Biodegradable microfibers deliver the antitumor drug temozolomide to glioma C6 cells in vitro
Biodegradable microfibers deliver the antitumor drug temozolomide to glioma C6 cells in vitro
复制标题
可生物降解的微纤维在体外将抗肿瘤药物替莫唑胺递送至胶质瘤 C6 细胞
DOI：
10.1691/ph.2010.0156
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发表时间：
2010-11-01
期刊：
影响因子：
1.6
通讯作者：
Liu, Yuguang
中科院分区：
文献类型：
--
作者：
Fan, Xiaoyong;Ni, Shilei;Liu, Yuguang
为了开发用于递送具有低初始突释和低神经毒性的3，4-二氢-3-甲基-4-氧代咪唑并[5，1 -4-d]-不对称-四嗪-8-甲酰胺（替莫唑胺; TM）的有效植入物，通过静电纺丝制备负载TM的聚碳酸亚丙酯（PPC）纤维。然后用藻酸盐（ALG）覆盖一些纤维片。考察了制备工艺参数对药物释放行为的影响。利用扫描电子显微镜和差示扫描量热仪研究了这些纤维的微观形态。观察两种剂型的体外释药特性，并评价其对C6胶质瘤细胞的细胞毒性。使用严格的制备参数，只有当PPC浓度为8重量%，在20 cm处，喷嘴和收集仪器之间的电压为15 kV时，才能获得光滑均匀的纤维。纤维直径约为3 μ m。用ALG覆盖后，药物纤维片的初始破裂减少。细胞毒性实验结果表明，两种形式的药物纤维对C6胶质瘤细胞均有持续的抑制作用，纯药物纤维片具有较强的细胞毒性。我们得出结论：（a）静电纺丝是一种可靠的制造方法M-负载PPC纤维;和（B）ALG涂层减少了纤维片的初始爆裂。
To develop effective implants for delivery of 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-4-d]-as-tetrazine-8-carboxamide (temozolomide; TM) with low initial burst and less neurotoxicity, TM-loaded poly-propylene carbonate (PPC) fiber was fabricated by electrospinning. Some of the fiber sheets were then covered with alginate (ALG). Influences of several preparation parameters on drug delivery behavior were investigated. The micro-morphology of these fibers was studied using scanning electron microscopy and differential scanning calorimetry. In vitro release properties of two forms of samples were observed and their cytotoxicity against C6 glioma cells was assessed. Using strict preparation parameters, smooth and uniform fiber could only be obtained when the PPC concentration was 8 % by weight, at 20 cm and a voltage of 15 kV between the nozzle and the collection instrument. Fiber diameter was about 3 mu m. The initial burst of drug-fiber sheets was reduced after the fiber sheets were covered with ALG. Cytotoxicity test results suggested that both forms of drug fibers inhibit the C6 glioma cells continuously; the pure drug-fiber sheets were strongly cytotoxic. We conclude that (a) electrospinning is a reliable fabrication method for M-loaded PPC fibers; and (b) an ALG coating reduces the initial burst of the fiber sheets.