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基于两亲性壳聚糖衍生物的脂质体:作为红景天苷缓释载体的合成、制备和性质。

Amphiphilic chitosan derivatives-based liposomes: synthesis, development, and properties as a carrier for sustained release of salidroside.

机构信息

State Key Laboratory of Food Science and Technology, Nanchang University , Nanchang, Jiangxi 330047, P.R. China.

出版信息

J Agric Food Chem. 2014 Jan 22;62(3):626-33. doi: 10.1021/jf4039925. Epub 2014 Jan 8.

Abstract

A novel amphiphilic chitosan derivative of N,N-dimethylhexadecyl carboxymethyl chitosan (DCMCs) was synthesized. The structure of DCMCs was confirmed via FT-IR and (1)H NMR, and the critical micelle concentration (CMC) was investigated by fluorescence spectroscopy. The results indicated that DCMCs has hydrophilic carboxyl and hydrophobic methylene groups and the CMC value was 23.00 mg·L(-1). The polymeric liposomes (DCMCs/cholesterol liposomes, DC-Ls) were developed, and its properties were evaluated. The DC-Ls exhibited multilamellar spheres with positive charge (+73.30 mV), narrow size distribution (PDI = 0.277), and good crystal properties. Salidroside was first to encapsulate into DC-Ls. Compared with traditional liposomes (phosphatidylcholine/cholesterol liposome, PC-Ls), DC-Ls showed higher encapsulation efficiency (82.46%) and slower sustained release rate. The in vitro salidroside release from DC-Ls was governed by two distinct stages (i.e., burst release and sustained release) and was dependent on the pH of the release medium. The case II transport and case I Fichian diffusion were the main release mechanisms for the entire release procedure. These results indicated that DC-Ls may be a potential carrier system for the production of functional foods that contain salidroside or other bioactive food ingredients.

摘要

合成了一种新型两亲性壳聚糖衍生物 N,N-二甲基十六烷基羧甲基壳聚糖(DCMCs)。通过傅里叶变换红外光谱(FT-IR)和(1)H 核磁共振(NMR)对 DCMCs 的结构进行了确认,并通过荧光光谱法研究了临界胶束浓度(CMC)。结果表明,DCMCs 具有亲水性的羧基和疏水性的亚甲基,CMC 值为 23.00mg·L(-1)。制备了聚合物脂质体(DCMCs/胆固醇脂质体,DC-Ls),并对其性质进行了评估。DC-Ls 呈带正电荷(+73.30mV)的多层球体,具有较窄的粒径分布(PDI=0.277)和良好的晶体性质。首次将红景天苷包封到 DC-Ls 中。与传统脂质体(磷脂酰胆碱/胆固醇脂质体,PC-Ls)相比,DC-Ls 具有更高的包封效率(82.46%)和更慢的持续释放速率。DC-Ls 中红景天苷的体外释放遵循两个不同的阶段(即突释和持续释放),并依赖于释放介质的 pH 值。在整个释放过程中,Ⅱ型传递和Ⅰ型 Fichian 扩散是主要的释放机制。这些结果表明,DC-Ls 可能是一种潜在的载药系统,可用于生产含有红景天苷或其他生物活性食品成分的功能性食品。

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