Vitamin E TPGS used as emulsifier in the solvent evaporation/extraction technique for fabrication of polymeric nanospheres for controlled release of paclitaxel (Taxol®)
Vitamin E TPGS used as emulsifier in the solvent evaporation/extraction technique for fabrication of polymeric nanospheres for controlled release of paclitaxel (Taxol®)
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DOI：
10.1016/s0168-3659(02)00025-1
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发表时间：
2002-04-23
影响因子：
10.8
通讯作者：
Feng, SS
中科院分区：
文献类型：
--
作者：
Mu, L;Feng, SS
以维生素E TPGS作为表面活性剂稳定剂，采用溶剂挥发/萃取法制备了紫杉醇PLGA纳米微球，并获得成功。激光散射系统（LLS）。扫描电子显微镜（SEM）、原子力显微镜（AFM）。差示扫描量热法（DSC）。采用傅里叶变换红外光谱（FTIR）和X射线光电子能谱（XPS）对不同配方和制备条件下制备的纳米球进行了粒度、粒度分布和表面形貌的表征。热谱特性和表面化学。采用高效液相色谱法测定包封率和体外释放度。讨论了抗癌药物紫杉醇（Taxol*）的聚合物纳米球递送系统的开发结果。发现所产生的纳米球为具有光滑表面的细球形，并且没有聚集或粘附。维生素E TPGS乳化的PLGA纳米球与PVA乳化的PLGA纳米球在形态上无显著差异。然而，与传统的化学乳化剂PVA相比，TPGS可以显著提高药物在PLGA纳米球中的包封率，其可以高达100%。维生素E TPGS乳化纳米球的粒径范围为300 - 800 nm，粒径分布窄，多分散性为0.005-0.045。XPS研究表明，虽然TPGS在纳米球形成过程中被相对彻底地洗脱，但表面活性剂分子仍残留在表面。这一发现也通过纳米球的FTIR-PAS研究得到证实。体外释放实验表明，紫杉醇从纳米球中的释放特性强烈依赖于制备中所采用的乳化剂类型。研究表明，维生素E TPGS是一种理想的高效乳化剂。(C)2002年，Elsevier Science BY。All rights reserved.
The D-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) was applied in the present investigation as surfactant stabiliser to fabricate paclitaxel-loaded PLGA nanospheres in the solvent evaporation/extraction technique with Successful achievement. Laser light scattering system (LLS). scanning electron microscopy (SEM), atomic force microscopy (AFM). differential scanning calorimetry (DSC). Fourier transform infra-red spectroscopy (FTIR), and X-ray photoelectron spectroscopy (XPS) were employed to characterise the nanopsheres fabricated in various recipes under various preparation conditions for size and size distribution, surface morphology. thermogram property and surface chemistry. Encapsulation efficiency and in vitro release was measured by the high-performance liquid chromatography (HPLC). The outcomes were discussed with respect to the development of polymeric nanospheres delivery system of the anticancer drug, paclitaxel (Taxol*). The produced nanospheres were found in fine spherical shape with smooth surfaces and without aggregation or adhesion. There was no significant difference in morphology between the vitamin E TPGS emulsified and PVA emulsified PLGA nanospheres. However, it was found that, in comparison with the traditional chemical emulsifier PVA, the TPGS could significantly improve the encapsulation efficiency of the drug in the PLGA nanospheres, which could be as high as 100%. The size of the vitamin E TPGS emulsified nanospheres ranged from 300 to 800 nm and the size distribution was narrow with polydispersity of 0.005-0.045. XPS investigation demonstrated that there were residual surfactant molecules remained on the surface although the TPGS could be washed out relatively thoroughly in the process of nanospheres formation. This finding was also confirmed by FTIR-PAS investigation of the nanospheres. The in vitro release indicated that the release property of paclitaxel from the nanospheres strongly depends on the emulsifier type employed in the fabrication. Our research shows that vitamin E TPGS could be an ideal and effective emulsifier. (C) 2002 Elsevier Science BY. All rights reserved.