원문정보
초록
영어
In this work, 5' -nitro-indirubinoxime (5' -NIO), which has a strong anticancer activity especially for head and neck cancer, has been formulated as solid dispersions using a supercritical aerosol solvent extraction system (ASES) process in order to enhance its solubility, dissolution rate and bioavailability.
Solid dispersions of 5' -NIO and poly(vinyl pyrrolidone) (PVP) were prepared in various weight percent ratios to investigate the effect of PVP level on the morphology and dissolution behavior of 5' -NIO. Ternary solid dispersions consisting of 5' -NIO, PVP, and poloxamer 188 were also prepared to study the influence of poloxamer 188. All samples were prepared at 35oC and 180 bar
using supercritical carbon dioxide. The particle sizes of all the solid dispersion samples were found to be much smaller than that of the original 5' -NIO. XRD results showed that the crystallinity of the original 5' -NIO was not found in the solid dispersions obtained by the ASES process. Higher solubility and faster dissolution rates were observed for the ternary solid dispersions because the arrangement of ethylene oxide and propylene oxide blocks of the poloxamer 188 enabled the formation of micelles in an aqueous phase. Our study confirmed that
the addition of block copolymers such as poloxamer 188 to solid dispersions is a promising method to improve the dissolution rate and solubility of poorly water-soluble drugs.