All-trans retinoic acid release from surfactant-free nanoparticles of poly(DL-lactide-co-glycolide)

Abstract

In this study, we prepared all-trans retinoic acid (ATRA)-encapsulated, surfactant-free, PLGA nanoparticles. The nanoparticles were formed by nanoprecipitation process, after which the solvent was removed by solvent evaporation or dialysis method. When a nanoparticle was prepared by the nanoprecipitation -solvent evaporation method, the nanoparticles were bigger than the nanoparticles of the nanoprecipitation -dialysis method, despite the higher although loading efficiency. Nanoparticles from the nanoprecipitation -dialysis method were smaller than 200 nm in diameter, while the loading efficiency was not significantly changed. Especially, nanoparticles prepared from DMAc, 1,4-dioxane, and DMF had a diameter of less than 100 nm. In the transmission electron microscopy (TEM) observations, all of the nanoparticles showed spherical shapes. The loading efficiency of ATRA was higher than 90 % (w/w) at all formulations with exception of THF. The drug content was increased with increasing drugfeeding amount while the loading efficiency was decreased. In the drug release study, an initial burst was observed for 2~6 days according to the variations of the formulation, after which the drug was continuously released over one month. Nanoparticles from the nanoprecipitation -dialysis method showed faster drug release than those from the nanoprecipitation -solvent evaporation method. The decreased drug release kinetics was observed at lower drug contents. In the tumor cell cytotoxicity test, ATRA-encapsulated, surfactant-free, PLGA nanoparticles exhibited similar cytotoxicity with that of ATRA itself.

All-trans retinoic acid-incorporated nanoparticles of deoxycholic acid-conjugated dextran for treatment of CT26 colorectal carcinoma cells

“…Antimetastatic effects of RA against mouse pulmonary metastatic model have been investigated by several researchers. 25,27 We also demonstrated the antimetastatic activity of RA-incorporated nanoparticles using mouse pulmonary metastatic model of CT26 cells, as shown in Figure 7. Suzuki et al reported that RA-encapsulated cationic liposome suppressed pulmonary metastasis of tumor cells.…”

“…3 As shown in Figure 3, RA with higher drug content was released slowly from the nanoparticles compared to lower drug loading, indicating that RA might be crystallized in the core of the nanoparticles and released slowly. In a previous report by Jeong et al, 27 RA was crystallized in the core of the nanoparticles at higher drug loading, and solubilization of crystallized drug into the release medium was delayed compared to molecular dispersion of drug. They demonstrated that RA can be crystallized in the nanoparticles at higher drug loading through analysis of powder X-ray diffraction.…”

Antitumor activity of sorafenib-incorporated nanoparticles of dextran/poly(dl-lactide-co-glycolide) block copolymer

“…Nanoparticles of Dex b LG copolymer were prepared by nanoprecipitation-dialysis method [ 13 ]. Nanoprecipitation-dialysis method was superior over direct dialysis in minimizing particle size of nanoparticles (data not shown) [ 14 ]. Empty nanoparticles of Dex b LG had a spherical shape with a diameter < 100 nm (Figure 2a ).…”

Thermally induced mesophase development in ethanesilica filmsvia macromolecular templating approach

“…The weight fraction of PEO blocks ( f PEO ) for the triblock copolymer prepared in the present study was found to be 0.38. [31][32][33][34][35] Preparation of Mesoporous Organosilica as Thin Film Form. Mesoporous organosilicate thin films were prepared using a silica sol solution containing PEO-PLGA-PEO (EO 16 Thin Film Characterization.…”