Abstract
A modified electrospraying process is exploited to enhance the dissolution profiles of a poorly water-soluble drug. With polyvinylpyrrolidone (PVP) as a hydrophilic polymer matrix and ketoprofen (KET) as a model drug, polymer-drug composites in the form of nanoparticles were prepared and characterized. The surface morphologies, the physical status of the drug, and the drug-polymer interactions were studied using FESEM, DSC, XRD, and ATR-FTIR. FESEM observations demonstrated that the nanoparticles gradually decreased in size from 640 ± 350, to 530 ± 320, 460 ± 200 and 320 ± 160 nm as the KET content increased from 0, to 9.1%, 16.7% and 33.3% w/w, respectively. Results from DSC and XRD suggested that KET was distributed in the PVP matrix in an amorphous manner at the molecular level. This is thought to be due to their compatibility, arising through hydrogen bonding as demonstrated by ATR- FTIR spectra. In vitro dissolution tests showed that the nanoparticles released the incorporated KET within 1 min, evidencing markedly improved dissolution over pure KET and a KET-PVP physical mixture. Electrospraying can hence offer a facile route to develop new polymer composites for biomedical applications, in particular for improving dissolution rate of poorly water-soluble drugs.
Highlights
The solubility behavior of poorly water-soluble drugs remains one of the most challenging aspects of formulation development [1,2]
In a typical electrospraying process, a liquid is fed to a metal capillary at the end of which a droplet is formed
To verify KET molecular integrity after the electrospraying process, drug-loaded electrosprayed nanoparticles were dissolved in DMSO-d6 and the resulting solutions were analyzed by 1H NMR
Summary
The solubility behavior of poorly water-soluble drugs remains one of the most challenging aspects of formulation development [1,2]. In the biomedical and drug delivery area, the Edirisinghe group has successfully prepared hollow microspheres, porous films, drug-loaded micro- and nanoparticles, and microbubbles using this technology [2931] All their investigations demonstrated that electrospraying is a useful tool for developing novel bimaterials and drug delivery systems. Polymer-based SDs have been demonstrated to be suitable for the formulation of poorly water-soluble drugs in the amorphous form, leading to enhancement of dissolution rates and bioperformance [32,33]. The polyvinylpyrrolidone (PVP) series of polymers is widely used in the pharmaceutical field for excipients, and these materials are suitable for the preparation of SDs by the solvent methods This is due to their high solubility in water (and in many organic solvents), rapid uptake of water, and their ability to prevent the crystallization of dispersed drugs [34]. With PVP as a polymer matrix and ketoprofen (KET) as a poorly water-soluble model drug, SDs in polymer-based nanoparticles prepared using an electrospraying process are reported in this paper
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