Preparation, characterization and in vitro evaluation of solid dispersions containing docetaxel.
Solid dispersions using water-soluble carriers were studied for improving the dissolution of docetaxel, a poorly soluble compound. In order to obtain the most optimized formulation, we prepared many solid dispersions with different carriers, different solvents, or at a series of drug-to-carrier ratios, and compared their dissolution. The accumulative dissolution of docetaxel from poloxamer 188 was more excellent than that from PVP(k30) and glyceryl monostearate, and the dissolution of docetaxel from solid dispersion was markedly higher than that of pure docetaxel; meanwhile the increased dissolution was partly dependent on the ratios of docetaxel and poloxamer 188. The ethanol used to prepare solid dispersion is of more significant effect on the dissolution of docetaxel than that of acetone. The docetaxel/poloxamer 188 system was characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and environmental scanning electron microscope (ESEM). The results of DSC, XRD, and ESEM analyses of docetaxel/poloxamer 188 system showed that there are intermolecular interactions between docetaxel and poloxamer, and the crystallinity of docetaxel disappeared. These results show that solid dispersion is a promising approach of developing docetaxel drug formulates.
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People's Republic of China.
Jie
J
Chen
Liyan
L
Qiu
Minxin
M
Hu
Yi
Y
Jin
Jieru
J
Han
D000970:Antineoplastic Agents / Q000737:chemistry*; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D000077143:Docetaxel; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D020442:Poloxamer / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D043823:Taxoids / Q000737:chemistry*; D014961:X-Ray Diffraction
D000970:Antineoplastic Agents; D004337:Drug Carriers; D005079:Excipients; D005989:Glycerides; D043823:Taxoids; D020442:Poloxamer; D000077143:Docetaxel; C048159:glyceryl monostearate; D011205:Povidone