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首页|期刊导航|广西医科大学学报|甘草酸、姜黄素和羟基喜树碱自组装纳米粒递药系统的工艺优化研究

甘草酸、姜黄素和羟基喜树碱自组装纳米粒递药系统的工艺优化研究OACSTPCD

Study on the process optimization of self-assembled nano-drug delivery system of glycyrrhi-zic acid,curcumin and hydroxycamptothecin

中文摘要英文摘要

目的:以两亲性药物分子甘草酸(GA)、疏水性药物姜黄素(CUR)和羟基喜树碱(HCPT)为材料,通过自组装形式构建GA、CUR和HCPT纳米粒递药系统(GA/CUR/HCPT-NPs),考察其制备工艺并进行质量评价.方法:采用反溶剂沉淀法和透析法相结合制备GA/CUR/HCPT-NPs,利用响应面Box-Behnken法对制备工艺进行优化,最终获得尺寸合适,稳定电荷,高载药量的GA/CUR/HCPT-NPs;并对优化出来的GA/CUR/HCPT-NPs进行核磁共振氢谱(1HNMR)、差示扫描量热法(DSC)、高分辨X射线衍射法(XRD)、傅里叶红外分光光度法(FTIR)、紫外分光光度法(UV)等表征和微观形态观察,并测定GA/CUR/HCPT-NPs中GA、CUR和HCPT含量大小.结果:得到的最优处方为去离子水体积30 mL,二甲基亚砜(DMSO)1 min内滴入去离子水,制备温度为40℃,确定GA、CUR、HCPT投药量分别为6.00 mg、10.03 mg、5.01 mg;测量GA/CUR/HCPT-NPs粒径为(146.37±0.15)nm,且带较高的稳定电荷-(34.43±0.77)mV,PDI为0.157±0.01,透射电子显微镜(TEM)和扫描电子显微镜(SEM)可观察到GA/CUR/HCPT-NPs是类球形或球形,并且均匀分布;1HNMR、DSC、XRD等证明了成功自组装成稳定的GA/CUR/HCPT-NPs,并且在7d内4℃保存条件下稳定性良好;高效液相色谱(HPLC)测定GA/CUR/HCPT-NPs中GA、CUR、HCPT的载药量分别为57.19%、39.17%和3.07%.结论:本研究通过优化的反溶剂沉淀法结合透析法成功制备尺寸合适、均匀分布的GA/CUR/HCPT-NPs,为进一步实验奠定了基础.

Objective:To construct the nano-drug delivery system(GA/CUR/HCPT-NPs)of glycyrrhizic acid(GA),curcumin(CUR)and hydroxycamptocampin(HCPT)with amphiphilic drug molecules GA,hydrophobic drug CUR and HCPT as materials by self-assembly,and to investigate its preparation technology as well as to evaluate its quality.Methods:GA/CUR/HCPT-NPs was prepared by the combination of anti-solvent precipita-tion method and dialysis method,and the preparation process was optimized by response surface methodology(Box-Behnken).Finally,the GA/CUR/HCPT-NPs with suitable size,stable charge and high drug loading was ob-tained,then the optimized GA/CUR/HCPT-NPs was characterized by H nuclear magnetic resonance spectrometer(1HNMR),differential scanning calorimetry(DSC),high-resolution X-ray diffractometer(XRD),Fourier trans-form infrared(FTIR)as well as ultraviolet-uisible spectropho(UV),and it's micromorphology was observed.The contents of GA,CUR and HCPT in GA/CUR/HCPT-NPs were determined.Results:The optimal prescrip-tion was 30 mL deionized water,dimethyl sulfoxide(DMSO)was dropped into the deionized water within 1 min,the preparation temperature was 40℃,and the dosage of GA,CUR and HCPT was determined to be 6.00 mg,10.03 mg and 5.01 mg,respectively.The particle size of GA/CUR/HCPT-NPs was(146.37±0.15)nm,with a high stable charge of(-34.43±0.77)mV,and the polydispersity index(PDI)was 0.157±0.01.GA/CUR/HCPT-NPs was spherical and uniformly distributed under transmission electron microscopy(TEM)and scanning electron micros-copy(SEM).1HNMR,DSC,XRD,etc.demonstrated that GA/CUR/HCPT-NPs had successful self-assembly,and had a great stability when stored at 4℃within 7 days.The drug loading contents of GA,CUR,and HCPT in GA/CUR/HCPT-NPs determined by high-performance liquid chromatography(HPLC)were 57.19%,39.17%,and 3.07%,respectively.Conclusion:In this study,GA/CUR/HCPT-NPs with appropriate size and uniform distribu-tion through optimized anti-solvent precipitation method combined with dialysis method is successfully prepared,which lays a foundation for further experiments.

冯丽珍;靳荣华;黄锦平;刘胜君;王瑶;黄冬怡;黄婷婷;廖伟菊;邓润芳;黄兴振

广西医科大学药学院,南宁 530021

药学

羟基喜树碱姜黄素甘草酸无载体绿色纳米递药系统工艺优化

hydroxycamptothecincurcumingycyrrhizic acidcarrier-free nano-drug delivery systemprocess optimization

《广西医科大学学报》 2024 (004)

598-607 / 10

国家自然科学基金资助项目(No.82360367);广西自然科学基金资助项目(No.2023GXNSFAA026316);广西生物活性分子研究与评价重点实验室资助项目

10.16190/j.cnki.45-1211/r.2024.04.017

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