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基于静电相互作用的新型羧甲基 Assam Bora 大米淀粉的合成与表征及其作为阳离子抗癌药物控释载体的研究。

Synthesis and characterization of novel carboxymethyl Assam Bora rice starch for the controlled release of cationic anticancer drug based on electrostatic interactions.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi, 110062, India.

Nanoformulation Research Laboratory, Faculty of Pharmacy, Hamdard University, New Delhi, India.

出版信息

AAPS PharmSciTech. 2018 Jan;19(1):134-147. doi: 10.1208/s12249-017-0824-z. Epub 2017 Jun 19.

Abstract

Carboxymethyl Assam Bora rice starch (CM-ABRS) was chemically synthesized in non-aqueous medium with the optimum degree of substitution (DS) of 1.23, and physicochemically characterized by FT-IR, DSC, XRD, and SEM analysis. Comparative evaluation of CM-ABRS with native starch (ABRS) for powder flow characteristics, swelling index, apparent solubility, rheological properties, textural properties, and mucoadhesive studies were carried out. The aim of the current work was to investigate the potential of CM-ABRS as a novel carrier for the water-soluble chemotherapeutic, doxorubicin hydrochloride (DOX). Formation of drug/polymer complex (DOX-CM-ABRS) via electrostatic interaction has been evaluated for the controlled release of DOX in three different pH media (phosphate-buffered saline (PBS), pH 7.4, 6.8, and 5.5). In vitro drug release studies illustrated faster release of drug in PBS at pH 5.5 as compared to pH 6.8 and pH 7.4, respectively, indicating the importance of pH-sensitive drug release from the DOX-CM-ABRS complex in malignant tissues.

摘要

羧甲基 Assam Bora 大米淀粉(CM-ABRS)在非水介质中通过化学合成得到,最佳取代度(DS)为 1.23,并通过傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)、X 射线衍射(XRD)和扫描电子显微镜(SEM)分析进行了物理化学表征。对 CM-ABRS 与天然淀粉(ABRS)的粉末流动特性、溶胀指数、表观溶解度、流变性能、质构性能和粘膜粘附性进行了比较评价。目前的工作旨在研究 CM-ABRS 作为一种新型载体用于水溶性化疗药物盐酸多柔比星(DOX)的潜力。通过静电相互作用形成药物/聚合物复合物(DOX-CM-ABRS),以评估在三种不同 pH 值介质(磷酸盐缓冲盐水(PBS),pH 值 7.4、6.8 和 5.5)中 DOX 的控制释放。体外药物释放研究表明,在 pH 值为 5.5 的 PBS 中药物释放速度较快,与 pH 值为 6.8 和 pH 值 7.4 相比,分别表明在恶性组织中从 DOX-CM-ABRS 复合物中释放 pH 敏感药物的重要性。

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