3D打印蛇床子素EVA螺旋环状储库型阴道环的制备

    Preparation of Osthole EVA Reservoir Type Spiral Annular Vaginal Rings Using the 3D Printing Technology

    • 摘要:
      目的 通过3D打印技术制备蛇床子素乙烯-醋酸乙烯酯(ethylene vinyl acetate,EVA)螺旋环状储库型阴道环,考察处方因素对其体外释放的影响。
      方法 使用熔融沉积3D打印技术,以蛇床子素和乙烯-醋酸乙烯酯40(EVA40),分别制备蛇床子素EVA40螺旋环状基质型阴道环和蛇床子素EVA40普通环状基质型阴道环;以蛇床子素和EVA40为含药内芯,以乙烯-醋酸乙烯酯9(EVA9)为外层控释层,制备蛇床子素EVA螺旋环状储库型阴道环。使用单因素法考察处方因素对药物体外释放的影响。使用红外光谱法和扫描电镜法对蛇床子素在阴道环中的状态进行表征。
      结果 所有制备的阴道环均为白色,表面平整,外观尺寸与设计一致。蛇床子素EVA40螺旋环状基质型阴道环比蛇床子素EVA40普通环状基质型阴道环具有更高的药物突释量和累积释放量。蛇床子素EVA螺旋环状储库型阴道环的药物突释量显著降低。随着控释层厚度增加,日均释药量降低。红外光谱和扫描电镜证明,蛇床子素结构没有发生变化,且与EVA40相容性较好。
      结论 蛇床子素EVA螺旋环状储库型阴道环能够降低药物前期突释,增强后期药物稳定释放。

       

      Abstract:
      OBJECTIVE To prepare osthole ethylene vinyl acetate(EVA) reservoir type spiral annular vaginal rings using 3D printing technique, to study the effect of prescription factors on the in vitro release of the vaginal ring.
      METHODS Fused deposition modeling 3D printing was employed to prepare osthole-loaded ethylene-vinyl acetate 40 (EVA40) spiral ring matrix-type vaginal rings and osthole-loaded EVA40 conventional ring matrix-type vaginal rings using osthole and EVA40. Osthole-loaded EVA spiral ring reservoir-type vaginal rings were fabricated with osthole, EVA40 as the drug-loaded inner core, and ethylene-vinyl acetate 9 (EVA9) as the outer controlled release layer. The single-factor method was used to evaluate the influence of formulation factors on the in vitro drug release of the drug. The Fourier transform infrared spectroscopy (FT-IR) and the scanning electron microscopy (SEM) were applied to characterize the state of osthole in the vaginal rings.
      RESULTS All prepared vaginal rings appeared white with smooth surfaces, and their external dimensions were consistent with the software design. The osthole-loaded EVA40 spiral ring matrix-type vaginal rings exhibited higher burst release and higher cumulative release than that of the osthole-loaded EVA40 conventional ring matrix-type vaginal rings. The burst release of osthole from the EVA spiral ring reservoir-type vaginal rings was significantly reduced. The daily drug release rate also decreased with the thickness of the controlled release layer increasing. Infrared spectroscopy and scanning electron microscopy proved that the structure of the osthole did not change and had good compatibility with EVA40.
      CONCLUSION  The osthole-loaded EVA spiral ring reservoir-type vaginal ring can reduce the drug burst release and enhance the stable release of drug in the later stage.

       

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