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介孔二氧化硅纳米颗粒作为提高紫杉醇药物溶解度的潜在载体。

Mesoporous silica nanoparticles as potential carriers for enhanced drug solubility of paclitaxel.

作者信息

He Yongju, Liang Shuquan, Long Mengqiu, Xu Hui

机构信息

School of Material Science and Engineering, Central South University, Changsha, Hunan 410083, China.

Institute of Super-microstructure and Ultrafast Process in Advanced Materials, School of Physics and Electronics, Central South University, Changsha, Hunan 410083, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Sep 1;78:12-17. doi: 10.1016/j.msec.2017.04.049. Epub 2017 Apr 8.

Abstract

In this study, paclitaxel (PTX), a typical chemotherapeutic agent with poor water-solubility, was selected as the model drug to evaluate the feasibility of mesoporous silica nanoparticles (MSN) to load a hydrophobic drug in different solvents. A sol-gel method was used to synthesize MSN. Drug loading was carried out in three different solvents: dichloromethane, ethanol and dimethyl sulfoxide (DMSO) via a solvent evaporation method, and their effects on drug loading were examined. We further studied the effects of drug loading period and mass ratio of drug to carrier on drug loading capacity of MSN, as well as the in vitro drug release was analyzed. Moreover, the cytotoxic effect of PTX loaded MSN on liver carcinoma (HepG2) cells was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The related materials were characterized by scanning electron microscope (SEM), transmission electron microscope (TEM), dynamic light scattering (DLS), fourier transform infrared spectrometer (FTIR), small-angle x-ray scattering (SAXS), wide-angle x-ray diffraction (XRD) and N adsorption-desorption analyses. The results demonstrated a highly improved solubility of PTX by using MSN as drug carriers compared to free PTX. In addition, drug loading content increased as the solvent polarity parameter decreased or the drug/carrier mass ratio increased. Compared with the blank MSN, the PTX loaded MSN could produce a significant cytotoxicity on HepG2 cells. Our results indicated that MSN could be very potential drug delivery carriers for poorly water soluble drugs.

摘要

在本研究中,选择紫杉醇(PTX)这种典型的水溶性差的化疗药物作为模型药物,以评估介孔二氧化硅纳米颗粒(MSN)在不同溶剂中负载疏水性药物的可行性。采用溶胶 - 凝胶法合成MSN。通过溶剂蒸发法在三种不同溶剂:二氯甲烷、乙醇和二甲基亚砜(DMSO)中进行载药,并考察它们对载药的影响。我们进一步研究了载药时间和药物与载体质量比对MSN载药能力的影响,并分析了体外药物释放情况。此外,通过3 -(4,5 - 二甲基噻唑 - 2 - 基)- 2,5 - 二苯基四氮唑溴盐(MTT)法评估载PTX的MSN对肝癌(HepG2)细胞的细胞毒性作用。相关材料通过扫描电子显微镜(SEM)、透射电子显微镜(TEM)、动态光散射(DLS)、傅里叶变换红外光谱仪(FTIR)、小角X射线散射(SAXS)、广角X射线衍射(XRD)和N吸附 - 脱附分析进行表征。结果表明,与游离PTX相比,使用MSN作为药物载体可显著提高PTX的溶解度。此外,载药量随着溶剂极性参数降低或药物/载体质量比增加而增加。与空白MSN相比,载PTX的MSN对HepG2细胞可产生显著的细胞毒性。我们的结果表明,MSN可能是水溶性差的药物非常有潜力的药物递送载体。

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