The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 μM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

Objectives: A compaction simulator (CS) is a single-punch instrument that records data during the powder compaction process. The aim of the study was to determine the behavior of lactose-based direct tableting agents (DTAs) by CS. The data recorded were used to evaluate the flowability and compressibility of powders. The focus of the study was on comparing the compressibility of StarLac (R) [alpha lactose monohydrate (85%) and white maize starch (15%)] and FlowLac (R) 100 (spray-dried alpha lactose monohydrate) in order to make tablets containing poorly flowable paracetamol. Materials and Methods: Two lactose-based DTAs were used. Physical characterization of these powders was done by measuring bulk, tapped, and true densities alongside scanning electron microscopy analysis. Flow properties were then calculated by the angle of repose, Hausner ratio, and Carr's compressibility index. Force, in-die thickness, and punch displacement data produced by the CS were captured during in-die compression. Compressibility was calculated using the Heckel equation. Results: The physical characterization test results showed no significant difference between the two DTAs. Hardness results revealed that tablet formulations containing FlowLac (R) had higher sensitivity to an increase in compression force in comparison with StarLac (R). From the Heckel plots generated by the CS during the compression cycle, yield pressure (Py) values were calculated for FlowLac (R) 100 and StarLac (R). The Heckel parameter (Py) for FlowLac (R) 100 and StarLac (R) was calculated as 87.5 MPa and 85.2 MPa, respectively, during the compaction cycle at 5 kN. These data indicated that both powders are compressible and have brittle behavior. Conclusion: StarLac (R) is less brittle, which was shown by its lower sensitivity to compression force. Py values obtained from the Heckel equation described the plasticity of particles, which gives distinct information on the compressibility of both DTAs in real time during the compaction cycle.

Multidrug resistance (MDR) and chemotherapy-associated toxicity remain major challenges limiting the success of cancer treatments. In this context, berberine (BBR), an isoquinoline derivative belonging to the barberry family, has emerged as a promising adjuvant that can enhance the efficacy of chemotherapy while potentially mitigating its side effects. The findings indicate that berberine enhances the therapeutic effect of several drugs, such as doxorubicin, cisplatin, tamoxifen, and 5-fluorouracil, through multiple mechanisms including the inhibition of ABC transporters, regulation of autophagy, and synergistic enhancement of reactive oxygen species generation. Advanced pharmaceutical and nanotechnological formulations, including cyclodextrin complexes, solid dispersions, liposomes, solid lipid nanoparticles, nanostructured lipid carriers, polymeric nanoparticles, chitosan-based systems, and inorganic nanoplatforms, have demonstrated significant improvements in the solubility, stability, cellular uptake, and oral bioavailability of berberine. However, knowledge gaps remain regarding optimal dosage determination, safety assessment in combination therapy, and establishing efficacy in large-scale clinical trials. Incorporating berberine into combination therapy strategies may improve treatment outcomes, overcome drug resistance, and potentially reduce the toxic burden associated with chemotherapy. Therefore, this review provides a comprehensive analytical framework for berberine’s potential as an adjuvant, elucidates its mechanistic synergistic interactions with standard therapies, explores pharmaceutical strategies to overcome bioavailability limitations, and suggests future research avenues to further its clinical development.

This study was performed to understand the behavior of poorly compressible paracetamol powder using a compaction simulator (CS), equipment that records data during the compaction process. The aim was to investigate the compressibility of paracetamol tablets using a dry granulation (slugging) process, with different formulation compositions. Formulations were prepared to observe the effect on compressibility with two different lactose-based fillers, Flowlac®100 and Granulac®70, and a binder, Kollidon® K90. In each combination, a total of four formulations were prepared with paracetamol to filler ratios of 1:1 and 0.8:1. Tablets were produced by single punch (11.28 mm) CS at six different pressures (152, 210, 263, 316, 400, and 452 MPa). During compression, upper punch displacement and force data were produced by the CS equipment. The compressed tablets were tested for hardness, thickness, and weight variation and compared with each other. All formulations reached maximum tensile strength at compaction pressures between 263 and 316 MPa. In the formulations without binder, those containing Granulac®70 had higher tensile strength than those containing Flowlac®100 at both filler ratios. The results obtained indicated that the addition of binder to the formulations (F-45-1, F-45-2, F-50-3, and F-50-4) improved the compressibility of paracetamol. Formulation F-45-2, containing Flowlac®100 and binder, showed better compressibility at 2.9 MPa tensile strength. Data from the CS were used to compare Young’s modulus and work of compaction on selected formulations (F-45-1 and F-45-2). The proposed lactose-based filler, Flowlac®100, with low pressure can be successfully applied for improving the compressibility of paracetamol. An optimum formulation can be designed with smaller amounts of materials using a compaction simulator.

Aim of the study is to evaluate the potential use of Thymus capitatus (L.) Hoffm. & Link and Origanum dubium Boiss. essential oils and their major constituents; thymol and carvacrol in cancer therapies. For this aim hMSC-telo1 cells and their tumorigenic counterpart were exposed to varying concentrations of Thymus capitatus (L.) Hoffm. & Link and Origanum dubium Boiss. essential oils, thymol and carvacrol and cellular viability and proliferation have been evaluated by MTT assay. TUNEL assay has used for evaluation of apoptosis. Study suggested that, Thymus capitatus (L.) Hoffm. & Link essential oil and thymol have an enhancer effect once combined with conventional chemotherapeutic agents. 0.005 v/v % of Thymus capitatus (L.) Hoffm. & Link, 0.005 v/v % and 0.05 v/v % of thymol showed enchancer effect by sparing the normal hMSC-telo1 cells from the cytotoxicity of Deferasirox while these combinations were cytotoxic towards tumorigenic hMSC-telo1 cells.