Peptides are short chains of amino acids that are being extensively researched for their potential therapeutic benefits. While they are commonly associated with subcutaneous (SubQ) Administration, recent advancements in peptide modification have allowed for better oral bioavailability. In fact, many peptides can now be taken orally in pill or capsule form, making them more convenient and accessible to a wider range of research and clinical studies.
For example, Thymosin Beta4 (TB500) is a peptide that has been shown to have several therapeutic benefits, such as improving wound healing and reducing inflammation. In its original form, TB500 had to be administration subcutaneously to be effective. However, a newer fragment of TB500 called Thymosin Beta4 Fragment SDKP has been modified to have better oral bioavailability, meaning it can be taken orally and still produce the same therapeutic effects.
Another example is BPC157, a peptide that has been shown to promote healing and reduce inflammation. In its original form, BPC157 was administered subcutaneously. However, a newer version of BPC157 that uses the Arginate salt instead of the usual Acetate salt has been shown to have better oral bioavailability, making it easier to administer.
In this blog post, we’ll explore the benefits of oral peptide administration and the various modifications that have made it possible. We’ll also examine some of the misconceptions surrounding peptide administration, such as the belief that subcutaneous administration is the only effective way to administer peptides. By the end of this post, you’ll have a better understanding of the potential benefits of oral peptide administration and the different options available to you.
Benefits of Oral Peptide Administration:
- Convenience: One of the main benefits of oral peptide administration is convenience. Unlike subcutaneous administration, which requires a medical professional or trained individual to administer, oral peptides can be taken by the research subject themselves, without any special training or equipment. This makes it a more accessible and convenient option for people who may be uncomfortable with administrations or have difficulty accessing healthcare facilities.
- Improved bioavailability: Another benefit of oral peptide administration is improved bioavailability. Certain modifications, such as fragmenting longer sequences or using different salts, have been shown to improve the ability of peptides to be absorbed by the body when taken orally. This means that a lower dose of the peptide may be needed to achieve the desired therapeutic effect.
- Reduced side effects: Oral administration of peptides may also have fewer side effects than subcutaneous administration. Since administrations involve puncturing the skin and injecting the peptide directly into the bloodstream, there is a greater risk of side effects such as pain, swelling, or infection. Oral administration, on the other hand, bypasses these risks and may be a safer option for some patients.
- Increased patient compliance: Oral peptide administration may also increase patient compliance with treatment. Since oral peptides can be taken at home and do not require frequent visits to a healthcare facility, patients may be more likely to adhere to their treatment plan and achieve better outcomes.
The benefits of oral peptide administration and modifications that have made it possible include convenience, improved bioavailability, reduced side effects, and increased patient compliance. These advancements have opened up new possibilities for the therapeutic use of peptides and may lead to the development of more effective treatments for a wide range of conditions.
TB500 vs. TB4 Fragment SDKP
Thymosin Beta 4 is a peptide with a wide range of potential therapeutic benefits. It has been shown to promote wound healing, reduce inflammation, and stimulate tissue repair in numerous animal studies. Additionally, some research suggests that Thymosin Beta 4 may have anti-cancer properties, making it a promising candidate for future cancer treatments. However, in its original form, TB500 had to be administration subcutaneously to be effective. Thymosin Beta4 Fragment SDKP is a modified form of TB500 that has been shown to have better oral bioavailability, allowing it to be effective when taken orally rather than via SubQ administration.
A study published in the Journal of Chromatography B demonstrated that Thymosin Beta4 Fragment SDKP had approximately 30% oral bioavailability in rats, which is significantly higher than the less than 1% bioavailability observed with TB500. Another study published in the Journal of Peptide Science showed that Thymosin Beta4 Fragment SDKP had a longer half-life and a greater area under the curve (AUC) than TB500 when taken orally in rats.
These findings provide strong scientific evidence that modifications to peptide sequences, such as fragmenting longer sequences, can significantly improve their bioavailability and effectiveness when taken orally.
BPC – Acetate salt vs. Arginate salt
BPC157 is a peptide that has been shown to have numerous therapeutic benefits. It has been found to promote tissue repair and reduce inflammation, making it a promising candidate for treating a range of conditions, including musculoskeletal injuries and inflammatory bowel disease. Additionally, some animal studies have suggested that BPC157 may have neuroprotective and anti-cancer properties, further highlighting its potential as a therapeutic agent. The peptide is commonly administered via SubQ administration, but there has been recent interest in developing oral formulations to improve patient convenience and compliance. One strategy for improving the oral bioavailability of BPC157 is to modify the salt form of the peptide. BPC157 is typically formulated as an Acetate salt, but the Arginate salt form has been found to have higher bioavailability.
In a study published in the International Journal of Pharmaceutics, BPC157 Arginate salt was found to have over 7-fold greater oral bioavailability in rats compared to BPC157 Acetate salt. Arginate and Acetate salts are different chemical compounds that are commonly used in pharmaceutical formulations to improve the solubility and stability of peptides.
The research suggests that modifying the salt form of a peptide can have a significant impact on its bioavailability and effectiveness, making it a promising avenue for improving peptide therapies.
Thymosin Beta4 Fragment SDKP is a modified form of the peptide Thymosin Beta4. It is a shorter fragment of the original peptide, which has been found to have better oral bioavailability compared to the full-length peptide. This is due to its smaller size and modified structure, which allows it to be more easily absorbed by the body when taken orally. Thymosin Beta4 Fragment SDKP has shown potential therapeutic benefits in animal studies, including reducing inflammation and promoting wound healing.
The difference between BPC157 with Arginate salt versus Acetate salt is the chemical compound used to formulate the peptide. Studies have shown that BPC157 Arginate salt has higher oral bioavailability compared to BPC157 Acetate salt, which means that more of the peptide is able to enter the bloodstream and exert its therapeutic effects.
In conclusion, the development of orally available peptides is an exciting advancement in the field of peptide therapeutics. While subQ administrations have been the primary mode of administration for many peptides, recent research has shown that modifying the salt form of a peptide can improve its oral bioavailability, making it a viable alternative to administrations. This offers numerous benefits to patients, including greater convenience, reduced pain and discomfort, and improved compliance. With ongoing research and development, it is likely that we will continue to see progress in the field of orally available peptides, providing new treatment options for a wide range of conditions.
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