首页|波棱瓜子自组装纳米粒的制备及其肠吸收机制研究

波棱瓜子自组装纳米粒的制备及其肠吸收机制研究

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该实验采用微沉淀法制备波棱瓜子自组装纳米粒(micro-precipitation self-assembled nanoparticles,MP-SAN),以平均粒径和多分散指数(polydispersity index,PDI)为评价指标进行工艺优化,并对最终工艺的粒径、PDI、Zeta电位和微观结构进行表征.通过大鼠在体单向肠灌流试验考察MP-SAN中去氢双松柏醇(dehydrodiconiferyl alcohol,DA)和波棱甲素(herpetrione,Her)的肠吸收机制.结果表明,优化的工艺参数为搅拌转速 800 r·min-1,搅拌时间5 min,旋蒸温度40℃.所制得的MP-SAN呈现类球状结构且形态均匀,其平均粒径为(267.63±13.27)nm、PDI为 0.062 0±0.043 9、Zeta电位为(-46.18±3.66)mV.DA在回肠段的吸收速率常数(Ka)和表观吸收系数(Papp)显著高于空肠段(P<0.05),而Her在回肠段和空肠段的吸收无显著差异.当药物浓度升高时,DA和Her的肠吸收参数呈上升趋势,其中高浓度组MP-SAN中DA的Ka 和Papp 显著高于低浓度组(P<0.01).P-糖蛋白抑制剂维拉帕米的加入并未显著影响DA和Her的肠吸收.而加入吲哚美辛后,MP-SAN中DA和Her的吸收均显著增加(P<0.05),表明DA和Her可能是多药耐药相关蛋白 2 的底物.
Preparation and intestinal absorption mechanism of self-assembled nanoparticles of Herpetospermum caudigerum
In this experiment,the micro-precipitation method was used to prepare self-assembled nanoparticles of Herpetospermum caudigerum Wall.(MP-SAN).The process was optimized using average particle size and polydispersity index(PDI)as evaluation indexes.The mean particle size,PDI,zeta potential,and microstructure of MP-SAN were characterized.The intestinal absorption mechanism of dehydrodiconiferyl alcohol(DA)and herpetrione(Her)in MP-SAN was investigated through single-pass intestinal perfusion in rats.The optimized process parameters for producing MP-SAN were a stirring speed of 800 r·min-1,stirring time of 5 min,and rotary evaporation temperature of 40℃.The resulting MP-SAN exhibited a spherical-like structure and uniform morphology,with a mean particle size of(267.63±13.27)nm,a PDI of 0.062 0±0.043 9,and a zeta potential of(-46.18±3.66)mV.The absorption rate constant(Ka)and apparent permeability coefficient(Papp)of DA in the ileal segment were significantly higher than those in the jejunal segment(P<0.05).However,there was no significant difference in the absorption of Her between the ileal and jejunal segments.Intestinal absorption parameters of DA and Her tended to increase with increasing drug concentration.Specifically,the Ka and Papp of DA in MP-SAN in the high-concentration group were significantly higher than those in the low-concentration group(P<0.01).The addition of verapamil,a P-glycoprotein inhibitor,did not significantly affect the intestinal absorption of DA and Her.However,the absorption of both DA and Her in MP-SAN was significantly increased by the addition of indomethacin(P<0.05),suggesting that DA and Her may be substrates for multidrug resistance-associated protein 2.

Herpetospermum caudigerumintestinal absorptionself-assemblednanoparticlessingle-pass intestinal perfusionde-coction

朱煜文、邓翔、陈莉、申宝德、薛玉叶、杭凌宇、袁海龙

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江西中医药大学 现代中药制剂教育部重点实验室,江西 南昌 330004

空军军医大学 空军特色医学中心 药学部,北京 100142

波棱瓜子 肠吸收 自组装 纳米粒 单向肠灌流 汤剂

国家自然科学基金面上项目国家自然科学基金面上项目

8217407481873092

2024

中国中药杂志
中国药学会

中国中药杂志

CSTPCD北大核心
影响因子:1.718
ISSN:1001-5302
年,卷(期):2024.49(12)
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