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Oral Shipment of Drugs Barriers & Advancements
Oral Shipment of Drugs Barriers & Advancements
Table of Contents

Challenges and Progress in the Delivery of Drugs via Oral Administration Canada

Oral delivery systems and absorption of peptides are the the central role behind many clinical investigations. Oral delivery systems of therapeutic peptides have various factors to consider such as the gastrointestinal tract, digestive enzymes, mucus layer and the small intestine can all reduce the absorption of peptides. In this blog, we investigate the use of such peptides for clinical use.  

History of Peptides

Since 1920, when insulin produced from the pancreas of pigs and cows revolutionised the way diabetes was treated, bioactive peptides have been employed in Canada medicine. Only organic, extracted peptides were employed as medications at first. Progress in peptide synthesis allowed for the development of the first synthetic peptide medications, oxytocin and vasopressin, in the 1950s. The role of peptides in Diabetes has evolved over the years, discover more information about diabetes management here.

With the invention of solid-phase peptide synthesis in 1963, Merrifield revolutionised chemical synthesis. Almost all peptides are accessible quickly and reliably using this approach. The first recombinant medicinal peptides, like insulin, were released onto the market twenty years later when scientists discovered how to alter genes.

Cohen, Bloom, and Edwards saw a sharp increase in the use of peptide medications in 1999, but they could only recognise natural peptides. Finding novel peptides for a larger range of targets was made easier with the development of in vitro display techniques and advancements in sequence synthesis libraries. The pharmacokinetic characteristics of peptides were also the focus of intense Canada research. All of these modifications led to an increase in the Canada peptide market.

Peptides Today

mk-677-ibutamoren-Double
MK677 is believed to have high oral bioavailability

Today, a significant factor driving interest in peptide treatments is macrocyclic peptides. They can target protein-protein interactions (PPI) and other “undruggable” targets due to their distinctive size and large binding surface area.

Currently, the FDA has approved more than 80 Canada peptides, and numerous others are undergoing human testing by the research team. Various diseases, including cancer, endocrinology, metabolic, bacterial infections, cardiovascular, and bone ailments, are treated using these peptide bonds. Recent Canada evaluations discuss peptide industry trends and approvals.

Improvements in peptide synthesis and a better success rate of peptide pharmaceuticals in Canada clinical development have led to a continuous growth of 7.7% in approvals for the global peptide industry over the past few decades, strengthening this trend. Additionally, patients and the Canada pharmaceutical industry are becoming increasingly accepting to medications like most peptides that cannot be administered orally.

Peptides as Therapeutic Agents

Peptides struggle as therapeutic agents for a variety of reasons, most notably because of their unfavourable pharmacokinetic properties. Absorption, distribution, metabolism, and excretion, or ADME, is a term frequently used to describe the pharmacokinetic characteristics of a pharmacological ingredient. A drug molecule’s physicochemical characteristics and ADME behaviour determine its systemic and tissue/organ exposures. The oral delivery of macromolecules is a new method of drug delivery systems under investigation by clinical trial. 

Oral Biodiversity of Peptides

The mechanism by which substances pass from the GI tract into the bloodstream after being eaten orally is difficult for peptides. A membrane can be made more permeable in two ways: through active transport and through para- and transcellular passive diffusion. For passive membrane permeability, a high lipophilicity is typically required.

According to Lipinksi, tiny compounds having molecular weights of 500 Da or less, five H-bond donors, ten H-bond acceptors, and logP values under five are more likely to cross membranes and be absorbed orally. The so-called “rule of five” is easily broken by peptides, making passive passage through a membrane unlikely.

In addition to low passive membrane permeability, a number of chemical and enzymatic barriers that form after oral consumption further reduce the oral bioavailability of peptides. A peptide may degrade chemically in the acidic environment of the stomach as well as enzymatically by digesting enzymes in the GI tract (such as pepsin, chymotrypsin, trypsin, and carboxypeptidase) and peptidases in the gut wall close to the border of the enterocyte brush. 

Research has identified the following peptides can have a high oral bioavailability including:

  • GHK-Cu – a peptide often used for studies around anti-aging and wound healing, view more information about GHK-cu capsules here
  • BPC-157 – One of the most popular oral peptide for joint health and injury repair has demonstrated success when administered via oral drug delivery. Find BPC-157 capsules here.
  • Tesofensine – a peptide growing in popularity due to its ability to burn fat thus sparking the interest of weight loss studies. Tesofensine capsules for research are available from Pharma Lab Global today.
  • BPC-157 and Thymosin Beta-4 – this combination of peptides in oral form can hold a myriad of benefits including those for cognitive, cardiovascular, and joint health, read more information here.

Peptides capsules can provide a promising approach to oral administration of proteins. They can provide a painless alternative to subcutaneous injections, which can have adverse effects.

Distribution of Peptides within the Body CanadaTesofensine Capsules

Peptides taken orally may be broken down in the intestine by microorganisms. Notably, salivary enzymes play a minor function in the breakdown of peptides because they mostly consist of amylases and lipases. Despite efforts to develop gut-stable peptides, the mucosal gut membrane layer remains the primary barrier preventing oral availability of peptide therapy. In addition, the high molecular weight and PSA of peptides prevent bloodstream diffusion, making parenteral administration of peptides the most preferred method of administration.

Peptides are largely found in the circulatory system, where they are distributed. Due to their large molecular weight and PSA, which inhibit passive transport through cell membranes, the majority of intracellular targets are excluded. The blood-brain barrier is one membrane that peptides cannot passively traverse (BBB). Antidiuretic hormone and thyrotropin-releasing hormone are two fascinating instances of peptides that can penetrate membranes and the BBB through a saturable transport mechanism. Additionally, peptide medicines have better tissue penetration than protein therapies.

The cost of large-scale peptide synthesis is around ten times higher than that of small-molecule synthesis, however advances in SPPS and peptide purification are steadily reducing this cost disparity. This is a more strategic disadvantage of peptides.

One of these developments is the “catch-and-release approach,” which only produces the appropriate peptide sequence with a free N-terminal amino group. It is used to synthesise linear peptides on a solid phase with a capping step after each coupling. Following peptide cleavage, a chemical linker that can be placed to a solid support is used to attach the free amino, quickly removing impurities and shortened sequences.

Pharma Lab Global Canada is committed to developing peptide capsules using peptides with high oral bioavailability for when research commands an ingestible administration. Drug absorption and the oral delivery of proteins is currently under investigation of randomized clinical trial. PharmaLabGlobal supplies research peptides for clinical research use only. View the full range of research peptide capsules here.  

References:

[1] Hamman JH, Enslin GM, Kotzé AF. Oral delivery of peptide drugs: barriers and developments. BioDrugs. 2005;19(3):165-77. 

[2] Bruno BJ, Miller GD, Lim CS. Basics and recent advances in peptide and protein drug delivery. Ther Deliv. 2013 Nov;4(11):1443-67. 

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