In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

• Published in: Pharmaceutics Vol. 13; no. 4; p. 556
• Main Authors: Uhljar, Luca Éva, Kan, Sheng Yuan, Radacsi, Norbert, Koutsos, Vasileios, Szabó-Révész, Piroska, Ambrus, Rita
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 15.04.2021; MDPI
• Subjects: amorphous solid dispersion; Antibiotics; Aqueous solutions; Bacterial infections; Bioavailability; ciprofloxacin; Drug delivery systems; Drug dosages; electrospinning; Fourier transforms; Gram-positive bacteria; Humidity; Infections; Investigations; Morphology; nanofibers; Permeability; Pharmaceuticals; Polymers; poorly water-soluble drug; Potassium; povidone; Scanning electron microscopy; Spectrum analysis; Hungary; United Kingdom > UK; United States > US; Switzerland; poorly water-soluble drug; electrospinning; povidone; nanofibers; amorphous solid dispersion; ciprofloxacin
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics13040556

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.