Subudhi M Biswaranjan, Jain Ankit, Jain Ashish, Hurkat Pooja, Shilpi Satish, Gulbake Arvind, Jain Sanjay K
Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Central University, Sagar 470 003, (MP), India.
Materials (Basel). 2015 Feb 27;8(3):832-849. doi: 10.3390/ma8030832.
In the present study, Eudragit S100 coated Citrus Pectin Nanoparticles (E-CPNs) were prepared for the colon targeting of 5-Fluorouracil (5-FU). Citrus pectin also acts as a ligand for galectin-3 receptors that are over expressed on colorectal cancer cells. Nanoparticles (CPNs and E-CPNs) were characterized for various physical parameters such as particle size, size distribution, and shape drug release studies revealed selective drug release in the colonic region in the case of E-CPNs of more than 70% after 24 h. cytoxicity assay (Sulphorhodamine B assay) was performed against HT-29 cancer cells and exhibited 1.5 fold greater cytotoxicity potential of nanoparticles compared to 5-FU solution. data clearly depicted that Eudragit S100 successfully guarded nanoparticles to reach the colonic region wherein nanoparticles were taken up and showed drug release for an extended period of time. Therefore, a multifaceted strategy is introduced here in terms of receptor mediated uptake and pH-dependent release using E-CPNs for effective chemotherapy of colorectal cancer with uncompromised safety and efficacy.
在本研究中,制备了Eudragit S100包衣的柑橘果胶纳米颗粒(E-CPNs)用于5-氟尿嘧啶(5-FU)的结肠靶向给药。柑橘果胶还作为半乳糖凝集素-3受体的配体,该受体在结肠癌细胞上过度表达。对纳米颗粒(CPNs和E-CPNs)的各种物理参数进行了表征,如粒径、粒径分布和形状。药物释放研究表明,在24小时后,E-CPNs在结肠区域的药物释放选择性超过70%。对HT-29癌细胞进行了细胞毒性测定(磺基罗丹明B测定),结果显示纳米颗粒的细胞毒性潜力比5-FU溶液高1.5倍。数据清楚地表明,Eudragit S100成功地保护纳米颗粒到达结肠区域,在该区域纳米颗粒被摄取并长时间显示药物释放。因此,本文引入了一种多方面的策略,即使用E-CPNs进行受体介导的摄取和pH依赖性释放,以实现对结肠癌的有效化疗,同时保证安全性和有效性。