School of Materials Science & Engineering, University of Shanghai for Science and Technology, 516 Jungong Road, Shanghai 200093, China.
School of Materials Science & Engineering, University of Shanghai for Science and Technology, 516 Jungong Road, Shanghai 200093, China.
Int J Pharm. 2020 Jun 15;583:119397. doi: 10.1016/j.ijpharm.2020.119397. Epub 2020 May 4.
Nanostructures and their related structure-performance relationships for "efficacious, safe and convenient" drug delivery are playing a more and more important role in the fast development of nanopharmaceutics. In this study, a core-shell fiber based nano depot (ND) is prepared for achieving a high drug loading and meanwhile ensuring a zero-order drug sustained release profile. With cellulose acetate (CA) as a filament-forming polymeric matrix and ferulic acid (FA) as a model drug, a triaxial electrospinning was implemented to generate the ND. An elaborate strategy was exploited to ensure a continuous, robust and effective preparation. The strategy comprised a solvent mixture as the outer fluid, a mixed solution containing FA and CA with a high CA concentration as the spinnable middle fluid, and a pure drug solution as the inner liquid for loading enough FA in the NDs as much as possible. TEM and SEM demonstrated the core-shell structure of NDs. The NDs had a drug loading of 71.5 ± 4.6%. The in vitro dissolution tests demonstrated that the loaded FA was able to release through a zero-order kinetics of Q (FA released percentage) to t (release time): Q = 12.03 + 1.89 t (R = 0.9928) during the 48 h. Only 3.6% of the loading FA was released during the late tailing-off period. Three different diffusion types about the drug sustained release mechanism are suggested.
用于“高效、安全、便捷”药物输送的纳米结构及其相关的结构-性能关系，在纳米药物学的快速发展中发挥着越来越重要的作用。在本研究中，制备了一种基于核壳纤维的纳米库（ND），以实现高载药量，同时确保零级药物持续释放。以醋酸纤维素（CA）为成丝聚合物基质，以阿魏酸（FA）为模型药物，采用三轴静电纺丝制备 ND。采用一种精心设计的策略来确保连续、稳健和有效的制备。该策略包括溶剂混合物作为外层流体，含有 FA 和 CA 且 CA 浓度较高的混合溶液作为可纺中间流体，以及含有足够 FA 的纯药物溶液作为内层液体，以尽可能多地将 FA 载入 ND 中。TEM 和 SEM 证明了 ND 的核壳结构。ND 的载药量为 71.5±4.6%。体外溶解试验表明，负载的 FA 能够通过零级动力学 Q（FA 释放百分比）对 t（释放时间）进行释放：Q=12.03+1.89t（R=0.9928），在 48 h 内。在后期拖尾期，只有 3.6%的加载 FA 被释放。提出了三种关于药物持续释放机制的不同扩散类型。
