Development of A Chemically Stable 10-Hydroxycamptothecin Nanosuspension Using A Combination of Microprecipitation and High Pressure Homogenization

摘要

@@Objects The purpose of this study was to prepare and characterize nanosuspensions loading the active lactone form of 10-hydroxycamptothecin (10-HCPT). Methods Nanosuspensions were prepared in terms of microprecipitation-high pressure homogenization method. As for the preparation processes, three important parameters, I.e. the agitation rate of stabilizer solution, homogenization pressure and cycle numbers, were investigated and optimized. The particle size, zeta potential, morphology of nanosuspensions and the solid state of 10-HCPT were characterized by the correlative methods, such as laser diffraction, Zeta Potential Analyzer, TEM, X-ray diffractometer and DSC, and so on. The chemical stability of 10-HCPT in nanosuspension compared to the solution at different pH values were tested by HPLC, and the dissolution studies of nanosuspesions and coarse suspensions were carried out by the paddle method of Chinese Pharmacopoeia 2005.