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氧化锌Eudragit FS30D纳米杂化物的合成:结构、表征及其作为肠道药物递送系统的应用。

Synthesis of Zinc Oxide Eudragit FS30D Nanohybrids: Structure, Characterization, and Their Application as an Intestinal Drug Delivery System.

作者信息

Luo Fan, Wang Mingjie, Huang Liting, Wu Ziqian, Wang Wenxiong, Zafar Ayesha, Tian Yunbo, Hasan Murtaza, Shu Xugang

机构信息

School of Chemistry and Chemical Engineering, Zhongkai University of Agriculture and Engineering, Guangzhou 510225, China.

School of Energy and Environment and State Key Laboratory of Marine Pollution, City University of Hong Kong, Kowloon 999077, Hong Kong, China.

出版信息

ACS Omega. 2020 May 13;5(20):11799-11808. doi: 10.1021/acsomega.0c01216. eCollection 2020 May 26.

Abstract

The present study was designed to develop multifunctional zinc oxide-encapsulated Eudragit FS30D (ZnO/EFS) nanohybrid structures as a biodegradable drug delivery system and as a promising successful carrier for targeting sites. The solvent evaporation method was used to fabricate the ZnO/EFS nanohybrids and the size, shape, stability, and antioxidant activity were characterized using transmission electron microscopy (TEM), scanning electron microscopy (SEM), X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), thermogravimetric analysis (TGA), and an antioxidant (1,1-diphenyl-2-picrylhydrazyl (DPPH)). Zinc oxide-encapsulated Eudragit FS30D (ZnO/EFS) nanohybrid structures consisted of irregularly shaped, 297.65 nm-sized ZnO/EFS microcapsule, enduring thermal stability from 251.17 to 385.67 °C. Nano-ZnO was encapsulated in EFS through the formation of hydrogen bonds, and the average encapsulation efficiency for nano-ZnO was determined to be 96.12%. In vitro intestinal-targeted drug release assay provided 91.86% with free nano-ZnO, only 9.5% in acidified ZnO/EFS nanohybrid structure but the rate ZnO/EFS nanohybrids reached 93.11% in succus entericus resultantly modified nano-ZnO was proven proficient intestinal-specific delivery system. The stability of the ZnO/EFS nanohybrid structures was confirmed using ζ-potential and antioxidant activity analysis. Hence, the EFS nanoencapsulation strategy of ZnO provided a stable, nontoxic, and pharmacokinetically active intestine-specific system that can become the best choice for an effective oral feed additive in future.

摘要

本研究旨在开发多功能氧化锌包裹的Eudragit FS30D(ZnO/EFS)纳米杂化结构,作为一种可生物降解的药物递送系统以及一种有前景的靶向部位成功载体。采用溶剂蒸发法制备ZnO/EFS纳米杂化物,并使用透射电子显微镜(TEM)、扫描电子显微镜(SEM)、X射线衍射(XRD)、傅里叶变换红外(FTIR)光谱、动态光散射(DLS)、热重分析(TGA)和抗氧化剂(1,1-二苯基-2-苦基肼(DPPH))对其尺寸、形状、稳定性和抗氧化活性进行表征。氧化锌包裹的Eudragit FS30D(ZnO/EFS)纳米杂化结构由形状不规则、尺寸为297.65 nm的ZnO/EFS微胶囊组成,热稳定性在251.17至385.67℃之间。纳米氧化锌通过氢键形成被包裹在EFS中,纳米氧化锌的平均包封率测定为96.12%。体外肠道靶向药物释放试验表明,游离纳米氧化锌的释放率为91.86%,酸化的ZnO/EFS纳米杂化结构中仅为9.5%,但ZnO/EFS纳米杂化物在肠液中的释放率达到93.11%,结果证明改性纳米氧化锌是一种高效的肠道特异性递送系统。通过ζ电位和抗氧化活性分析证实了ZnO/EFS纳米杂化结构的稳定性。因此,ZnO的EFS纳米包封策略提供了一种稳定、无毒且具有药代动力学活性的肠道特异性系统,未来有望成为有效的口服饲料添加剂的最佳选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e83e/7254796/66f1c5401985/ao0c01216_0001.jpg

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