Micronization of taxifolin by supercritical antisolvent process and evaluation of radical scavenging activity.

The aim of this study was to prepare micronized taxifolin powder using the supercritical antisolvent precipitation process to improve the dissolution rate of taxifolin. Ethanol was used as solvent and carbon dioxide was used as an antisolvent. The effects of process parameters, such as temperature (35-65 °C), pressure (10-25 MPa), solution flow rate (3-6 mL/min) and concentration of the liquid solution (5-20 mg/mL) on the precipitate crystals were investigated. With a lower temperature, a stronger pressure and a lower concentration of the liquid solution, the size of crystals decreased. The precipitation temperature, pressure and concentration of taxifolin solution had a significant effect. However, the solution flow rate had a negligible effect. It was concluded that the physicochemical properties and dissolution rate of crystalline taxifolin could be improved by physical modification such as particle size reduction using the supercritical antisolvent (SAS) process. Further, the SAS process was a powerful methodology for improving the physicochemical properties and radical scavenging activity of taxifolin.

Insulin nanoparticles for transdermal delivery: preparation and physicochemical characterization and in vitro evaluation.

AIM: This work is aimed to study the feasibility of insulin nanoparticles for transdermal drug delivery (TDD) using supercritical antisolvent (SAS) micronization process. METHODS: The influences of various experimental factors on the mean particle size (MPS) of insulin nanoparticles were investigated. Moreover, the insulin nanoparticles obtained were characterized by scanning electron microscopy (SEM), dynamic light scattering (DLS), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and thermogravimetric (TG) analyses. RESULTS: Under optimum conditions, uniform spherical insulin nanoparticles with a MPS of 68.2 +/- 10.8 nm were obtained. The Physicochemical characterization results showed that SAS process has not induced degradation of insulin. Evaluation in vitro showed that insulin nanoparticles were accorded with the Fick's first diffusion law and had a high permeation rate. CONCLUSION: These results suggest that insulin nanoparticles can have a great potential in TDD systems of diabetes chemotherapy.

Preparation and characterization of chitosan-polyvinyl alcohol blend hydrogels for the controlled release of nano-insulin.

Chitosan (CS)-polyvinyl alcohol (PVA) blend hydrogels were prepared using glutaraldehyde as the cross-linking agent. The obtained hydrogels, which have the advantages of both PVA and CS, can be used as a material for the transdermal drug delivery (TDD) of insulin. The nano-insulin-loaded hydrogels were prepared under the following conditions: 1.2g of polyethylene glycol, 1.5 g of CS, 1.2 g of PVA, 1.2 mL of 1% glutaraldehyde solution, 16 mL of water, and 40 mg of nano-insulin with 12 min of mixing time and 3 min of cross-linking time. The nano-insulin-loaded hydrogels were characterized using scanning electron microscopy, energy dispersive spectrometry, Fourier-transform infrared spectroscopy, differential scanning calorimetry, thermogravimetric analysis, X-ray diffraction, and its mechanical properties were analyzed. The results show that all molecules in the hydrogel have good compatibility and they formed a honeycomb-like structure. The hydrogel also showed good mechanical and thermal properties. The in vitro drug release of the hydrogel showed that the nano-insulin accorded with Fick's first law of diffusion and it has a high permeation rate (4.421 µg/(cm(2)h)). These results suggest that the nano-insulin-loaded hydrogels are a promising non-invasive TDD system for diabetes chemotherapy.

Process optimization for the preparation of oligomycin-loaded folate-conjugated chitosan nanoparticles as a tumor-targeted drug delivery system using a two-level factorial design method.

Oligomycin-A (Oli-A), an anticancer drug, was loaded to the folate (FA)-conjugated chitosan as a tumor-targeted drug delivery system for the purpose of overcoming the nonspecific targeting characteristics and the hydrophobicity of the compound. The two-level factorial design (2-LFD) was applied to modeling the preparation process, which was composed of five independent variables, namely FA-conjugated chitosan (FA-CS) concentration, Oli-A concentration, sodium tripolyphosphate (TPP) concentration, the mass ratio of FA-CS to TPP, and crosslinking time. The mean particle size (MPS) and the drug loading rate (DLR) of the resulting Oli-loaded FA-CS nanoparticles (FA-Oli-CSNPs) were used as response variables. The interactive effects of the five independent variables on the response variables were studied. The characteristics of the nanoparticles, such as amount of FA conjugation, drug entrapment rate (DER), DLR, surface morphology, and release kinetics properties in vitro were investigated. The FA-Oli-CSNPs with MPS of 182.6 nm, DER of 17.3%, DLR of 58.5%, and zeta potential (ZP) of 24.6 mV were obtained under optimum conditions. The amount of FA conjugation was 45.9 mg/g chitosan. The FA-Oli-CSNPs showed sustained-release characteristics for 576 hours in vitro. The results indicated that FA-Oli-CSNPs obtained as a targeted drug delivery system could be effective in the therapy of leukemia in the future.