Polymeric nanospheres fabricated with natural emulsifiers for clinical administration of an anticancer drug paclitaxel (Taxol®)
Polymeric nanospheres fabricated with natural emulsifiers for clinical administration of an anticancer drug paclitaxel (Taxol®)
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DOI：
10.1016/s0928-4931(02)00017-6
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发表时间：
2002-05-31
期刊：
影响因子：
--
通讯作者：
Pack, D
中科院分区：
文献类型：
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作者：
Feng, SS;Mu, L;Pack, D
紫杉醇（紫杉醇(R)）是近几十年来从自然界中发现的最有效的抗癌药物之一，可治疗卵巢癌、乳腺癌、脑癌、结肠癌、肺癌等多种癌症，以及艾滋病相关癌症。由于其水溶性较低，因此必须使用辅助剂，如可引起严重副作用的Cremophor EL。我们的目标是开发一种替代的给药系统，以达到更好的治疗效果和最小的副作用。采用改进的溶剂萃取/蒸发技术制备了负载紫杉醇的可生物降解聚合物纳米球。采用磷脂、胆固醇和维生素代替传统的化学乳化剂，可获得较高的包封效率和理想的药物释放率。采用光散射、扫描电镜和原子力显微镜对不同条件下制备的纳米球进行了形貌表征；差示扫描量热法（DSC）测定聚合物基质内药物的物理状态；表面电荷性质的ζ电位测量x射线光电子能谱（XPS）用于表面化学。采用高效液相色谱法测定其体外释放动力学。最佳设计是为了开发一种癌症化疗产品。(C) 2002 Elsevier Science b.v.版权所有
Paclitaxel (Taxol(R))) is one of the most effective anticancer drugs found from nature in recent decades, which can treat various cancers including ovarian, breast, brain, colon and lung cancer, and AIDS-related cancer. Due to its low aqueous solubility, adjuvants such as Cremophor EL, which causes serious side effects, have to be used in its administration. Our aim is to develop an alternative delivery system to achieve better therapeutic effects with minimum side effects. Paclitaxel-loaded nanospheres of biodegradable polymers were prepared by an improved solvent extraction/evaporation technique. Phospholipids, cholesterol and vitamins were used to replace traditional chemical emulsifiers to achieve high encapsulation efficiency (EE) and desired release rate of the drug. Nanospheres prepared under various conditions are characterized by the light scattering for size and size distribution, the scanning electron microscopy (SEM) and the atomic force microscopy (AFM) for surface morphology; differential scanning calorimetry (DSC) for the physical status of the drug within the polymeric matrix; the zeta-potential measurement for the surface charge properties; and X-ray photoelectron spectroscopy (XPS) for the surface chemistry. In-vitro release kinetics were measured by high-performance liquid chromatography (HPLC). Best design was pursued to develop a product for cancer chemotherapy. (C) 2002 Elsevier Science B.V All rights reserved.