Synthesis and characterization of PEG-graft-quaternized chitosan and cationic polymeric liposomes for drug delivery

Synthesis and characterization of PEG-graft-quaternized chitosan and cationic polymeric liposomes for drug delivery
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DOI:
10.1002/app.35171
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发表时间:
2012-07
影响因子:
3
通讯作者:
Xiaofei Liang;Yanming Sun;Y. Duan;Yingsheng Cheng
Xiaofei Liang;Yanming Sun;Y. Duan;Yingsheng Cheng
中科院分区:
化学3区
文献类型:
--
作者:
Xiaofei Liang;Yanming Sun;Y. Duan;Yingsheng Cheng

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合成了聚乙二醇接枝十八烷基季铵化羧甲基壳聚糖(PEG-g-OQC)共聚物,以改善OQC的生物相容性,并将其与胆固醇和PEG-g-OQC混合,形成PEG化阳离子聚合物脂质体(CPL)。采用傅里叶变换红外光谱(FTIR)、核磁共振氢谱(1H-NMR)和X射线衍射(XRD)对共聚物的结构进行了表征。L929细胞MTT法证实PEG修饰可降低OQC的细胞毒性。通过在混合物中加入不同重量比的PEG-g-OQC可以制备PEG化CPL纳米颗粒(NP)。成功地将紫杉醇掺入PEG化的CPL中,具有高的药物包封率(>90%)和药物负载量(>15%)。物理稳定性实验表明,在加入甘露醇的冷冻干燥条件下和高温高压条件下,载紫杉醇的PEG化CPL稳定性较好,粒径和粒径分布变化不大。载药聚乙二醇化CPL的粉末或试剂显示紫杉醇的缓慢稳定释放曲线。这些结果表明PEG-g-OQC和CPL作为药物递送载体具有潜在的应用。© 2012 Wiley Periodicals,Inc.应用聚合物科学杂志,2012年
Poly(ethylene glycol) grafted octadecyl quaternized carboxymethyl chitosan (PEG-g-OQC) copolymers were synthesized to both improve the biocompatibility of OQC and form PEGylated cationic polymeric liposomes (CPLs), which composed of the mixture of OQC, cholesterol, and PEG-g-OQC. Structure of the copolymers was characterized by using Fourier transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance spectroscopy (1H-NMR), and X-ray diffraction (XRD). The methyl tetrazolium (MTT) assay with L929 cell lines confirmed that PEGylation can decrease the cytotoxicity of OQC. PEGylated CPL nanoparticles (NPs) can be prepared by adding different weight ratio of PEG-g-OQC in the mixture. Paclitaxel was successfully incorporated into PEGylated CPLs with high drug encapsulating efficiency (>90%) and drug loading capacity (>15%). Physical stability experiment showed that paclitaxel-loaded PEGylated CPLs was stable with little change of particle size and size distribution in the condition of freeze-dried by adding mannitol or in high temperature and high pressure. Power or reagent of drug-loaded PEGylated CPLs showed a slow steady release profile for paclitaxel. These results show that PEG-g-OQC and CPLs have potential application as a drug delivery vehicle. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012