Hydrophilic nanofibers as a supersaturating delivery system for carvedilol
| Autor: | Tanja Potrč, Petra Kocbek, Katja Murnc |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Nanofibers
Pharmaceutical Science Poloxamer 02 engineering and technology 030226 pharmacology & pharmacy Polyethylene Glycols 03 medical and health sciences 0302 clinical medicine Amphiphile Copolymer medicine Dissolution Carvedilol Supersaturation Chemistry 021001 nanoscience & nanotechnology Electrospinning Solubility Chemical engineering Nanofiber Poloxamer 407 Polyvinyls 0210 nano-technology Hydrophobic and Hydrophilic Interactions medicine.drug |
| Zdroj: | International Journal of Pharmaceutics. 603:120700 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2021.120700 |
| Popis: | Polymer nanofibers represent a promising delivery system for poorly water-soluble drugs; however, their supersaturating potential has not been explored yet. Here, carvedilol-loaded nanofibers based on poly(ethyleneoxide) and on amphiphilic block copolymer poloxamer 407 were produced by electrospinning. These nanofibers provided high carvedilol loading and improved dissolution of carvedilol. Their dissolution resulted in a supersaturated system that was not stable, and thus to avoid carvedilol precipitation, hydroxypropyl methylcelluloses or polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol graft copolymer (Soluplus) were additionally incorporated into the nanofibers. The morphology of the electrospun product was not affected by incorporation of carvedilol and the polymer precipitation inhibitors, as shown by scanning electron microscopy. The hydroxypropyl methylcelluloses were not effective polymer precipitation inhibitors for carvedilol. Incorporation of Soluplus significantly extended the duration of carvedilol supersaturation (>24 h) compared to the dissolution of nanofibers without Soluplus. Moreover, after 1 h of dissolution, incorporation of Soluplus into the nanofibers provided significantly higher carvedilol concentration (94.4 ± 2.5 μg/mL) compared to the nanofibers without Soluplus (32.7 ± 5.8 μg/mL), the polymer film (24.0 ± 2.2 μg/mL), and the physical mixture (3.3 ± 0.4 μg/mL). Thus, this study shows the great potential for hydrophilic nanofibers as a delivery system for sustained carvedilol supersaturation. |
| Databáze: | OpenAIRE |
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