包载槲皮素P/O/W多重皮克林乳液的制备及表征
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江南大学

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国家重点研发计划资助


Preparation and characterization of P/O/W double Pickering emulsion loaded with quercetin
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Jiangnan University

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National Key R&D Program of China

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    摘要:

    为解决槲皮素溶解度低透皮性能差的问题,以疏水二氧化硅AEROSIL?R202、亲水二氧化硅AEROSIL?200为乳化剂,一缩二丙二醇和甘油为内醇相,制备水包油包醇(P/O/W)多重Pickering乳液,用其对槲皮素进行了包载。考察了内醇相(一缩二丙二醇和甘油)质量分数、疏水二氧化硅AEROSIL?R202质量分数、水乳比、亲水二氧化硅AEROSIL?200质量分数对P/O/W多重Pickering乳液性能的影响,得到最佳制备条件为:内醇相〔m(甘油):m(一缩二丙二醇)=6:4〕质量分数为20%、疏水二氧化硅质量分数为3%、m(水):m(初乳)=5:5、亲水二氧化硅质量分数为2%。对各相染色用激光共聚焦显微镜(CLSM)观察证明,成功制备了P/O/W多重Pickering乳液。X射线衍射仪(XRD)结果表明,槲皮素经多重乳液包载后结晶峰消失,表明该多重乳液对槲皮素有良好的包载效果。离心法测定包载槲皮素P/O/W多重乳液载药量达0.45 %± 0.02%。体外透皮实验和猪皮CLSM显示,槲皮素经该多重乳液包载后透皮性能得到改善,这主要是由于槲皮素在内醇相〔m(甘油):m(一缩二丙二醇)=6:4〕中的溶解度可达60±2.1 mg/g,远大于在水 (<0.5 μg/g)或油 (<1 mg/g)中的溶解度。

    Abstract:

    To solve the problem of low solubility and poor transdermal performance of quercetin, Polyol-in-oil-in-water(P/O/W) double Pickering emulsions were prepared to encapsulate quercetin with hydrophobic silica AEROSIL?R202 and hydrophilic silica AEROSIL?200 as emulsifiers, dipropylene glycol and glycerol as polyol phases. The effects of mass fraction of internal polyol phase (dipropylene glycol and glycerol), mass fraction of hydrophobic silica AEROSIL?R202, water-to-primary emulsion ratio, and mass fraction of hydrophilic silica AEROSIL?200 on the P/O/W double Pickering emulsion were investigated, and the best preparation conditions were: mass fraction of internal alcohol phase〔m(glycerol):m(dipropylene glycol)=6:4〕was 20%, mass fraction of hydrophobic silica was 3%, water-to-emulsion ratio m(water):m(primary emulsion)=5:5, and mass fraction of hydrophilic silica was 2%. Confocal laser scanning microscope (CLSM) observation proved that the P/O/W double Pickering emulsions were successfully prepared. X-ray diffraction (XRD) results showed that the crystalline peak of quercetin disappeared after being encapsulated by the double emulsions, indicating that the double emulsions had a good encapsulation effect on quercetin. The drug loading efficiency of the P/O/W double emulsion loaded with quercetin determined by centrifugation reached (0.45 ± 0.02) %. The in vitro transdermal experiment and pigskin CLSM showed that the transdermal performance of quercetin after the double emulsion encapsulation improved, this is mainly due to the fact that the solubility of quercetin in the internal alcohol phase〔m (glycerol):m (dipropylene glycol) = 6:4〕can reach 60±2.1 mg/g, which is much greater than that in water (<0.5 μg/g/g). g) or solubility in oil (<1 mg/g).

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杨佳慧,梁蓉,杨成.包载槲皮素P/O/W多重皮克林乳液的制备及表征[J].精细化工,2022,39(7):

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  • 收稿日期:2021-12-30
  • 最后修改日期:2022-03-21
  • 录用日期:2022-04-01
  • 在线发布日期: 2022-06-10
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