结合
化学
纳米载体
硬脂酸
药物输送
菊粉
两亲性
生物结合
细胞毒性
纳米颗粒
壳聚糖
多糖
毒品携带者
褐藻糖胶
生物化学
纳米技术
体外
有机化学
材料科学
共聚物
聚合物
数学分析
数学
作者
Ashok Kumar Jangid,Raghu Solanki,Sunita Patel,Deep Pooja,Hitesh Kulhari
标识
DOI:10.1016/j.ijbiomac.2022.02.031
摘要
Achieving controlled and site-specific delivery of hydrophobic drugs in the colon environment is a major challenge. The primary goal of this research was to synthesize inulin-stearic acid (INU-SA) conjugate and to evaluate its potential in the site-specific delivery of genistein (GEN) for the treatment of colon cancer. INU is a hydrophilic polysaccharide biological macromolecule was modified with hydrophobic SA to form amphiphilic conjugate (INU-SA) which can self-assemble into spherical nanoparticles with interesting drug release properties. The hydrophobic GEN was encapsulated into the INU-SA conjugate to prepare GEN loaded nanoparticles (GNP). The prepared GNP possessed nano size (115 nm), good colloidal dispersibility (0.066 PDI), and high drug encapsulation efficiency (92.2%). The release behaviour of GNP indicated the site-specific release of GEN, only 3.4% at gastric pH while 94% at intestinal pH. The prepared GNP showed potential cytotoxicity against HCT 116 human colorectal cancer cells, as demonstrated by antiproliferation and apoptosis assays. The observed half maximum inhibitory concentration (IC50) value of GNP (5.5 μg/mL) was significantly lower than pure GEN (28.2 μg/mL) due to higher cellular internalization of GNP than free GEN. Therefore, this research suggests a way to improve the therapeutic effectiveness of natural biomolecules using modified and biocompatible polysaccharide INU.
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