The aim of this study was to assess whether nanofibrous drug mats have potential as delivery systems for poorly water-soluble drugs. Amorphous nanofiber mats from a model poorly water-soluble active pharmaceutical ingredient (API), niflumic acid, together with the polymer excipient, polyvinyl pyrrolidine, were prepared by nozzle-free electrospinning. This technique offers a scalable way for drug formulation, and by increasing the surface area of the drug, the dissolution rate and therefore bioavailability of the API can be improved. In this study, both the amount of the dissolved active ingredient and the dissolution kinetics has been improved significantly when the nanofibrous mats were used in the drug formulation. A 15fold increase in the dissolved amount of the produced amorphous niflumic acid nanofiber was observed compared to the dissolved amount of the raw drug within the first 15 minutes. Capsule formulation was made by mixing the electrospun nanofibers with a microcrystalline cellulose filler agent. When comparing the dissolution rate of the capsule formulation on the market with the nanofibrous capsules, a 14-fold increase was observed in the dissolved drug amount within the first 15 minutes.
This study investigates the effects of drug-loaded nanofibers on the solubility of the poorly water-soluble drug, loratadine. Amorphous morphologies of electrospun loratadine nanofibers were prepared using a 3D-printed electrospinning setup. Polyvinylpyrrolidone was used as a carrier in the solvent preparation method. The prepared nanofibers were characterized by scanning electron microscopy, differential scanning calorimetry, X-ray diffraction analysis, Fourier transform infrared spectroscopy, solubility and in vitro dissolution studies with kinetic behavior evaluation. The scanning electron microscope images showed smooth nanofiber surfaces with a mean diameter of 372 nm. Moreover, both differential scanning calorimetry and X-ray diffraction analysis confirmed the amorphous state of the prepared nanofibers. FT-IR results suggested that loratadine lost its original crystal structure by hydrogen bonding interactions. The fabricated nanofibrous drug samples demonstrated a remarkable 26-fold increase in solubility when compared to the pure drug in phosphate buffer at pH 7.4. Furthermore, dissolution studies showed that 66% of the drug from the nanofibrous mat was released in the first 10 min, which is significantly higher than the maximum of 4% drug release of the reference samples within the same time. Thus, Loratadine nanofibers can be considered as an alternative dosage form with improved physicochemical properties.
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