Colon Targeted Delivery and In Vitro Evaluation of Curcumin for Colon Cancer

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2023-08-30 DOI:10.2174/2210303113666230830125337
A. Pandey, U. Sara
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Abstract

The second most common cause of mortality by cancer is thought to be colorectal cancer, which is one of the most prevalent tumours in the world. Many health advantages have been linked to curcumin, which is the key component of turmeric. The goal of the current study was to create a colon-targeted microbead method coated with Eudragit S100 to improve curcumin targeting in the colon by speeding up the rate of its dissolution. The ionotropic gelation process was used to create the formulations. The surface phenomena, bead shape, entrapment effectiveness, drug loading, and in vitro drug release were all assessed for formulations. Moreover, calcium alginate beads with an improved core were enteric coated with Eudragit S100. The polymer concentration and curing duration significantly affected particle size and entrapment effectiveness, respectively. The particle size of the improved formulation was 705 µm, drug entrapment efficiency was 83.56%, drug loading was 28.64%, and in vitro release was 81.66% after 6 hours in phosphate buffer at pH 6.8. After 10 hours, enteric coating with Eudragit S100 of optimized calcium alginate microbeads revealed a 64.09±0.16% drug release. The calculated values of the regression coefficients for the Higuchi, first-order, and zero-order models were 0.9494, 0.8913, and 0.9579, respectively. The 50% inhibitory concentration value was 2.676 based on the percentage of cell viability. To effectively treat colorectal cancer, the enteric-coated calcium alginate microbeads can deliver curcumin selectively to the colon when taken orally.
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姜黄素结肠靶向递送及对结肠癌的体外评价
第二常见的癌症致死原因被认为是结直肠癌,这是世界上最常见的肿瘤之一。许多健康益处都与姜黄素有关,姜黄素是姜黄的关键成分。本研究的目的是建立一种以Eudragit S100包被的结肠靶向微珠方法,通过加快姜黄素的溶解速度来提高其在结肠中的靶向性。该配方采用了离子化胶凝工艺。对制剂的表面现象、珠状、包封效果、载药量和体外释药进行了评价。此外,改良核心的海藻酸钙珠被乌龙茶S100肠溶包被。聚合物浓度和固化时间分别对粒径和包埋效果有显著影响。改进后的配方粒径为705µm,包封率为83.56%,载药量为28.64%,在pH为6.8的磷酸盐缓冲液中作用6 h,体外释放率为81.66%。经优化后的海藻酸钙微球经Eudragit S100肠溶后10 h,释药率为64.09±0.16%。Higuchi模型、一阶模型和零阶模型的回归系数计算值分别为0.9494、0.8913和0.9579。根据细胞存活率计算,50%抑制浓度为2.676。为了有效治疗结直肠癌,肠道包被的海藻酸钙微珠口服后可以选择性地将姜黄素输送到结肠。
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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