Tetracycline Water Soluble Formulations with Enhanced Antimicrobial Activity

The negligible water solubility of tetracycline ( ), a well-known antibiotic of clinical use, is the major disadvantage for its oral administration. With the aim to improve the water solubility of the micelles of formulae and ( = sodium lauryl sulphate and = cetrimonium bromide) were synthesized. Th...

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Bibliographic Details
Published in:	Antibiotics (Basel) Vol. 9; no. 12; p. 845
Main Authors:	Meretoudi, A, Banti, C N, Siafarika, P, Kalampounias, A G, Hadjikakou, S K
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 26-11-2020 MDPI
Subjects:	antibiotic Antibiotics Antiinfectives and antibacterials Antimicrobial activity Antimicrobial agents Artemia Bacteria Biocompatibility biological inorganic chemistry Calorimetry Cetyltrimethylammonium bromide Composite materials Cornea Decomposition Differential scanning calorimetry Differential thermal analysis E coli Enzymes Evaluation Gram-negative bacteria Infrared spectroscopy Melting point Melting points Micelles Microorganisms Minimum inhibitory concentration NMR Nuclear magnetic resonance Oral administration Phase transitions Pseudomonas aeruginosa Sodium dodecyl sulfate Sodium lauryl sulfate Solubility Spectroscopy Spectrum analysis Staphylococcus epidermidis Strains (organisms) Streptococcus infections Surfactants tetracycline Thermal analysis Thermogravimetric analysis Toxicity antibiotic toxicity biological inorganic chemistry tetracycline antimicrobial activity micelles
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Summary:	The negligible water solubility of tetracycline ( ), a well-known antibiotic of clinical use, is the major disadvantage for its oral administration. With the aim to improve the water solubility of the micelles of formulae and ( = sodium lauryl sulphate and = cetrimonium bromide) were synthesized. The micelles and were characterized by melting point (m.p.), thermogravimetric differential thermal analysis (TG-DTA), differential scanning calorimetry (DTG/DSC), attenuated total reflection spectroscopy (FT-IR-ATR), ultra-violet visible (UV/vis) spectroscopy, proton nucleus magnetic resonance ( H-NMR) spectroscopy, and the ultrasonically-induced biregringence technique. The antimicrobial activity of and was evaluated, by means of minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and inhibition zone (IZ), against the Gram negative bacterial strains ( ) and and the Gram positive ones of the genus (S. ) and ( ). Generally, both micelles show better activity than that of against the microbial strains tested. Thus, the MIC value of is 550-fold higher than that of free against . Despite the stronger activity of than against both Gram negative and Gram positive microbes, is classified as a bactericidal agent (in that it eliminates 99.9% of the microbes), in contrast to , which is bacteriostatic one (inhibits, but does not kill the organisms). The toxicity of and was evaluated against human corneal eukaryotic cells (HCECs). Moreover, and exhibit low in vivo toxicity against , even at concentrations up to threefold higher than those of their MIC . Therefore, and can be candidates for the development of new antibiotics.
ISSN:	2079-6382 2079-6382
DOI:	10.3390/antibiotics9120845