Dos Reis Antunes Junior Osmar, Antônio Emilli, Mainardes Rubiana Mara, Khalil Najeh Maissar
Laboratory of Pharmaceutical Nanotechnology, Department of Pharmacy, Universidade Estadual do Centro-Oeste/UNICENTRO, Guarapuava/PR, Brazil.
Laboratory of Pharmaceutical Nanotechnology, Department of Pharmacy, Universidade Estadual do Centro-Oeste/UNICENTRO, Guarapuava/PR, Brazil.
J Trace Elem Med Biol. 2017 Jan;39:176-185. doi: 10.1016/j.jtemb.2016.09.010. Epub 2016 Oct 1.
In this study, we developed, characterized and evaluated the antioxidant activity of poly (lactic acid) nanoparticles containing diphenyl diselenide (PhSe). Nanoparticles were characterized in terms of mean particle size, polydispersity index, zeta potential, encapsulation efficiency, in vitro release profile, physical stability, polymer-drug interactions and thermal properties. Also, the antioxidant activity of nanoparticles on hypochlorous acid (HOCl) was assessed. Nanoparticles presented a mean size of 210nm, had low polydispersity, zeta potential of -24mV, and an encapsulation efficiency over 90%. Differential scanning calorimetry and X-ray diffraction results showed (PhSe) is dispersed in PLA matrix in an amorphous state. Lyophilized nanoparticles maintained physical stability over three months, while nanoparticles dispersed in water did not present stability over 7days. In vitro release assay was characterized by a biphasic release pattern with burst effect in 8h followed by a sustained release diffusion governed over 192h. Nanoencapsulation did not alter the antioxidant activity of (PhSe) on HOCl. The study concludes these properties of (PhSe)-loaded nanoparticles can be useful to extend the biological effects of (PhSe).
在本研究中，我们制备了含二苯基二硒醚（PhSe）的聚乳酸纳米粒子，对其进行了表征并评估了其抗氧化活性。纳米粒子的表征涉及平均粒径、多分散指数、zeta电位、包封率、体外释放曲线、物理稳定性、聚合物-药物相互作用和热性质。此外，还评估了纳米粒子对次氯酸（HOCl）的抗氧化活性。纳米粒子的平均粒径为210nm，多分散性低，zeta电位为-24mV，包封率超过90%。差示扫描量热法和X射线衍射结果表明，PhSe以无定形状态分散在聚乳酸基质中。冻干的纳米粒子在三个月内保持物理稳定性，而分散在水中的纳米粒子在7天内不稳定。体外释放试验的特征是双相释放模式，在8小时内有突释效应，随后在192小时内由持续释放扩散控制。纳米包封并未改变PhSe对HOCl的抗氧化活性。该研究得出结论，负载PhSe的纳米粒子的这些性质可能有助于扩展PhSe的生物学效应。
