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pH responsive release of paclitaxel by self-assembling Chitosan-ethyl vanillin@GNRs nanocomposites
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2021-08-24 , DOI: 10.1016/j.ijpharm.2021.121047
Ying Fang 1 , KangRui Wang 1 , Qin Li 2 , ChengHong Huang 1
Affiliation  

Carboxylation chitosan achieved by alkalization linked with ethyl vanillin to obtain Chitosan-ethyl vanillin (EV-CMCS) compound through Schiff base reaction and confirmed by FT-IR, UV, XRD, TG and NMR. EV-CMCS refluxed with GNRs for acquisition of EV-CMCS@GNRs nanocomposites for PTX Loading and release. Results demonstrated that both EV-CMCS and EV-CMCS@GNRs are nanoscale composites with excellent solubilization due to their micelle structure taking CMC values of 0.06683 mg/mL and 0.06537 mg/mL. It was found that the loading and encapsulation rate of EV-CMCS and EV-CMCS@GNRs for PTX are 19.59~37.64% and 60.36~80.79% as well as 20.99~37.02% and 58.78~79.77%. Compared with only the delayed release of EV-CMCS that it have 11.5% and 18.7% accumulative release amount for 24 h and 14.9% and 23.7% for 48 h under both pH 6.8 and 7.4, the EV-CMCS@GNRs represent sudden release that it have an accumulative release amount of 90.2% for 24 h and 96.0% for 48 h at pH 6.8. It deduced that the broken Schiff base under acidic condition can increase CMC of EV-CMCS@GNRs, which offered an alternative way for paclitaxel delivery for tumor therapy.



中文翻译:

自组装壳聚糖-乙基香草醛@GNRs纳米复合材料对紫杉醇的pH响应释放

羧化壳聚糖通过碱化与乙基香兰素连接,通过席夫碱反应得到壳聚糖-乙基香兰素(EV-CMCS)化合物,并经FT-IR、UV、XRD、TG和NMR证实。EV-CMCS 与 GNRs 回流以获取用于 PTX 加载和释放的 EV-CMCS@GNRs 纳米复合材料。结果表明,EV-CMCS 和 EV-CMCS@GNRs 都是纳米级复合材料,由于其胶束结构的 CMC 值为 0.06683 mg/mL 和 0.06537 mg/mL,因此具有优异的增溶性。发现 EV-CMCS 和 EV-CMCS@GNRs 对 PTX 的负载和封装率分别为 19.59~37.64% 和 60.36~80.79%,以及 20.99~37.02% 和 58.78~79.77%。与仅缓释EV-CMCS相比,它在pH 6.8和7.4下24小时累积释放量分别为11.5%和18.7%,48小时累积释放量分别为14.9%和23.7%,EV-CMCS@GNRs 代表突然释放,它在 pH 6.8 下 24 小时的累积释放量为 90.2%,48 小时的累积释放量为 96.0%。推断酸性条件下断裂的希夫碱可以增加EV-CMCS@GNRs的CMC,为紫杉醇递送用于肿瘤治疗提供了一种替代途径。

更新日期:2021-08-30
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