College of Chemistry and Chemical Engineering, Ministry of Education, Central South University, Changsha, Hunan 410083, PR China.
Langmuir. 2012 Oct 16;28(41):14553-61. doi: 10.1021/la303062j. Epub 2012 Oct 5.
Nanoencapsulation is a promising method to improve the bioavailability of tea polyphenol (TPP). In this work, we adopted a green process to develop a new kind of complex coacervation core micelles (C3Ms) based on biopolymers for efficient tea polyphenol delivery. First, gelatin-dextran conjugate was synthesized using Maillard reaction. Then the C3Ms were produced by mixing gelatin-dextran conjugate with TPP. Variable factors on the self-assembly of the C3Ms were investigated. Under optimal conditions, the obtained C3Ms are of nanosize (average 86 nm in diameter) with narrow distribution. The formation of the C3Ms is attributed to hydrophobic interaction and hydrogen bonding instead of electrostatic interaction. Transmission electron microscope (TEM) and scanning electron microscope (SEM) results showed that C3Ms have a spherical shape with core-shell structure. ζ-Potential measurement suggested that the core is composed of gelatin with TPP, whereas the shell is composed of dextran segments. The encapsulation efficiency of the C3Ms is pH-independent, but the loading capacity is controllable and as high as 360 wt % (weight/weight of protein). In addition, the C3Ms show sustained release of TPP in vitro. MTT assay revealed that the C3Ms have comparable or even stronger cytotoxicity against MCF-7 cells than free TPP.
纳米胶囊化是提高茶多酚(TPP)生物利用度的一种有前途的方法。在这项工作中,我们采用绿色工艺,基于生物聚合物开发了一种新型的复合凝聚核胶束(C3Ms),用于有效递送茶多酚。首先,通过美拉德反应合成了明胶-葡聚糖缀合物。然后,通过将明胶-葡聚糖缀合物与 TPP 混合来制备 C3Ms。考察了影响 C3Ms 自组装的可变因素。在最佳条件下,得到的 C3Ms 为纳米级(平均直径为 86nm),分布较窄。C3Ms 的形成归因于疏水相互作用和氢键,而不是静电相互作用。透射电子显微镜(TEM)和扫描电子显微镜(SEM)结果表明,C3Ms 呈球形,具有核壳结构。ζ-电位测量表明,核由含有 TPP 的明胶组成,而壳由葡聚糖段组成。C3Ms 的包封效率与 pH 无关,但载药量是可控的,高达 360wt%(蛋白质重量/重量)。此外,C3Ms 在体外显示出 TPP 的持续释放。MTT 测定表明,C3Ms 对 MCF-7 细胞的细胞毒性与游离 TPP 相当,甚至更强。