Department of Life Sciences, Via Campi 103, University of Modena and Reggio Emilia, 41124 Modena, Italy.
CIGS, Centro Interdipartimentale Grandi Strumenti, University of Modena and Reggio Emilia, Italy.
Int J Pharm. 2017 Feb 25;518(1-2):281-288. doi: 10.1016/j.ijpharm.2016.12.038. Epub 2016 Dec 23.
The aim of this study is to formulate and characterize streptomycin-loaded apoferritin nanoparticles (ApoStrep NPs) for their potential therapeutic use in bacterial resistant infections (i.e. tuberculosis). ApoStrep NPs were prepared by disassembly/reassembly process via pH method and changing apoferritin/drug molar ratio, purified by dialyses process also associated with gel filtration chromatography and characterized in their chemico-physical and technological parameters as yield, size distribution, polidispersivity, morphology, internal structure, zeta potential and loading efficacy. The results showed that spherical reproducible NPs could be obtained by using apoferritin/drug molar ratio lower than 1:25 and purification based on the combination of dialysis and gel filtration chromatography. Photon correlation spectroscopy, Uv-visible detection and electron microscopy showed the maintenance of the native apoferritin chemico-physical properties and structure. When formulated with apoferritin/drug 1:10 and 1:25 molar ratio, ApoStrep NPs showed remarkable encapsulation efficacy (35% and 28%, respectively) along with kinetic profile of drug delivery, approximately 15% at 37 °C in 72h, as evidenced by "in vitro" release experiments.
本研究旨在制备并表征载链霉素脱铁铁蛋白纳米粒(ApoStrep NPs),以探索其在细菌耐药性感染(如结核病)中的潜在治疗用途。ApoStrep NPs 采用 pH 法通过解组装/再组装过程制备,并改变脱铁铁蛋白/药物的摩尔比,通过透析过程进行纯化,同时还进行凝胶过滤色谱纯化,并对其化学物理和技术参数(产率、粒径分布、多分散性、形态、内部结构、Zeta 电位和载药效率)进行了表征。结果表明,使用低于 1:25 的脱铁铁蛋白/药物摩尔比并结合透析和凝胶过滤色谱进行纯化,可以得到球形、重现性好的 NPs。光相关光谱、紫外可见检测和电子显微镜表明,脱铁铁蛋白的化学物理性质和结构得以保持。当以脱铁铁蛋白/药物 1:10 和 1:25 的摩尔比进行制剂时,ApoStrep NPs 表现出显著的包封效率(分别为 35%和 28%),并具有药物释放动力学特征,在 37°C 下 72 小时内约为 15%,这可通过“体外”释放实验证实。