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Nanomaterials 2018, 8(5), 304;

A Method for Efficient Loading of Ciprofloxacin Hydrochloride in Cationic Solid Lipid Nanoparticles: Formulation and Microbiological Evaluation

Section of Pharmaceutical Technology, Department of Drug Sciences, University of Catania, 95125 Catania, Italy
NANO-i, Research Centre on Ocular Nanotechnology, University of Catania, 95125 Catania, Italy
Section of Microbiology, Department of Biomedical and Biotechnological Sciences, BIOMETEC, University of Catania, 95125 Catania, Italy
Author to whom correspondence should be addressed.
Received: 27 February 2018 / Revised: 9 April 2018 / Accepted: 2 May 2018 / Published: 6 May 2018
(This article belongs to the Special Issue Antibacterial Activity of Nanomaterials)
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The aim of the study was the production of solid lipid nanoparticles (SLN) loaded with ciprofloxacin (CIP) through two different production techniques, quasi-emulsion solvent diffusion (QESD) and solvent injection (SI). In order to efficaciously entrap the commercial salt form (hydrochloride) of the antibiotic in these lipid systems, a conversion of CIP hydrochloride to the free base was realized in situ, through the addition of triethylamine. To ensure physical stability to the carriers over time and ameliorate the interaction with bacterial cell membranes, positively charged SLN were produced by addition of the cationic lipid didecyldimethylammonium bromide (DDAB). Homogeneous SLN populations with a mean particle sizes of 250–350 nm were produced by both methods; drug encapsulation was over 85% for most samples. The SLN were physically stable for up to nine months both at 4 °C and 25 °C, although the former condition appears more suitable to guarantee the maintenance of the initial particle size distribution. As expected, CIP encapsulation efficiency underwent a slight reduction after nine months of storage, although the initial high drug content values would ensure a residual concentration of the antibiotic in the SLN still appropriate to exert an acceptable antibacterial activity. Selected SLN formulations were subjected to an in vitro microbiological assay against different bacterial strains, to verify the effect of nanoencapsulation on the cell growth inhibitory activity of CIP. In general, CIP-SLN produced without DDAB showed MIC values for CIP comparable to those of the free drug. Conversely, addition of increasing percentages of the cationic lipid, reflected by a progressive increase of the positive value of the Zeta potential, showed a variety of MIC values against the various bacterial strains, but with values 2–4 order of dilution lower than free CIP. An hypothesis of the effect of the cationic lipid upon the increased antibacterial activity of CIP in the nanocarriers is also formulated. View Full-Text
Keywords: SLN; triethylamine; positive charge; DDAB; antimicrobial activity; drug encapsulation SLN; triethylamine; positive charge; DDAB; antimicrobial activity; drug encapsulation

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Pignatello, R.; Leonardi, A.; Fuochi, V.; Petronio Petronio, G.; Greco, A.S.; Furneri, P.M. A Method for Efficient Loading of Ciprofloxacin Hydrochloride in Cationic Solid Lipid Nanoparticles: Formulation and Microbiological Evaluation. Nanomaterials 2018, 8, 304.

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