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Preparation and in vitro evaluation of PEG-modified shikonin nanostructured lipid carrier |
Hits 912 Download times 741 Received:June 02, 2021 |
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DOI
10.11656/j.issn.1673-9043.2021.05.23 |
Key Words
shikonin;nanostructured lipid carrier;MCF-7 cell |
Author Name | Affiliation | E-mail | QIN Huan | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | ZHANG Bing | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China College of Food and Biological Engineering, Xuzhou University of Technology, Xuzhou 221008, China | | MA Zhe | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | ZHANG Ying | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | ZHANG Yukun | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | LIU Zhidong | State Key Laboratory of Component Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | liuzhidong@tjutcm.edu.cn |
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Abstract
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[Objective] A PEG-modified shikonin nanostructured lipid carrier with long circulation effect has been prepared, and its physicochemical characterization and anti-tumor effect were evaluated in vitro.[Methods] The shikonin nanostructured lipid carrier was prepared by emulsification evaporation-low temperature solidification method, and the encapsulation efficiency was measured by ultracentrifugation;the formulation was characterized by particle size, polydispersity index(PDI), Zeta potential, transmission electron microscope, differential scanning volume heat, X-ray, etc. The CCK-8 method was used to investigate the activity of breast cancer MCF-7 cells, and coumarin-6 and Hoechst 33342 were used as fluorescent probes to quantitatively investigate the cellular uptake.[Results] The particle size of the PEG-modified shikonin nanostructured lipid carrier was (19.68±1.25) nm, and the PDI was 0.28±0.68, and the Zeta potential was[-(20.27±1.27)] mV. The average encapsulation rate was 98%, and the preparation had a spherical appearance and uniform size distribution. Shikonin was contained in the formulation in an amorphous form. The anti-tumor effect of shikonin was concentration-dependent. The anti-tumor activity of the medium and high-dose PEG-modified preparation group was significantly higher than that of the unmodified preparation group and the solution group. The results of the cellular uptake experiment was consistent with the results of the cytotoxicity experiment.[Conclusion] The PEG-modified shikonin nanostructured lipid carrier has good encapsulation efficiency, small particle size, stable system, good anti-tumor and cell uptake effects in vitro. |
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