甘草苷纳米胶束的制备与评价  

Preparation and evaluation of liquiritin nanomicelles

作　　者：邢小燕[1] 果秋婷[1] 徐长青[1] 惠毅[2] XING Xiaoyan;GUO Qiuting;XU Changqing;HUI Yi(Xianyang Vocational College,Xianyang 712000,China;Shaanxi University of Traditional Chinese Medicine,Xianyang 712000,China)

机构地区：[1]咸阳职业技术学院,咸阳712000 [2]陕西中医药大学,咸阳712000

出　　处：《西北药学杂志》2023年第2期129-134,共6页Northwest Pharmaceutical Journal

基　　金：陕西省咸阳市科技局重点研发计划项目(编号:2020k02-117)。

摘　　要：目的 制备甘草苷纳米胶束(Lip-NMs)以提高药物的渗透性,并通过衰老模型大鼠评估其抗衰老作用。方法 以聚氧乙烯聚氧丙烯醚嵌段共聚物(Pluronic?F127)和聚乙烯己内酰胺-聚醋酸乙烯酯-聚乙二醇接枝共聚物(Soluplus?)作为载体材料,采用溶剂蒸发-薄膜水化分散法将甘草苷制备成纳米胶束,并以临界胶束浓度、稀释稳定性、粒径分布、多聚分散系数(PDI)、Zeta电位和包封率作为评价指标,通过单因素实验确定Lip-NMs处方中Pluronic?F127和Soluplus?用量的配比;考察甘草苷混悬液和Lip-NMs在不同pH介质溶液中的药物释放情况;评估Lip-NMs对Caco-2细胞的毒性,并进行细胞跨膜转运研究;比较甘草苷混悬液和Lip-NMs对D-半乳糖所致衰老模型大鼠的抗衰老作用。结果 通过综合评估确定Lip-NMs的最优处方:Pluronic?F127和Soluplus?的质量比为25∶75;在透射电镜下可观察到Lip-NMs呈圆整球形;Lip-NMs在不同pH介质溶液中均表现为缓慢释药特性;Lip-NMs能够有效提高药物的渗透性;与对照组相比,Lip-NMs可显著提高衰老模型大鼠脑组织中超氧化物歧化酶(superoxide dismutase, SOD)、谷胱甘肽过氧化酶(glutathione peroxidase, GSH-Px)的含量,降低丙二醛(malondialdehyde, MDA)的含量,有效提高脑的抗氧化能力。结论 将Pluronic?F127和Soluplus?作为载体材料,将甘草苷制备成纳米胶束,有望促进药物吸收,达到更好的抗衰老作用。Objective To prepare liquiritin nanomicelles(Liq-NMs) to improve the drug permeability, and to evaluate its anti-aging effect on aging model rats.Methods Poly(oxyethylene)-poly(oxypropylene)-(polyoxyethylene) triblock copolymer(Pluronic?F127) and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer(Soluplus?) were used as carrier materials, and Lip-NMs were prepared by solvent evaporation-film hydration dispersion method. By using critical micelle concentration(CMC), dilution stability, particle size distribution, polydispersity, Zeta potential and encapsulation efficiency as evaluation indicators, the mass ratio of Pluronic?F127 and Soluplus?in Lip-NMs formulations were determined by single factor experiments. The drug release of liquiritin suspension and Lip-NMs in different pH medium solutions was investigated. The toxicity of Lip-NMs to Caco-2 cells was evaluated, and the cell transmembrane transport properties were studied. The anti-aging effects of liquiritin suspension and Lip-NMs on D-galactose-induced aging model rats were compared.Results The optimal formulation of Lip-NMs was determined by comprehensive evaluation: the mass ratio of Pluronic?F127 and Soluplus?was 25∶75. Lip-NMs were observed to be spherical under transmission electron microscope. Lip-NMs showed slow drug release characteristics in different pH medium solutions. Lip-NMs could effectively improve the permeability of drugs. Compared with the control group, Lip-NMs could significantly increase the content of superoxide dismutase(SOD) and glutathione peroxidase(GSH-Px), reduce the content of malondialdehyde(MDA) in the brain tissue of aging model rats. Lip-NMs could effectively improve the antioxidant capacity in the brain.Conclusion Pluronic?F127 and Soluplus?were used as carrier materials to prepare liquiritin into nanomicelles, which was expected to promote drug absorption and achieve better anti-aging effects.

关 键 词：甘草苷 纳米胶束 渗透性 吸收 抗衰老 

分 类 号：R94[医药卫生—药剂学]