A kind of bone-targeting polymer, bone-targeting polymer vesicle and its preparation method and application
A polymer, bone-targeting technology, applied in the fields of polymer materials and biomedical engineering, can solve the problems of single treatment, poor biocompatibility, diagnosis of malignant bone tumors, etc., achieve good biocompatibility, reduce side effects, inhibit The effect of bone resorption
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[0049] (2) Preparation steps of bone-targeted polymer vesicles:
[0050] The bone-targeting polymer obtained in step (1) is completely dissolved in the second type of solvent, and deionized water 2 to 10 times the volume of the organic solvent is added dropwise at a stirring speed of 150 to 400 rpm. After dialysis, the product containing Aqueous solutions of bone-targeting polymersomes.
[0051] Wherein, the second type of solvent is one or more of ethyl acetate, p-xylene, dioxane, dimethyl sulfoxide or tetrahydrofuran, and the volume of the organic solvent is 1.00-20.0 mL.
[0052] (3) 99m Preparation steps of Tc chelated bone-targeted polymer vesicles:
[0053] Add stannous chloride to the aqueous solution of the bone-targeted polymer vesicles obtained in step (2) and stir for 1 to 4 hours, and add the nuclide under stirring conditions 99m Tc, get 99m Aqueous solutions of Tc-chelating bone-targeting polymersomes.
[0054] Wherein, the molar ratio of the added amount of ...
Embodiment 1
[0063] (1) Synthesis steps of bone targeting polymer:
[0064] Dissolve polycaprolactone-block-polyglutamic acid polymer (10.0 mg, 0.530 μmol) in 2.00 mL of dimethylformamide, and add 20.0 mL of Ionized water, after the dropwise addition is completed, dialyze to remove the residual organic solvent, the solution after dialyzing is used as the first solution, and then add 1-[3-(dimethylamino)propyl]-3-ethyl to the first solution Carbodiimide methyl iodide (5.20 mg, 17.5 μmol) was stirred for 20 min, and alendronate (4.21 mg, 17.0 μmol) was dissolved in 20.0 mL of deionized water as a second solution, and the second solution was Add dropwise into the first solution at a rate of 12-30 d / min under stirring, stir and react at 25-37°C for 12 hours after the dropwise addition, dialyze and freeze-dry the reaction solution to obtain the bone-targeted polymer;
[0065] (2) Preparation steps of bone-targeted polymer vesicles:
[0066] Dissolve polycaprolactone-block-polyglutamic acid po...
Embodiment 2
[0072] Compared with Example 1, the molar ratio of polycaprolactone-block-polyglutamic acid polymer and alendronic acid in this example is 1:14. At this time, the preparation of bone-targeted polymer vesicles The method includes the following steps:
[0073] (1) Synthesis steps of bone targeting polymer:
[0074]Dissolve polycaprolactone-block-polyglutamic acid polymer (5.00mg, 0.270μmol) in 5.00mL dimethylformamide, add 10.0mL of Ionized water, after the dropwise addition is completed, dialyze to remove the residual organic solvent, the solution after dialyzing is used as the first solution, and then add 1-[3-(dimethylamino)propyl]-3-ethyl to the first solution Carbodiimide methyl iodide (1.52 mg, 5.13 μmol) was stirred for 20 min, and alendronate (0.942 mg, 3.78 μmol) was dissolved in 1.00 mL of deionized water as the second solution, and the second solution was Add dropwise into the first solution at a rate of 12-30 d / min under stirring, stir and react at 25-37°C for 8 ho...
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