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新型壳聚糖衍生物温敏超声双敏感脂质体微泡凝胶

Novel chitosan derivative for temperature and ultrasound dual-sensitive liposomal microbubble gel.

机构信息

School of Pharmacy, Yantai University, Yantai, People's Republic of China.

出版信息

Carbohydr Polym. 2013 Apr 15;94(1):17-23. doi: 10.1016/j.carbpol.2012.12.069. Epub 2013 Jan 5.

Abstract

In this study, a novel liposome-loaded microbubble gel based on N-cholesteryl hemisuccinate-O-sulfate chitosan (NCHOSC) was designed. The structure of the NCHOSC was characterized by FTIR and (1)H NMR. The liposomal microbubble gel based on NCHOSC with a high encapsulation efficiency of curcumin was formed and improved the solubility of curcumin. The diameter of most liposomal microbubble was about 950 nm. The temperature-sensitive CS/GP gel could be formulated at room temperature and would form a gel at body temperature. Simultaneously, the ultrasound-sensitive induced release of curcumin was 85% applying ultrasound. The results of cytotoxicity assay indicated that encapsulated curcumin in Cur-LM or Cur-LM-G was less toxic. The anti-tumor efficacy in vivo suggested that Cur-LM-G by ultrasound suppressed tumor growth most efficiently. These findings have shed some light on the potential NCHOSC material used to liposome-loaded microbubble gel for temperature and ultrasound dual-sensitive drug delivery.

摘要

在这项研究中,设计了一种基于 N-胆甾基琥珀酸半酯-O-磺基壳聚糖(NCHOSC)的新型脂质体负载微泡凝胶。通过傅里叶变换红外光谱(FTIR)和(1)H 核磁共振(NMR)对 NCHOSC 的结构进行了表征。基于 NCHOSC 的载药脂质体微泡凝胶具有较高的姜黄素包封效率,提高了姜黄素的溶解度。大多数脂质体微泡的直径约为 950nm。CS/GP 温敏凝胶可在室温下配制,并在体温下形成凝胶。同时,超声敏感的姜黄素释放率为 85%。细胞毒性实验结果表明,载药姜黄素在 Cur-LM 或 Cur-LM-G 中的毒性较小。体内抗肿瘤效果表明,超声联合 Cur-LM-G 治疗能最有效地抑制肿瘤生长。这些发现为 NCHOSC 材料用于温度和超声双重敏感的载药脂质体微泡凝胶提供了一些启示。

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