Biodegradable amphiphilic polymers, polymer vesicles prepared therefrom and their application in the preparation of drugs for targeted therapy of lung cancer
A polymer and amphiphilic technology, applied in the field of biodegradable polymer materials, can solve the problems of lack of nano-carriers of hydrophilic small-molecule anticancer drugs, and high-efficiency nano-drugs with low toxicity and side effects, so as to overcome the instability of internal circulation , the effect of simplifying the operation steps
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Embodiment 1
[0055] Example 1 Synthesis of cyclic carbonate monomer (CDC) containing disulfide five-membered ring functional group
[0056] Sodium hydrosulfide monohydrate (28.25 g, 381.7 mmol) was dissolved in 400 mL N,N-dimethylformamide (DMF), heated at 50°C until completely dissolved, and dibromoneopentyl glycol (20 g, 76.4 mmol), reacted for 48 hours. The reactant was evaporated under reduced pressure to remove the solvent DMF, then diluted with 200 mL of distilled water, extracted four times with 250 mL of ethyl acetate, and finally the organic phase was rotary evaporated to obtain yellow viscous compound A, yield: 70%; dissolved in 400 mL of tetrahydrofuran Compound A in (THF) was placed in the air for 24 hours, and the intermolecular thiols were oxidized into sulfur-sulfur bonds to obtain compound B with a yield of >98%. Under nitrogen protection, compound B (11.7 g, 70.5 mmol) was dissolved in In dry THF (150 mL), stir until completely dissolved. Following cooling to 0 °C, ethyl...
Embodiment 2
[0057] Example 2 Two-block side chain containing disulfide five-membered ring polymer PEG5k-P (CDC4.9k- co - Synthesis of TMC19k)
[0058] Under a nitrogen atmosphere, 0.1 g (0.52 mmol) of CDC monomer and 0.4 g (3.85 mmol) of trimethylene carbonate (TMC) were dissolved in 3 mL of dichloromethane and added to a sealed reactor, followed by 0.1 g ( 0.02 mmol) CH 3 O-PEG5000 and 0.5 mL catalyst bis(bistrimethylsilyl)amine zinc dichloromethane solution (0.1 mol / L), then seal the reactor well, transfer it out of the glove box, and react in an oil bath at 40 °C for 2 Two days later, the reaction was terminated with glacial acetic acid, precipitated in glacial ether, and finally filtered and vacuum-dried to obtain PEG5k-P (CDC4.9k-co-TMC19.0k). The NMR picture is attached figure 1 , 1 H NMR (400 MHz, CDCl 3 ): 2.08 (t, -COCH 2 CH 2 CH 2 O-), 3.08 (s, -CCH 2 ), 3.30 (m, -OCH 3 ), 3.65 (t, -O CH 2 CH 2 O-), 4.28 (t, -COCH 2 CH 2 CH 2 O-), 4.31 (m, -CCH 2 ). Acco...
Embodiment 3
[0060] Example 3 Two-block side chain containing disulfide five-membered ring polymer Mal-PEG6k-P (CDC4.8k- co - Synthesis of TMC19.2k)
[0061] Under nitrogen atmosphere, 0.1 g (0.52 mmol) of CDC monomer and 0.4 g (3.85 mmol) of TMC were dissolved in 3 mL of dichloromethane and added to the sealed reactor, then 0.12 g (0.02 mmol) of Mal-PEG6000 and 0.1 mol / L catalyst bis(bistrimethylsilyl)amine zinc in dichloromethane solution (0.1 mol / L), then seal the reactor well, transfer it out of the glove box, react in an oil bath at 40 °C for 2 days, and place on ice Acetic acid terminated the reaction, precipitated in glacial ether, and finally filtered and vacuum-dried to obtain Mal-PEG6k-P (CDC4.8k-co-TMC19.2k). 1 H NMR (400 MHz, CDCl 3 ): 2.08 (t, -COCH 2 CH 2 CH 2 O-), 3.08 (s, -CCH 2 ), 3.30 (m, -OCH 3 ), 3.65 (t, -O CH 2 CH 2 O-), 4.28 (t, -COCH 2 CH 2 CH 2 O-), 4.31 (m, -CCH 2 ), and 6.70 (s, Mal). In the following formula calculated by NMR, k=136, x=25, ...
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