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Effect of Introduction of Polymers on the Antibacterial Activity of Crystalline Antibiotics
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| Author:
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QUTAIBA AKRAM ISMAEL, GHAIDAA S. HAMEED, FITUA M. AZIZ
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| Abstract:
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This is the first study that emphasizes on the relationship between the antibacterial activity of three selected poorly water-soluble antibiotics azithromycin (AZ), cefixime (CX) and ciprofloxacin (CP) and their solid-state change.
A Pre-formulation study of their solubility was done via conversion of these drugs from crystalline form to the semi-crystalline or complete amorphous form by amorphous solid dispersion method in order to enhance their low water solubility and hence bioavailability. The three selected antibiotics (azithromycin, cefixime, and ciprofloxacin) was mixed with three different polymers: Polyethylene glycol (PEG), Polyvinylpyrrolidone (PVP), and Hydroxypropyl Methylcellulose (HPMC). Then, by solvent evaporation method we prepare the following solid dispersion formulas: azithromycin-PEG (AZ-SD), cefixime-PVP (CX-SD), and ciprofloxacin-HPMC (CP-SD). All formulas are characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XPRD) to check the partial or complete conversion of the crystalline to amorphous state. Both azithromycin and cefixime showed complete conversion while ciprofloxacin was partially converted to the amorphous state. Dissolution test was performed to demonstrates the effect of the solid-state conversion on the percentage of the drug release. The results showed an increasing in the percentage of the drug release for all selected drugs after conversion to amorphous solid dispersion.
Furthermore, agar-well diffusion was used to evaluate the antibacterial activity. Zones of inhibition was measured and compared with the pure antibiotics. The results showed an enhancement of antibiotics activity for SDs formulas compared to pure drug which might related to greater drug diffusivity into the agar medium as a result of solubility enhancement.
This improvement in the dissolution and antibacterial activity might attract drug manufacturing companies with further study to apply this method in production of the antibiotics with high antibacterial activity.
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| Keyword:
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Azithromycin, Cefixime, Ciprofloxacin, PEG, PVP, HPMC, Solid dispersion, SD, Antibacterial activity
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2020.12.03.483
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| Download:
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