Asymmetric flow field-flow fractionation (AF4) for the quantification of nanoparticle release from tablets during dissolution testing.
Asymmetric flow field-flow fractionation (AF4) for the quantification of nanoparticle release from tablets during dissolution testing.
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DOI：
10.1016/j.ijpharm.2013.11.044
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发表时间：
2014-01
影响因子：
5.8
通讯作者：
A. Engel;M. Plöger;D. Mulac;K. Langer
中科院分区：
文献类型：
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作者：
A. Engel;M. Plöger;D. Mulac;K. Langer
由聚(DL-丙交酯-乙交酯)(PLGA)组成的纳米粒子是提高药物靶向性的最有前途的胶体药物载体。虽然大多数研究活动都集中在这些载体的静脉应用上，但口服给药被描述为提高难溶药物的生物利用度。基于这些见解，手稿描述了PLGA纳米颗粒的模型片剂配方，特别是关于纳米药物载体的分析特征。除了根据药典对片剂进行物理化学表征外，本研究的主要目的是开发一种合适的分析方法来定量片剂中纳米粒的释放。建立并验证了一种分析流场-流动分馏(AF4)方法，该方法可测定固体制剂中纳米粒的含量，并可在溶出度试验中定量颗粒释放。对于颗粒检测，多角度光散射(MALS)探测器被耦合到AF4-系统。溶出度测试后，动态光散射和扫描电子显微镜证实了未改变的PLGA纳米粒的存在。
Nanoparticles composed of poly(DL-lactide-co-glycolide) (PLGA) represent promising colloidal drug carriers for improved drug targeting. Although most research activities are focused on intravenous application of these carriers the peroral administration is described to improve bioavailability of poorly soluble drugs. Based on these insights the manuscript describes a model tablet formulation for PLGA-nanoparticles and especially its analytical characterisation with regard to a nanosized drug carrier. Besides physico-chemical tablet characterisation according to pharmacopoeias the main goal of the study was the development of a suitable analytical method for the quantification of nanoparticle release from tablets. An analytical flow field-flow fractionation (AF4) method was established and validated which enables determination of nanoparticle content in solid dosage forms as well as quantification of particle release during dissolution testing. For particle detection a multi-angle light scattering (MALS) detector was coupled to the AF4-system. After dissolution testing, the presence of unaltered PLGA-nanoparticles was successfully proved by dynamic light scattering and scanning electron microscopy.