Borate functionalized pluronic polymer, preparation method and application to preparation of drug delivery system
A delivery system and a technology for preparing drugs, which are applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as toxic side effects, strong hydrophilicity, and unstable carriers, and achieve The effect of improving stability
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Embodiment 1
[0053] Preparation of borate-functionalized pluronic polymers:
[0054] The synthetic route of borate-functionalized pluronic polymers is shown below:
[0055]
[0056] The preparation method of the pluronic polymer of borate functionalization comprises the following steps:
[0057] S1. Preparation of carboxyl-modified pranix shown in formula Ⅰ-2:
[0058] Add Plavonic P123 (10g, 1.7mmol), adipic anhydride (0.7g, 5.5mmol), anhydrous triethylamine (0.55g, 5.4mmol) to a 100mL round In the bottom reaction flask, add 20 mL of dichloromethane as solvent. After reacting for 12 hours, the dichloromethane was removed by rotary evaporation, and the product was dissolved in ethanol, and dialyzed with a dialysis bag with a molecular weight cut-off of 3500 Da. The dialysate was 80% ethanol and deionized water, respectively, for 24 hours each. Freeze-dry to obtain 8.7 g of the carboxy-modified pluronic product shown in formula I-2, with a yield of 85.04%.
[0059] S2. Preparation of b...
Embodiment 2
[0063] Preparation of micelles and their particle size and morphology:
[0064] 1. Preparation of pranik P123 blank micelles:
[0065] Weigh 30mg of Pluronic P123 shown in formula Ⅰ-1 and place it in a 25mL eggplant-shaped bottle, add 1mL of dichloromethane, spin steam at 50°C for 30min, and then put it in a 60°C oven to dry overnight; then put the round bottom bottle in 50 Hydrate and heat in a water bath at ℃ for 15 minutes, add 10 mL of deionized water (pH 7.4) at 50 ℃ to the bottle, stir and vortex quickly, filter the solution with a 0.22 μm filter head, and obtain a milky white or transparent micellar emulsion, which is Pulan Nick P123 blank micelles.
[0066] Take 1mL of micellar emulsion and use the Nanoparticle Sizer (DLS) to detect the particle size, and use the transmission electron microscope to detect the shape. The results are as follows: Figure 3a with Figure 3b .
[0067] Depend on Figure 3a with Figure 3b It can be seen that the particle size of Plani...
Embodiment 3
[0073] Encapsulation efficiency, drug loading efficiency and particle size of drug-loaded micelles:
[0074] 1. Preparation of Pluronic P123 drug-loaded micelles:
[0075] Weigh 30mg of Pluronic P123 and doxorubicin and dissolve them in 1mL of anhydrous dichloromethane, rotary steam at 50°C for 30min, and then dry in a 60°C oven overnight; then put the round bottom bottle into a water bath at 50°C Heat for 15 minutes, add 10mL of 50°C deionized water (pH 7.4) to the bottle, stir and vortex quickly, filter the solution with a 0.22μm filter head, and obtain a red emulsion or transparent solution, which is Pluronic P123 drug-loaded gel bundle.
[0076] 2. Preparation of borate-functionalized Pluronic polymer drug-loaded micelles:
[0077] Weigh 30 mg of borate-functionalized pramicol polymer and doxorubicin and dissolve it in 1 mL of anhydrous dichloromethane, spin evaporate at 50 ° C for 30 min, and then put it in a 60 ° C oven to dry overnight; then put the round bottom bottl...
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