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目的合成甘草次酸-聚乙二醇-胆固醇偶合物,并运用该材料制备具有肝细胞靶向作用的阳离子脂质体DNA复合物。方法丁二酰化甘草次酸和丁二酰化胆固醇与聚乙二醇通过酯键偶联,合成甘草次酸-聚乙二醇-胆固醇偶合物,并通过芘荧光探针法测定其临界胶束浓度;采用前、后聚乙二醇化法制备阳离子脂质体DNA复合物,以粒径为指标优选制备工艺。结果甘草次酸-聚乙二醇-胆固醇偶合物是一种具有低临界胶束浓度的载体材料,临界胶束质量浓度为5.9×10-4～3×10-3g.L-1;前、后聚乙二醇化法制备的阳离子脂质体DNA复合物粒径分别为(297.9±8.16),(178.7±5.4)nm,Zeta电位分别为(28.34±1.23),(26.72±0.52)mV。结论具有低临界胶束浓度的甘草次酸-聚乙二醇-胆固醇偶合物合成工艺简单、成本低廉,宜用于聚乙二醇化法制备具有潜在肝细胞靶向的阳离子脂质体DNA复合物。
Objective To synthesize glycyrrhetinic acid - polyethylene glycol - cholesterol conjugate and use this material to prepare cationic liposome DNA complex with hepatocyte targeting effect. Methods Glycyrrhetic acid-polyethylene glycol-cholesterol conjugate was synthesized by the coupling of succinylated glycyrrhetinic acid and succinylated cholesterol with polyethylene glycol through the ester bond. The critical gums were determined by pyrene fluorescence probe method Beam concentration; cationic liposome DNA complexes were prepared by the method of PEGylation before and after, and the preparation process was optimized by the particle size. Results Glycyrrhetinic acid-polyethylene glycol-cholesterol conjugate was a carrier material with a low critical micelle concentration of 5.9 × 10-4 ~ 3 × 10-3g.L-1. The particle sizes of the cationic liposome DNA complexes prepared by post-PEGylation were (297.9 ± 8.16) and (178.7 ± 5.4) nm, respectively, with Zeta potentials of (28.34 ± 1.23) and (26.72 ± 0.52) mV, respectively. CONCLUSION Glycyrrhetinic acid-polyethylene glycol-cholesterol conjugates with low critical micelle concentration are simple and inexpensive to synthesize, and suitable for PEGylation of cationic liposome DNA complexes with potential hepatocyte targeting .