PH-sensitive epsilon-polylysine and preparation method and application thereof
A technology of polylysine and polylysine chains, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of ε-polylysine toxicity and limited application, Achieve high selectivity and reduce toxicity
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[0041] A method for preparing the pH-responsive ε-polylysine as described above, at least comprising the following steps:
[0042] Dissolving ε-polylysine in a mixed solution of 4-hydroxyethylpiperazineethanesulfonic acid and NaOH;
[0043] Weigh the excess pH responsive small molecule and dissolve it in ethanol;
[0044] The two solutions obtained above were mixed and stirred;
[0045] Ultrafiltration centrifugation was performed, and then the sample was lyophilized to obtain a powdery pH-responsive ε-polylysine product.
[0046] Preferably, the ratio of the amino group in the ε-polylysine chain to the pH-responsive small molecule substance is 1:1˜1:100. Here, the pH responds to an excess of small molecules, in order to ensure that the amino groups on the ε-polylysine fully react.
[0047] Preferably, the mass concentration of ε-polylysine in the mixed solution of 4-hydroxyethylpiperazineethanesulfonic acid and NaOH is 0.1mg / ml-100mg / ml, such as 0.1mg / ml, 15mg / ml, 50mg / ml ...
Embodiment 1
[0054] Dissolve a certain amount of ε-polylysine in a mixed solution of 100mM HEPES and 125mM NaOH; weigh excess 2,3-dimethylmaleic anhydride and dissolve in ethanol, add to the above solution and mix well, Stir at room temperature under protection for 0.5-3 hours; put the obtained product into an ultrafiltration centrifuge tube for concentration and purification, and finally freeze-dry the sample to obtain a powdery pH-responsive ε-polylysine product.
Embodiment 2
[0056] Dissolve a certain amount of ε-polylysine in a mixed solution of 100mM HEPES and 125mM NaOH; weigh an excess of citraconic anhydride and dissolve it in ethanol, add it to the above solution and mix well, and stir at room temperature for 0.5-3 hours under the protection of argon ; Put the obtained product into an ultrafiltration centrifuge tube for concentration and purification, and finally freeze-dry the sample to obtain a powdered pH-responsive ε-polylysine product.
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