The administration of most peptides orally is impossible because of bioavailability – the accessibility of a compound to its target biological destination. Sermorelin bioavailability, for example, is determined by the percentage of the drug that reaches the growth hormone-releasing hormone (GHRH) receptor.

In this context, bioavailability measures how much a peptide reaches its target when ingested orally.

Several factors such as resilience, size and structure, and first-pass effect can affect the bioavailability of a substance.

  • Resilience: One of the many factors affecting oral peptide bioavailability is the resilient ability of a peptide to the GI tract environment. The pH range in the GI tract ranges from 1.7 in the stomach to about 8 in the large intestine. The pH value of blood is 7.4 as a standard. Most peptides may not survive their transportation via the GI tract; therefore, their transport is through blood. Due to this, absorption may not be possible as the peptides may disintegrate before absorption occurs.
    Some peptides can be transported via the Gi tract and impact the stomach, the small intestine, and the large intestines and still be affected by absorption from the blood. However, these peptides will need to be resilient enough to withstand the high pH levels of the GI tract otherwise absorption would not occur. 
  • Size and Structure: Absorption is one of the many factors affecting oral peptide bioavailability, and the absorption rate depends on its size and structure. Peptides that are too large may not pass through the GI tract without being absorbed into the bloodstream. Another factor affecting absorption rate is the electrostatic charges incompatible with the transport apparatus—structures that make transporter binding impossible and competition from other compounds. Thus, some drugs should be ingested with food, while others should be ingested on an empty stomach.
  • First-Pass Effect: Drug clearance may affect a peptide upon entrance into the bloodstream. The GI tract blood supply passes through the liver before entering circulation. During passage through the liver, the organ removes free radicals, potential pathogens, and toxins before distribution to the various parts of the body. Therefore, if a peptide is subject to damage or removal by the liver, it will be cleared from the system and cannot be taken orally.

The Best Oral Peptides

Patients can take the following peptides orally; BPC-157, Tributyrin, PEA (Palmitoylethanolamide), KPV, etc.

BPC-157

BPC-157 is a naturally derived peptide for body protection. The peptide encompasses rapid wound healing features and reduces inflammation in the GI tract and throughout the numerous body tissues.

  • BPC-157 is one of the best oral peptides because it is resistant to the pH of the GI tract, allowing the peptide to impact the GI conditions like inflammatory bowel disease and ulcers. However, BPC-157 absorption in the GI tract is incomplete, so intramuscular administration is vital for it to be functional in wound healing or non-GI tract settings.
  • According to scientific research on animals, the oral administration of BPC-157 induces healing in numerous gastrointestinal conditions. On the other hand, injecting BPC-157 affects tendon and ligament injuries while topical administration affects dermal wounds.
  • Modern biochemistry has developed two different forms of BPC-157 — BPC-157 acetate and BPC-157 arginate. BPC-157 acetate is the first form of the peptide with a relatively long half-life in powder form, 98% of which disintegrates in the gastric acid after a couple of hours. BPC-157 arginate has a longer half-life than BPC-157 acetate, 90% of which is bioavailable in the gastric acid after 5 hours

Tributyrin

  • Tributyrin is a fatty acid naturally present in butter. After absorption, it converts to butyric acid in the bloodstream. Butyric acid reduces the growth and metastasis of cancer cells in the human colon. Tributyrin is stable and subject to rapid GI tract absorption, while butyric acid is not.

KPV

  • KPV consists of a three-length amino acid developed from the alpha-melanocyte stimulating hormone. The peptide has significant anti-inflammatory abilities. The peptide’s administration can be intravenously, orally, or transdermally. KPV can be ingested orally by passive and active transport while retaining certain features of the alpha-melanocyte stimulating hormone.

PEA (Palmitoylethanolamide)

  • PEA is a fatty acid that can protect the Central Nervous System (CNS) and reduce pain perception and inflammation. PEA absorption occurs through the GI tract and is resistant to disintegration. PEA impacts the endocannabinoid system and can minimize 𝛃-amyloid-induced neuroinflammation following Alzheimer’s disease.

Other Oral Peptides

There are numerous oral peptides, most of which are:

  • Tesofensine
  • NMN (Nicotinamide Mononucleotide)
  • MK-677 (Ibutamoren)
  • Larazotide
  • 5-Amino-1 MQ
  • Ac-SDKP

Each has specific functions in test subjects and can survive the harsh GI tract environment without degrading.

Conclusion

A compound can still function effectively in the body, whether taken orally or not. It is dependent on the factors affecting absorption and bioavailability. An in-depth understanding of compounds’ biochemical processes, ranging from action to absorption characteristics, etc., is required to produce oral peptides.

Disclaimer: The products mentioned are not for human or animal consumption. All the information shared in this article is for educational purposes only.

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