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载钛茂金属配合物聚己内酯(PCL)电纺纤维的体外抗肿瘤活性增强。

Enhanced in vitro antitumor activity of a titanocene complex encapsulated into polycaprolactone (PCL) electrospun fibers.

机构信息

Department of Industrial Engineering, University of Salerno, Fisciano, Salerno - Italy.

出版信息

J Appl Biomater Funct Mater. 2013 Jun 24;11(1):e61-70. doi: 10.5301/JABFM.5000155.

Abstract

PURPOSE

The purpose of this work was to achieve detailed biomaterials characterization of a drug delivery system for local cancer treatment based on electrospun titanocene trichloride-loaded resorbable polycaprolactone (PCL) fibers.

METHODS

The PCL fibers were characterized for their structural, morphologic and physical properties. The drug release kinetics of the titanocene complex was investigated at different concentrations, to obtain a set of correlations between structure and tuneable release. After exposing cancer cells directly onto the surface of PCL fibers, the anti-proliferative effects of titanocene-loaded PCL were assessed by: (i) counting viable cells via live/dead staining methods, and (ii) analyzing cell apoptosis.

RESULTS AND CONCLUSIONS

Titanocene concentration influenced fiber diameters reduced for PCL filled with titanocene. X-ray analysis suggested that the titanocene, encapsulated into the PCL fibers, is not allowed to crystallize and exists as amorphous aggregates into the fibers. The titanocene release curves presented two stages unrelated to PCL degradation: an initial burst release followed by a release linear with time, extending for a very long time. All of the titanocene-loaded fibers revealed sustained drug release properties suggesting their potential clinical applicability for the treatment of local cancer diseases.

摘要

目的

本工作旨在对局部癌症治疗用载双(三氯合)钛药物输送系统进行详细的生物材料特性分析,该系统基于电纺钛双(三氯合)载可吸收聚己内酯(PCL)纤维。

方法

对 PCL 纤维的结构、形态和物理性能进行了表征。考察了不同浓度下双(三氯合)钛配合物的释药动力学,以获得结构与可调释药之间的一系列相关性。将癌细胞直接暴露在 PCL 纤维表面后,通过:(i)死活染色法计数活细胞,和(ii)分析细胞凋亡,评估载双(三氯合)钛 PCL 的抗增殖作用。

结果和结论

钛双(三氯合)浓度影响纤维直径,填充钛双(三氯合)的 PCL 纤维直径减小。X 射线分析表明,封装在 PCL 纤维内的双(三氯合)钛不能结晶,而是以无定形聚集体存在于纤维内。双(三氯合)钛的释放曲线呈现两个与 PCL 降解无关的阶段:初始突释后,随时间呈线性释放,持续很长时间。所有载双(三氯合)钛的纤维均表现出持续的药物释放特性,表明其在局部癌症治疗中的潜在临床应用。

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