Abstract
Purpose: To incorporate ciprofloxacin (CIP) into solid lipid nanoparticles (SLN) in order to enhance its biopharmaceutical properties and antibacterial activity.Methods: A sonication melt-emulsification method was employed for the preparation of CIP-loaded SLN. The composition of the SLN was varied in order to investigate factors such as lipid type and combination ratio, drug to lipid ratio, and surfactant ratio. The produced SLN formulations wereevaluated for their particle size and shape, zeta potential, and entrapment efficiency. In addition, the effect of SLN formulation composition on its drug release profile and antimicrobial activity against Escherichia coli, Pseudomonas Aeruginosa, and Staphylococcus Aureus was also investigated.Results: The generated nanoparticles had particle size in the range of 165 to 320 nm. The zetapotential values were generally low within ± 5. All formulations exhibited entrapment efficiency between 50 and 90 %. CIP release exhibited a biphasic release profile with a low burst phase, followed by uniform controlled-release behavior of various rates. SLN-loaded CIP exhibited one-fold reduction in minimum inhibitory concentration (MIC) and caused significant inhibition of all the three bacterial strains tested, when compared with pure CIP.Conclusion: Loading of CIP into SLN significantly enhances its antimicrobial activity in vitro which can translate to significant enhancement of therapeutic outcomes by minimizing the dose-dependent adverse and side effects and/or enhancing the antimicrobial spectrum of activity.
 Keywords: Solid lipid nanoparticles, Sonication melt-emulsification, Ciprofloxacin, Escherichia coli, Pseudomonas aeruginosa
Highlights
Solid lipid nanoparticles (SLN) are relatively new pharmaceutical delivery systems made of lipids which remain solid at room temperature as well as body temperature [1]
Comparing the results obtained with F6 – F9 with F2, one can conclude that the highest magnitude of increase in particle size (369 ± 3.34 nm) was observed with F8 containing Softisan 154 in 1:1 ratio, while the lowest magnitude (198 ± 3.48 nm) was observed with F6 containing Imwitor 900
The mean particle size, polydispersity index, and zeta potential for all the formulations are presented in Figures 1 - 3
Summary
Solid lipid nanoparticles (SLN) are relatively new pharmaceutical delivery systems made of lipids which remain solid at room temperature as well as body temperature [1]. Their appropriateness for large-scale production using standard production lines in pharmaceutical industry such as high-pressure homogenization and super. The advantages of SLN can be translated to a number of useful applications in drug therapy including; enhancing solubility [1], controlling release and targeting [2,3], enhancing bioavailability and reducing dose [4], and/or improving stability [2,3]. SLN were used as targeting carriers for some anticancer drugs to the brain [4]
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