Encapsulation of Anticancer Drugs (5-Fluorouracil and Paclitaxel) into Polycaprolactone (PCL) Nanofibers and In Vitro Testing for Sustained and Targeted Therapy.

Encapsulation of Anticancer Drugs (5-Fluorouracil and Paclitaxel) into Polycaprolactone (PCL) Nanofibers and In Vitro Testing for Sustained and Targeted Therapy.
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将抗癌药物(5-氟尿嘧啶和紫杉醇)封装到多丙酮酸酯(PCL)纳米纤维中,并在体外测试进行持续和靶向治疗。

DOI:
10.1166/jbn.2017.2353
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发表时间:
2017-04
影响因子:
2.9
通讯作者:
Khan M
Khan M
中科院分区:
工程技术3区
文献类型:
--
作者:
Iqbal S;Rashid MH;Arbab AS;Khan M

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我们报道了一种连续纳米级的抗癌药物5-氟尿嘧啶(FU)和紫杉醇的封装到生物相容性聚己内酯(PCL)纳米纤维(NF)使用核鞘静电纺丝过程。采用19- 23.2kV的高压电场,从专用同轴喷嘴中引出复合溶液射流。在芯和鞘两者中使用DMF导致在50-160 nm内的NF沿着具有大珠状结构。在鞘层中添加三氯甲烷(TCM)或三氟乙醇(TFE)可使纳米纤维的结构更加均匀和细。紫杉醇包覆纤维的直径范围为22-90 nm,包覆率为77.5%,载药量仅为鞘层聚合物的4 ~ 5%。在芯内加入PVA导致鞘外形成药物包封物,包封效率差(52%),在前3天内具有快速初始释放(52-53%)。在不同pH下的NFs的药物释放试验显示,随着介质pH的降低,释放速率增加。在人前列腺癌PC 3细胞中,FU包封的NFs的体外细胞活力试验显示,在5 μM浓度下,38%的细胞存活,而在原始FU中,43%的细胞存活。与原始抗癌药物相比,紫杉醇包封的NF与乳腺癌细胞也表现出增加的功效。细胞密度的持续降低表明癌症药物从NF中缓慢释放。PCL+Paclitaxel和PCL+5 FU处理的条件均导致40%至50%的乳腺癌细胞死亡。
We report a continuous nanoscale encapsulation of cancer drugs 5-Fluorouracil (FU) and Paclitaxel into biocompatible polycaprolactone (PCL) nanofibers (NFs) using core-sheath electrospinning process. A high potential electric field of 19–23.2 kV was used to draw a compound solution jet from a specialized coaxial spinneret. Using of DMF in both core and Sheath resulted in NFs within 50–160 nm along with large beaded structures. Addition of Trichloromethane (TCM) or Trifluoroethanol (TFE) in sheath turned NFs in more uniform and thin fiber structure. The diameter range for paclitaxel encapsulated fibers was 22–90 nm with encapsulation efficiency of 77.5% and the amount of drug was only 4 to 5% of sheath polymer. Addition of PVA within core resulted drug nanocrystal formation outside of sheath and poor encapsulation efficiency (52%) with rapid initial release (52–53%) in first 3 days. Drug release test of NFs in different pH exhibited increase of release rate with the decrease of media pH. In-vitro cell viability test with FU encapsulated NFs in human prostatic cancer PC3 cells exhibited 38% alive cells at 5 μM concentration while in pristine FU 43% cells were alive. Paclitaxel encapsulated NFs with breast cancer cells also exhibited increased efficacy in comparison to pristine anticancer drugs. Continuous decrease of cell density indicated the slow release of cancer drugs from the NFs. Both PCL+Paclitaxel and PCL+5FU treated conditions caused breast cancer cell death between 40% to 50%.
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