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吉非替尼和紫杉醇单药及双药负载血蚶壳衍生文石型碳酸钙纳米颗粒的合成与表征

Synthesis and Characterization of Gefitinib and Paclitaxel Mono and Dual Drug-Loaded Blood Cockle Shells ()-Derived Aragonite CaCO Nanoparticles.

作者信息

Chemmalar S, Intan-Shameha Abdul Razak, Abdullah Che Azurahanim Che, Ab Razak Nor Asma, Yusof Loqman Mohamad, Ajat Mokrish, Gowthaman N S K, Bakar Md Zuki Abu

机构信息

Natural Medicines and Products Research Laboratory, Institute of Bioscience, Universiti Putra Malaysia (UPM), Serdang 43400, Selangor, Malaysia.

Department of Veterinary Preclinical Sciences, Faculty of Veterinary Medicine, Universiti Putra Malaysia (UPM), Serdang 43400, Selangor, Malaysia.

出版信息

Nanomaterials (Basel). 2021 Aug 2;11(8):1988. doi: 10.3390/nano11081988.

Abstract

Calcium carbonate has slowly paved its way into the field of nanomaterial research due to its inherent properties: biocompatibility, pH-sensitivity, and slow biodegradability. In our efforts to synthesize calcium carbonate nanoparticles (CSCaCONP) from blood cockle shells (), we developed a simple method to synthesize CSCaCONP, and loaded them with gefitinib (GEF) and paclitaxel (PTXL) to produce mono drug-loaded GEF-CSCaCONP, PTXL-CSCaCONP, and dual drug-loaded GEF-PTXL-CSCaCONP without usage of toxic chemicals. Fourier-transform infrared spectroscopy (FTIR) results reveal that the drugs are bound to CSCaCONP. Scanning electron microscopy studies reveal that the CSCaCONP, GEF-CSCaCONP, PTXL-CSCaCONP, and GEF-PTXL-CSCaCONP are almost spherical nanoparticles, with a diameter of 63.9 ± 22.3, 83.9 ± 28.2, 78.2 ± 26.4, and 87.2 ± 26.7 (nm), respectively. Dynamic light scattering (DLS) and N adsorption-desorption experiments revealed that the synthesized nanoparticles are negatively charged and mesoporous, with surface areas ranging from ~8 to 10 (m/g). Powder X-ray diffraction (PXRD) confirms that the synthesized nanoparticles are aragonite. The CSCaCONP show excellent alkalinization property in plasma simulating conditions and greater solubility in a moderately acidic pH medium. The release of drugs from the nanoparticles showed zero order kinetics with a slow and sustained release. Therefore, the physico-chemical characteristics and in vitro findings suggest that the drug loaded CSCaCONP represent a promising drug delivery system to deliver GEF and PTXL against breast cancer.

摘要

碳酸钙因其固有的生物相容性、pH敏感性和缓慢的生物降解性等特性,已逐渐进入纳米材料研究领域。在我们从血蚶壳合成碳酸钙纳米颗粒(CSCaCONP)的过程中,我们开发了一种简单的方法来合成CSCaCONP,并将吉非替尼(GEF)和紫杉醇(PTXL)负载于其上,以制备单药负载的GEF-CSCaCONP、PTXL-CSCaCONP以及双药负载的GEF-PTXL-CSCaCONP,且无需使用有毒化学物质。傅里叶变换红外光谱(FTIR)结果表明药物与CSCaCONP结合。扫描电子显微镜研究显示,CSCaCONP、GEF-CSCaCONP、PTXL-CSCaCONP和GEF-PTXL-CSCaCONP均为近似球形的纳米颗粒,直径分别为63.9±22.3、83.9±28.2、78.2±26.4和87.2±26.7(纳米)。动态光散射(DLS)和N吸附-脱附实验表明,合成的纳米颗粒带负电荷且为介孔结构,表面积范围约为8至10(平方米/克)。粉末X射线衍射(PXRD)证实合成的纳米颗粒为文石。CSCaCONP在模拟血浆条件下表现出优异的碱化性能,在中等酸性pH介质中的溶解度更高。纳米颗粒中药物的释放呈现零级动力学,具有缓慢且持续的释放特性。因此,物理化学特性和体外研究结果表明,负载药物的CSCaCONP是一种有前景的药物递送系统,可用于递送GEF和PTXL以对抗乳腺癌。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6877/8398682/d7b4b72d7e5a/nanomaterials-11-01988-g0A1.jpg

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