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以果胶磁性纳米载体包裹的奥沙利铂作为癌症治疗潜在靶向给药系统的研发。

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

作者信息

Dutta Raj Kumar, Sahu Saurabh

机构信息

Analytical Chemistry Laboratory, Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee 247667, India.

出版信息

Results Pharma Sci. 2012 May 22;2:38-45. doi: 10.1016/j.rinphs.2012.05.001. eCollection 2012.

DOI:10.1016/j.rinphs.2012.05.001
PMID:25755993
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4210274/
Abstract

Superparamagnetic iron oxide nanoparticles (SPIONs) and oxaliplatin (OHP) were in-situ encapsulated in pectin cross-linked with Ca(2+) 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 (M s=45.65 emu/g). The superparamagnetic property of MP-OHP was confirmed from the blocking temperature (T B) 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.

摘要

超顺磁性氧化铁纳米颗粒(SPIONs)和奥沙利铂(OHP)原位包封于与Ca(2+)交联的果胶中,形成尺寸为100 - 200 nm的磁功能化果胶纳米载体,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)研究显示形成了球形纳米结构。通过振动样品磁强计(VSM)进行的磁性测量显示出高饱和磁化强度(Ms = 45.65 emu/g)。通过超导量子干涉装置(SQUID)磁力测定法从场冷和零场冷磁化强度确定的阻塞温度(TB)证实了MP - OHP的超顺磁性。MP - OHP纳米载体水分散体的稳定性通过其高ζ电位(-30.5 mV)得到证实。通过电感耦合等离子体质谱(ICPMS)测量OHP和MP - OHP批次中的相应铂含量,确定了MP - OHP纳米载体中的药物包封效率(55.2±4.8% w/w)和药物负载量(0.10±0.04 wt%)。这些纳米载体在pH值为5.5和7.4的磷酸盐缓冲溶液中表现出奥沙利铂的持续释放,其药物释放曲线符合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值大于5 mg/mL,并且与游离药物的等效浓度相比,其细胞毒性高10倍。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b29/4210274/dab1fa6a5905/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b29/4210274/dab1fa6a5905/fx1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b29/4210274/dab1fa6a5905/fx1.jpg

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