SeMet/ CS纳米复合微球的制备、缓释性能及抑制肿瘤活性

Preparation and sustained-release property of SeMet/CS microsphere and its inhibitory effects on cancer cells

摘要:

研究SeMet硒化物的可控缓释系统。以CS为壁材、SeMet为药物模型，采用乳化交联法制备SeMet/ CS纳米复合微球，以单因素实验和正交试验优化制备工艺，结合原子荧光光谱、IR、热重分析及SEM对产物的形貌、结构及性能进行评价和表征，并对其体外缓释和抑制人乳腺癌细胞MCF-7细胞生长等性能进行研究。结果表明：最优工艺条件(0.1%的投药量、2%的交联剂用量、50℃交联10min)制备的SeMet/ CS微球，形貌优良，包封率和载药量分别为31.94%和0.54%，体外缓释硒的性能良好，对MCF-7细胞的生长抑制率随微球缓释时间增加而增加。SeMet/ CS缓释硒复合微球有效避免了硒的突释效应，实现了硒剂量的把控，可作为硒化药物或硒补充剂应用于医疗、食品和精细化工等相关行业。

Abstract:

SeMet/CS Nanocomposite microspheres were prepared using SeMet as a core material and chitosan(CS) as a wall material using emulsion crosslinking. The work in this paper focused on the indicators of microspheric form, drug-loading rate, entrapment efficiency and slow-release property using the single-factor and orthogonal test to optimize the preparation technology. During the processes, a scanning electron microscope, a Fourier infrared spectrometer, a thermal analyzer and double-channel atomic fluorescence were applied for detection, analysis and characterization. Furthermore, in vitro tests, such as for the selenium-releasing property and anticancer activity, were studied for the prepared selenium microsphere. The data indicated that the SeMet/CS microsphere prepared under the optimum conditions of 0.1% dosage and 2% dosage of crosslinking agent were crosslinked at 50℃ for 10 min. The obtained SeMet/CS microspheres exhibited superior features, with an Excellent morphology and an embedding ratio and drug loading of 31.94% and 0.59%, respectively. They displayed excellent sustained-release capability in an SBF model. Regarding anticancer activity, they showed a significant inhibitory effect on MCF-7 human breast cancer cells, and there was a positively correlated between the inhibition rate and the content of selenium in the sustained-release liquid. The SeMet/CS microsphere can effectively avoid a burst effect for selenium, allowing a controlled selenium dose. Thus, it can be used in selenide or selenium supplements for further application in medical, food and fine chemical industries.