Chemical Engineering Department, Faculty of Engineering, Ferdowsi University of Mashhad, Mashhad, Iran.
Department of Emergency Medicine, Faculty of Medicine, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Antimicrob Resist Infect Control. 2020 Feb 10;9(1):28. doi: 10.1186/s13756-020-0690-4.
Ceftriaxone is one of the most common types of antibiotics used to treat most deadly bacterial infections. One way to alleviate the side effects of medication is to reduce drug consumption by changing the ordinary drug forms into nanostructured forms. In this study, a nanostructured lipid carrier (NLC) containing hydrophilic ceftriaxone sodium drug is developed, and its effect on eliminating gram-negative bacteria Escherichia coli death is investigated.
Double emulsion solvent evaporation method is applied to prepare NLC. Mathematical modeling based on the solubility study is performed to select the best materials for NLC preparation. Haftyzer-Van Krevelen and Hoy's models are employed for this purpose. Drug release from optimized NLC is examined under in vitro environment. Then, the efficacy of the optimized sample on eliminating gram-negative bacteria Escherichia coli is investigated.
Mathematical modeling reveals that both methods are capable of predicting drug encapsulation efficiency trends by chaining solid and liquid lipids. However, Haftyzer-Van Krevelen's method can precisely predict the particle size trend by changing the surfactant types in water and oily phases of emulsions. The optimal sample has a mean particle size of 86 nm and drug entrapment efficiency of 83%. Also, a controlled drug release in prepared nanostructures over time is observed under in-vitro media. The results regarding the effectiveness of optimized NLC in killing Escherichia coli bacteria suggests that by cutting drug dosage of the nanostructured form in half, an effect comparable to that of free drug can be observed at longer times.
Results confirm that NLC structure is an appropriate alternative for the delivery of ceftriaxone drug with a controlled release behavior.
头孢曲松是治疗大多数致命细菌感染最常用的抗生素之一。减轻药物副作用的一种方法是通过将普通药物形式转变为纳米结构形式来减少药物的使用。在本研究中,开发了一种含有亲水性头孢曲松钠药物的纳米结构脂质载体(NLC),并研究了其消除革兰氏阴性菌大肠杆菌死亡的效果。
采用双乳液溶剂蒸发法制备 NLC。通过基于溶解度研究的数学建模来选择 NLC 制备的最佳材料。为此目的,采用 Haftyzer-Van Krevelen 和 Hoy 模型。在体外环境下检查优化后的 NLC 的药物释放情况。然后,研究优化样品对消除革兰氏阴性菌大肠杆菌的功效。
数学建模表明,这两种方法都能够通过连接固体和液体脂质来预测药物包封效率趋势。然而,Haftyzer-Van Krevelen 方法可以通过改变乳化剂在水相和油相中的类型来精确预测粒径趋势。最佳样品的平均粒径为 86nm,药物包封效率为 83%。此外,在体外介质中观察到制备的纳米结构中药物的控释随时间的释放。关于优化的 NLC 杀死大肠杆菌的有效性的结果表明,通过将纳米结构形式的药物剂量减半,可以在更长的时间内观察到与游离药物相当的效果。
结果证实,NLC 结构是一种具有控释行为的头孢曲松药物递送的合适替代方法。