Application of miscibility analysis and determination of Soluplus solubility map for development of carvedilol-loaded nanofibers

Abstract

Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, χ, and the difference between the total solubility parameters, Δd. A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characterizing the nanofibers formed. Miscibility studies showed that carvedilol and Soluplus can form a miscible system (χ=-2.3054; Δδ<7.0MPa). Based on the Soluplus solubility map, acetone: chloroform (90:10; w/w) represents a suitable solvent system for electrospinning of carvedilol-loaded Soluplus nanofibers. Scanning electron microscopy of these nanofiber samples showed smooth surface morphology. The nanofibers had a regular cylindrical morphology. Beads appeared along the nanofibers more frequently in formulations with lower percentages of carvedilol. Differential scanning calorimetry showed no melting endothermic peak for carvedilol, which suggests its complete conversion from the crystalline to the amorphous form (at polymer: carvedilol 1:1). The infrared spectrum of the carvedilol-loaded Soluplus nanofibers showed no characteristic carvedilol peak at 3344.5cm, which suggests interactions between carvedilol and Soluplus. Dissolution studies of these nanofibers showed improved pure carvedilol dissolution properties, with >85% of the carvedilol released in the first 15min, versus 20% for pure carvedilol. The use of miscibility analysis and polymer solubility studies demonstrate great technological potential to tackle the challenge for inadequate dissolution of poorly water-soluble drugs.

The Incorporated Drug Affects the Properties of Hydrophilic Nanofibers

“…The comparison of the obtained drug release profiles with the literature data revealed similar drug release kinetics irrespective of the polymer composition of nanofibers for ibuprofen [37,96,97], carvedilol [52], and paracetamol [93,97,98]. Remarkably, in a previous study, PEO nanofibers exhibited a slower release of carvedilol compared to the nanofibers examined in our study [53].…”

Development of an Electrospun Patch Platform Technology for the Delivery of Carvedilol in the Oral Mucosa

“…Additionally, the CVD characteristic peak at 3340 cm −1 attributed to the N–H stretching is not observed in any of the CVD-loaded fibers. This could be related to the potential interaction between the –NH group of CVD and the –CO groups of the matrices as previously reported [ 40 ].…”

Novel Honokiol-eluting PLGA-based scaffold effectively restricts the growth of renal cancer cells

“…Of such methods, the distinguishing property of the electropsun scaffolds, is their ability to be tuned and provide various release kinetics of the drug, depending on the selection of the polymer used to fabricate the scaffold [39]. For example, to achieve immediate release of the drug, usually more hydrophilic polymers such as Soluplus, Polyvinyl pyrrolidone (PVP), and combination of Polyvinyl alcohol (PVA) are used to fabricate the scaffold [40][41][42][43]. Electrospun fibers can also be manipulated to provide a more sustained release of the drug by using Polycaprolactone (PCL), poly(acrylic acid), PLGA, shellac, silk fibroin or a combination of them [43][44][45][46][47].…”