Pinzón-García Ana D, Sinisterra Ruben, Cortes Maria, Mesa Fredy, Ramírez-Clavijo Sandra
Chemistry Department, Instituto de Ciências Exatas, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
Restorative Dentistry Department, Faculty of Dentistry, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
PeerJ. 2021 Oct 27;9:e12124. doi: 10.7717/peerj.12124. eCollection 2021.
Breast cancer is the second leading cause of death in women, and tamoxifen citrate (TMX) is accepted widely for the treatment of hormone receptor-positive breast cancers. Several local drug-delivery systems, including nanofibers, have been developed for antitumor treatment. Nanofibers are biomaterials that mimic the natural extracellular matrix, and they have been used as controlled release devices because they enable highly efficient drug loading. The purpose of the present study was to develop polycaprolactone (PCL) nanofibers incorporating TMX for use in the treatment of breast tumors. Pristine PCL and PCL-TMX nanofibers were produced by electrospinning and characterized physiochemically using different techniques. In addition, an in vitro study of TMX release from the nanofibers was performed. The PCL-TMX nanofibers showed sustained TMX release up to 14 h, releasing 100% of the TMX. The Resazurin reduction assay was used to evaluate the TMX cytotoxicity on MCF-7 breast cancer cell line and PBMCs human. The PCL-TMX nanofiber was cytotoxic toPBMCs and MCF-7. Based on these results, the PCL-TMX nanofibers developed have potential as an alternative for local chronic TMX use for breast cancer treatment, however tissue tests must be done.
乳腺癌是女性死亡的第二大主要原因，枸橼酸他莫昔芬（TMX）被广泛用于治疗激素受体阳性乳腺癌。包括纳米纤维在内的几种局部给药系统已被开发用于抗肿瘤治疗。纳米纤维是模仿天然细胞外基质的生物材料，由于它们能够实现高效的药物负载，因此已被用作控释装置。本研究的目的是开发用于治疗乳腺肿瘤的载有TMX的聚己内酯（PCL）纳米纤维。通过静电纺丝制备原始PCL和PCL-TMX纳米纤维，并使用不同技术对其进行物理化学表征。此外，还对纳米纤维中TMX的释放进行了体外研究。PCL-TMX纳米纤维在长达14小时内显示出TMX的持续释放，释放了100%的TMX。使用刃天青还原试验评估TMX对MCF-7乳腺癌细胞系和人外周血单核细胞（PBMCs）的细胞毒性。PCL-TMX纳米纤维对PBMCs和MCF-7具有细胞毒性。基于这些结果，所开发的PCL-TMX纳米纤维有潜力作为局部长期使用TMX治疗乳腺癌的替代品，然而必须进行组织测试。
