| 华丽萍,翟競.芹菜素混合胶束的制备及其降血糖研究[J].安徽医药,2025,29(5):908-913. |
| 芹菜素混合胶束的制备及其降血糖研究 |
| Preparation of apigenin mixed micelles for the treatment of mellitus |
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| DOI：10.3969/j.issn.1009-6469.2025.05.011 |
| 中文关键词: 芹菜素 混合胶束 生物利用度 糖尿病 |
| 英文关键词: Apigenin Micelles Bioavailability Mellitus |
| 基金项目:国家自然科学基金项目( 82003180) |
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| 摘要点击次数: 57 |
| 全文下载次数: 23 |
| 中文摘要: |
| 目的制备包封芹菜素( API)的普朗尼克 105(P105)和聚乙烯己内酰胺 -聚乙酸乙烯酯 -聚乙二醇接枝共聚物的混合胶束(API-MPMs)，对其主要性质进行表征，并进行药效学和药动学评价。方法 2023年 4―12月，以胶束粒径、载药量和包封率为评价指标，优选最佳载体比例，并用透射电镜观察优选处方的胶束结构，透析袋法考察胶束的体外释放；通过大鼠灌胃给药后，对芹菜素原料药和 API-MPMs的口服生物利用度进行考察，随后考察芹菜素原料药和 API-MPMs对糖尿病小鼠的降糖和肝脏保护作用，并监测相关糖脂代谢指标，最后考察胶束的稳定性。结果当 Soluplus和 P105比例为 3∶1时，制备得到的胶束载药量和包封率最高，分别为( 7.8±0.11)%和( 71.3±0.08)%；透射电镜显示所制备的胶束呈圆球形且粒径均一；药动学实验结果表明 API-MPMs可以显著提高药物的生物利用度，血药达峰浓度( Cmax)为( 211.38±34.32)mg/L，血药浓度 -时间曲线下面积(AUC0-t)为( 2 477.17±208.15)h·mg-1 ·L-1；药效学实验表明 API-MPMs可以显著降低糖尿病小鼠的血糖，血糖由( 9.34±1.44) mmol/L降低至( 7.27±1.89)mmol/L，并可以改善其肝脏受损情况和糖脂代谢情况，其中三酰甘油( TG)、总胆固醇( TC)降低，胰岛素( INS)值显著升高，超氧化物歧化酶( SOD)和血红素氧合酶 1(HO-1)呈现一定的上升，丙二醛( MDA)呈现一定的下降；定性实验表明此胶束在水中、模拟胃肠道环境及模拟生理环境下稳定性良好。结论制备 P105和 Soluplus为混合载体的芹菜稳 |
| 英文摘要: |
| Objective To prepare Apigenin (API) P105/Soluplus mixed micelles, characterize main properties and evaluate pharma-codynamics and pharmacokinetics of mixed micelles.Methods From April to December 2023, particle size, drug loading and encap-sulation efficiency were used as evaluation indicators to optimize the carrier ratio of the formulation. The structure of optimized mixedmicelles was observed by using transmission electron microscopy, and the in vitro release of mixed micelles was investigated by usingdialysis bag method. The bioavailability of API and API-MPMs were compared by oral administration in rats. Subsequently, the effects of API and API-MPMs on diabetic mice were analyzed and glucolipid metabolism related indicators were determined at the same time.Finally, the stability of API-MNMs was conducted by detecting particle size.Results The optimized ratio of Soluplus/P105 was 3∶1,and the obtained micelles exhibited the highest drug loading and encapsulation efficiency, which reached to (7.8±0.11)% and (71.3±0.08)% , respectively. Transmission electron microscopy showed that the micelles were spherical and possessed the uniform particlesize. Pharmacokinetics results in rats showed that the micelles could significantly increase the bioavailability of the drug. Cwas max (211.38±34.32) mg/L and AUC0-t was (2 477.17±208.15) h·mg-1·L-1. Pharmacodynamics experiments showed that the API-MPMs could significantly reduce the blood sugar in diabetes mice, lowering the blood sugar from (9.34±1.44) mmol/L to (7.27±1.89) mmol/L and re-pair the damaged liver and regulate the glycolipid metabolism, in which TC and TG values decreased, INS values increased significant-ly, SOD and HO-1 values increased to a certain extent. The stability experiment showed that the mixed micelles were relatively stablein water, simulated physiological conditions and serum. Conclusion API-P105/Soluplus mixed micelles can increase the solubilityand bioavailability of API, and significantly improve the therapeutic efficacy of API. |
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