| Title | Development and in vitro evaluation of deacety mycoepoxydiene nanosuspension |
| Authors | Wang, Yancai Liu, Zhaoping Zhang, Dianrui Gao, Xihui Zhang, Xiaoyu Duan, Cunxian Jia, Lejiao Feng, Feifei Huang, Yaojian Shen, Yuemao Zhang, Qiang |
| Affiliation | Shandong Univ, Ctr New Drug Evaluat, Jinan 250012, Peoples R China. Shandong Univ, Coll Pharm, Jinan 250012, Peoples R China. Xiamen Univ, Sch Life Sci, Xiamen 361005, Peoples R China. Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China. |
| Keywords | Deacety mycoepoxydiene Nanosuspension Dissolution velocity Delivery system Cancer therapy POORLY SOLUBLE DRUGS DISSOLUTION RATE ENHANCEMENT HIGH-PRESSURE HOMOGENIZATION PHARMACOKINETIC EVALUATION NANOCRYSTALS DELIVERY FORMULATION NANOPARTICLES SUSPENSIONS TECHNOLOGY |
| Issue Date | 2011 |
| Publisher | colloids and surfaces b biointerfaces |
| Citation | COLLOIDS AND SURFACES B-BIOINTERFACES.2011,83,(2),189-197. |
| Abstract | Deacety mycoepoxydiene (DM), extracted from Phomopsis sp. A123 of thalassiomycetes, is a novel and potent anti-cancer agent. Due to its physicochemical characteristics, the drug, a poorly water-soluble weak acid, shows poor solubility and dissolution characteristics. To improve the solubility and dissolution, formulation of DM as nanosuspension has been performed in this study. Nanosuspensions were developed by high-pressure homogenization (HPH) (DissoCubes (R) Technology) and transformed into dry powder by freeze-drying. The nanosuspension produced was then investigated using optical microscope, photon correlation spectroscopy (PCS), zeta potential measurement, SEM, TEM, AFM, DSC and XRD. To verify the theoretical hypothesis on the benefit of increased surface area, in vitro saturation solubility and dissolution profile were investigated. In addition, the in vitro cell cytotoxicity was examined. Results showed that a narrow size distributed nanosuspension composed of unchanged crystalline state with a mean particle size of 515 +/- 18 nm, a polydispersity index of 0.12 +/- 0.03 and a zeta potential of -23.1 +/- 3.5 mV was obtained. In the in vitro dissolution test an accelerated dissolution velocity and increased saturation solubility could be shown for the MD nanosuspension. The in vitro cytotoxicity experiments provided evidence for an enhanced efficacy of the DM nanosuspension formulation compared to free DM solution. Taken together, these results illustrate the opportunity to formulate DM in nanosuspension form as an anti-prostate cancer delivery system. (C) 2010 Published by Elsevier B.V. |
| URI | http://hdl.handle.net/20.500.11897/240362 |
| ISSN | 0927-7765 |
| DOI | 10.1016/j.colsurfb.2010.10.029 |
| Indexed | SCI(E) EI |
| Appears in Collections: | 药学院 |
