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由纳米纤维和微珠组成的用于地塞米松缓释的混合电纺聚己内酯垫

Hybrid Electrospun Polycaprolactone Mats Consisting of Nanofibers and Microbeads for Extended Release of Dexamethasone.

作者信息

Hsu Kuan-Hui, Fang Sheng-Po, Lin Chang-Lin, Liao Yan-Shin, Yoon Yong-Kyu, Chauhan Anuj

机构信息

Chemical Engineering, University of Florida, Gainesville, Florida, 32611-6005, USA.

Electrical and Computer Engineering, University of Florida, Gainesville, Florida, 32611, USA.

出版信息

Pharm Res. 2016 Jun;33(6):1509-16. doi: 10.1007/s11095-016-1894-4. Epub 2016 Mar 14.

Abstract

PURPOSE

We designed electrospun polycaprolactone mats consisting of nanofibers and microbeads for extended delivery of dexamethasone.

METHODS

Thin flexible dexamethasone loaded polycaprolactone mats were prepared by electrospinning. The solvents, polymer loading, voltage and tip-to-collector distance were varied to explore the effects on microstructure of the mats. The microstructure was determined by scanning electron microscope imaging; drug transport was measured and modeled, and X-ray diffraction was used to gauge the crystallinity. Drug transport and X-ray diffraction studies were also conducted with a spin cast film for comparison.

RESULTS

Thin mats, about 10 μm in thickness, were prepared by electrospinning. By controlling the voltage and tip-to-collector distance, we achieved a hybrid structure comprising of nanorods (nanofibers) and microbeads. The release profiles were fitted to the diffusion equation to obtain the diffusivities in the spheres and the rods. The diffusivity in the electrospun nanofibers was significantly lower compared to the casted films due to increased crystallinity, which was estimated from X-ray diffraction analysis. The electrospun hybrid mats sustained drug release for the desired duration of a month, in spite of the small thickness of about 10 μm. By comparison, a ten-fold thicker cast film sustains release for about the same duration suggesting about 100-fold decrease in diffusivity in the electrospun mats due to increased crystallinity.

CONCLUSIONS

Electrospun polycaprolactone mats are optimal for achieving long release durations due to increased crystallinity. Designing a hybrid structure by controlling the electrospinning parameters can be a useful approach to increase the release durations.

摘要

目的

我们设计了由纳米纤维和微珠组成的电纺聚己内酯垫,用于长效递送地塞米松。

方法

通过静电纺丝制备负载地塞米松的薄而柔韧的聚己内酯垫。改变溶剂、聚合物浓度、电压和针尖到收集器的距离,以探究其对垫微观结构的影响。通过扫描电子显微镜成像确定微观结构;测量并模拟药物转运,并使用X射线衍射来评估结晶度。还使用旋涂膜进行药物转运和X射线衍射研究以作比较。

结果

通过静电纺丝制备了厚度约为10μm的薄垫。通过控制电压和针尖到收集器的距离,我们获得了一种由纳米棒(纳米纤维)和微珠组成的混合结构。将释放曲线拟合到扩散方程,以获得球体和棒体中的扩散系数。由于结晶度增加,静电纺纳米纤维中的扩散系数明显低于浇铸膜,这是通过X射线衍射分析估计得出的。尽管静电纺混合垫厚度仅约10μm,但仍能在长达一个月的预期时间内持续释放药物。相比之下,厚度为其10倍的浇铸膜持续释放时间大致相同,这表明由于结晶度增加,静电纺垫中的扩散系数降低了约100倍。

结论

由于结晶度增加,静电纺聚己内酯垫最适合实现长效释放。通过控制静电纺丝参数设计混合结构可能是延长释放时间的一种有效方法。

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