木犀草素磷脂复合物介孔二氧化硅纳米粒的制备、表征和药动学研究  

Luteolin phospholipids complex mesoporous silica nanoparticles:Preparation,characterization and pharmacokinetics study

作　　者：房伟[1] 王彦阁 王奎鹏[1] 决利利 FANG Wei;WANG Yange;WANG Kuipeng;JUE Lili(The First Affiliated Hospital of Henan University of TraditionalChinese Medicine,Zhengzhou 450000,China;Zhengzhou University of Industrial Technology,Zhengzhou 451100,China)

机构地区：[1]河南中医药大学第一附属医院,河南郑州450000 [2]郑州工业应用技术学院,河南郑州451100

出　　处：《现代药物与临床》2025年第2期330-340,共11页Drugs & Clinic

基　　金：河南省高等学校重点科研项目计划(23B310010)。

摘　　要：目的制备木犀草素磷脂复合物介孔二氧化硅纳米粒(Lut-PC-MSNs),并进行药动学评价。方法采用溶剂挥发法制备Lut-PC-MSNs。以包封率、载药量、粒径和Zeta电位为指标,选择MSNs粉末与Lut-PC用量比、木犀草素质量浓度和搅拌时间为主要影响因素,Box-Behnken设计-效应面法筛选Lut-PC-MSNs最优处方。进行Lut-PC-MSNs样品表征,考察Lut-PC-MSNs在模拟胃肠液中的释药行为。SD大鼠ig给予Lut-PC-MSNs(以木犀草素计40 mg/kg),测定血药浓度,计算主要药动学参数和相对生物利用度。结果Lut-PC-MSNs最佳处方工艺为:MSNs粉末与Lut-PC用量比为1.45∶1.0,木犀草素质量浓度为1.1 mg/mL,搅拌时间为8.25 h。Lut-PC-MSNs粉末分散于纯化水后即可形成外观均一的混悬液。木犀草素在Lut-PC-MSNs以无定形状态存在。Lut-PC-MSNs在模拟胃肠液中累积释放度明显增加,释药行为符合Weibull模型。Lut-PC-MSNs药动学行为发生很大变化,口服吸收生物利用度提高至5.24倍。结论Lut-PC-MSNs处方简单,贮存稳定性好,显著增加了木犀草素口服吸收生物利用度。Objective To prepare luteolin phospholipids complex mesoporous silica nanoparticles(Lut-PC-MSNs),and evaluate bioavailability.Methods Solvent evaporation method was employed to prepare Lut-PC-MSNs.Entrapment efficiency,drug loading,particle size,and Zeta potential were selected as indexes,MSNs powder to Lut-PC dosage ratio,luteolin concentration,and stirring time were selected as main influencing factors,and Box-Behnken design-response surface methodology was used to screen the optimal prescription of Lut-PC-MSNs.Lut-PC-MSNs samples were characterized,and release behavior in simulate gastrointestinal fluid were also investigated.SD rats were ig administered with Lut-PC-MSNs(calculated by luteolin,40 mg/kg),its main pharmacokinetic parameters and relative bioavailability were calculated.Results Optimal formulation of Lut-PC-MSNs:dosage ratio of MSNs powder to Lut-PC was 1.45∶1.0,luteolin concentration was 1.1 mg/mL,and stirring time was 8.25 h.Lut-PC-MSNs powder could be dispersed in purified water to form a homogeneous suspension with a uniform appearance.Luteolin existed as an amorphous state in Lut-PCMSNs powder,cumulative release rate in simulate gastrointestinal fluid was obviously increased,and drug release behavior accorded with Weibull model.The pharmacokinetic behavior of Lut-PC-MSNs underwent significant changes,and oral bioavailability was increased to 5.24-fold.Conclusion Prescription of Lut-PC-MSNs is simple with its good storage stability,and can significantly increase the bioavailability of luteolin.

关 键 词：木犀草素磷脂复合物介孔二氧化硅纳米粒 木犀草素 包封率 载药量 药动学 生物利用度 

分 类 号：R943[医药卫生—药剂学] R969.1[医药卫生—药学]