Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study
Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study
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DOI：
10.1186/s13756-020-0690-4
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发表时间：
2020-02-10
影响因子：
5.5
通讯作者：
Ebrahimi, Mohsen
中科院分区：
文献类型：
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作者：
Ebrahimi, Sahar;Farhadian, Nafiseh;Ebrahimi, Mohsen
背景 头孢曲松是用于治疗最致命的细菌感染的最常见抗生素类型之一。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消耗。本研究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。方法采用双乳化溶剂蒸发法制备NLC。进行基于溶解度研究的数学建模，以选择用于 NLC 制备的最佳材料。 Haftyzer-Van Krevelen 和 Hoy 的模型就是用于此目的。在体外环境下检查优化 NLC 的药物释放。然后，研究了优化样品消除革兰氏阴性菌大肠杆菌的功效。结果数学模型表明，两种方法都能够通过链接固体和液体脂质来预测药物包封效率趋势。然而，Haftyzer-Van Krevelen 的方法可以通过改变乳液水相和油相中的表面活性剂类型来精确预测粒径趋势。最佳样品平均粒径为86 nm，药物包封率为83%。此外，在体外介质下观察到随着时间的推移，所制备的纳米结构中的受控药物释放。关于优化 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少一半，可以在更长的时间内观察到与游离药物相当的效果。结论 结果证实 NLC 结构是具有控释行为的头孢曲松药物递送的合适替代方案。
Background 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. Methods 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. Results 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. Conclusion Results confirm that NLC structure is an appropriate alternative for the delivery of ceftriaxone drug with a controlled release behavior.