Peptide therapeutics are characterized by high potency, exquisite specificity, and low toxicity, and have therefore been widely adopted for the clinical management of diverse diseases. However, their inherently low gastrointestinal permeability, rapid enzymatic degradation, and multiple physiological barriers collectively result in extremely low oral bioavailability, necessitating parenteral administration. Compared with the more convenient and patient-compliant oral route, chronic injection is associated with poor adherence and an increased incidence of adverse reactions. In recent years, extensive research has focused on permeation enhancers (PEs) based strategies to improve the oral bioavailability of peptide drugs. This review systematically summarizes the mechanisms of action and clinical applications of representative PEs-including surfactants (sodium caprylate, sodium caprate, alkyl glycosides, bile salts), chelating agents, chitosan and cell-penetrating peptides. It also summarizes related patented technologies (EligenTM, TPETM, GIPETTM, PODTM, PeptelligenceTM) to facilitate the development and clinical translation of oral peptide formulations.
| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |