Modified Preparation Method and Characteristics of NimodipineLoaded PLGA Microspheres
CHANG Si1, LI Xiu-Juan1, GONG Jun-Bo1,3, YANG Ming-Shi2, WEI Zhen-Ping1,3
1.School of Chemical Engineering and Technology, Tianjin , China； 2.Faculty of Pharmaceutical Sciences, University of Copenhagen; 3.Tianjin Key Laboratory for Modern Drug Delivery & HighEfficiency, School of Pharmaceutical Science and Technology, Tianjin University
Abstract The effect of petroleum ether, as an organic phase co-solvent, on the characteristics of nimodipine (NMP)-loaded poly (lactide-co-glycolide) (PLGA) microspheres prepared via the emulsionsolvent evaporation/extraction process was studied. Different ratio of petroleum ether to dichloromethane (DCM) (0, 1∶10, 1∶8, 1∶4, and 1∶2, v/v) caused different solidification rate, leading to different properties of microspheres. At the ratio of 1∶10, the initial burst of microspheres was attenuated, and the encapsulation efficiency was improved significantly. To perform the orthogonal design for process optimization, polymer concentration, drug/PLGA ratio and ratio of petroleum ether/DCM were set as the factors for investigation. After optimization, the encapsulation efficiency of microspheres was improved by 52.2%, and the initial burst was declined by 58.8%. Drug was encapsulated in the matrix as amorphous state. Compared with microspheres prepared by single solvent, the morphology of the optimal formulation was modified evidently, therefore NMP was released in a more controlled fashion.
CHANG Si, LI Xiu-Juan, GONG Jun-Bo, YANG Ming-Shi, WEI Zhen-Ping.Modified Preparation Method and Characteristics of NimodipineLoaded PLGA Microspheres[J] Chemcial Industry and Engineering, 2013,V30(1): 1-7
2013, Vol. 30 
