目的:合成不同的PLGA-PEG-PLGA温敏水凝胶,并研究水凝胶相变温度及流变学与原料比例的关系。方法:以混旋丙交酯(DLlactide)、乙交酯(Glycolide)和PEG为原料,异辛酸亚锡为催化剂,采用开环聚合法,通过改变投料配比和PEG的分子量,制备PLGA-...目的:合成不同的PLGA-PEG-PLGA温敏水凝胶,并研究水凝胶相变温度及流变学与原料比例的关系。方法:以混旋丙交酯(DLlactide)、乙交酯(Glycolide)和PEG为原料,异辛酸亚锡为催化剂,采用开环聚合法,通过改变投料配比和PEG的分子量,制备PLGA-PEGPLGA嵌段共聚物。倒转试管法测定共聚物水溶液的相变温度和沉淀温度;同时用Anton Paar MCR301对水凝胶流变学进行研究。结果:原料比例不同,合成的水凝胶流变学参数和相变温度也不同。结论:改变聚乙二醇的分子量和丙交酯与乙交酯的比例来控制合成共聚物的流变学参数以及相变温度,也可以通过改变共聚物的浓度来小范围地调节其流变学参数和相变温度。展开更多
Docetaxel is a member of taxan family of antineoplastic agents widely used in cancer chemotherapy. However, application of conventional chemotherapy with commercial formulation has been accompanied with matters of con...Docetaxel is a member of taxan family of antineoplastic agents widely used in cancer chemotherapy. However, application of conventional chemotherapy with commercial formulation has been accompanied with matters of concern regarding drug’s biodistribution, pharmacokinetics, and pharmacodynamics. Polymeric nanoparticles have been widely used as unique drug delivery vehicles to circumvent such problems. Docetaxel-loaded poly (lactide-co-glycolide) (PLGA) and poly (lactide-co-glycolide)-poly (ethylene glycol) (PLGA-PEG) nanoparticles fit well in modifying drug’s pharmacokinetic characteristics as intravenous (IV) sustained-release delivery vehicles. In such circumstances, characterization of nanoparticles in terms of their drug-payload would be a necessary step. The majority of studies have used HPLC analysis method for docetaxel quantitation in polymeric nanoparticles. Herein, a rapid ESI-MS/MS method for quantitative analysis of docetaxel in polymeric matrices of PLGA and PLGA-PEG nanoparticles through direct injection to mass spectrometer has been developed and validated. The assay was validated over a range of 3.9 - 1000 ng/ml and 125 - 16,000 ng/ml. Samples were directly injected to the instrument through an isocratic elution (0.1% formic acid in methanol) and detection was performed on a Hybrid Triple Quadrupole/Linear Ion trap mass spectrometer with multiple reaction monitoring (MRM) mode via positive electrospray ionization (ESI) source. The run time and retention time were 2 and 0.6 minutes respectively. The method demonstrated acceptable level of accuracy and precision and was successfully applied for quantitative analysis of docetaxel in polymeric nanoparticles of PLGA and PLGA-PEG.展开更多
文摘目的:合成不同的PLGA-PEG-PLGA温敏水凝胶,并研究水凝胶相变温度及流变学与原料比例的关系。方法:以混旋丙交酯(DLlactide)、乙交酯(Glycolide)和PEG为原料,异辛酸亚锡为催化剂,采用开环聚合法,通过改变投料配比和PEG的分子量,制备PLGA-PEGPLGA嵌段共聚物。倒转试管法测定共聚物水溶液的相变温度和沉淀温度;同时用Anton Paar MCR301对水凝胶流变学进行研究。结果:原料比例不同,合成的水凝胶流变学参数和相变温度也不同。结论:改变聚乙二醇的分子量和丙交酯与乙交酯的比例来控制合成共聚物的流变学参数以及相变温度,也可以通过改变共聚物的浓度来小范围地调节其流变学参数和相变温度。
文摘Docetaxel is a member of taxan family of antineoplastic agents widely used in cancer chemotherapy. However, application of conventional chemotherapy with commercial formulation has been accompanied with matters of concern regarding drug’s biodistribution, pharmacokinetics, and pharmacodynamics. Polymeric nanoparticles have been widely used as unique drug delivery vehicles to circumvent such problems. Docetaxel-loaded poly (lactide-co-glycolide) (PLGA) and poly (lactide-co-glycolide)-poly (ethylene glycol) (PLGA-PEG) nanoparticles fit well in modifying drug’s pharmacokinetic characteristics as intravenous (IV) sustained-release delivery vehicles. In such circumstances, characterization of nanoparticles in terms of their drug-payload would be a necessary step. The majority of studies have used HPLC analysis method for docetaxel quantitation in polymeric nanoparticles. Herein, a rapid ESI-MS/MS method for quantitative analysis of docetaxel in polymeric matrices of PLGA and PLGA-PEG nanoparticles through direct injection to mass spectrometer has been developed and validated. The assay was validated over a range of 3.9 - 1000 ng/ml and 125 - 16,000 ng/ml. Samples were directly injected to the instrument through an isocratic elution (0.1% formic acid in methanol) and detection was performed on a Hybrid Triple Quadrupole/Linear Ion trap mass spectrometer with multiple reaction monitoring (MRM) mode via positive electrospray ionization (ESI) source. The run time and retention time were 2 and 0.6 minutes respectively. The method demonstrated acceptable level of accuracy and precision and was successfully applied for quantitative analysis of docetaxel in polymeric nanoparticles of PLGA and PLGA-PEG.
