Reversible crosslinked biodegradable polymer vesicle having positive charges on inner membrane, preparation method thereof and application in preparation of antineoplastic drugs
A technology for degrading polymers and anti-tumor drugs, applied in the field of medicine, can solve the problems of small toxic and side effects, high efficiency nanovesicles, and poor efficiency, and achieve the effects of avoiding loss and toxic side effects, efficient loading, and promoting cell proliferation
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Embodiment 1
[0077] Example 1 Synthetic polymer PEG5k-P(DTC4.6k-TMC13.5k)-SP
[0078] The synthesis is divided into two steps. First, ring-opening polymerization is used to prepare PEG5k-P (DTC4.6k-TMC13.5k) diblock copolymer. The specific operation is as follows. Under nitrogen environment, MeO-PEG-OH ( M n = 5.0 kg / mol, 0.20 g, 40 μmol), TMC (0.6 g, 5.9 mmol) and DTC (0.192g, 1.0 mmol) were dissolved in dichloromethane (DCM, 6.8 mL), and the ring-opening polymerization catalyst was added rapidly, Such as zinc bis(bistrimethylsilyl)amine (7.7 mg, 20 μmol). The airtight reactor was sealed and placed under magnetic stirring in an oil bath at 40 °C for 24 hours. After terminating the reaction with glacial acetic acid, precipitate twice in glacial ether, filter with suction, and dry under vacuum at room temperature to obtain the product. Yield: 90.3%. 1 H NMR (400 MHz, DTCl 3 ): PEG: δ 3.38,3.65; TMC: δ 4.24, 2.05; DTC: δ 4.32, 3.02. According to NMR calculation, the molecular weight o...
Embodiment 2
[0082] Example 2 Synthesis of block copolymer Mal-PEG6k-P (DTC4.8k-TMC15.2k)-SP
[0083] The synthesis of Mal-PEG6k-P (DTC4.8k-TMC15.2k)-SP is similar to that of Example 1, and is also divided into two steps, except that the initiator MeO-PEG-OH in the first step is replaced by Malay Imide-functionalized Mal-PEG6k-OH, ring-opening polymerization of TMC and DTC to obtain Mal-PEG6k-P (DTC4.8k-TMC15.2k), then its terminal hydroxyl was activated with NPC, and then reacted with the primary amine of spermine be made of. The specific operation is similar to the first embodiment. Yield: 90.2%. 1H NMR (400 MHz, DTCl3): PEG: δ3.38, 3.65; TMC: δ 4.24, 2.05; DTC: δ 4.32, 3.02, and the characteristic peaks of Mal and spermine. The number-average molecular weight of the polymer was calculated as 6.0-(4.8-15.2)-0.2 kg / mol through the integral ratio of the characteristic peak area.
Embodiment 3
[0084] Example 3 Synthesis of Targeted Diblock Polymer DP8-PEG6.5k-P(DTC6k-TMC15k)
[0085] The synthesis of DP8-PEG6.5k-P(DTC6k-TMC15k) is similar to that of Example 1, which is also divided into two steps. In the first step, the initiator MeO-PEG-OH in the first step of Example 1 is replaced by NHS-PEG6.5k-OH functionalized with N-hydroxysuccinimide, and ring-opening polymerization of TMC and DTC is carried out to obtain NHS-PEG6 .5k-P(DTC6k-TMC15k), that is, add 0.15 g ( 0.781 mmol) DTC, 0.43 g of TMC, 0.2 g ( 0.0154 mmol) NHS-PEG6.5k-OH and 5 ml DCM was dissolved, and then 5.9 mg (0.0154 mmol) of a ring-opening polymerization catalyst such as bis(bistrimethylsilyl)amine zinc was added, and the subsequent treatment was the same as in Example 1. NMR calculated NHS-PEG6.5k-P (DTC6k-TMC15k) by integral area. In the second step, the polypeptide DMAPTVLP (DP8) is added according to the molar ratio of its amino group to NHS-PEG6.5k-P (DTC6k-TMC15k) 3:1, amidation reaction at 30...
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