Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer
Design and development of ligand-appended polysaccharidic nanoparticles for the delivery of oxaliplatin in colorectal cancer
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DOI：
10.1016/j.nano.2009.03.002
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发表时间：
2010-02-01
影响因子：
5.4
通讯作者：
Beg, Aadil M.
中科院分区：
文献类型：
--
作者：
Jain, Anekant;Jain, Sanjay K.;Beg, Aadil M.
制备了透明质酸偶联的壳聚糖纳米颗粒（含奥沙利铂，L-OHP），包被在Eudragit s100包被的微球中，用于结肠肿瘤的有效递送。采用USP溶出度试验桨型仪器研究了该药物在不同模拟胃肠道液体中的体外释放。在治疗实验中，以10 mg /kg体重的L-OHP/透明质酸偶联和不偶联壳聚糖纳米颗粒的剂量口服荷瘤Balb/c小鼠。体内实验数据显示，透明质酸偶联壳聚糖纳米颗粒在作用12小时后，分别在结肠和肿瘤组织中递送1.99 +/- 0.82和9.36 +/- 1.10 μ g的L-OHP/g，反映了其对结肠和肿瘤的靶向潜力。这些给药系统在结肠环境和结肠肿瘤中显示出相对较高的局部药物浓度，并且暴露时间较长，这为结肠癌治疗提供了提高抗肿瘤疗效和低全身毒性的潜力。来自临床编辑：在这项研究中，开发了一种纳米颗粒系统来将奥沙利铂输送到结直肠肿瘤。在小鼠模型中，随着暴露时间的延长，该给药系统在结肠肿瘤中显示出较高的局部药物浓度，这可能会增强其抗肿瘤功效，同时具有较低的系统毒性。(C) 2010爱思唯尔公司版权所有。
Hyaluronic acid-coupled chitosan nanoparticles bearing oxaliplatin (L-OHP) encapsulated in Eudragit S100-coated pellets were developed for effective delivery to colon tumors. The in vitro drug release was investigated using a USP dissolution rate test paddle-type apparatus in different simulated gastrointestinal tract fluids. In therapeutic experiments the pellets of free drug, and hyaluronic acid-coupled and uncoupled chitosan nanoparticles bearing L-OHP were administered orally at the dose of 10 mg L-OHP/kg body weight to tumorbearing Balb/c mice. In vivo data showed that hyaluronic acid-coupled chitosan nanoparticles delivered 1.99 +/- 0.82 and 9.36 +/- 1.10 mu g of L-OHP/g of tissue in the colon and tumor, respectively after 12 hours, reflecting its targeting potential to the colon and tumor. These drug delivery systems show relatively high local drug concentration in the colonic milieu and colonic tumors with prolonged exposure time, which provides a potential to enhance antitumor efficacy with low systemic toxicity for the treatment of colon cancer.From the Clinical Editor: In this study, a nanoparticle system was developed to deliver oxaliplatin to colorectal tumors. In murine models, the drug delivery system showed relatively high local drug concentration in colonic tumors with prolonged exposure time, which provides a potential for enhanced antitumor efficacy with low systematic toxicity. (C) 2010 Elsevier Inc. All rights reserved.