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Development of oxaliplatin encapsulated in magnetic nanocarriers of pectin as a potential targeted drug delivery for cancer therapy

机译:果胶磁性纳米载体中封装的奥沙利铂作为癌症治疗的潜在靶向药物的开发

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摘要

Superparamagnetic iron oxide nanoparticles (SPIONs) and oxaliplatin (OHP) were in-situ encapsulated in pectin cross-linked with Ca2+ forming 100–200 nm sized magnetically functionalized pectin nanocarriers, referred here as MP-OHP nanocarriers. The scanning electron microscopy (SEM) and transmission electron microscopy (TEM) studies revealed formation of spherical nanostructures. The magnetic measurements by vibration sample magnetometer (VSM) revealed high saturation magnetization (Ms=45.65 emu/g). The superparamagnetic property of MP-OHP was confirmed from the blocking temperature (TB) determined from field cooled and zero field cooled magnetization, measured by superconducting quantum unit interference device (SQUID) magnetometry. The stability of the aqueous dispersion of MP-OHP nanocarriers was confirmed from its high zeta potential (−30.5 mV). The drug encapsulation efficiency (55.2±4.8% w/w) and the drug loading content (0.10±0.04 wt%) in MP-OHP nanocarriers were determined from corresponding platinum contents in OHP and MP-OHP batches measured by inductively coupled plasma mass spectrometry (ICPMS). These nanocarriers exhibited a sustained release of OHP in phosphate buffer solution maintained at pH 5.5 and 7.4, where the drug release profile satisfied a combination of diffusion and swelling controlled mechanism. The cytotoxicity effect of MP-OHP nanocarriers was studied on MIA-PaCa-2 (pancreas) cancer cell line, where the GI50 values were more than 5 mg/mL and it exhibited 10 folds higher cytoxicity than the equivalent concentration of free drug.
机译:将超顺磁性氧化铁纳米颗粒(SPIONs)和奥沙利铂(OHP)原位包裹在与Ca 2 + 交联的果胶中,形成100-200 nm大小的磁性官能化果胶纳米载体,在此称为MP-OHP纳米载体。扫描电子显微镜(SEM)和透射电子显微镜(TEM)研究表明形成了球形纳米结构。振动样品磁力计(VSM)的磁性测量显示出高饱和磁化强度(Ms = 45.65emu / g)。 MP-OHP的超顺磁性是通过通过超导量子单位干涉装置(SQUID)磁力测定法测量的磁场冷却和零磁场冷却的磁化强度确定的结温(TB)确认的。从MP-OHP纳米载体的水分散体的高Zeta电位(-30.5 mV)可以证实其稳定性。 MP-OHP纳米载体中的药物封装效率(55.2±4.8%w / w)和载药量(0.10±0.04 wt%)是通过感应耦合等离子体质谱法测量的OHP和MP-OHP批次中相应的铂含量确定的(ICPMS)。这些纳米载体在维持pH 5.5和7.4的磷酸盐缓冲溶液中表现出OHP的持续释放,其中药物释放曲线满足扩散和溶胀控制机制的组合。研究了MP-OHP纳米载体对MIA-PaCa-2(胰腺)癌细胞系的细胞毒性作用,其GI50值超过5 mg / mL,并且其细胞毒性比同等浓度的游离药物高10倍。

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