The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was the purpose of this survey. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of several amounts of them on the dissolution behaviour of indomethacin was investigated. It is worth mentioning that the ratio of microcrystalline cellulose (carrier) to silica (coating powder material) was 20 in all formulations. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, the differential scanning calorimeter (DSC) was used. The results showed that the liquisolid formulations exhibited significantly higher drug dissolution rates in comparison with directly compressed tablet. The enhanced rate of indomethacin dissolution derived from liquisolid tablets was probably due to an increase in wetting properties and surface area of drug particles available for dissolution. Moreover, it was indicated that the fraction of molecularly dispersed drug (FM) in the liquid medication of liquisolid systems was directly proportional to their indomethacin dissolution rate (DR). An attempt was made to correlate the percentage drug dissolved in 10 min with the solubility of indomethacin in PEG 200 and glycerin. In conclusion, the liquisolid compacts technique can be a promising alternative for the formulation of water insoluble drugs, such as indomethacin into rapid release tablets.

Background: In the current investigation, the evaluation of model congruence alongside experimental determinations of the solid-liquid phase boundary concerning sildenafil citrate (SICI) within aqueous binary blends of polyethylene glycol 200 has been conducted. Methods: Solubility values were measured using a classical method of Shake-flask at various temperatures. Results: It was observed that the dissolution profile of SICI in the specified binary media demonstrated a positive thermal coefficient. For the determined solubility data, mathematical cosolvency models were employed for the fitting and prediction tasks, showcasing a commendable capability in forecasting the solubility patterns of SICI in the aqueous solutions of polyethylene glycol 200. In addition, apparent thermodynamic quantities pertaining to the dissolution of SICI were computed utilizing both Gibbs and van’t Hoff equations, facilitating an in-depth comprehension of the solubilization phenomena within the studied solvents. Conclusion: The insights gleaned from the rigorous interrogation and validation of the solubility for SICI promise to enhance crystallization methodologies, scale-up production, and pharmaceutical formulation studies.

Background: Adapting controlled release technologies to the delivery of DNA has the great potential to overcome extracellular barriers that limit gene delivery. This study investigates the effect of different mass ratio of PLA: PEG in the various tri block poly (lactic acid)-poly (ethylene glycol)-Poly (lactic acid) copolymer (PLA-PEG-PLA) on the properties of the resulting nanoparticles. Methods: The various tri block PLA-PEG-PLA copolymers were prepared via ring-opening polymerization by poly (ethylene glycol) (PEG), lactic acid and stannous octoate as raw material and catalyst, respectively. DNA or siRNA-FAM was incorporated into the tree block PLA-PEG-PLA copolymer using double emulsion solvent evaporation technique. Properties of these nanoparticles, such as morphology and particles size of nanoparticles, DNA release kinetics, in vitro cytotoxicity and siRNA-FAM transfer efficiency were evaluated. Results: Scanning electron microscope (SEM) showed that PLA-PEG-PLA/DNA nanoparticles have spherical morphology with smooth surface. Dynamic light scattering results showed the particle size of PLA– PEG-PLA copolymers increased with an increase in the mass ratio of PLA in PLA-PEG-PLA copolymers. The release profile of the PLA-PEG-PLA/DNA nanoparticles measured using nanodrop and the results showed that, decrease in mass ratio of PLA, increased the release profile of DNA from PLA-PEG-PLA/DNA nanoparticles. Moreover the percentage of siRNA-FAM transfer to MCF-7 cells by various PLA-PEG-PLA copolymers, measuring using flow cytometry and fluorescence microscopy. Conclusion: These results showed that there is same relation between the mass ratio of PLA and percentage of siRNA-FAM delivery into the MCF-7 cells.