研究动态
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探索以Eudragit L100包覆的富含槲皮素/阿司匹林的壳聚糖纳米粒子在大鼠诱导性结直肠癌治疗中的潜力。

Exploring the potential of quercetin/aspirin-loaded chitosan nanoparticles coated with Eudragit L100 in the treatment of induced-colorectal cancer in rats.

发表日期:2023 Mar 31
作者: Mohammed Elmowafy, Khaled Shalaby, Mohammed H Elkomy, Omar Awad Alsaidan, Hesham A M Gomaa, Omnia M Hendawy, Mohamed A Abdelgawad, Hazim M Ali, Yasmin M Ahmed, Khalid M El-Say
来源: PHARMACOLOGY & THERAPEUTICS

摘要:

越来越多的证据表明槲皮素和阿司匹林可能具有抗癌特性,特别是在结直肠癌的情况下。本研究旨在创建注射用柔性黏性剂Pluronic F127和聚乙二醇4000的固体分散物,加载壳聚糖纳米粒子,实现结肠内的槲皮素和阿司匹林输送。在1:1的聚合物化学计量比下,验证了溶解度和复合物形成。在理想条件下,生成了直径为244.45 ± 8.5 nm,表面电荷为34.1 ± 3.3 mV,包封效率为76.3 ± 4.3%的固体分散物负载的壳聚糖纳米粒子。在某些情况下,涂覆Eudragit L100导致Zeta电位降低和粒径增加。涂覆的配方以pH依赖方式释放活性成分,考虑其物理化学特性。令人惊讶的是,与活性成分悬浮液和未涂覆配方相比,涂覆配方具有更大的抗炎功效,在结肠组织中显着降低了PGE2和IL-8的产生(分别为16.9 ± 7.9 ng/ g组织和134.9 ± 10.1 pg/ g组织)。它还扭转了大多数二甲基肼引起的结肠组织的组织学改变。它还证明在结肠组织中对TNF表达的降低更大。因此,建议使用Eudragit L100涂覆的QT/AS负载壳聚糖纳米粒子提供了结肠输送槲皮素和阿司匹林的潜在平台。©2023年受控释放学会。
Growing evidence suggests quercetin and aspirin may have anticancer properties, notably in the case of colorectal cancer. The goal of this study was to create Pluronic F127 and polyethylene glycol4000 solid dispersion-loaded chitosan nanoparticles for colonic quercetin and aspirin delivery. In 1:1 polymeric stoichiometric ratio, solubility and complex formation were verified. Solid dispersion-loaded chitosan nanoparticles with a diameter of 244.45 ± 8.5 nm, a surface charge of 34.1 ± 3.3 mV, and encapsulation effectiveness of 76.3 ± 4.3% were generated under ideal conditions. In some cases, coating with Eudragit L100 resulted in a decrease in zeta potential and an increase in particle size. The coated formulation released the actives in a pH-dependent manner, considering their physicochemical features. Surprisingly, when compared to the actives' suspension and uncoated formulation, the coated formulation had greater anti-inflammatory efficacy, with a substantial reduction of PGE2 and IL-8 production in colonic tissues (16.9 ± 7.9 ng/g tissue and 134.9 ± 10.1 pg/g tissue, respectively). It also reversed most of the dimethyl hydrazine-induced histological alterations in the colon. It also demonstrated a greater reduction in TNF expression in colonic tissues. As a result, Eudragit L100-coated QT/AS-loaded chitosan nanoparticles are suggested to provide a potential platform for colonic delivery of quercetin and aspirin.© 2023. Controlled Release Society.