College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Gungdong, Yuseonggu, Daejeon, South Korea.
Int J Nanomedicine. 2011;6:2225-34. doi: 10.2147/IJN.S24547. Epub 2011 Oct 7.
Nanoparticles fabricated from the biodegradable and biocompatible polymer, polylactic-co-glycolic acid (PLGA), are the most intensively investigated polymers for drug delivery systems. The objective of this study was to explore fully the development of a PLGA nanoparticle drug delivery system for alternative preparation of a commercial formulation. In our nanoparticle fabrication, our purpose was to compare various preparation parameters.
Docetaxel-loaded PLGA nanoparticles were prepared by a single emulsion technique and solvent evaporation. The nanoparticles were characterized by various techniques, including scanning electron microscopy for surface morphology, dynamic light scattering for size and zeta potential, x-ray photoelectron spectroscopy for surface chemistry, and high-performance liquid chromatography for in vitro drug release kinetics. To obtain a smaller particle, 0.2% polyvinyl alcohol, 0.03% D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), 2% Poloxamer 188, a five-minute sonication time, 130 W sonication power, evaporation with magnetic stirring, and centrifugation at 8000 rpm were selected. To increase encapsulation efficiency in the nanoparticles, certain factors were varied, ie, 2-5 minutes of sonication time, 70-130 W sonication power, and 5-25 mg drug loading.
A five-minute sonication time, 130 W sonication power, and a 10 mg drug loading amount were selected. Under these conditions, the nanoparticles reached over 90% encapsulation efficiency. Release kinetics showed that 20.83%, 40.07%, and 51.5% of the docetaxel was released in 28 days from nanoparticles containing Poloxamer 188, TPGS, or polyvinyl alcohol, respectively. TPGS and Poloxamer 188 had slower release kinetics than polyvinyl alcohol. It was predicted that there was residual drug remaining on the surface from x-ray photoelectron spectroscopy.
Our research shows that the choice of surfactant is important for controlled release of docetaxel.
由可生物降解和生物相容的聚合物聚乳酸-共-羟基乙酸（PLGA）制成的纳米颗粒是最受关注的用于药物传递系统的聚合物。本研究的目的是充分探索 PLGA 纳米颗粒药物传递系统的开发，以替代商业制剂的制备。在我们的纳米颗粒制备中，我们的目的是比较各种制备参数。
采用单乳液技术和溶剂蒸发法制备载多西紫杉醇的 PLGA 纳米颗粒。通过各种技术对纳米颗粒进行了表征，包括扫描电子显微镜观察表面形态、动态光散射测量粒径和 Zeta 电位、X 射线光电子能谱分析表面化学、高效液相色谱法测定体外药物释放动力学。为了获得更小的粒径，选择了 0.2%聚乙烯醇、0.03%D-α-生育酚聚乙二醇 1000 琥珀酸酯（TPGS）、2%泊洛沙姆 188、5 分钟超声时间、130 W 超声功率、带磁搅拌的蒸发以及 8000 rpm 的离心。为了提高纳米颗粒的包封效率，改变了某些因素，即 2-5 分钟的超声时间、70-130 W 的超声功率和 5-25 mg 的药物载量。
选择了 5 分钟的超声时间、130 W 的超声功率和 10 mg 的药物载量。在这些条件下，纳米颗粒的包封效率超过 90%。释放动力学表明，含有泊洛沙姆 188、TPGS 或聚乙烯醇的纳米颗粒在 28 天内分别释放了 20.83%、40.07%和 51.5%的多西紫杉醇。TPGS 和泊洛沙姆 188 的释放动力学比聚乙烯醇慢。X 射线光电子能谱预测表明，表面仍有残留药物。
我们的研究表明，表面活性剂的选择对多西紫杉醇的控制释放很重要。
