In-Vitro Assessment of Magnetic Dextran-Spermine Nanoparticles for Capecitabine Delivery to Cancerous Cells

Authors

  • Farzad Kobarfard Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
  • Fatemeh Atyabi Nanotechnology Research Centre, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
  • Maryam Ghadiri Biomedical Engineering Division, Faculty of Chemical Engineering, Tarbiat Modares University, Tehran, Iran.
Abstract:

Cationic polymeric nanoparticles have great potential for developing drug delivery systemswith limited side effects for tumor medication. The goal of this research is investigation ofcationic dextran-spermine polymer (DS) efficacy for improvement of hydrophilic drug deliveryto negatively charged cancerous cells. Capecitabine (as a hydrophilic antineoplastic drug) wasloaded into the magnetic dextran-spermine nanoparticles (DS-NPs) via ionic gelation. Designof experiments was applied to specify how the significant factors affect size, surface charge andcapecitabine entrapment efficiency of the DS-NPs. Physicochemical properties, in-vitro releaseprofile and cellular studies of the optimized DS-NPs were evaluated. The experimental resultsindicated that DS-NPs with favorable properties can be achieved at an optimized condition of2 mg/mL DS and 0.75 mg/mL tri-polyphosphate (TPP) concentrations, TPP addition rate of 35mL/min, pH 3 of DS solution and super paramagnetic iron oxide nanoparticles (SPION)/DSmass ratio of 0.5. The entrapment efficiency of capecitabine was 26.1% at optimum conditionand drug release at neutral pH after 24 h and acidic pH within 3 h was 56 and 98%, respectively.The cytotoxicity assessment exhibited that capecitabine loaded DS-NPs was more toxic thancorresponding free drug as control. Significant cellular uptake of capecitabine loaded DS-NPsby U87MG glioblastoma cells were proved by Prussian blue staining and TEM, qualitatively.DS-NPs are suitable candidates for delivery of the hydrophilic drugs in cancer treatment anddue to positive charge of the dextran-spermine, the uptake of the hydrophilic drugs by thecancerous cells was improved.

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Journal title

volume 16  issue 4

pages  1320- 1334

publication date 2017-11-01

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