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介孔硅球作为头孢唑林的双功能骨药物传递系统。

Mesoporous silica pellets as bifunctional bone drug delivery system for cefazolin.

机构信息

Department of Physical Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland.

Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Gdańsk, Hallera 107, 80-416 Gdańsk, Poland.

出版信息

Int J Pharm. 2020 Oct 15;588:119718. doi: 10.1016/j.ijpharm.2020.119718. Epub 2020 Aug 1.

Abstract

For decades, bone drug delivery systems dedicated for osteomyelitis treatment have been investigated as bifunctional materials that exhibit prolonged drug release and mineralization potential. Herein, composite-type pellets based on cefazolin-loaded amino-modified mesoporous silica SBA-15 and microwave-assisted hydroxyapatite were investigated as potential bone drug delivery system in vitro. Pellets were obtained by granulation, extrusion and spheronization methods in laboratory scale and studied in terms of physical properties, drug release, mineralization potential, antimicrobial activity and cytotoxicity towards human osteoblasts. The obtained pellets were characterized for hardness and friability which indicated the pellets durability during further investigations. Prolonged (5-day) release of cefazolin from pellets was observed. The pellets exhibited mineralization potential in simulated body fluid, i.e., a continuous layer of bone-like apatite was formed on the surface of pellets after 28 days of incubation. An antimicrobial assay of pellets revealed an antibacterial effect against Staphylococcus aureus strain during 6 days. No cytotoxic effects of pellets towards human osteoblasts were observed. The obtained results proved that proposed pellets appear to have potential applications as bone drug delivery systems.

摘要

几十年来,专门用于治疗骨髓炎的骨药物输送系统一直被研究为具有双重功能的材料,具有延长药物释放和矿化潜力。在此,研究了基于载头孢唑啉的氨基修饰介孔硅 SBA-15 和微波辅助羟基磷灰石的复合型微丸作为潜在的骨药物输送系统的体外性能。通过在实验室规模上进行造粒、挤出和滚圆的方法获得微丸,并对其物理性能、药物释放、矿化潜力、抗菌活性和对人成骨细胞的细胞毒性进行了研究。对获得的微丸进行了硬度和脆性的表征,这表明了微丸在进一步研究中的耐久性。从微丸中观察到头孢唑啉的延长(5 天)释放。微丸在模拟体液中表现出矿化潜力,即在孵育 28 天后,微丸表面形成了连续的骨样磷灰石层。微丸的抗菌试验显示,在 6 天内对金黄色葡萄球菌菌株具有抗菌作用。微丸对人成骨细胞没有细胞毒性作用。所得结果表明,所提出的微丸作为骨药物输送系统具有潜在的应用前景。

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