School of Mechanical and Aerospace Engineering, Nanyang Technological University, 50 Nanyang Avenue, Singapore 639798, Singapore.
Int J Pharm. 2010 Jan 4;383(1-2):285-92. doi: 10.1016/j.ijpharm.2009.09.030. Epub 2009 Sep 23.
Evaporative precipitation of nanosuspension (EPN) was used to fabricate nanoparticles of a poorly water-soluble antimalarial drug, artemisinin (ART), with the aim of enhancing its dissolution rate. We investigated the nanoparticle fabrication of ART via a full factorial experimental design considering the effects of drug concentration and solvent to antisolvent ratio on the physical, morphological and dissolution properties of ART. Characterization of the original ART powder and EPN prepared ART nanoparticles was carried out by scanning electron microscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD) and dissolution tester. DSC and XRD studies suggested that the crystallinity of EPN prepared ART nanoparticles decreased with increasing drug concentration and ratio of solvent to antisolvent. The particle diameters of EPN prepared ART nanoparticles were found to be 100-360 nm. The dissolution of EPN prepared ART nanoparticles markedly increased as compared to the original ART powder. A percent dissolution surface-response model was used to elucidate the significant and direct relationships between drug concentration and solvent to antisolvent ratio on one hand and percent dissolution on the other hand. The best dissolution percent was found to be 75.9%, at the drug concentration of 15 mg/mL and solvent to antisolvent ratio (by volume) of 1:20.
纳米混悬剂的蒸发沉淀(EPN)被用于制备一种难溶性抗疟药物青蒿素(ART)的纳米粒子,旨在提高其溶解速率。我们通过全因子实验设计研究了 ART 的纳米粒子制备,考虑了药物浓度和溶剂与抗溶剂比对 ART 的物理、形态和溶解性能的影响。通过扫描电子显微镜、差示扫描量热法(DSC)、X 射线衍射(XRD)和溶解测试仪对原始 ART 粉末和 EPN 制备的 ART 纳米粒子进行了表征。DSC 和 XRD 研究表明,EPN 制备的 ART 纳米粒子的结晶度随着药物浓度和溶剂与抗溶剂比的增加而降低。EPN 制备的 ART 纳米粒子的粒径为 100-360nm。与原始 ART 粉末相比,EPN 制备的 ART 纳米粒子的溶解明显增加。使用溶解百分比表面响应模型来阐明药物浓度和溶剂与抗溶剂比与溶解百分比之间的显著直接关系。发现最佳溶解百分比为 75.9%,药物浓度为 15mg/mL,溶剂与抗溶剂比(体积比)为 1:20。