scholarly journals Hydrophobic ion pairing of a GLP-1 analogue for incorporating into lipid nanocarriers designed for oral delivery

2020 ◽  
Vol 152 ◽  
pp. 10-17 ◽  
Author(s):  
Ruba Ismail ◽  
Thi Nhu Quynh Phan ◽  
Flavia Laffleur ◽  
Ildikó Csóka ◽  
Andreas Bernkop-Schnürch
2016 ◽  
Vol 14 (8) ◽  
pp. 983-995 ◽  
Author(s):  
Mariana Silva Oliveira ◽  
Gisele Castro Assis Goulart ◽  
Lucas Antônio Miranda Ferreira ◽  
Guilherme Carneiro

2017 ◽  
Vol 15 (1) ◽  
pp. 216-225 ◽  
Author(s):  
Hoang D. Lu ◽  
Paradorn Rummaneethorn ◽  
Kurt D. Ristroph ◽  
Robert K. Prud’homme

2021 ◽  
Vol 17 (6) ◽  
pp. 1199-1207
Author(s):  
Hanmei Li ◽  
Hongyi Zhuo ◽  
Dan Yin ◽  
Wei Li ◽  
Yamei Zhang ◽  
...  

Tetramethylpyrazine (TMP), isolated from the rhizome of the traditional Chinese medicinal plant Chuanxiong (Ligusticum wallichii Franchat) shows therapeutic efficacy against osteoarthritis. After intra-articular injection, the retention time of TMP in the joint cavity is short, which limits its treatment effect. To avoid this problem, the present study explored the preparation of a TMP nanosuspension (TMP-NS) based on hydrophobic ion pairing. TMP-NS showed a particle size of approximately 588 nm and, after intra-articular injection in rats, it had longer retention in the articular cavity, higher TMP concentrations in joints, and greater anti-osteoarthritic efficacy than TMP solution. TMP-NS didn’t cause significant inflammation at the joint. These results suggest that TMP-NS may strengthen and prolong the therapeutic efficacy of TMP against osteoarthritis without systemic toxicity.


2018 ◽  
Vol 549 (1-2) ◽  
pp. 76-86 ◽  
Author(s):  
Abrar S. Torky ◽  
May S. Freag ◽  
Maha M.A. Nasra ◽  
Ossama Y. Abdallah

2004 ◽  
Vol 54 (5) ◽  
pp. 441-448 ◽  
Author(s):  
Lixin Feng ◽  
Alexandra De Dille ◽  
Vicky J. Jameson ◽  
Leia Smith ◽  
William S. Dernell ◽  
...  

OCL ◽  
2022 ◽  
Vol 29 ◽  
pp. 1
Author(s):  
Camille Dumont

Therapeutic peptides can treat a wide variety of diseases with selective and potent action. Their oral bioavailability is strongly limited by an important proteolytic activity in the intestinal lumen and poor permeation across the intestinal border. We have evaluated the capacity of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to overcome both oral bioavailability limiting aspects, using leuprolide (LEU) as model peptide. Lipidization of LEU by formation of a hydrophobic ion pair (HIP) with sodium docusate enables a significant increase of peptide encapsulation efficiency in both SLN and NLC. The nanocarriers, obtained by high-pressure homogenization, measured 120 nm and were platelet shaped. Regarding the protective effect towards proteolytic degradation, only NLC maintained LEU integrity in presence of trypsin. Intestinal transport, evaluated on Caco-2 (enterocyte-like model) and Caco-2/HT29-MTX (mucin-secreting model) monolayers, showed nanocarriers internalization by enterocytes but no improvement of LEU permeability. Indeed, the combination of nanoparticles platelet-shape with the poor stability of the HIP in the transport medium induces a high burst release of the peptide, limiting nanoparticles capacity to transport LEU across the intestinal border. Stability of peptide lipidization needs to be improved to withstand biorelevant medium to benefit from the advantages of encapsulation in solid lipid nanocarriers and consequently improve their oral bioavailability.


2020 ◽  
Vol 151 ◽  
pp. 73-80 ◽  
Author(s):  
Richard Wibel ◽  
Julian David Friedl ◽  
Sergey Zaichik ◽  
Andreas Bernkop-Schnürch

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