FASTSORB SUB-BUCCAL TABLET DELIVERY SYSTEM IS SUPERIOR AND MORE EFFICACIOUS
THAN CONVENTIONAL ORAL DOSING!

Over the past 5 years, scientists at MuscleMeds have been developing an advanced alternative oral delivery system. Termed FastSorb sub-buccal tablet delivery system, this unique patent pending oral delivery approach offers distinct absorption and function advantages when used with compatible ingredients.  

Overview

Most supplement products are designed for traditional oral (peroral) route delivery, such as conventional tablets, capsules, liquid gel caps and other solid dosage forms. However, this peroral dosing can have disadvantages for certain compounds that are subject to a high level of degradation in the gastrointestinal tract and once absorbed into the bloodstream can be subjected to further degradation from first pass metabolism in the liver. Another factor that often reduces delivery of ingredients into the body is poor absorption from the intestines. This poor absorption of ingredients causes them to simply pass through the intestinal tract and they end up being excreted from the body. Collectively, these obstructive processes can greatly reduce the ultimate bioactivity of ingredients.

Theoretically, the active constituents of an ingredient or product starts out with 100% bioactive potential, meaning that if it was 100% absorbed into the bloodstream and was not subject to any degradation along the way to its destination within the body tissues, there could be 100% bioactivity. However, 100% bioactivity for all substances is rarely achievable through the peroral dosage delivery route of administration and for certain compounds, the actual effective bioactivity score can be reduced to only 10% or lower. So, 100 milligrams of actives in the tablet may only deliver 10 milligrams of usable ingredients into the body.    

With ingredients that are subject to high rates of degradation and/or low gastrointestinal absorption, transmucosal routes of delivery, such as sub-buccal/sublingual, can offer major advantages over peroral route delivery. For these sensitive compounds, the transmucosal route of delivery avoids gastrointestinal tract and first pass liver metabolism alteration and destruction of the bioactive substance(s). Destruction that can take place includes molecular cleavage, functional group alterations and even compounding with other molecules.

Molecular Alteration and Destruction

Molecular cleavage can involve the breaking apart of a molecule that primarily occurs from the action of destructive type of enzymes. Many of these destructive enzymes occupy the gastrointestinal system and liver and play a vital role to break down food for use in the body. However, these same enzymes also destroy certain bioactives used in products, rendering them ineffective. Functional group alteration involves modification of the active part(s) of a molecule’s structure that are responsible for its bioactivity in the body. During digestion or in the liver when the alteration of the bioactive’s function group occurs, this can deactivate the molecule, preventing it from performing its function. The other major way a bioactive molecule’s function in the body can be prevented occurs when one bioactive molecule interacts with another bioactive molecule to form an entirely new compound. As you can imagine, there are many other molecules and molecule fragments present in the gastrointestinal system and bloodstream. Based on the molecular architecture of a bioactive, it may react with these other substances to form a new compound that does not function as originally intended.    

As depicted in Figure 1, within the oral (buccal) cavity, the mucosal tissues lining the mouth are highly vascularized with a rich supply of blood. The buccal mucosal membrane is also selectively permeable and can uptake certain substances for delivery directly into the bloodstream. But while the transmucosal bioactive delivery route seems very attractive, there are characteristics that make using this route of administration challenging. These challenges include: 1) adhesion of the bioactives to the mucosal membrane 2) penetration of the bioactives through the mucosal membrane and 3) transport through the mucosal tissue layers to the bloodstream.

Clinical Validation Shows Transmucosal is Superior to Peroral Dosing for Certain Compounds

A good example of comparing peroral versus transmucosal delivery system routes is reported in research examining anabolic substances such as testosterone and androstendiol. When using the transmucosal delivery route substantially lower amounts of testosterone and androstendiol were needed to produce the same effects as much higher dosages of perorally administered dosage forms. Transmucosal delivery yielded results similar to injected dosage administration.

Dr. Wang and co-researchers 1 reported that sublingual administration of 5mg of testosterone led to marked increases in serum total and free testosterone within 30 minutes. Increases in strength, lean body mass and sexual function were reported from this study using sublingual testosterone during a 6 month period. To further demonstrate the effectiveness of sublingual delivery, in another research project, Dr. Brown and co-researchers 2 examined the effectiveness of sublingual androstenediol. These researchers pointed out that using conventional orally ingested androstenediol was determined to have very low absorption, very low bioavailability and very low effectiveness in raising blood serum levels of testosterone and androstenediol. In comparison, their research study found that when eight strength trained young men (average age 22.9 years) were administered just 20mg sublingual androstenediol, their serum levels of androstenediol and testosterone were increased within 30 to 60 minutes. The researchers noted that because 200mg of androstenediol taken orally does not change serum free or total testosterone levels in young men (as reported in another study), sublingual dosing is superior for the delivery of androstenediol to the peripheral tissues and conversion to testosterone; over 10 times more effective.     

In addition to being effective for improving the delivery and effectiveness of steroidal type molecules like testosterone, androstenediol and ingredients such as in Arimatest (androst 1,4,6 triene 3,17 dione, 6 bromo androst 1,4 diene 3, 17 dione alpha isomer, and 6 bromo androst 1,4 diene 3, 17 dione alpha isomer), sub-buccal delivery also offers advantages for other categories of molecules, such as large peptides. For example, when researching for substances that could dramatically boost the levels of IGF-1, it was determined that the hexapeptide (6 chain peptide) molecule used in Hexaghen, GHRP-2 Hexapeptide Acetate, was very effective via intravenous injection. However, the gastrointestinal system is only capable of absorbing free amino acids, di-peptides and tri-peptides, therefore peroral administration would be ineffective. But MuscleMeds researchers found a way to deliver GHRP-2 to the body using MuscleMeds sub-buccal tablet technology by bioengineering a liposomal based formula for delivering this hexapeptide directly into the bloodstream through the oral mucosal membrane.

The sublingual/sub-buccal delivery system approach is advantageous when matched with the right bioactive(s). As you will read in the following information, MuscleMeds’ FastSorb technology takes sub-buccal delivery to an entirely new level of effectiveness. FastSorb technology allows for far greater potency and effectiveness of many common ingredients over conventional peroral administration. Research demonstrates that even commonly used ingredients such as caffeine, synephrine, octopamine, certain amino acids, vitamin B-12 and co-enzyme Q10 are far more potent and effective via sub-buccal/sublingual delivery. And even more importantly, FastSorb Technology also opens up a new opportunity for the administration of new novel highly effective compounds such as long chain peptides, like those in Hexaghen, and novel steroidal aromatase inhibitors like those used in Arimatest and future MuscleMeds proprietary bioactives currently in research and development. 

FastSorb Sub-Buccal Tablet Technology

In the development of MuscleMeds products, like Arimatest and Hexaghen, it was apparent early on that there would be a low bioactivity score using conventional peroral administration. Therefore, MuscleMeds researchers chose to utilize their patent pending FastSorb sub-buccal tablet technology for achieving 100% absorption, bioavailability and effectiveness. During the MuscleMeds product development phase review process, every ingredient undergoes a function and form evaluation. During this evaluation, vital ingredient characteristics are scrutinized, such as:  

• Bio-molecular structure
• Modifications to bioactive molecule for enhancing absorption, bioavailability, and effectiveness
• Synergistic effects when combined with other ingredients
• Liposomal carrier optimization

The oral mucosa of the mouth is composed of distinct layers of cells. The outermost cell layer is called the epithelium, the next layer of cells is called the lamina propria and this is followed by the innermost layer called the submucosa. The target of the FastSorb delivery system is this submucosa layer of cells. This submucosal cell layer is highly vascularized and has a rich supply of blood. When designing the FastSorb tablet, MuscleMeds researchers ensured that the tablets would dissolve quickly, adhere to the buccal membrane and rapidly delivery the bioactives through the buccal membrane into the bloodstream. Refer to Figure 1 for details.

MuscleMeds Bio-Compatible Liposomal Technology

MuscleMeds scientists undertook an arduous bioengineering effort to ensure that customized liposomes are developed based on the specific bioactive to achieve liposomal optimization, which translates into greatly enhancing the delivery and effectiveness of the bioactives. FastSorb tablets are therefore custom designed to take advantage of all the transmucosal pathways for the most rapid and complete delivery and absorption into the bloodstream. They are designed for rapid tablet disintegration and dissolution of the bioactive in the mouth. Liposomes are stable in salvia, quickly saturate the buccal mucosa tissue lining and permeate into this highly vascularized tissue. In this way, the bioactives are delivered directly into the bloodstream, completely intact, with up to 100% delivery. This avoids the unwanted destruction that can take place passing through the GI and liver. The bioactives are also designed to have improved stability in the bloodstream to maintain bioactivity for longer periods of time, and greatly enhancing the effectiveness of the product formula. The painstaking Bio-Compatible Liposomal development process involves achieving three critical bioengineering design goals:

• Preparation of the bioactive molecule(s) for stabilization, optimum liposomal compatibility and maximum bio-effectiveness
• Development of the precisely bioengineered custom liposome
• Design of the FastSorb tablet matrix for liposomal optimization   

The first bioengineering design goal is to ensure that the bioactive ingredients are bioengineered for stability in the tablet and in the body. Bioengineered stability of the bioactives provides for maximum potency and prolonged bioactivity in the body. This includes choosing the ingredients with the optimal molecular structure or slightly modifying the molecular structure for maximum results. Once the molecular customization is finalized, the specific bioactive solution determination and preparation is undertaken to guarantee compatibility with the liposomalization process.   

The second bioengineering design goal is to employ the MuscleMeds proprietary technology required to create the most highly effective customized lipophilized micro-particulates (liposomes) housing the bioactives. For each product ingredient, the liposomes are custom designed to possess vital functioning once the FastSorb tablet is dissolved in the mouth. Liposomes primarily function to stabilize and preserve potency of the bioactives, promote bio-adherence to the mucosal membrane once dissolved in the mouth, facilitate immediate penetration and transmucosal uptake and ensure the fastest migration of bioactives to the highly vascularized submucosal tissue layer for delivery directly into the bloodstream.

The third bioengineering design goal is to design the FastSorb tablet matrix to dissolve quickly and disperse the liposomes over a maximal area of the mucosal membrane. Other design goals that are achieved include using mucosal absorption and permeation enhancers that are designed to facilitate the penetration and uptake process. The FastSorb liposomal and tablet matrix design therefore both stabilized the bioactives and allowed for rapid and high levels of absorption directly into the bloodstream primarily through buccal cavity absorption, as Figure 1 demonstrates.

Conclusion

In summary, MuscleMeds FastSorb Tablet Technology has provided a superior option for the administration of select and new novel compounds. This breakthrough technology has allowed MuscleMeds to develop extremely effective products capable of achieving results previously unobtainable through conventional peroral means. MuscleMeds commitment to sourcing and developing highly specialized ingredients, coupled with their FastSorb sub-buccal delivery, has set a new precedent of product efficacy.

 References:

 1 Wang, C., et al., Sublingual Testosterone Replacement Improves Muscle Mass and Strength, Decreases Bone Resorption, and Increases Bone Formation Markers in Hypogonadal Men – A Clinical Research Center Study., J Clin Endocrinol Metab 81:3654-3662, 1996.

2 Brown, G.A., et al., Acute hormonal response to sublingual androstenediol intake in young men., J Appl Physiol 92:142-146, 2002.