College of pharmacy, Xinxiang Medical University, 453003, Xinxiang, PR China.
College of pharmacy, Xinxiang Medical University, 453003, Xinxiang, PR China.
Colloids Surf B Biointerfaces. 2018 May 1;165:235-242. doi: 10.1016/j.colsurfb.2018.02.037. Epub 2018 Feb 21.
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.
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。