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辛基没食子酸酯负载聚甲基丙烯酸甲酯纳米粒的体外抗利什曼原虫活性增强。

Increased in vitro leishmanicidal activity of octyl gallate loaded poly(methyl methacrylate) nanoparticles.

机构信息

a Department of Chemical Engineering and Food Engineering , Federal University of Santa Catarina , Florianópolis , Brazil.

b Department of Microbiology Immunology and Parasitology , Federal University of Santa Catarina , Florianópolis , Brazil.

出版信息

Pharm Dev Technol. 2019 Jun;24(5):593-599. doi: 10.1080/10837450.2018.1547747.

Abstract

The current paucity of effective and affordable drugs for the treatment of leishmaniasis renders the search for new therapeutic alternatives a priority. Gallic acid-related compounds display anti-parasitic activities and their incorporation into drug carrier systems, such as polymeric nanoparticles may be a viable alternative for leishmaniasis treatment. Therefore, this study focused on the synthesis and characterization of octyl gallate (G8) loaded poly(methyl methacrylate) (PMMA) nanoparticles via miniemulsion polymerization in order to increase the leishmanicidal activity of this compound. G8 loaded PMMA nanoparticles presented a spherical morphology with a mean size of 108 nm, a negatively charged surface (-33 ± 5 mV) and high encapsulation efficiency (83% ± 5). Fourier-transform infrared spectroscopy and X-ray diffraction analysis confirmed that G8 was encapsulated in PMMA nanoparticles and presented a biphasic release profile. The G8 loaded PMMA nanoparticles did not present cytotoxic effect on human red blood cells. G8 loaded PMMA nanoparticles displayed a leishmanicidal activity almost three times higher than free G8 while the cytotoxic activity against human THP-1 cells remained unchanged.

摘要

目前,用于治疗利什曼病的有效且负担得起的药物稀缺,因此寻找新的治疗方法成为当务之急。没食子酸相关化合物具有抗寄生虫活性,将其纳入药物载体系统(如聚合纳米粒子)可能是治疗利什曼病的一种可行方法。因此,本研究专注于通过细乳液聚合合成并表征辛基没食子酸酯(G8)负载的聚甲基丙烯酸甲酯(PMMA)纳米粒子,以提高该化合物的杀利什曼原虫活性。G8 负载的 PMMA 纳米粒子呈球形,平均粒径为 108nm,带负电荷(-33±5mV),包封效率高(83%±5)。傅里叶变换红外光谱和 X 射线衍射分析证实 G8 被包封在 PMMA 纳米粒子中,并呈现出两相释放曲线。G8 负载的 PMMA 纳米粒子对人红细胞没有细胞毒性。G8 负载的 PMMA 纳米粒子的杀利什曼原虫活性几乎是游离 G8 的三倍,而对人 THP-1 细胞的细胞毒性保持不变。

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