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Synthesis and characterization of a pH responsive and mucoadhesive drug delivery system for the controlled release application of anti-cancerous drug
Arabian Journal of Chemistry ( IF 6 ) Pub Date : 2020-05-01 , DOI: 10.1016/j.arabjc.2020.03.005
R. Surya , Manohar D. Mullassery , Noeline B. Fernandez , Diana Thomas , Prasad S. Jayaram

Abstract In this work a novel pH sensitive composite, polyacrylamide grafted succinyl chitosan intercalated bentonite (AAm-g-NB/SC) was prepared as a drug carrier system for the controlled delivery of paclitaxel. Characterization of the drug delivery system was carried out using Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), thermal analysis etc. The equilibrium swelling behaviour of the composite was studied and the result showed a maximum at pH 7.4. The in vitro drug release study of paclitaxel indicated that about 15.6% of drug release was found to be occurred at pH 1.2 within 16 h, whereas about 82.5% of drug release was occurred at the intestinal pH condition of 7.4. In vitro biocompatibility study was performed and the result showed good biocompatibility of the composite in the concentration range 6.25–100 µg/mL. The cytotoxicity assay was carried out in cancerous cell line of Human colorectal Adenocarcinoma. Mucous glycoprotein assay study showed that the drug delivery system having good apparent adhering property towards mucin. The investigation indicated that paclitaxel, an anticancer drug can be successfully entrapped in the AAm-g-NB/SC composite for the controlled and targeted delivery for colorectal cancer therapy.

中文翻译:

用于抗癌药物控释应用的 pH 响应和黏膜粘附给药系统的合成与表征

摘要 在这项工作中,制备了一种新型的 pH 敏感复合材料,聚丙烯酰胺接枝琥珀酰壳聚糖插层膨润土(AAm-g-NB/SC)作为紫杉醇可控递送的药物载体系统。使用傅里叶变换红外光谱 (FTIR)、X 射线衍射 (XRD)、扫描电子显微镜 (SEM)、热分析等对药物递送系统进行表征。研究了复合材料的平衡溶胀行为,结果表明在 pH 7.4 时达到最大值。紫杉醇的体外药物释放研究表明,约 15.6% 的药物释放发生在 pH 1.2 的 16 小时内,而约 82.5% 的药物释放发生在肠道 pH 值为 7.4 的条件下。进行了体外生物相容性研究,结果表明复合材料在 6.25–100 µg/mL 的浓度范围内具有良好的生物相容性。细胞毒性试验在人结直肠腺癌的癌细胞系中进行。粘液糖蛋白测定研究表明,药物递送系统对粘蛋白具有良好的表观粘附特性。研究表明,抗癌药物紫杉醇可以成功包埋在 AAm-g-NB/SC 复合物中,用于大肠癌治疗的受控和靶向递送。
更新日期:2020-05-01
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