Introduction
Application of Peptides-Fatty Acids Conjugation
Improving drug solubility and absorption
Fatty acid is an important component of membrane phospholipid, which can maintain membrane fluidity and participate in the assembly of cell membrane, and it is also the basic substance of human body fat and lipids. Therefore, Peptides-Fatty acids conjugation drugs help to improve the affinity of drugs to cells, thus promoting the absorption of drugs by epithelial cells. The side chain of insulin molecule was modified with palmitic acid to obtain the more lipophilic palmitic acylated insulin. The results of isotopic tracer analysis showed that the plasma concentration of bispalmitic acid derivatives was significantly higher than that of unmodified insulin.
Prolonging the half-life of peptide drugs in the circulation
The enzymatic degradation of protease in vivo is one of the main reasons leading to the short half-life and low bioavailability of protein and peptide drugs. Fatty acid modification can cover the areas where protein peptides are susceptible to enzyme attack, thus delaying or inhibiting the destruction of proteolytic enzymes and prolonging the time of action in vivo.
Enhancing plasma albumin binding rate
Fatty acid can reversibly bind to human serumalbumin (HSA) in vivo. The combined complex is restricted by excessive molecular size in transmembrane transport. Therefore, fatty acid modification can prolong the retention time of drugs in vivo.
Improving drug solubility and absorption
Fatty acid is an important component of membrane phospholipid, which can maintain membrane fluidity and participate in the assembly of cell membrane, and it is also the basic substance of human body fat and lipids. Therefore, Peptides-Fatty acids conjugation drugs help to improve the affinity of drugs to cells, thus promoting the absorption of drugs by epithelial cells. The side chain of insulin molecule was modified with palmitic acid to obtain the more lipophilic palmitic acylated insulin. The results of isotopic tracer analysis showed that the plasma concentration of bispalmitic acid derivatives was significantly higher than that of unmodified insulin.
Prolonging the half-life of peptide drugs in the circulation
The enzymatic degradation of protease in vivo is one of the main reasons leading to the short half-life and low bioavailability of protein and peptide drugs. Fatty acid modification can cover the areas where protein peptides are susceptible to enzyme attack, thus delaying or inhibiting the destruction of proteolytic enzymes and prolonging the time of action in vivo.
Enhancing plasma albumin binding rate
Fatty acid can reversibly bind to human serumalbumin (HSA) in vivo. The combined complex is restricted by excessive molecular size in transmembrane transport. Therefore, fatty acid modification can prolong the retention time of drugs in vivo.
Contact Info
Address:
45-16 Ramsey Road, Shirley, NY 11967, USA
Shirley, NY
New York 11967
United States
Shirley, NY
New York 11967
United States
Tel:
6316197922
Website:
https://www.creative-peptides.com/services/peptides-fatty-acids-conjugation.html
Hours of operation
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