Ph-responsive galactosylated chitosan-polyethylene glycol polymer bonded doxorubicin prodrug and its preparation and use
A technology of polyethylene glycol and chitosan, which is applied in the fields of polymer materials and biomedical engineering, can solve the problems of small drug loading, uncertain drug loading, and the release rate of drugs cannot be released quickly, so as to reduce toxicity. , the effect of good pH responsiveness
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Embodiment 1
[0024] Preparation of galactosylated chitosan-polyethylene glycol polymer:
[0025] (1) Galactosylation of chitosan: Weigh 3.2g of commercially available chitosan in 2% (v / v) 60ml acetic acid aqueous solution, stir at room temperature for 1h, after chitosan is fully swollen, add 0.3 g lactose, stirred in a water bath at 40°C for 24 hours, added a weak reducing agent sodium cyanoborohydride and stirred for 1 hour, put the reaction solution in a dialysis bag (MWCO=3500), dialyzed with distilled water, and freeze-dried to obtain a galactosified shell glycans. The grafting rate of galactose was measured by sulfuric acid phenol method, and the grafting rate of galactose in the obtained galactosylated chitosan was determined to be 0.315%.
[0026] (2) Carboxylation of monomethyl ether polyethylene glycol: Weigh 1.4 g of monomethyl ether polyethylene glycol and 0.426 g of 3,3'-dithiodipropionic anhydride, dissolve in molecular sieve-dried N,N-dipropionic anhydride Add 4-dimethylami...
Embodiment 2
[0049] Prepare galactosylated chitosan and carboxylated polyethylene glycol according to the same method in Example 1, accurately weigh galactosylated chitosan 1.0g, carboxylated polyethylene glycol 0.417g, and add 1-ethylene glycol Base-(3-dimethylaminopropyl) carbodiimide hydrochloride was stirred and reacted for 48h. After the reaction, the reaction solution was placed in a dialysis bag, dialyzed with distilled water, and freeze-dried to obtain galactosylated chitosan-polyethylene Glycol polymer.
[0050] Amino protection with doxorubicin was carried out under the same conditions as in Example 1. Formylation of histidine: Weigh 0.1648 g of histidine and add it into the ethanol solution of KOH (solution A), and stir until completely dissolved. Measure 2ml of glutaraldehyde (containing 0.5g of glutaraldehyde) and dissolve it in ethanol (solution B), and heat to 40°C. The A solution was slowly added dropwise to the B solution, and the addition was completed within 0.5h, and ...
Embodiment 3
[0052] The galactosylation of chitosan: take by weighing commercially available chitosan 3.2g in the 60ml acetic acid aqueous solution of 2% (v / v), stir 1h under normal temperature, after chitosan is fully swollen, add 0.2g lactose, Stir in a water bath at 35°C for 36 hours, add weak reducing agent sodium cyanoborohydride and stir for 1 hour, place the reaction solution in a dialysis bag (MWCO=3500), dialyze with distilled water, freeze-dry to obtain galactosylated chitosan, spare. The grafting rate of galactose was measured by sulfuric acid phenol method, and the grafting rate of galactose in the obtained galactosylated chitosan was determined to be 0.275%.
[0053] Prepare carboxylated polyethylene glycol according to Example 1, accurately weigh galactosylated chitosan 1.0g, carboxylated polyethylene glycol 0.625g, and add 1-ethyl-(3-dimethylaminopropyl ) carbodiimide hydrochloride was stirred and reacted for 48 hours. After the reaction, the reaction solution was placed in...
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