果胶改性及其在药物递送载体中的应用进展Q

Progress of pectin modification and its application in drug delivery carriers

摘要:

果胶主要是由α-1, 4-D-半乳糖醛酸单元组成的杂多糖，侧基由不同的中性糖残基通过至少22种糖苷键连接而成。相较于纤维素、海藻酸钠及壳聚糖等多糖，果胶具有抗肿瘤，调节血压、血脂和血压等生理活性，为其在药物递送载体中的研究提供了条件。但是，果胶分子量较低，且其分子中含有大量的羟基和羧基官能团，致使果胶具有良好的水溶性，使得果胶基药物递送载体表现出较差的释药性能。尽管如此，通过化学修饰，改变果胶分子中的羟基、羧基、甲酯基以及酰胺基等官能团的含量，可有效改变果胶的亲疏水性和分子量，从而为其在药物递送载体方面的开发提供条件，相关基础研究正在逐渐拓展并展现出较大的应用潜力。基于此，本文对果胶理化性质以及其在药物递送载体制备中的成果进行了梳理和总结，主要包括果胶改性方法、果胶基前药、果胶基复合载体和杂化材料的制备以及果胶基Pickering乳液的制备，并对现阶段上述领域中存在的主要问题和未来发展进行展望。

Abstract:

Pectin is a heteropolysaccharide consisted of α-1, 4-D-galactouronic acid with different neutral sugar residues which was linked by at least 22 glycosidic bonds. Compared with polysaccharides such as cellulose, sodium alginate and chitosan, the unique physiological activities of pectin including anti-tumor, regulating blood pressure, blood lipids and blood pressure provide the potential in drug sustained release carriers. However, the pectin generally present low molecular weight, and consist of abundant hydroxyl and carboxyl groups induced well water solubility of pectin, resulting in its poor release performance. Even so, coordination, nucleophilic addition and elimination reaction can occur on the sites of hydroxyl, carboxyl and amide functional group, which significantly influence its hydrophilic and hydrophobic properties, and molecular weight. Thus, the basic research of pectin-based drug delivery carrier is gradually expanded and show great potential. In this paper, the physicochemical properties of pectin and preparation of drug control-released carrier were reviewed and summarized. It can be divided into modification methods, pectin-based prodrug, hybrid materials, composite materials, and Pickering emulsion. Finally, the main problems and future in these areas are expected.