Abstract
BackgroundCeftriaxone 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.MethodsDouble 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.ResultsMathematical 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.ConclusionResults confirm that NLC structure is an appropriate alternative for the delivery of ceftriaxone drug with a controlled release behavior.
Highlights
Ceftriaxone sodium is an antibiotic commonly used for the treatment of bacterial infection such as middle ear infection, meningitis, bone, and joint infection, intraabdominal infection, skin infection, and pelvic inflammatory diseases [1]
The use of lipids for the formation of nanoparticles such as solid lipid nanoparticles (SLN) or nanostructured lipid carrier (NLC), offers multiple benefits compared to other materials, which is due to low cytotoxicity and controlled drug release [4]
Given that particle size and drug entrapment efficiency have a noticeable effect on the bacteria death efficacy, we investigate the methods of determining the best materials for forming small-size particles with high drug encapsulation efficiency
Summary
Ceftriaxone sodium is an antibiotic commonly used for the treatment of bacterial infection such as middle ear infection, meningitis, bone, and joint infection, intraabdominal infection, skin infection, and pelvic inflammatory diseases [1]. The controlled drug release can be applied to both hydrophilic and hydrophobic drugs. Tamoxifen hydrochloride, as a hydrophilic drug, is encapsulated in a microemulsion system with a controlled release. It is effective in the breast cancer treatment in comparison with the commercial forms of the drug [6]. Raloxifene [7] and Clozapine [8], as hydrophobic drugs in microemulsion and nanostructured lipid forms, have exhibited essential growth in the drug release compared to free dugs. 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
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