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

Iranian Journal of Pharmaceutical Research

关键词: Cancer;    Controlled release;    Drug delivery systems;    Factorial design;    U87MG;   

DOI  :  

学科分类：社会科学、人文和艺术（综合）

来源: Shaheed Beheshti Medical University * School of Pharmacy

【 摘 要 】

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.

【 授权许可】

CC BY