Nandita Deb

This study aims to improve the biopharmaceutical, mechanical, and tableting properties of a poorly soluble drug, ibuprofen (IBP), by preparing amorphous solid dispersion (ASD) followed by a sustained-release tablet formulation. A suitable polymer to develop an ASD system was chosen by utilizing the apparent solubility of IBP in various polymer solutions. ASDs containing various ratios of IBP and selected polymer were prepared by the melt fusion (MF) method. ASD containing optimized drug-polymer ratio prepared by freeze-drying (FD) method was characterized and compared physicochemically. The solubility of IBP in water increased 28-fold and 35-fold when formulated as ASD by MF and FD, respectively. Precise formulations showed amorphization of IBP and increased surface area, improving solubility. The dissolution pattern of optimized ASD-IBP in pH 6.8 phosphate buffer after 60 min in MF and FD was enhanced 3-fold. In addition, direct compression tablets comprising optimized ASD granules from MF and FD were made and assessed using compendial and noncompendial methods. ASD-IBP/MF and ASD-IBP/FD formulations showed a similar drug release profile. In addition, 12 h of sustained IBP release from the ASD-IBP-containing tablets was obtained in a phosphate buffer with a pH of 6.8. From the dissolution kinetics analysis, the Weibull model fitted well. The drug release pattern indicated minimal variations between tablets formed using ASD-IBP prepared by both procedures; however, pre- and postcompression assessment parameters differed. From these findings, the application of ASD and sustained-release polymers in matrix formation might be beneficial in improving the solubility and absorption of poorly soluble drugs such as IBP.

Magnetic iron oxide nanoparticles have versatile applications in biomedical science that require control over shape and size distribution. Thermal decomposition is one of the best methods for controlling the size and shape of produced nanoparticles (NPs). The size distribution can be tuned (5–30 nm) by varying the reaction environment such as precursor concentration, amount of solvent used, temperature ramp, and reflux time. Iron oleate was used as a precursor solution and heated up to reflux temperature (310 °C) for 10 min within the oxygen-free environment by applying N2 gas flow. The XRD pattern confirmed the formation of NPs with a crystallite size of 17 ± 2.45 nm. Transmission electron microscope images showed moderately cubic shapes with a mean particle size of 28.67 ± 7.12 nm. Magnetic properties such as saturation magnetization, coercivity, and remanence were calculated at 23.48 emu/gm, 33 Oe, and 0.6 emu/gm, respectively, which indicated the ferromagnetic nature of the NPs. The Verwey transition was identified from the magnetization vs temperature (FC-ZFC) plot. The bondings of the oleic acid surfactant with the produced NPs were confirmed from Fourier transformation infrared spectroscopy (FTIR) data analysis. For the application of hyperthermia, the hydrophobic phase was transferred to the hydrophilic phase using cetyltrimethylammonium bromide, which was assured by the FTIR data analysis. The hyperthermia heating of NPs was measured for different concentrations of NPs (0.25, 0.5, 1, 2, and 4 mg/ml), from which specific loss power (SLP) was calculated. Among them, 0.25 mg/ml produced the most prominent SLP (2149 ± 309 w/g) that can be applied for targeted cancer treatment.