<i>In-Vitro</i> Assessment of Magnetic Dextran-Spermine Nanoparticles for Capecitabine Delivery to Cancerous Cells

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.