Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Enhancement of ciprofloxacin activity by incorporating it in solid lipid nanoparticles

Saqer Alarifi¹, Salam Massadeh^1,2, Mohammed Al-Agamy^3,4, Manal Al Aamery², Abdulkareem Al Bekairy¹, Alaa Eldeen Yassin^1,2

¹College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences; ²King Abdullah International Medical Research Center, and King Abdulaziz Medical City, National Guard Health Affairs; ³Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; ⁴Department of Microbiology and Immunology, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.

For correspondence:- Alaa Eldeen Yassin Email: yassina@ksau-hs.edu.sa Tel:+966509426323

Accepted: 22 April 2020 Published: 31 May 2020

Citation: Alarifi S, Massadeh S, Al-Agamy M, Al Aamery M, Al Bekairy A, Yassin A. Enhancement of ciprofloxacin activity by incorporating it in solid lipid nanoparticles. Trop J Pharm Res 2020; 19(5):909-918 doi: 10.4314/tjpr.v19i5.1

© 2020 The authors.
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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 were evaluated 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 zeta-potential 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