Bioavailable Peptides: How Oral Peptide Delivery Works

Overview

This article explores how advances in peptide engineering and formulation have enabled effective oral delivery, countering the belief that subcutaneous injections are the only viable route. It outlines key advantages of oral administration—convenience, potential for improved bioavailability, fewer injection-related side effects, and better adherence—and highlights two examples: Thymosin Beta4 Fragment (SDKP), a shortened derivative with markedly higher oral bioavailability in animals, and BPC157 in arginate salt form, which shows substantially greater oral absorption than the acetate form in rats. While much evidence is preclinical, these results show how sequence modification and salt selection can enhance stability and absorption, expanding therapeutic possibilities for peptides.

Peptide Bioavailability

Peptides, which are short amino acid chains, are being heavily studied for their possible health benefits. Although they are often linked with subcutaneous (SubQ) injections, recent progress in modifying peptides has improved their ability to be absorbed when taken by mouth, resulting in more bioavailable peptides. This has led to the creation of peptides that can be effectively taken orally and more stable oral peptide formulations. Nowadays, many peptides are available in pill or capsule form, which makes them easier and more convenient to use in various research and clinical trials. For many participants, having an oral peptide option simplifies participation.

For instance, Thymosin Beta4, also known as TB500, is a peptide known for its therapeutic benefits, like aiding in wound healing and reducing inflammation. Initially, TB500 needed to be injected under the skin to be effective. However, there’s a newer version called Thymosin Beta4 Fragment SDKP, which has been altered to be more easily absorbed when taken by mouth, retaining its therapeutic properties.

Another example is BPC157, a peptide known for aiding in healing and decreasing inflammation. Initially, BPC157 was delivered through subcutaneous injections. However, a new version of BPC157, using Arginate salt instead of the traditional Acetate salt, has shown improved oral bioavailability, simplifying administration.

In this blog post, we’re going to look into the advantages of taking peptides orally and the changes that have made this method viable. We’ll also address some misunderstandings about peptide administration, like the idea that injecting under the skin is the only effective method. People often ask, do oral peptides work, and which ones are the best oral peptides in current studies? By the end of this, you should have a clearer view of the possible benefits of oral peptide use and the options you have.

Oral Peptide Administration Advantages:

1. Convenience: A key advantage of taking peptides orally is ease of use. Unlike subcutaneous methods that need a healthcare professional or someone with training to administer, oral peptides can be taken by the research participants themselves. This process doesn’t require special skills or tools, making it more accessible and practical for those uneasy about procedures or who have trouble getting to healthcare centers.
2. Improved bioavailability: One more advantage of delivering peptides orally is enhanced bioavailability. By making specific changes like breaking down longer sequences or using various salts, peptides can be absorbed more efficiently by the body when taken by mouth as an oral peptide. This can lead to needing a smaller dose to reach the therapeutic goal, aiding scientists in creating peptides with better bioavailability.
3. Reduced Side Effects: Taking peptides orally could result in fewer side effects than injecting them under the skin. Injections require breaking the skin and delivering peptides directly into the bloodstream, which can lead to pain, swelling, or infection. Oral consumption of peptides bypasses these problems, possibly offering a safer option for some people.
4. Enhanced patient adherence: Taking peptides orally could lead to better adherence to treatments. Since they are easy to take at home and do not necessitate frequent visits to a healthcare facility, patients might be more likely to follow their treatment plan closely and experience improved outcomes.

Administering peptides orally offers advantages such as convenience, better bioavailability, fewer side effects, and higher patient compliance. These improvements enable broader use of peptides in therapy, paving the way for potentially more effective treatments for various conditions.

TB500 vs. TB4 Fragment SDKP

Thymosin Beta 4 is a peptide that might offer several therapeutic benefits. Research indicates it can aid in wound healing, reduce inflammation, and encourage tissue repair based on animal studies. There is also some evidence suggesting that Thymosin Beta 4 could have anti-cancer effects, making it a potential option for future cancer treatments. Typically, TB4 had to be injected subcutaneously to work effectively. However, Thymosin Beta 4 Fragment SDKP is a modified version of TB500 that can be absorbed better when taken orally, removing the need for subcutaneous injections.

A study in the Journal of Chromatography B found that Thymosin Beta4 Fragment SDKP had around 30% oral bioavailability in rats, much higher than the less than 1% seen with TB500. Another study in the Journal of Peptide Science indicated that when taken orally in rats, Thymosin Beta4 Fragment SDKP had a longer half-life and a larger area under the curve (AUC) than TB500.

These results give solid scientific proof that altering peptide sequences, like breaking down longer ones, can greatly enhance their bioavailability and effectiveness when taken by mouth.

BPC – Acetate salt vs. Arginate salt

BPC157 is a peptide known for its various therapeutic advantages. It aids in tissue repair and reduces inflammation, making it a potential treatment for conditions like musculoskeletal injuries and inflammatory bowel disease. Animal studies also indicate that BPC157 might have neuroprotective and anti-cancer effects, showcasing its promise as a therapeutic agent. Usually, this peptide is delivered through SubQ administration, but there is growing interest in creating oral versions to make it more convenient and ensure better patient adherence. Enhancing the oral bioavailability of BPC157 could involve altering its salt form. While it’s commonly made as an Acetate salt, the Arginate salt form shows greater bioavailability.

A study in the International Journal of Pharmaceutics revealed that BPC157 Arginate salt has more than seven times the oral bioavailability in rats compared to BPC157 Acetate salt. Arginate and Acetate salts are different chemical forms often used in drug formulations to enhance the solubility and stability of peptides. In translational research discussions, these well-optimized formulations are sometimes considered top candidates for oral peptides, although further clinical tests are needed for confirmation.

Research indicates that changing the salt form of a peptide could greatly influence its bioavailability and effectiveness, offering a promising path for enhancing peptide treatments.

In Summary

Thymosin Beta4 Fragment SDKP is an altered version of the peptide Thymosin Beta4. This shorter piece of the original peptide has shown improved oral bioavailability, meaning it’s absorbed more efficiently in the body than the full-length peptide. Its smaller size and changes in structure contribute to this improved absorption when taken orally. In animal studies, Thymosin Beta4 Fragment SDKP has demonstrated potential therapeutic advantages, such as decreasing inflammation and aiding wound healing.

BPC157 with Arginate salt and BPC157 with Acetate salt differ in the chemical compound used in their formulation. Research indicates that BPC157 Arginate salt offers better oral bioavailability compared to BPC157 Acetate salt. This higher bioavailability means a larger amount of the peptide can reach the bloodstream, enhancing its therapeutic effectiveness.

To sum up, the progress in creating peptides that can be taken by mouth marks an exciting step forward in peptide medicine. Traditionally, peptides have been given using subcutaneous injections, but recent studies indicate that changing a peptide’s salt form can boost its effectiveness when taken orally. This development presents several benefits for patients, such as ease of use, lessened pain and discomfort, and better compliance. With continued research and development, it is expected that there will be further advancements in orally available peptides. This progress will likely lead to new treatment possibilities for many conditions and expand the tools for designing more bioavailable peptides.

About the Author

Name: Michael Phelps

Title: Marketing Director & Biochemistry Specialist at Prymalab

Michael is an Air Force veteran and the Marketing Director at Prymalab. With a specialized background in biochemistry and over 10 years in the biotech industry, he applies military-grade precision to research standards and quality control. Michael is dedicated to bridging the gap between complex scientific studies and practical application, providing accurate, science-backed information on peptide protocols like Bioavailable Peptides.

References:

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He L, Feng D, Guo H, et al. Pharmacokinetics, distribution, metabolism, and excretion of body-protective compound 157, a potential drug for treating various wounds, in rats and dogs.Front Pharmacol . 2022;13:1026182. Published 2022 Dec 14. doi:10.3389/fphar.2022.1026182

Zhang G, Murthy KD, Binti Pare R, Qian Y. Protective effect of Tβ4 on central nervous system tissues and its developmental prospects. European Journal of Inflammation. 2020;18. doi:10.1177/2058739220934559

Kassem KM, Vaid S, Peng H, Sarkar S, Rhaleb NE. Tβ4-Ac-SDKP pathway: Any relevance for the cardiovascular system?.Can J Physiol Pharmacol . 2019;97(7):589-599. doi:10.1139/cjpp-2018-0570