Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar, India.
Nanomedicine. 2010 Feb;6(1):179-90. doi: 10.1016/j.nano.2009.03.002. Epub 2009 May 15.
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 tumor-bearing Balb/c mice. In vivo data showed that hyaluronic acid-coupled chitosan nanoparticles delivered 1.99 +/- 0.82 and 9.36 +/- 1.10 microg 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.
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.
载有奥沙利铂（L-OHP）的透明质酸偶联壳聚糖纳米粒被包封在 Eudragit S100 包衣丸中，用于有效递送至结肠肿瘤。采用 USP 溶出度试验桨式装置在不同模拟胃肠道液中研究了体外药物释放情况。在治疗实验中，将游离药物、透明质酸偶联和未偶联载有 L-OHP 的壳聚糖纳米粒丸以 10 mg L-OHP/kg 体重的剂量口服给予荷瘤 Balb/c 小鼠。体内数据显示，12 小时后，透明质酸偶联壳聚糖纳米粒分别在结肠和肿瘤组织中递送了 1.99 +/- 0.82 和 9.36 +/- 1.10 microg 的 L-OHP/g 组织，反映了其对结肠和肿瘤的靶向潜力。这些药物递送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，并具有延长的暴露时间，这为治疗结肠癌提供了增强抗肿瘤疗效和降低全身毒性的潜力。
在这项研究中，开发了一种纳米颗粒系统来将奥沙利铂递送至结直肠肿瘤。在小鼠模型中，该药物递送系统在延长暴露时间的情况下，在结肠肿瘤中显示出相对较高的局部药物浓度，这为增强抗肿瘤疗效和降低全身毒性提供了潜力。
