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首页> 外文期刊>RSC Advances >Poly(lactic-co-glycolic) acid nanoparticles improve oral bioavailability of hypocrellin A in rat
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Poly(lactic-co-glycolic) acid nanoparticles improve oral bioavailability of hypocrellin A in rat

机译：聚（乳酸 - 共乙醇酸）酸纳米颗粒改善了大鼠假泌毛蛋白A的口服生物利用度

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摘要

Hypocrellin A (HA), a perihydroxylated polycyclic quinone isolated from the fungus of Shiraia bambusicola, exhibits a wide spectrum of biological activities in pre-clinical studies. However, poor water solubility is a major clinical constraint factor of HA, leading to unpredictable bioavailability. In this study, HA-loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles (PLGA/HA NPs) were prepared by the single-emulsion solvent-evaporation technique. Characterization of PLGA/HA NPs showed that HA was successfully encapsulated on the PLGA. The drug-loading content and encapsulation efficiency (EE) were 7.0% and 57.5%, respectively. The in vitro release profile demonstrated that HA was released more slowly from nanoparticles in pH 1.5 and pH 6.8 than in pH 7.4. Furthermore, the highest solubility of PLGA/HA NPs in aqueous solution was approximately 35.67-fold that of native HA (n-HA). PLGA/HA NPs had more superior stability compared with n-HA in physiological conditions. In this paper, a sample and sensitive LC-MS/MS method was validated for the first time to quantify HA in rat plasma. The pharmacokinetic parameters and bioavailability of HA between PLGA/HA NPs and n-HA were compared after oral administration in rat. The results implied that the relative bioavailability of PLGA/HA NPs was 2.67-fold that of n-HA, and PLGA/HA NPs had a longer half-life. Therefore, these results suggested that PLGA-blend nanoparticles improved the solubility, stability and bioavailability of HA, and could become a potential and promising carrier for the oral delivery of HA.
机译：HypOcrellin A（HA）是从Shiraia Bambusicola的真菌中分离的白唑仑化的多环醌，在临床前研究中表现出广谱的生物活性。然而，不良水溶性是HA的主要临床约束因子，导致不可预测的生物利用度。在该研究中，通过单乳液溶剂蒸发技术制备了HA负载的聚（乳酸共乙醇酸）（PLGA）纳米颗粒（PLGA / HA NPS）。 PLGA / HA NP的表征显示HA已成功包封在PLGA上。药物负载含量和包封效率（EE）分别为7.0％和57.5％。体外释放曲线证明，HA从pH 1.5和pH 6.8中的纳米颗粒中的纳米颗粒释放得更缓慢于pH7.4。此外，PLGA / HA NP在水溶液中的最高溶解度约为天然HA（N-HA）的35.67倍。与在生理条件下的N-HA相比，PLGA / HA NPS具有更优异的稳定性。在本文中，首次验证了样品和敏感的LC-MS / MS方法以在大鼠等离子体中量化HA。在大鼠口服给药后比较PLGA / HA NPS和N-HA之间HA的药代动力学参数和生物利用度。结果暗示PLGA / HA NP的相对生物利用度为N-HA的相对生物利用度为2.67倍，PLGA / HA NPS具有较长的半衰期。因此，这些结果表明，PLGA共混纳米颗粒改善了HA的溶解度，稳定性和生物利用度，并且可以成为HA口服递送的潜在和有前途的载体。

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  • 来源
    《RSC Advances》 |2017年第67期|共10页
  • 作者

    Guo Ling-Yuan; Yan Shu-Zhen; Li Qiang; Xu Qiao; Lin Xi; Qi Shan-Shan; Yu Shu-Qin; Chen Shuang-Lin;

  • 作者单位

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Jiangsu Prov Key Lab Mol &

    Med Biotechnol Nanjing 210046 Jiangsu Peoples R China;

    Nanjing Normal Univ Coll Life Sci Nanjing 210046 Jiangsu Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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