Abstract
Deferasirox (DFX) is an oral iron-chelating agent and classified into class II of the Biopharmaceutics Classification System. Low bioavailability of the drug due to insufficient solubility in physiological fluids is the main drawback of DFX. The idea of the current study was to explore the potential of solid dispersion (SD) as an effective method to improve the dissolution rate of DFX in pellets. The SDs were made by the solvent evaporation technique using polyethylene glycol 4000 (PEG 4000) and polyvinylpyrrolidone K25 with different drug-to-carrier ratios. Then, the dispersion was milled and mixed with other components and the mixture layered on sugar-based cores by pan coating technique. The pellets were evaluated in terms of size distribution, morphology (SEM), and dissolution behaviour. Drug-polymer interactions were studied using differential scanning calorimetry (DSC), X-ray diffraction study (XRD), and Fourier transformation infrared (FTIR) spectroscopy. The pellets coated with SD showed a remarkable rise in the solubility of DFX than that of free drug-loaded pellets. The dispersion with PVP K25 showed a faster dissolution rate as compared to other mixtures. The DSC and XRD analysis indicated that the drug was in the amorphous state when dispersed in the polymer. The FTIR studies demonstrated any ruled out interaction between drug and polymer. The SEM showed smoothness on the surface of the pellets. It is resolved that the SD method considerably enriched the dissolution rate of DFX in pellets, which can also be utilized for other poorly water-soluble drugs.
Highlights
Oral administration is still the most accessible and favorite way of drug delivery among patients because of its simple application
Phase solubility indicated that the solubility of DFX enhanced as a consequence of the concentration of polymers added to the formulation
This report disclosed that the preparation of drug-polymer solid dispersion (SD) had a significant effect on the solubility and dissolution rate of DFX
Summary
Oral administration is still the most accessible and favorite way of drug delivery among patients because of its simple application. This interest led researchers to focus on enhancing the dissolution of low-soluble drugs for oral delivery through an enhancement in solubility and control of drug release, making the formulations more biocompatible, and improving bioavailability. The solubility of molecules in the biological fluid is the major and essential process for the intestinal absorption of drug compounds. One of the main reasons for low absorption and high individual variability of drugs is the lack of solubility in physiological fluids. 40% of novel drugs discovered by pharmaceutical corporations have difficulties in aqueous solubility, and many formulations have failed because of insufficient biopharmaceutical properties [2, 3]
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