超临界CO2流体辅助中性γ-CD-MOF载小白菊内酯工艺优化与体外释放评价

Optimization and in vitro Release Evaluation of Parthenolide-Loaded Neutral γ-CD-MOF Assisted with ScCO2 Fluid

    摘要
  • 摘要:
      目的  以K+离子与γ-环糊精(γ-CD)自组装形成的环糊精金属有机骨架(γ-CD-MOF)作为小白菊内酯(Parthenolide, PTL)的载体, 以期改善PTL的溶解性和稳定性。
      方法  采用溶剂热法制备γ-CD-MOF, 中性化处理得Neu-γ-CD-MOF, 再以超临界CO2流体技术(Supercritical carbon dioxide fluid, scCO2)活化Neu-γ-CD-MOF。考察并优化了scCO2法载药工艺, 对载PTL的Neu-γ-CD-MOF(PTL@Neu-γ-CD-MOF)进行系统表征和体外释药评价。
      结果  scCO2活化后可得分散均一的Neu-γ-CD-MOF。使用scCO2辅助PTL载入Neu-γ-CD-MOF, 载药量可高达26.58%。以优化工艺制备的PTL@Neu-γ-CD-MOF可显著增加PTL的水溶解度, 药物在水中的表观溶解度为PTL原料药的2.2倍, 并显著提高药物溶出速率及累积释放度。
      结论  scCO2法可提高Neu-γ-CD-MOF的载药效率, PTL@Neu-γ-CD-MOF纳米粒可解决PTL低溶解度的问题, 改善药物溶出特征, 从而实现PTL的高效递送。

     

    Abstract:
      OBJECTIVES  Cyclodextrin metal-organic framework (γ-CD-MOF) formed self-assembly by K+ions and γ-cyclodextrin (γ-CD) was used as the carrier of PTL in order to improve its solubility and stability.
      METHODS  γ-CD-MOF was prepared by solvothermal method. Neu-γ-CD-MOF was obtained by neutralization and then activated by supercritical carbon dioxide fluid (scCO2). The preparation of PTL-loaded Neu-γ-CD-MOF assisted with scCO2 method was optimized, and the PTL@Neu-γ-CD-MOF was systematically characterized and evaluated for release in vitro.
      RESULTS  Neu-γ-CD-MOF with nanoscale particle size and uniform dispersion is obtained after scCO2 activation. Drug loading of PTL@Neu-γ-CD-MOF is 26.58% assisted with scCO2. PTL@Neu-γ-CD-MOF significantly increases the water solubility of PTL, and the apparent solubility of PTL in water is 2.2 times of free PTL. The dissolution rate and cumulative release of PTL are both significantly improved.
      CONCLUSION  ScCO2 can improve drug loading efficiency of Neu-γ-CD-MOF, and PTL@Neu-γ-CD-MOF increases the solubility and dissolution rate of PTL effectively.

     

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