Sodium Acetate Coated Tenofovir-Loaded Chitosan Nanoparticles for Improved Physico-Chemical Properties.
Sodium Acetate Coated Tenofovir-Loaded Chitosan Nanoparticles for Improved Physico-Chemical Properties.
复制标题
DOI：
10.1007/s11095-015-1795-y
复制
发表时间：
2016-02
影响因子：
3.7
通讯作者：
Youan BB
中科院分区：
文献类型：
--
作者：
Ngo AN;Ezoulin MJ;Murowchick JB;Gounev AD;Youan BB
假设乙酸钠（SA）可用于原位涂覆载药的壳聚糖NP以改善物理化学性质。替诺福韦（TFV）被用作模型药物。通过离子凝胶化制备未涂覆的壳聚糖NP。SA由乙酸与氢氧化钠的半中和原位产生，并在冷冻干燥期间包覆壳聚糖NPs。通过动态光散射、分光光度法、Korsmeyer-Peppas模型、透射电子显微镜（TEM）分别表征纳米粒的理化性质[例如，颗粒平均直径（PMD）和ζ电位（ζ电位）、EE%、药物释放曲线、形态]。熔点（MP）、非水滴定、傅里叶变换红外（FTIR）分析和X射线粉末衍射（XRD）图案评估SA涂覆的壳聚糖NP。通过中性红、刃天青、亚硝酸盐（NO）和细胞因子测定来评估NPs对巨噬细胞Raw 264.7的细胞毒性。FTIR、XRD、MP和TEM数据共同证实SA包覆壳聚糖NP。PMD范围为136-348 nm（未涂覆）和171-379 nm（涂覆）NP。Δ V值范围为+24.3-28.5 mV（无涂层）和0.1-3.1 mV（有涂层）。EE%范围为5.5- 11.7%（未涂覆的NP），并且增加至8-17倍（涂覆后为86.3-92.7%）。SA还防止NP在冷冻干燥期间聚集。核壳型纳米粒对TFV的释放遵循反常转运机制（R2~0.99）。包被的纳米颗粒无细胞毒性（细胞活力~100%），并且没有任何促炎反应。这些SA涂覆的壳聚糖纳米颗粒可能有助于（i）有效封装，（ii）掩盖味道，（iii）控制药物释放并提高药物溶解度。
It is hypothesized that sodium acetate (SA) can be used for in situ coating of drug loaded chitosan NPs for improved physico-chemical properties. Tenofovir (TFV) is used as a model drug. Uncoated chitosan NPs are prepared by ionic gelation. SA is generated in situ from half neutralization of acetic acid with sodium hydroxide, and coats chitosan NPs during freeze-drying. The NPs physico-chemical properties [e.g. particle mean diameters (PMD) and zeta potential (ζ), EE%, drug release profile, morphology] are characterized by dynamic light scattering, spectrophotometry, Korsmeyer-Peppas model, transmission electron microscopy (TEM), respectively. Melting point (MP), non-aqueous titration, Fourier transform infrared (FTIR) analysis, and X-ray powder diffractometry (XRD) pattern evaluated the SA coated chitosan NPs. The NPs cytotoxicity on macrophages Raw 264.7 is assessed by neutral red, resazurin, nitrite oxide (NO) and cytokines assay. Collectively, FTIR, ζ, XRD, MP, and TEM data confirmed that SA coats chitosan NPs. The PMD range is 136–348 nm (uncoated) and 171–379 nm (coated) NPs. The ζ values range is +24.3–28.5 mV (uncoated) and 0.1–3.1 mV (coated). The EE% ranges from 5.5–11.7 % (uncoated NPs) and increased up to 8–17 fold (86.3–92.7% after coating). The SA also prevents NPs aggregation’s during the freeze-drying. The core-shell NPs exhibited a sustain release of TFV following anomalous transport mechanism (R2~0.99). Coated NPs are non-cytotoxic (cell viability ~100%) and without any proinflammatory response. These SA coated chitosan NPs may be useful for (i) efficient encapsulation, (ii) masking tastes, (iii) controlling the release and improving solubility of drug.
登录
查看更多内容
影响因子：
5.8
作者：
Chavanpatil, Mahesh D.;Jain, Paras;Vavia, Pradeep R.
通讯作者：
Vavia, Pradeep R.
影响因子：
5.8
作者：
Bigucci, Federica;Abruzzo, Angela;Luppi, Barbara
通讯作者：
Luppi, Barbara
影响因子：
4.1
作者：
Costa, Cristina;Conte, Amalia;Del Nobile, Matteo Alessandro
通讯作者：
Del Nobile, Matteo Alessandro
影响因子：
6.7
作者：
Introini A;Vanpouille C;Lisco A;Grivel JC;Margolis L
通讯作者：
Margolis L
影响因子：
4.8
作者：
López-García J;Lehocký M;Humpolíček P;Sáha P
通讯作者：
Sáha P