Effect of Physicochemical Properties of Drugs on Morphology and Release of Microspheres

1,3-bis(-2-chloroethyl)-1-nitrosourea (BCNU)-loaded and paclitaxel-loaded poly(D,L-lactide) (PDLLA) microspheres, respectively, were prepared by the spray-drying method. The influence of the physicochemical properties of the two drugs on the morphology, encapsulation efficiency, and in vitro drug release behavior were studied. The results show that the plasticization of BCNU to PDLLA greatly affects the morphology and release behavior of the microspheres. The microparticles prepared with BCNU had a spherical shape when the initial loading amount was less than 10%. With a further increase in the BCNU loading amount, the microspheres began to aggregate and lost their spherical shape. Compared to paclitaxel-loaded microspheres, BCNU-loaded ones exhibited remarkable burst release behavior due to active macromolecule motion. The cytotoxicity experiments show that the long-term cytotoxicity on tumor cells of BCNU-loaded microspheres was similar to that of paclitaxel-loaded microspheres, and that both the drug loaded in microsphere exhibited a superior inhibition effect on tumor cells to their commercial form.

並列關鍵字

1,3-bis(-2-chloroethyl)-1-nitrosourea (BCNU) ； Paclitaxel ； Microspheres ； Spray drying ； Physicochemical properties

國際替代計量

全文下載

主題瀏覽