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Alendronate sodium-polymeric nanoparticles display low toxicity in gastric mucosal of rats and Ofcol II cells
NanoImpact ( IF 4.9 ) Pub Date : 2021-08-27 , DOI: 10.1016/j.impact.2021.100355
Bruno Iles 1 , Isabela Ribeiro de Sá Guimarães Nolêto 1 , Flaviane França Dourado 2 , Fábio de Oliveira Silva Ribeiro 2 , Alyne Rodrigues de Araújo 2 , Taiane Maria de Oliveira 2 , Jessica Maria Teles Souza 3 , Ayslan Batista Barros 3 , Gabrielle Costa Sousa 1 , Antônia Carla de Jesus Oliveira 4 , Conceição da Silva Martins 5 , Mariana de Oliveira Viana Veras 5 , Renata Ferreira de Carvalho Leitão 5 , José Roberto de Souza de Almeida Leite 6 , Durcilene Alves da Silva 2 , Jand Venes Rolim Medeiros 1
Affiliation  

The use of bisphosphonates constitutes the gold-standard therapy for the control and treatment of bone diseases. However, its long-term use may lead to gastric problems, which limits the treatment. Thus, this study aimed to formulate a nanostructured system with biodegradable polymers for the controlled release of alendronate sodium. The nanoparticles were characterized, and its gastric toxicity was investigated in rats. The synthesis process proved to be effective for encapsulating alendronate sodium, exhibiting nanoparticles with an average size of 51.02 nm and 98.5% of alendronate sodium incorporation. The release tests demonstrated a controlled release of the drug in 420 min, while the morphological analyzes showed spherical shapes and no apparent roughness. The biological tests demonstrated that the alendronate sodium nanoformulation reversed the gastric lesions, maintaining the normal levels of malondialdehyde and myeloperoxidase. Also, the encapsulated alendronate sodium showed no toxicity in murine osteoblastic cells, even at high concentrations.



中文翻译:

阿仑膦酸钠聚合物纳米颗粒在大鼠胃黏膜和Ofcol II细胞中表现出低毒性

双膦酸盐的使用构成了控制和治疗骨病的金标准疗法。然而,它的长期使用可能会导致胃部问题,从而限制了治疗。因此,本研究旨在用可生物降解的聚合物配制纳米结构系统,以控制阿仑膦酸钠的释放。对纳米颗粒进行了表征,并在大鼠中研究了其胃毒性。该合成过程被证明对封装阿仑膦酸钠是有效的,显示出平均尺寸为 51.02 nm 的纳米颗粒和 98.5% 的阿仑膦酸钠掺入。释放测试显示药物在 420 分钟内受控释放,而形态分析显示球形且没有明显的粗糙度。生物学测试表明,阿仑膦酸钠纳米制剂可逆转胃部病变,维持丙二醛和髓过氧化物酶的正常水平。此外,封装的阿仑膦酸钠在小鼠成骨细胞中没有显示出毒性,即使在高浓度下也是如此。

更新日期:2021-08-31
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