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羧甲基纤维素水凝胶珠包埋石墨烯量子点交联壳聚糖作为 pH 响应性生物纳米复合材料用于口服给药载体。

Encapsulation of graphene quantum dot-crosslinked chitosan by carboxymethylcellulose hydrogel beads as a pH-responsive bio-nanocomposite for the oral delivery agent.

机构信息

Faculty of Chemistry, Shahid Beheshti University, G. C., P. O. Box 19396-4716, Tehran, Iran.

Faculty of Chemistry, Shahid Beheshti University, G. C., P. O. Box 19396-4716, Tehran, Iran.

出版信息

Int J Biol Macromol. 2019 Feb 15;123:389-397. doi: 10.1016/j.ijbiomac.2018.11.118. Epub 2018 Nov 13.

DOI:10.1016/j.ijbiomac.2018.11.118
PMID:30445077
Abstract

Oral delivery most commonly used due to the non-invasive nature and the fact that avoids patient pain and discomfort in compression with the intravenous administration. Herein, the obtained graphene quantum dots (GQDs) from citric acid were employed as a cross-linker for chitosan (CS). Sodium salicylate (SS) as a model drug was loaded in the prepared graphene quantum dots-crosslinked chitosan hybrid bio-nanocomposite beads (CS-GQD). SS-loaded CS-GQD (CS-GQD/SS) was protected with pH-sensitive biopolymeric carboxymethylcellulose (CMC) hydrogel beads. The CMC encapsulated CS-GQD/SS bio-nanocomposite hydrogel beads (CS-GQD/SS@CMC) were characterized using FT-IR, PL and SEM analysis. For determination of surficial charge of the carrier, pH point of zero charges (pH) was measured. In-vitro drug delivery tests were carried out in simulating the gastrointestinal tract conditions for proving the efficiency of the prepared beads as a controlled oral drug delivery. The synergistic effects of CMC and CS enhanced the stability of drug dosing for a long time with controlling the drug releases in the gastrointestinal tract conditions. The MTT test confirmed that the bio-nanocomposite beads have low toxicity against human colon adenocarcinoma HT29 cells. The obtained results showed that the prepared novel CS-GQD/SS@CMC could potentially be used as a safe carrier for oral drug delivery.

摘要

口服给药最常用,因为它具有非侵入性,并且避免了静脉给药时患者的疼痛和不适。在此,从柠檬酸中获得的石墨烯量子点 (GQDs) 被用作壳聚糖 (CS) 的交联剂。将水杨酸纳 (SS) 作为模型药物载入制备的石墨烯量子点交联壳聚糖杂化生物纳米复合材料珠 (CS-GQD) 中。用 pH 敏感的生物聚合物羧甲基纤维素 (CMC) 水凝胶珠对 SS 负载的 CS-GQD (CS-GQD/SS) 进行保护。使用 FT-IR、PL 和 SEM 分析对 CMC 包封的 CS-GQD/SS 生物纳米复合材料水凝胶珠 (CS-GQD/SS@CMC) 进行了表征。为了确定载体的表面电荷,测量了 pH 值零电荷点 (pH)。在模拟胃肠道条件下进行了体外药物释放试验,以证明所制备的珠作为控制口服药物释放的有效性。CMC 和 CS 的协同作用增强了药物剂量的稳定性,可长时间控制药物在胃肠道条件下的释放。MTT 试验证实,生物纳米复合材料珠对人结肠腺癌细胞 HT29 具有低毒性。所得结果表明,所制备的新型 CS-GQD/SS@CMC 可能可作为口服药物递送的安全载体。

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