A kind of oral glp-1 polypeptide nano preparation and its preparation method and application
A GLP-1, nano-formulation technology, applied in pharmaceutical formulations, peptide/protein components, medical preparations with non-active ingredients, etc., can solve problems such as toxic and side effects, achieve stable properties, reverse insulin resistance, and reduce blood sugar concentration Effect
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Embodiment 1
[0086] Example 1 Polylysine-Maleimide Derivatives-Biotin (PLL-M-B)-Exenatide Nano-Preparation
[0087] (1) Weigh 76.8 mg of polylysine, dissolve it in 5 mL of anhydrous DMF, add the same molar amount of EDCI, and activate the reaction for 2 hours.
[0088] (2) Weigh 48.8 mg of biotin and 33.8 mg of maleimide derivatives, and dissolve them in 5 mL of DMF.
[0089] (3) Add the solution obtained in step (2) dropwise to the polylysine reaction solution in step (1), react overnight, precipitate with 10 times the volume of ether, centrifuge at 4000rpm for 5 minutes, discard the supernatant, The obtained precipitate was the crude product PLL-M-B, which was reconstituted with a small amount of water after evaporating ether, and dialyzed in a dialysis bag with Mw: 8000-14000 for 24 hours.
[0090] Dissolve 10 mg of PLL-M-B in 10 mL of deionized water, add 2 mg of exenatide to react overnight, and obtain PLL-M-B-exenatide nano-preparation.
[0091] The polylysine, maleimide derivative...
Embodiment 2
[0096] Example 2 Chitosan-sodium tripolyphosphate-sodium alginate (CS-TPP-ALG)-exenatide nano-preparation and its polysaccharide solution
[0097] Dissolve 2 mg of exenatide solution in 100 μL of ultrapure water, add 10 mL of 1 mg / mL chitosan 1% acetic acid aqueous solution, stir overnight, add 2 mL of 0.7 mg / mL sodium tripolyphosphate aqueous solution, and stir for 30 minutes, according to Add 0.3 mg / mL sodium alginate solution at a ratio of CS:ALG=5:1, stir for 60 minutes, and freeze-dry to obtain chitosan-sodium tripolyphosphate-sodium alginate (CS-TPP-ALG)-Exena Peptide Nanoformulations.
[0098] The transmission electron microscope characterization of the CS-TPP-ALG-exenatide nano-preparation of the present embodiment is as follows: Figure 4 As shown, the results show that the shape of the CS-TPP-ALG-Exenatide nano-preparation is round, the particle size is about 300nm, the particle size is relatively uniform, and the dispersion is good.
[0099] The chitosan-sodium tr...
Embodiment 3
[0100] Example 3 Polyglutamic acid-chitosan (γ-PGA-CS)-liraglutide nano-preparation
[0101] Prepare 2 mg / mL liraglutide solution, adjust pH=7.4, take 250 μL and add it to 1.2 mg / mL chitosan 2% acetic acid solution, keep at 4°C overnight under magnetic stirring, and then adjust the pH of the mixture to 6 . 250 μL of γ-PGA (Mw: 700 KDa) aqueous solution with a concentration of 2 mg / mL was drawn and added to the above mixture to form γ-PGA-CS-liraglutide nano-preparation at room temperature. The γ-PGA-CS-liraglutide nano-formulation was collected by centrifugation at 2000 rpm at 4°C for 10 minutes, and stored at 4°C until use.
[0102] For the γ-PGA-CS-liraglutide nano-preparation of this example, the particle size was characterized by a Malvern Zetasizer Nano ZS90 series laser particle size analyzer, and the morphology was characterized by a transmission electron microscope.
[0103] Such as Figure 5 As shown, the particle size analysis and electron microscope test results ...
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