Résumé
Objective: Using ethanol as solvent, deionized water as anti-solvent, and HPMC as the surfactant, to prepare trans-cinnamic acid (TCA) micro powder by single factor analysis. The effects of five experimental parameters on the mean particle size (MPS) and morphology of TCA nanosuspension were investigated. Methods: Transmission electron microscope (TEM), laser granulometric analysis, Fourier transform infrared spectroscopy (FTIR), high performance liquid chromatography-mass spectrometry (LC-MS), X-ray diffraction (XRD), differential scanning calorimetry (DSC), and dissolution were used to analyze the characteristic of micronized TCA nanosuspension. Results: The micronized TCA with an MPS of 130 nm was obtained under the optimum conditions. The dissolution rate of TCA nanosuspension was 1.67 times of raw drug. Conclusion: Using anti-solvent recrystallization to prepare micronized TCA can improve the solubility and dispersion of TCA nanosuspension in water, and they provide the basis for further formulation development.
Résumé
To study the preparation, activity and targeting ability evaluation in vitro on epigallocatechin-3-gallate (EGCG) bovine serum albumin nanoparticles targeting to PC-3 cells, the folate mediated EGCG bovine serum albumin nanoparticles (FA-EGCG-BSANP) were prepared by desolvation process. The morphology and particle size of the nanoparticles were determined by atomic force microscope (AFM). HPLC was used to analyse the entrapment efficiency and drug loading rate of EGCG The amount of folate conjugation on the BSANP was determined by quantitative ultraviolet (UV) spectrophotometer analysis. The targeting ability to PC-3 was observed using laser scanning confocal microscope (LSCM) and fluorophotometer microscope. And the activity of FA-EGCG-BSANP was mensurated by MTT method. The morphology and particle size distribution of FA-EGCG-BSANP were uniform and even with the mean particle size of 200 nm. The entrapment efficiency and loading rate of EGCG were (81.5 +/- 1.8) % and (29.3 +/- 0.6) %, respectively, and the amount of folate conjugation was 18.363 microg x mg(-1) BSA. The FA-EGCG-BSANP uptakes by cultured PC-3 cells were 23.65 times the amount of EGCG-BSANP in a concentration dependant manner. The lethality of PC-3 cells treated with FA-EGCG-BSA was 82.8%, while those treated with EGCG and EGCG-BSANP were 58.6% and 55.1%, respectively. And lethality of PC-3 cells was positively correlated with the nanoparticles uptake amount. FA-EGCG-BSANP can significantly promote EGCG to PC-3 cells sites and improve their efficacy, which is considered to an experimental foundation for further research on its activity, targeting ability and metabolism in vivo.