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.
Purposes Reactive oxygen species production is harmful to human’s health. The presence of antioxidants in the body may help to diminish reactive oxygen species. Trans-ferulic acid is a good antioxidant, but its low water solubility excludes its utilization. The study aims to explore whether a vesicular drug delivery could be a way to overcome the poor absorption of trans-ferulic acid hence improving its antimicrobial efficiency and antioxidant effect. Methods Niosomal vesicles containing the drug were prepared by film hydration method. The obtained vesicles were investigated in terms of morphology, size, entrapment efficiency, release behavior, cellular cytotoxicity, antioxidant, cellular protection study, and antimicrobial evaluations. Results The optimized niosomal formulation had a particle size of 158.7 nm and entrapment efficiency of 21.64%. The results showed that the optimized formulation containing 25 μM of trans-ferulic acid could enhance the viability of human foreskin fibroblast HFF cell line against reactive oxygen species production. The minimum effective dose of the plain drug and the niosomal formulation against Staphylococcus aurous (ATCC 29213) was 750 µg/mL and 375 µg/mL, respectively, and for Escherichia coli (ATCC 25922), it was 750 µg/mL and 187/5 µg/mL, respectively. The formulation could also improve the minimum bactericidal concentration of the drug in Staphylococcus aurous, Escherichia coli, and Acinobacter baumannii (ATCC 19606). Conclusion These results revealed an improvement in both antibacterial and antioxidant effects of the drug in the niosomal formulation.
Background: Pelargonium graveolens L'Hér has traditionally been used to reduce skin inflammation, and recent studies have confirmed antioxidant compounds in the plant's extract. The present study aimed to prepare a lipogel formulation from P. graveolens hydroalcoholic extract and evaluate its efficacy on the wound healing process in an animal model. Material and Methods: The aerial part extract of P. graveolens was prepared through percolation. Additionally, plastibase was prepared by mixing 5% of low-molecular-weight polyethylene with hot mineral oil (130 ˚C). The extract (5%) was levigated in the mineral oil (5-15%) and dispersed in the cooled plastibase. The physical properties of the lipogel, thermal stability, and microbial limits were tested. Further, the effect of the lipogel on the wound healing rate was examined among male Wistar rats, and skin tissue samples were assessed histologically. Results and Discussion: The results represented the best rheological and thermal stability characteristics in the formulation with 5% mineral oil (as the levigator). The lipogel-treated group had the least burn area compared to the silver sulfadiazine and negative control groups (p<0.05). The microscopic examination of tissue samples revealed increased collagen fiber production and maturation and significantly also faster epithelial repair among lipogel-treated rats than the other two groups (p<0.05). Conclusion: The results indicated the significant therapeutic effects of P. graveolens lipogel on burn healing. The suitable physicochemical properties and low lipogel production cost facilitate further scale-up studies.
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