supplements, one of the things that we watch for is toxicity to the kidney. So when we culture-study kidney cells, we accomplish two things. We assay the biological effect of a hormone and observe whether or not there is any toxicity that might be directed to other organs. Dr. Hatfield:
...In one portion of your research, you showed the total cellular protein output of the kidney cells treated with Lipotropin and GH, was greater than the kidney cells treated with growth hormone alone. Can you comment? Dr. Bernal:
...In solution, the growth hormone alone showed some binding to the target cells, in this case, the kidney cells. But the presence of the liposome allowed much higher amounts of the growth hormone to bind to the kidney cells. We felt the enhanced binding due to stability was responsible for the increase in the total cellular protein output increase. In order for the target cells to respond by increasing their protein synthesis, they have to be proportional to the amount of hormone that is bound to the cell receptor.
... So the action of the liposome was to increase the amount of growth hormone bound to the target cells and, because there was an increased level of the hormone bound, there was also a higher biological action resulting in increased protein synthesis by the cells. Dr. Hatfield:
... I understand microscopic examination reveals that the kidney cell membrane and liposome fuse. Does this have significance? Dr. Bernal:
...After the administration of the liposomal growth hormone [Lipotropin], the liposomes bind to the surface membrane of the target cell. By monitoring the amount of the growth hormone that is actually bound to the surface, plus the amount of growth hormone that is present inside the cells, we find that, after the liposome binds to the cell membrane, there is fusion. The membrane of the liposome, being similar to the normal human cell membrane, starts to fuse with it — they become one. The next step is when the liposome combines with the cell membrane of the cell, practically all of the contacts within the liposome are delivered inside the cell. We can see the shift in the presence of the growth hormone from outside the cell, to the membrane of the cell, finally to inside the cell - into the cytoplasm and eventually to the nucleus. When we tried to do this with a growth hormone alone without the presence of the liposome, there was much less binding to the cell membrane and much less growth hormone that winds up inside the cell, cytoplasm and nucleus. The liposome radically increases the amount of GH ultimately delivered to the nucleus. Dr. Hatfield:
...Once fusion occurs, the growth hormone that is trapped within the liposome is able to remain inside the cell and presumably affect function — growth? Dr. Bernal:
...We believe this is correct. Dr. Hatfield:
...And the same thing that happens with the kidney cells also happens with muscle and liver. Dr. Bernal:
...Yes. Dr. Hatfield:
...Did you expect to see such a high protein output from the cells treated with Lipotropin? Dr. Bernal:
...No. This was a pleasant surprise. Normally when we try to increase the activity of a drug, we see increases in activity by 30 to 50 percent. In this case, we clearly observed 200 to 300 percent. Protein synthesis increased radically as a result of the liposome plus the growth hormone as compared to growth hormone in solution by itself. Dr. Hatfield:
...Unreal. Is it unique that the liposomes aid in the delivery of the growth hormone molecule to the nucleus of the cell? Dr. Bernal:
...Yes, we are using varying size pharmaceutical liposomes, similar to what we use in cancer treatment. In this case the liposomes are designed to react. And they will react as soon as they come into contact with a target cell. The pharmaceutical liposomes are more dynamic. Dr. Hatfield:
...Have you formed any preliminary conclusion that Lipotropin will raise growth hormone levels from the research that you have performed? Dr. Bernal:
...Yes. The cell culture models that we used in the laboratory for the growth hormone research was the same cell culture system that we would use in pharmaceutical drug development. The advantage of this model system is that we can make correlations about what we find in the laboratory with what we ultimately find in the clinic. The result we have from the model system in the laboratory is extremely favorable. Dr. Hatfield:
...Well let's speculate. Will this increased circulating growth hormone effect IGF-1 and add muscle with training? Dr. Bernal:
... Yes. In fact, compared to the administration of only growth hormone (in solution) by itself, definitely. We would predict that if you only administered the growth hormone or even a growth-hormone-releasing factor by itself in solution [without a liposome carrier] it is not likely to be able to have enough of a biological effect. This biological effect, by the administration of these supplements through a buccal route, we would predict, would be highly accelerated by the use of liposomes. Of course, injected human growth hormone is effective, as it avoids being in a solution. Dr. Hatfield:
... In the world of elite, competitive bodybuilding, you are aware that many of these guys are now using IGF-1 injections along with insulin, HgH and cortisol-blocking agents? Dr. Bernal:
... They are directly injecting all these substances? Dr. Hatfield:
... Yes, indeed. And when it began, I'd say about 10 years ago, the body-builders of today are probably 10-20 percent bigger and harder than any body-builders in the history of the sport. I firmly believe this to be due to escalating steroid doses, but also IGF-1 together with several other drugs (like huge amounts of HgH) and even insulin. Dr. Bernal:
... Wow. Dr. Hatfield:
... So my question is when you say that growth hormone in solution alone [without a liposome carrier] is not likely to have - or even growth hormone releasing factor — is it not likely to have an effect on IGF-1? Dr. Bernal:
... Not likely. Dr. Hatfield:
... But [with] the liposome, ingested in-solution growth hormone does have an effect on IGF1 output? Dr. Bernal:
... That is correct. But I’m fascinated. I didn't realize that people were injecting IGF-1. Dr. Hatfield:
... Yes, in a big way. It's been going on for nearly 10 years. Dr. Bernal:
... Really? I must assume the manufacturers of IGF-1 pretend that they don't know how this is being used? Dr. Hatfield:
... I don't know. My last question — the dose of 2,000 nanograms that you recommend - is that sufficient enough to generate some of your speculated cellular responses? Dr. Bernal:
... Each serving of Lipotropin has this amount, however we observed a biological effect at 200 [nanograms] using our immunoperoxidite acid. This was used to quantitate the number of molecules that bound to the cell membrane and how much of it got into the cell. Again, even using 200 nanograms of Lipotropin in the liposomal format allowed us to see delivery into the membrane, the cytoplasm and the nucleus. Dr. Hatfield:
... In conclusion, getting 2,000 nanograms delivered on a daily basis into the target cells is easily sufficient to cause an increase in muscle mass and all the other growth hormone related responses. Dr. Bernal:
... Based on our extensive laboratory research, this what we predict:
... To test our thesis, we are currently planning clinical trials. Mind you, there are other like-products on the market that contain similar amounts of growth hormone but the big caveat is that these do not have this unique liposome delivery and the liposome we believe critical. If you were to just use 2,000 or even 10,000 nanograms under the tongue it is unlikely to be able to deliver something. But in the buccal format, in the presence of the liposomes, we also detect actual mucosal cells in culture. And the presence of the liposomes accelerates the penetration even to the mucosal cells. So, starting from the mucosal cells, once it gets into the bloodstream — especially with the presence of the small liposomes, along with the large — it is much more likely to be able to have a biological effect.To test our thesis, we are currently planning clinical trials. Mind you, there are other like-products on the market that contain similar amounts of growth hormone but the big caveat is that these do not have this unique liposome delivery and the liposome we believe critical. If you were to just use 2,000 or even 10,000 nanograms under the tongue it is unlikely to be able to deliver something. But in the buccal format, in the presence of the liposomes, we also detect actual mucosal cells in culture. And the presence of the liposomes accelerates the penetration even to the mucosal cells. So, starting from the mucosal cells, once it gets into the bloodstream — especially with the presence of the small liposomes, along with the large — it is much more likely to be able to have a biological effect.
... With daily lipotropin use for a couple of weeks, you would see an effect.
... But the peak — the peak level — if one were going to measure the amount of IGF-1 — you see, we cannot really measure the growth hormone after administration, because it's protein bound. It's not likely to be able to be detected. But the way to measure the effect is really to measure IGF, of course.
... But if you were going to inject it, what you would see is a very high peak within minutes.
... You are aware that growth hormones, like other polypeptide hormones, do not go up and down like an injection does, but instead they usually are released a little bit at a time throughout the day.
... So we think that the buccal — mucosal administration, particularly with the liposomal format, recreates what the body needs. Dr. Hatfield:
... On behalf of Planet Muscle thank you for making this promising research and product available to our industry. Note: From Jeff Everson ... Human growth hormone has typically been most effective in target populations over 40 (and repressed pituitary function from illness or drugs or other, at any age), via injection, the efficacious way to mimic all the physiologic and biologic functions attributable to growth hormone. However, to this point no efficacy had been demonstrable by oral or nasal injection by so called GH-secratogogues.
... The reasons have been two-fold: one, due to the size of the molecules and two, the instability in solution in the gut whereby the GH is degraded before having any effect. Perhaps with Dr. Bernal's research, all of this may now change!
... Planet Muscle has been quite fortunate to obtain a very limited supply of Lipotropin and it is our opinion that before George Dubyah Bush can get his tax bill passed the FDA may swoop in and make Lipo a prescription entity. But, right now it's not, but nonetheless, it's still limited so we suggest you not lollygag and get it while you can.
... The manufacturer suggests that the correct best way to use Lipo is a 2-dose spray in the morning and a 4-dose spray at night. This delivers 2,000-nanograms of the patented Lipotropin-complex along with 1,000-nanograms of human growth hormone stimulating polypeptide complex.
... Dr. Squat, Dr. Sam Bernal and the patent inventor, Kurt Cahill, excitedly feel that Lipo may blow the doors off bodybuilding supplementation. We shall see. | 
Name: Lipotropin by Pure Life Science (30ml)