Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals
Recently, two oral-administered peptide pharmaceuticals, semaglutide and octreotide, have been developed and are considered as a breakthrough in peptide and protein drug delivery system development. In 2019, the Food and Drug Administration (FDA) approved an oral dosage form of semaglutide developed...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/12/1585 |
| _version_ | 1797455760659054592 |
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| author | Jae Cheon Kim Eun Ji Park Dong Hee Na |
| author_facet | Jae Cheon Kim Eun Ji Park Dong Hee Na |
| author_sort | Jae Cheon Kim |
| collection | DOAJ |
| description | Recently, two oral-administered peptide pharmaceuticals, semaglutide and octreotide, have been developed and are considered as a breakthrough in peptide and protein drug delivery system development. In 2019, the Food and Drug Administration (FDA) approved an oral dosage form of semaglutide developed by Novo Nordisk (Rybelsus<sup>®</sup>) for the treatment of type 2 diabetes. Subsequently, the octreotide capsule (Mycapssa<sup>®</sup>), developed through Chiasma’s Transient Permeation Enhancer (TPE) technology, also received FDA approval in 2020 for the treatment of acromegaly. These two oral peptide products have been a significant success; however, a major obstacle to their oral delivery remains the poor permeability of peptides through the intestinal epithelium. Therefore, gastrointestinal permeation enhancers are of great relevance for the development of subsequent oral peptide products. Sodium salcaprozate (SNAC) and sodium caprylate (C8) have been used as gastrointestinal permeation enhancers for semaglutide and octreotide, respectively. Herein, we briefly review two approved products, Rybelsus<sup>®</sup> and Mycapssa<sup>®</sup>, and discuss the permeation properties of SNAC and medium chain fatty acids, sodium caprate (C10) and C8, focusing on Eligen technology using SNAC, TPE technology using C8, and gastrointestinal permeation enhancement technology (GIPET) using C10. |
| first_indexed | 2024-03-09T15:58:02Z |
| format | Article |
| id | doaj.art-108ff98093dd48429f36f9d14e0cd0de |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T15:58:02Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-108ff98093dd48429f36f9d14e0cd0de2023-11-24T17:17:44ZengMDPI AGPharmaceuticals1424-82472022-12-011512158510.3390/ph15121585Gastrointestinal Permeation Enhancers for the Development of Oral Peptide PharmaceuticalsJae Cheon Kim0Eun Ji Park1Dong Hee Na2College of Pharmacy, Chung-Ang University, Seoul 06974, Republic of KoreaD&D Pharmatech, Seongnam 13486, Republic of KoreaCollege of Pharmacy, Chung-Ang University, Seoul 06974, Republic of KoreaRecently, two oral-administered peptide pharmaceuticals, semaglutide and octreotide, have been developed and are considered as a breakthrough in peptide and protein drug delivery system development. In 2019, the Food and Drug Administration (FDA) approved an oral dosage form of semaglutide developed by Novo Nordisk (Rybelsus<sup>®</sup>) for the treatment of type 2 diabetes. Subsequently, the octreotide capsule (Mycapssa<sup>®</sup>), developed through Chiasma’s Transient Permeation Enhancer (TPE) technology, also received FDA approval in 2020 for the treatment of acromegaly. These two oral peptide products have been a significant success; however, a major obstacle to their oral delivery remains the poor permeability of peptides through the intestinal epithelium. Therefore, gastrointestinal permeation enhancers are of great relevance for the development of subsequent oral peptide products. Sodium salcaprozate (SNAC) and sodium caprylate (C8) have been used as gastrointestinal permeation enhancers for semaglutide and octreotide, respectively. Herein, we briefly review two approved products, Rybelsus<sup>®</sup> and Mycapssa<sup>®</sup>, and discuss the permeation properties of SNAC and medium chain fatty acids, sodium caprate (C10) and C8, focusing on Eligen technology using SNAC, TPE technology using C8, and gastrointestinal permeation enhancement technology (GIPET) using C10.https://www.mdpi.com/1424-8247/15/12/1585peptidesoral deliverypermeation enhancersmedium chain fatty acidssodium salcaprozate |
| spellingShingle | Jae Cheon Kim Eun Ji Park Dong Hee Na Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals Pharmaceuticals peptides oral delivery permeation enhancers medium chain fatty acids sodium salcaprozate |
| title | Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals |
| title_full | Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals |
| title_fullStr | Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals |
| title_full_unstemmed | Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals |
| title_short | Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals |
| title_sort | gastrointestinal permeation enhancers for the development of oral peptide pharmaceuticals |
| topic | peptides oral delivery permeation enhancers medium chain fatty acids sodium salcaprozate |
| url | https://www.mdpi.com/1424-8247/15/12/1585 |
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