Turos Edward, Reddy G Suresh Kumar, Greenhalgh Kerriann, Ramaraju Praveen, Abeylath Sampath C, Jang Seyoung, Dickey Sonja, Lim Daniel V
Center for Molecular Diversity in Drug Design, Discovery, and Delivery, Department of Chemistry, 4202 East Fowler Avenue, CHE 207, University of South Florida, Tampa, FL 33620, USA.
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3468-72. doi: 10.1016/j.bmcl.2007.03.077. Epub 2007 Mar 27.
This report describes the preparation of antibacterially active emulsified polyacrylate nanoparticles in which a penicillin antibiotic is covalently conjugated onto the polymeric framework. These nanoparticles were prepared in water by emulsion polymerization of an acrylated penicillin analogue pre-dissolved in a 7:3 (w:w) mixture of butyl acrylate and styrene in the presence of sodium dodecyl sulfate (surfactant) and potassium persulfate (radical initiator). Dynamic light scattering analysis and atomic force microscopy images show that the emulsions contain nanoparticles of approximately 40 nm in diameter. The nanoparticles have equipotent in vitro antibacterial properties against methicillin-susceptible and methicillin-resistant forms of Staphylococcus aureus and indefinite stability toward beta-lactamase.
本报告描述了具有抗菌活性的乳化聚丙烯酸酯纳米颗粒的制备方法，其中青霉素抗生素共价连接到聚合物骨架上。这些纳米颗粒是通过在十二烷基硫酸钠（表面活性剂）和过硫酸钾（自由基引发剂）存在下，将预溶解于丙烯酸丁酯和苯乙烯7:3（w:w）混合物中的丙烯酸化青霉素类似物进行乳液聚合，在水中制备而成。动态光散射分析和原子力显微镜图像显示，乳液中含有直径约40nm的纳米颗粒。这些纳米颗粒对甲氧西林敏感和耐甲氧西林形式的金黄色葡萄球菌具有等效的体外抗菌性能，并且对β-内酰胺酶具有无限稳定性。
