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由定制天然多糖制备的 Al3+ 离子交联互穿聚合物网络微球。

Al3+ ion cross-linked interpenetrating polymeric network microbeads from tailored natural polysaccharides.

机构信息

School of Pharmaceutical Sciences, IFTM University, Moradabad 244001, Uttar Pradesh, India.

出版信息

Int J Biol Macromol. 2012 Dec;51(5):1173-84. doi: 10.1016/j.ijbiomac.2012.08.029. Epub 2012 Sep 7.

Abstract

Interpenetrating network (IPN) microbeads of sodium carboxymethyl locust bean gum (SCMLBG) and sodium carboxymethyl cellulose (SCMC) containing diclofenac sodium (DS), a non steroidal anti-inflammatory drug were prepared by single water-in-water (w/w) emulsion gelation process using AlCl(3) as cross-linking agent in a complete aqueous environment. The influence of different variables like total polymer concentration, gelation time and crosslinker content on in vitro physico-chemical characteristics and drug release rate in different media was investigated. Drug loaded microbeads were evaluated through Fourier transform infra-red (FTIR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analyses. Scanning electron microscopy (SEM) micrograph of the beads suggested the formation of spherical particles. FTIR analysis indicated the stable nature of the drug in the blend microbeads. DSC and XRD analysis revealed amorphous state of drug after encapsulation. The drug release profile in acidic medium was considerably less in comparison to alkaline media. Formulations showed non-Fickian type transport mechanism. These tri-valent ion crosslinked beads not only improve drug encapsulation efficiency but also enhance drug release in phosphate buffer.

摘要

载有双氯芬酸钠(一种非甾体类抗炎药)的互穿网络(IPN)角豆胶钠(SCMLBG)和羧甲基纤维素钠(SCMC)微球是通过单水包水(w/w)乳液胶凝过程在完全水介质中用三氯化铝(AlCl(3))作为交联剂制备的。考察了不同变量,如总聚合物浓度、凝胶时间和交联剂含量对不同介质中体外物理化学特性和药物释放速率的影响。通过傅里叶变换红外(FTIR)、X 射线衍射(XRD)和差示扫描量热法(DSC)分析对载药微球进行了评价。微球的扫描电子显微镜(SEM)照片表明形成了球形颗粒。FTIR 分析表明药物在共混微球中稳定。DSC 和 XRD 分析表明药物包封后呈无定形态。与碱性介质相比,在酸性介质中的药物释放曲线明显较少。制剂表现出非菲克扩散机制。这些三价离子交联珠不仅提高了药物包封效率,而且增强了在磷酸盐缓冲液中的药物释放。

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