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基于壳聚糖和甲氧基聚乙二醇甲基丙烯酸酯-共-聚甲基丙烯酸的聚电解质复合物纳米粒用于布洛芬的口服传递。

Polyelectrolyte complex nanoparticles based on chitosan and methoxy poly(ethylene glycol) methacrylate-co-poly(methylacrylic acid) for oral delivery of ibuprofen.

机构信息

College of pharmacy, Xinxiang Medical University, 453003, Xinxiang, PR China.

College of pharmacy, Xinxiang Medical University, 453003, Xinxiang, PR China.

出版信息

Colloids Surf B Biointerfaces. 2018 May 1;165:235-242. doi: 10.1016/j.colsurfb.2018.02.037. Epub 2018 Feb 21.

Abstract

In this study, the copolymer of methoxy poly(ethylene glycol) methacrylate-co-poly(methylacrylic acid) [poly(mPEGMA-co-MAA)] was synthesized via radical polymerization. Based on this copolymer, novel chitosan-modified poly(mPEGMA-co-MAA) nanoparticles (CS/NPs) were developed to improve the bio-availability of ibuprofen (IBU). Fourier transform infrared spectroscopy (FTIR) and H nuclear magnetic resonance (H NMR) spectra were used to confirm the synthesis of the copolymers. The morphology of CS/NPs was investigated with transmission electron microscopy (TEM). Thermogravimetric analysis (TGA) was used to reveal the thermodynamic properties of the CS/NPs. The cytotoxicity of CS/NPs was assessed by the cell viability of 293T cells. FTIR and H NMR spectra confirmed the synthesis of the novel copolymer. TEM photographs showed that the CS/NPs had a core-shell structure. High cell viability indicated that the CS/NPs were nontoxic. The in vitro release profiles suggested that the CS/NPs released IBU in pH 7.4 buffer in a continuous manner. Furthermore, the IBU-CS/NPs showed a long antifebrile effect. Animal experiments showed that the IBU-CS/NPs had obvious antifebrile effects. Therefore, CS/NPs could reduce the dosing frequency of IBU, and improve its bio-availability.

摘要

在这项研究中,通过自由基聚合合成了甲氧基聚(乙二醇)甲基丙烯酸酯-共-聚(甲基丙烯酸)[聚(mPEGMA-co-MAA)]共聚物。基于该共聚物,开发了新型壳聚糖修饰的聚(mPEGMA-co-MAA)纳米粒子(CS/NPs),以提高布洛芬(IBU)的生物利用度。傅里叶变换红外光谱(FTIR)和 H 核磁共振(H NMR)谱用于证实共聚物的合成。通过透射电子显微镜(TEM)研究了 CS/NPs 的形态。热重分析(TGA)用于揭示 CS/NPs 的热力学性质。通过 293T 细胞的细胞活力评估 CS/NPs 的细胞毒性。FTIR 和 H NMR 谱证实了新型共聚物的合成。TEM 照片显示 CS/NPs 具有核壳结构。高细胞活力表明 CS/NPs 无毒。体外释放曲线表明 CS/NPs 在 pH 7.4 缓冲液中以连续方式释放 IBU。此外,IBU-CS/NPs 表现出持久的解热作用。动物实验表明,IBU-CS/NPs 具有明显的解热作用。因此,CS/NPs 可以减少 IBU 的给药频率,提高其生物利用度。

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