Folic acid-targeted acid sensitive core-crosslinked drug-loaded micelles based on polyphosphoester
A polyphosphate, folic acid targeting technology, used in antitumor drugs, drug combinations, pharmaceutical formulations, etc., to achieve the effect of prolonging the circulation time in the body
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Embodiment 1
[0063] Example 1: Preparation of polyphosphate block copolymer (PBYP-b-PEOP-OH)
[0064] Dry the ampoule with a stirrer in an oven at 120°C for at least 24 hours, take it out, connect the ampoule to the double-row tube, pump it with an oil pump, and cool it to room temperature, repeat the pumping and inflation three times, and finally fill it with nitrogen. Next, add 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU, 0.2738 g, 0.18 mmol), dichloromethane (CH 2 Cl 2, 1.5 mL), isopropanol (IPA, 0.1121 g, 0.12 mmol) and the monomer 2-ynbutyl-2-oxo-1, 3, 2-dioxaphospholane (BYP, 0.8453 g, 4.8 mmol), put the reaction vial into an oil bath set at 25°C, and react under stirring for 30 minutes. After the reaction, the monomer 2-ethyl-2-oxo-1, 3, 2-dioxaphospholane (EOP, 0.73 g, 4.8 mmol) was added, and the reaction was continued in an oil bath at 25°C for 30 minute.
[0065] After the ring-opening reaction, the product was concentrated, and then the concentrated solution was dropped into me...
Embodiment 2
[0066] Example 2: Preparation of folic acid-modified polyphosphate block copolymer (PBYP-b-PEOP-FA)
[0067] After treating the branched vial and the ground glass stopper equipped with a stirring bar according to the method of Example 1, it was filled with nitrogen, and under the condition of nitrogen, folic acid (FA, 0.0159 g, 0.036 mmol), dimethyl sulfoxide (DMSO, 10 mL), dicyclohexylcarbodiimide (DCC, 0.0096 g, 0.0468 mmol), N-hydroxysuccinimide (NHS, 0.0054 g, 0.0468 mmol) and 4-dimethylaminopyridine (DMAP, 0.0057 g, 0.0468 mmol). The reaction bottle was filled with nitrogen, and the reaction was stirred at 25°C for 12 hours. After the reaction, weigh the PBYP 43 -b-PEOP 41 -OH (0.4161 g, 0.0300 mmol) was added to the reaction liquid, and the reaction was continued for 24 hours.
[0068] After the reaction, the product was transferred to a molecular weight cut-off of 3500 g·mol -1 In a dialysis bag, dialyze in deionized water for 24 hours, freeze-dry to obtain a light...
Embodiment 3
[0069] Example Three: Acid-sensitive Tetraethylene Glycol (N 3 -a-TEG-a-N 3 ) preparation
[0070] Weigh tetraethylene glycol (TEG, 0.97 g, 5 mmol) and pyridinium 4-methylbenzenesulfonate (PPTS, 0.2513 g, 1 mmol) into a 100 mL vial equipped with a magnetic stirring bar, add toluene ( 20 mL), azeotropically remove water twice, and then dissolve the azeotropic mixture in anhydrous dichloromethane (30 mL), slowly add 2-chloroethyl vinyl ether (CEVE, 2.5 mL , 25 mmol) and anhydrous dichloromethane (10 mL) into a branched vial, after the dropwise addition, the reaction was stirred in an ice-water bath for 0.5 hours.
[0071] After the reaction was completed, 5% sodium carbonate aqueous solution was added to terminate the reaction, diluted with dichloromethane (30 mL), and then saturated sodium chloride phosphate buffer solution (pH 10.0, 10 mL) was added. The lower organic phase was removed, and the aqueous phase was extracted with dichloromethane (20 mL). The organic phases wer...
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