Micelle based on non-linear polyethylene glycol-polylactic acid block copolymer and preparation method thereof
A technology of block copolymer and polyethylene glycol, which is applied in the direction of medical preparations and pharmaceutical formulations of non-active ingredients, can solve the problems of low drug loading and single micelle morphology, and achieve high biocompatibility , increase water solubility, increase the effect of drug efficacy
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Embodiment 1
[0025] Embodiment 1: two-terminal tetrahydroxypolyethylene glycol ((HO) 2 -PEG-(OH) 2 )Synthesis
[0026] Get the PEG (polyethylene glycol) that 8g molecular weight is 1000, the 2 of 1.392g dihydroxyl protection, 2-dimethylol propionic acid, 2.472g DCC (dicyclohexylcarbodiimide) and 0.244gDMAP (4-di aminopyridine), dissolved in 100 mL of anhydrous CH 2 Cl 2 , reacted at room temperature for 48 hours. After the reaction, the white insoluble matter was filtered off, the remaining solution was concentrated under reduced pressure, and then poured into 100 mL of ether to obtain a white precipitate, which was dried overnight under vacuum, and then the white product was dissolved in 100 mL of methanol, and 2 g of The ion exchange resin DOWEX HCR-W2 acidified with 6 wt% hydrochloric acid was stirred at room temperature for 32 hours. Afterwards, the resin was filtered off, the remaining solution was concentrated under reduced pressure, and settled in 100 mL of ether to obtain 7 g ...
Embodiment 2
[0027] Embodiment 2: two-terminal tetrahydroxypolyethylene glycol ((HO) 2 -PEG-(OH) 2 )Synthesis
[0028] Get 32g molecular weight to be the PEG (polyethylene glycol) of 4000, the 2,2-dimethylol propionic acid of 1.390g double hydroxyl protection, 2.472g DCC (dicyclohexylcarbodiimide) and 0.244gDMAP (4-di aminopyridine), dissolved in 100 mL of anhydrous CH 2 Cl 2 , reacted at room temperature for 48 hours. After the reaction, the white insoluble matter was filtered off, the remaining solution was concentrated under reduced pressure, and then poured into 200 mL of ether to obtain a white precipitate, which was dried overnight under vacuum, and then the white product was dissolved in 100 mL of methanol, and 8 g of The ion exchange resin DOWEX HCR-W2 acidified with 6 wt% hydrochloric acid was stirred at room temperature for 32 hours. Afterwards, the resin was filtered off, the remaining solution was concentrated under reduced pressure, and settled in 200 mL of ether to obtai...
Embodiment 3
[0029] Embodiment 3: single-end dihydroxypolyethylene glycol (MPEG (OH)2 )Synthesis
[0030] Take 10 g of MPEG (monomethoxypolyethylene glycol) with a molecular weight of 2000, 1.74 g of dihydroxy-protected 2,2-dimethylolpropionic acid, 3.09 g of DCC (dicyclohexylcarbodiimide) and 0.305 g of DMAP (4-Dimethylaminopyridine), dissolved in 150 mL of anhydrous CH 2 Cl 2 , reacted at room temperature for 48 hours. After the reaction, the white insoluble matter was filtered off, the remaining solution was concentrated under reduced pressure, and then poured into 200 mL of ether to obtain a white precipitate, which was dried overnight under vacuum, and then the white product was dissolved in 100 mL of methanol, and 2.5 g of The ion exchange resin DOWEX HCR-W2 acidified with 6 wt% hydrochloric acid was stirred at room temperature for 32 hours. Afterwards, the resin was filtered off, the remaining solution was concentrated under reduced pressure, and settled in 200 mL of ether to obt...
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