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EP39010
Abstract: Peptide drugs have poor oral bioavailability due to the complex physiological barrier of gastrointestinal tract, making most of the listed peptide drugs are administered by injection, which is not only cumbersome to operate, but also brings great challenges to patients who need long-term injection of peptide drugs (such as insulin), including pain, aversion to injection and local irritation, seriously reducing the patient's compliance.
In order to improve patients' compliance with medication, oral administration becomes the best way of drug delivery. However, how to overcome various barriers to oral absorption of peptide drugs and develop oral drug delivery technology with high bioavailability has become a hot spot and a difficult area of research at present.
Challenges Of Oral Peptide Therapeutics
When taken orally, peptide drugs must overcome four major barriers in the gastrointestinal tract before they enter the circulation and begin to work ( Figure 1).
Gastrointestinal-tract-barriers.jpg
Figure 1. Challenges of oral peptide drugs
Enzymatic barrier: Peptides are subject to destruction by gastric acid and enzymatic degradation in the gastrointestinal tract. The pH of gastric acid is around 1 to 2.5, and most peptides lose their biological activity. And the small intestine contains gram quantities of peptidases secreted by the intestinal mucosa include trypsin, carboxypeptidase and many dipeptidases and aminopeptidases, which can degrade both peptides
Mucus barrier: The mucus layer of the gastrointestinal tract is a physicochemical barrier to peptides. Foreign drug-containing particles are "trapped" by the mucus layer due to adhesion or spatial blockage and are removed within the next few minutes to hours, resulting in decreased drug bioavailability.
Transcellular barrier: The absorption of peptide drugs in the gastrointestinal tract is mainly dependent on the transcellular pathway. However, the epithelial cell surface of the GI tract lacks peptide transport receptors and the peptide has poor ability to cross the cell membrane directly, at the same time the cell will also deliver the peptide into the cell and degrade it by lysosomes.
Individual variability: Individual variability is also a barrier that limits the development of oral peptides. The absorption process of peptides in the gastrointestinal tract is influenced by various individualized factors such as meal intake, gastrointestinal digestive fluid and mucosal surface area and intestinal flora, in addition to the co-morbidities of patients.
Oral Peptide Therapeutics Development
Oral peptide drugs are difficult to develop, yet the attention is high. However, there are relatively few successfully developed drugs.Summary: In order to improve patients' compliance with medication, oral administration becomes the best way of drug delivery. However, how to overcome various barriers to oral absorption of peptide drugs and develop oral drug delivery technology with high bioavailability has become a hot spot and a difficult area of research at present.
In order to improve patients' compliance with medication, oral administration becomes the best way of drug delivery. However, how to overcome various barriers to oral absorption of peptide drugs and develop oral drug delivery technology with high bioavailability has become a hot spot and a difficult area of research at present.
Challenges Of Oral Peptide Therapeutics
When taken orally, peptide drugs must overcome four major barriers in the gastrointestinal tract before they enter the circulation and begin to work ( Figure 1).
Gastrointestinal-tract-barriers.jpg
Figure 1. Challenges of oral peptide drugs
Enzymatic barrier: Peptides are subject to destruction by gastric acid and enzymatic degradation in the gastrointestinal tract. The pH of gastric acid is around 1 to 2.5, and most peptides lose their biological activity. And the small intestine contains gram quantities of peptidases secreted by the intestinal mucosa include trypsin, carboxypeptidase and many dipeptidases and aminopeptidases, which can degrade both peptides
Mucus barrier: The mucus layer of the gastrointestinal tract is a physicochemical barrier to peptides. Foreign drug-containing particles are "trapped" by the mucus layer due to adhesion or spatial blockage and are removed within the next few minutes to hours, resulting in decreased drug bioavailability.
Transcellular barrier: The absorption of peptide drugs in the gastrointestinal tract is mainly dependent on the transcellular pathway. However, the epithelial cell surface of the GI tract lacks peptide transport receptors and the peptide has poor ability to cross the cell membrane directly, at the same time the cell will also deliver the peptide into the cell and degrade it by lysosomes.
Individual variability: Individual variability is also a barrier that limits the development of oral peptides. The absorption process of peptides in the gastrointestinal tract is influenced by various individualized factors such as meal intake, gastrointestinal digestive fluid and mucosal surface area and intestinal flora, in addition to the co-morbidities of patients.
Oral Peptide Therapeutics Development
Oral peptide drugs are difficult to develop, yet the attention is high. However, there are relatively few successfully developed drugs.Summary: In order to improve patients' compliance with medication, oral administration becomes the best way of drug delivery. However, how to overcome various barriers to oral absorption of peptide drugs and develop oral drug delivery technology with high bioavailability has become a hot spot and a difficult area of research at present.
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