Binary and Ternary Complexes of Norfloxacin to Improve the Solubility of the Active Pharmaceutical Ingredient

Ponce-Ponte, Micaela; Aloisio, Carolina; Romero-Guerra, Diana Marcela; Gracia-Vásquez, Sandra; Garnero, Claudia; Longhi, Marcela R.

doi:10.4155/tde-2018-0028

Cited by 7 publications

(4 citation statements)

References 28 publications

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“…The results obtained for the in vitro antimicrobial activity of norfloxacin:β-CD:AA against Bacillus subtilis , S. aureus , and E. coli also showed better antimicrobial activity as compared to the pure drug. Other ternary complexes of norfloxacin with HP-β-CD were prepared, using glutamic acid, proline, or lysine as the third component [ 183 ]. The highest dissolution rate was obtained with glutamic acid, a negatively charged amino acid.…”

Section: Quinolonesmentioning

confidence: 99%

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

Boczar

Michalska

2022

Pharmaceutics

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Cyclodextrins (CDs) are a family of cyclic oligosaccharides, consisting of a macrocyclic ring of glucose subunits linked by α-1,4 glycosidic bonds. The shape of CD molecules is similar to a truncated cone with a hydrophobic inner cavity and a hydrophilic surface, which allows the formation of inclusion complexes with various molecules. This review article summarises over 200 reports published by the end of 2021 that discuss the complexation of CDs with antibiotics and antibacterial agents, including beta-lactams, tetracyclines, quinolones, macrolides, aminoglycosides, glycopeptides, polypeptides, nitroimidazoles, and oxazolidinones. The review focuses on drug-delivery applications such as improving solubility, modifying the drug-release profile, slowing down the degradation of the drug, improving biological membrane permeability, and enhancing antimicrobial activity. In addition to simple drug/CD combinations, ternary systems with additional auxiliary substances have been described, as well as more sophisticated drug-delivery systems including nanosponges, nanofibres, nanoparticles, microparticles, liposomes, hydrogels, and macromolecules. Depending on the desired properties of the drug product, an accelerated or prolonged dissolution profile can be achieved when combining CD with antibiotics or antimicrobial agents.

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Section: Quinolonesmentioning

confidence: 99%

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

Boczar

Michalska

2022

Pharmaceutics

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“…To overcome this problem, Ponce Ponte et al studied the possibility of preparing multicomponent complexes using AAs (glutamic acid, lysine and proline) and HPβCD. In this case, glutamic acid was the best candidate with which to form ternary complexes [ 32 ]. Chloramphenicol is an antibacterial drug that is slightly soluble in water and has serious side effects.…”

Section: Amino Acids As Auxiliary Agentsmentioning

confidence: 99%

Cyclodextrin Multicomponent Complexes: Pharmaceutical Applications

et al. 2021

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Cyclodextrins (CDs) are naturally available water-soluble cyclic oligosaccharides widely used as carriers in the pharmaceutical industry for their ability to modulate several properties of drugs through the formation of drug–CD complexes. The addition of an auxiliary substance when forming multicomponent complexes is an adequate strategy to enhance complexation efficiency and to facilitate the therapeutic applicability of different drugs. This review discusses multicomponent complexation using amino acids; organic acids and bases; and water-soluble polymers as auxiliary excipients. Special attention is given to improved properties by including information on the solubility, dissolution, permeation, stability and bioavailability of several relevant drugs. In addition, the use of multicomponent CD complexes to enhance therapeutic drug effects is summarized.

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“…1 H NMR assay A Bruker Avance II 400 spectrometer was used to record the NMR spectra at 298 K using D 2 O and tetramethylsilane as an internal standard. The following Equation 1 was used to calculate the changes induced in the 1 H chemical shifts for β-CD, originated due to their complexations [32]:…”

Section: Phase Solubility Analysismentioning

confidence: 99%

“…Preparation of KET:β-CD:NAC solid samples Freeze dried (FD) KET:β-CD:NAC (1:1:2 M ratio) was obtained by the freeze-drying technique using a Freeze Dryer 4.5, Labconco Corp., MI, USA, with 50 mbar vacuum for 96 h. KET:β-CD:NAC complex (1:1:2) and pure drugs aqueous solutions were prepared, sonicated (2 h), filtered, frozen at -48 • until complete solidification and then carry out the freeze-drying process. On the contrary, a physical mixture (PM) was prepared by simple mixing of KET, β-CD and NAC in an agate mortar [32].…”

Section: Phase Solubility Analysismentioning

confidence: 99%

Simultaneous Improvement of Ketoconazole solubility, Antifungal and Antibiofilm Activity By Multicomponent Complexation

et al. 2020

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Background: A novel multicomponent complex (MC) of ketoconazole (KET) with β-cyclodextrin (β-CD) and N-acetylcysteine (NAC) was developed with the purpose of improving the solubility as well as the antifungal and antibiofilm activity of KET against Candida albicans. Results & methodology: The interactions among the components were studied using nuclear magnetic resonance, thermal analysis, powder x-ray diffraction, infrared spectroscopy and scanning electron microscopy. Phase-solubility studies demonstrated a considerable increase in the solubility of the MC. An enhancement in antibiofilm and antifungal activity of MC was determined against C. albicans by XTT assay and microbiological studies. Conclusion: This MC, with improvements in the drug pharmaceutical performance, might have an important potential in the development of new pharmaceutical formulations of KET.

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Binary and Ternary Complexes of Norfloxacin to Improve the Solubility of the Active Pharmaceutical Ingredient

Abstract: NOR:HPβCD:GA was the best approach for improving the bioavailability of NOR.

Cited by 7 publications

References 28 publications

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

Cyclodextrin Inclusion Complexes with Antibiotics and Antibacterial Agents as Drug-Delivery Systems—A Pharmaceutical Perspective

Cyclodextrin Multicomponent Complexes: Pharmaceutical Applications

Simultaneous Improvement of Ketoconazole solubility, Antifungal and Antibiofilm Activity By Multicomponent Complexation

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