达沙替尼白蛋白胶束的制备与表征
Preparation and characterization of dasatinib albumin micelles
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摘要: 研究制备一种聚乙二醇和十二醛双修饰的牛血清白蛋白(PEG-DSA),并探讨其作为达沙替尼(dasatinib,DAS)新型高效胶束载体的初步可行性。采用圆二色谱、核磁共振氢谱、元素分析、红外光谱等方法进行材料结构表征,采用单因素考察法进行PEG-DSA/DAS胶束和非PEG化对照胶束DSA/DAS的工艺优化。结果表明,PEG-DSA与DAS质量比为4∶1时可以获得理化性质合适且稳定、载药量高的最优制剂:平均粒径为(37.21 ± 0.21)nm,多分散指数PDI为0.24 ± 0.04,Zeta电位为?(15.68 ± 0.19)mV,载药量(DL)为(10.22 ± 0.34)%,包封率(EE)为(42.73 ± 1.15)%。与文献报道的DAS纳米制剂相比,PEG-DSA/DAS胶束的载药量显著提高,具有进一步开发的潜力。Abstract: In this study, a polyethylene glycol and dodecaldehyde modified bovine serum albumin (PEG-DSA) was developed, and its feasibility as a new high-efficiency micellar carrier for dasatinib (DAS) was explored.Circular dichroism, 1H NMR, elemental analysis, FT-IR and other methods were used to characterize the material structure and the single factor method was used to optimize the process of PEG-DSA/DAS micelles and non-PEGylated control micelles DSA/DAS.The results indicated that the optimal formulation was obtained with a mass ratio of 4∶1 between PEG-DSA and DAS, with average particle size of (37.21 ± 0.21) nm, polydispersion index (PDI) of (0.24 ± 0.04), Zeta potential of ? (15.68 ± 0.19) mV, drug loading (DL) capacity of (10.22 ± 0.34) %, and encapsulation efficiency (EE) of (42.73 ± 1.15) %. Compared with the currently reported nano-formulations of DAS, the drug loading of PEG-DSA/DAS micellar formulations was significantly increased with potential for further development.
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Keywords:
- dasatinib /
- albumin amphiphilic modification /
- albumin micelle /
- preparation /
- characterization
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