负载染料木素纳米脂质体的制备 及其体外抗炎活性研究Preparation and in vitro anti-inflammatory activity of genistein-loaded nanoliposomes

Abstract

为了提高染料木素（Gen）的生物利用率以及为脂溶性生物活性物质在新型功能食品中的开发提供参考，采用薄膜分散法，以大豆卵磷脂和胆固醇为原料，制备了负载Gen的纳米脂质体（Gen@Lip），并对其基本指标、结构、储存稳定性、体外释放特性和抗炎活性进行分析。结果表明：制备的Gen@Lip的Gen负载量为36%，Gen@Lip的平均粒径为（242.73±2.03）nm，多分散指数为0.32，Zeta-电位为（-16.33±1.16）mV；结构表征结果证实Gen被有效包埋在Gen@Lip中；Gen@Lip具有良好的储存稳定性；Gen@Lip能够有效地通过胃进入到肠道实现缓释作用；相较于游离的Gen，Gen@Lip对Raw 264.7细胞有更强的抑炎效果，且在使用范围（＜100 μmol/L）内无毒副作用。综上，所制备的Gen@Lip可提高Gen的生物利用率，并具有明显的抗炎效果。To improve the bioavailability of genistein (Gen)as well as to provide a reference for the development of lipid-soluble bioactive substances in novel functional foods, nanoliposomes loaded with Gen (Gen@Lip) were prepared by film dispersion method using soy lecithin and cholesterol as raw materials, and their basic indexes, structure, storage stability, in vitro release characteristics and anti-inflammatory activity were investigated. The results showed that the Gen loading, average particle size, polydispersity index, and Zeta potential of the prepared Gen@Lip was 36%, (242.73±2.03) nm, 0.32 and (-16.33±1.16) mV, respectively. The structural characterization results confirmed that Gen was effectively embedded in Gen@Lip, and Gen@Lip had good storage stability. Gen@Lip was able to efficiently pass through the stomach to enter into the intestines to achieve a slow release effect. Compared with free Gen, Gen@Lip had a stronger anti-inflammatory effect on the Raw 264.7 cells and had no toxic side effects within the range of use (＜100 μmol/L). In conclusion, the Gen@Lip prepared can improve the bioavailability of Gen and has significant anti-inflammatory effects.

Keywords

• 染料木素；脂质体；缓释；抗炎
• genistein; liposomes; slow release; anti-inflammatory