Musumeci T, Vicari L, Ventura C A, Gulisano M, Pignatello R, Puglisi G
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, v.le A. Doria, 6-I-95125 Catania, Italy.
J Nanosci Nanotechnol. 2006 Sep-Oct;6(9-10):3118-25. doi: 10.1166/jnn.2006.452.
The preparation and technological characterization of nanosphere formulations (NS) containing the anticancer drug paclitaxel (PTX) are reported. Poly(lactide) (PLA) and poly(lactide-co-glycolide) (PLGA) nanospheres (NS) were prepared by a solvent displacement method. They showed a mean particle size in the range 150-300 nm, with a high homogeneity (polydispersity index < 0.3). For long term stability, NS require additional procedures, such as freeze-drying. In this study, the effect on NS particle size and surface charge of different lyoprotectants (mono- and disaccharides, polyalcohols, and hydroxypropyl-beta-cyclodextrin) at various concentrations was tested by means of light scattering size analysis. The formulations freeze-dried with the addition of 10% glucose (w/v) showed interesting characteristics after freeze-drying. They were chosen for specific studies on drug encapsulation efficiency, in vitro drug release and biological activity on the human anaplastic thyroid carcinoma cell line 8305C. The PLGA NS, in particular, showed a cell growth inhibitory activity comparable to the free drug.
报道了含抗癌药物紫杉醇（PTX）的纳米球制剂（NS）的制备及其技术特性。通过溶剂置换法制备了聚乳酸（PLA）和聚乳酸-乙醇酸共聚物（PLGA）纳米球（NS）。它们的平均粒径在150 - 300 nm范围内，具有高度均一性（多分散指数<0.3）。为实现长期稳定性，纳米球需要额外的处理步骤，如冷冻干燥。在本研究中，通过光散射尺寸分析测试了不同浓度的冻干保护剂（单糖和二糖、多元醇以及羟丙基-β-环糊精）对纳米球粒径和表面电荷的影响。添加10%葡萄糖（w/v）冻干的制剂在冻干后表现出有趣的特性。它们被选用于药物包封效率、体外药物释放以及对人间变性甲状腺癌细胞系8305C的生物活性的特定研究。特别是PLGA纳米球表现出与游离药物相当的细胞生长抑制活性。
