Department of Pharmacy and Pharmaceutical Technology, University of Granada, Spain.
Colloids Surf B Biointerfaces. 2010 May 1;77(1):111-6. doi: 10.1016/j.colsurfb.2010.01.030. Epub 2010 Feb 4.
Even though 5-fluorouracil has been demonstrated to display antitumor activity against a wide variety of cancers, high doses are needed to bring out the required therapeutic activity that could simultaneously lead to severe side effects. We hypothesized that the efficient delivery of 5-fluorouracil to tumors using a magnetic nanoplatform could reduce the dose required to obtain sufficient anticancer response. Thus, we have formulated a 5-fluorouracil-loaded magnetic nanomedicine consisting of a magnetic core (iron) and a biocompatible polymeric shell (ethylcellulose). These core/shell nanoparticles were synthesized by an emulsion solvent evaporation process, and 5-fluorouracil loading was assayed by surface incorporation onto the preformed nanocomposites, and by drug incorporation into the magnetic colloid. The contributions of both the surface and the polymeric network to the overall drug loading were investigated by means of optical absorbance and electrophoretic mobility determinations. 5-Fluorouracil entrapment into the polymeric matrix yielded a higher drug loading and a slower drug release profile as compared with drug adsorption. These preliminary results suggest the potential of this stimuli-sensitive drug carrier for cancer targeting.
尽管 5-氟尿嘧啶已被证明对多种癌症具有抗肿瘤活性,但需要高剂量才能发挥所需的治疗活性,而这同时可能导致严重的副作用。我们假设使用磁性纳米平台将 5-氟尿嘧啶有效地递送到肿瘤中,可以减少获得足够抗癌反应所需的剂量。因此,我们已经制备了一种负载 5-氟尿嘧啶的磁性纳米药物,它由磁性核(铁)和生物相容性聚合物壳(乙基纤维素)组成。这些核/壳纳米粒子通过乳液溶剂蒸发法合成,通过表面结合到预先形成的纳米复合材料上以及通过药物掺入磁性胶体中来测定 5-氟尿嘧啶的负载量。通过光吸收和电泳迁移率测定研究了表面和聚合物网络对整体药物负载的贡献。与药物吸附相比,将 5-氟尿嘧啶包埋在聚合物基质中可获得更高的药物负载和更慢的药物释放曲线。这些初步结果表明,这种对刺激敏感的药物载体具有用于癌症靶向的潜力。