Gagliardi Agnese, Paolino Donatella, Iannone Michelangelo, Palma Ernesto, Fresta Massimo, Cosco Donato
Department of Experimental and Clinical Medicine, University "Magna Græcia" of Catanzaro, Catanzaro, Italy.
CNR, Section of Pharmacology, Institute of Neurological Sciences, Borgia, Italy.
Int J Nanomedicine. 2018 Jan 30;13:601-614. doi: 10.2147/IJN.S156930. eCollection 2018.
The use of biopolymers is increasing in drug delivery, thanks to the peculiar properties of these compounds such as their biodegradability, availability, and the possibility of modulating their physico-chemical characteristics. In particular, protein-based systems such as albumin are able to interact with many active compounds, modulating their biopharmaceutical properties. Zein is a protein of 20-40 kDa made up of many hydrophobic amino acids, generally regarded as safe (GRAS) and used as a coating material.
In this investigation, zein was combined with various surfactants in order to obtain stable nanosystems by means of the nanoprecipitation technique. Specific parameters, eg, temperature, pH value, Turbiscan Stability Index, serum stability, in vitro cytotoxicity and entrapment efficiency of various model compounds were investigated, in order to identify the nanoformulation most useful for a systemic drug delivery application.
The use of non-ionic and ionic surfactants such as Tween 80, poloxamer 188, and sodium deoxycholate allowed us to obtain nanoparticles characterized by a mean diameter of 100-200 nm when a protein concentration of 2 mg/mL was used. The surface charge was modulated by means of the protein concentration and the nature of the stabilizer. The most suitable nanoparticle formulation to be proposed as a colloidal drug delivery system was obtained using sodium deoxycholate (1.25% w/v) because it was characterized by a narrow size distribution, a good storage stability after freeze-drying and significant feature of retaining lipophilic and hydrophilic compounds.
The sodium deoxycholate-coated zein nanoparticles are stable biocompatible colloidal carriers to be used as useful drug delivery systems.
由于生物聚合物具有诸如生物可降解性、可得性以及调节其物理化学特性的可能性等特殊性质,其在药物递送中的应用正在增加。特别是,基于蛋白质的系统如白蛋白能够与许多活性化合物相互作用,调节它们的生物药剂学性质。玉米醇溶蛋白是一种由许多疏水氨基酸组成的20 - 40 kDa的蛋白质,一般被认为是安全的(GRAS)并用作包衣材料。
在本研究中,将玉米醇溶蛋白与各种表面活性剂结合,通过纳米沉淀技术获得稳定的纳米系统。研究了特定参数,例如温度、pH值、Turbiscan稳定性指数、血清稳定性、各种模型化合物的体外细胞毒性和包封率,以确定对全身药物递送应用最有用的纳米制剂。
当使用2 mg/mL的蛋白质浓度时,使用非离子和离子表面活性剂如吐温80、泊洛沙姆188和脱氧胆酸钠能够获得平均直径为100 - 200 nm的纳米颗粒。表面电荷通过蛋白质浓度和稳定剂的性质进行调节。使用脱氧胆酸钠(1.25% w/v)获得了最适合作为胶体药物递送系统提出的纳米颗粒制剂,因为它具有窄的粒径分布、冷冻干燥后良好的储存稳定性以及保留亲脂性和亲水性化合物的显著特性。
脱氧胆酸钠包被的玉米醇溶蛋白纳米颗粒是稳定的生物相容性胶体载体,可用作有用的药物递送系统。