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通过温度调制固化法制备的载他莫昔芬固体脂质纳米粒的物理化学表征、细胞毒性活性及生物相容性研究

Physico-chemical characterisation, cytotoxic activity, and biocompatibility studies of tamoxifen-loaded solid lipid nanoparticles prepared via a temperature-modulated solidification method.

作者信息

Lakkadwala Sushant, Nguyen Sanko, Lawrence Joseph, Nauli Surya M, Nesamony Jerry

机构信息

Division of Industrial Pharmacy, Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, University of Toledo , Toledo, Ohio , USA .

出版信息

J Microencapsul. 2014;31(6):590-9. doi: 10.3109/02652048.2014.898707. Epub 2014 Apr 3.

Abstract

CONTEXT

Solid lipid nanoparticles (SLNs) can efficiently and efficaciously incorporate anti-cancer agents.

OBJECTIVE

To prepare and characterise tamoxifen (TAM)-loaded SLNs.

MATERIALS AND METHODS

Glyceryl monostearate, Tween-80, and trehalose were used in SLNs. SLNs were tested via dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR).

RESULTS

Characterisation studies revealed SLNs of about 540 nm with a negative surface charge and confirmed the entrapment of TAM in the SLNs. The entrapment efficiency was estimated to be 60%.

DISCUSSION

The in vitro drug release profile demonstrated a gradual increase followed by a release plateau for several days. A drug concentration-dependent increase in cytotoxic activity was observed when the SLNs were evaluated in cell cultures.

CONCLUSION

Biocompatible and stable lyophilised SLNs were successfully prepared and found to possess properties that may be utilised in an anti-cancer drug delivery system.

摘要

背景

固体脂质纳米粒(SLNs)能够有效且高效地包载抗癌药物。

目的

制备并表征载有他莫昔芬(TAM)的固体脂质纳米粒。

材料与方法

固体脂质纳米粒中使用了单硬脂酸甘油酯、吐温-80和海藻糖。通过动态光散射(DLS)、透射电子显微镜(TEM)、差示扫描量热法(DSC)、X射线衍射(XRD)和傅里叶变换红外光谱(FTIR)对固体脂质纳米粒进行检测。

结果

表征研究显示固体脂质纳米粒直径约为540 nm,表面带负电荷,并证实他莫昔芬被包载于固体脂质纳米粒中。包封率估计为60%。

讨论

体外药物释放曲线显示,药物释放先逐渐增加,随后几天保持释放平台期。在细胞培养中评估固体脂质纳米粒时,观察到细胞毒性活性随药物浓度增加而增强。

结论

成功制备了具有生物相容性且稳定的冻干固体脂质纳米粒,发现其具有可用于抗癌药物递送系统的特性。

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