Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.
Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, 576104, India.
Carbohydr Polym. 2021 Jun 1;261:117893. doi: 10.1016/j.carbpol.2021.117893. Epub 2021 Mar 3.
Glycosylated pH-sensitive mesoporous silica nanoparticles (MSNs) of capecitabine (CAP) were developed for targeting colorectal cancer. The MSNs possessed an average pore diameter of 8.12 ± 0.43 nm, pore volume of 0.73 ± 0.21 cm/g, and particle size of 245.24 ± 5.75 nm. A high loading of 180.51 ± 5.23 mg/g attributed to the larger pore volume was observed. The surface of the drug-loaded MSNs were capped with chitosan-glucuronic acid (CHS-GCA) conjugate to combine two strategies viz. pH-sensitive, and lectin receptor mediated uptake. In vitro studies demonstrated a pH-sensitive and controlled release of CAP which was further enhanced in the presence of rat caecal content. Higher uptake of the (CAP-MSN)CHS-GCA was observed in HCT 116 cell lines. The glycosylated nanoparticles revealed reduction in the tumors, aberrant crypt foci, dysplasia and inflammation, and alleviation in the toxic features. This illustrated that the nanoparticles showed promising antitumor efficacy with reduced toxicity and may be used as a effective carrier against cancer.
载有卡培他滨的糖基化 pH 敏感介孔硅纳米粒子（MSNs）被开发用于靶向结直肠癌。MSNs 具有平均孔径为 8.12 ± 0.43nm、孔体积为 0.73 ± 0.21cm/g 和粒径为 245.24 ± 5.75nm。观察到高载药量为 180.51 ± 5.23mg/g，这归因于较大的孔体积。载药 MSNs 的表面用壳聚糖-葡萄糖醛酸（CHS-GCA）缀合物封闭，结合了两种策略，即 pH 敏感和凝集素受体介导的摄取。体外研究表明 CAP 具有 pH 敏感性和控制释放，在存在大鼠盲肠内容物的情况下进一步增强。在 HCT 116 细胞系中观察到（CAP-MSN）CHS-GCA 的摄取增加。糖基化纳米粒子显示出肿瘤、异常隐窝病灶、发育不良和炎症的减少，以及毒性特征的缓解。这表明，纳米粒子表现出有前途的抗肿瘤功效，毒性降低，可作为有效的抗癌载体。
