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| Pharmacokinetic study of OX26/ApoE co-modified berberine-loaded mesoporous silica nanoparticles |
| Hits 1151 Download times 779 Received:August 08, 2020 |
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| DOI
10.11656/j.issn.1673-9043.2020.06.21 |
| Key Words
berberine;mesoporous silica nanoparticles;brain targeting;OX26;ApoE;pharmacokinetics |
| Author Name | Affiliation | E-mail | | 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 | | | LI Xinyue | 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 | | | SONG Xunan | 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 | | | SUN Xinru | 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 | | | 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 | | | GUO Pan | 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 | guopan@tjutcm.edu.cn。 | | 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] To prepare mesoporous silica nanoparticles functionalized with carboxyl groups (MSNs-COOH),and couple transferrin receptor monoclonal antibody (OX26) and apolipoprotein E (ApoE) through surface to make the mesoporous silica carrier loaded with berberine (BBR-MSNs) penetrate the blood-brain barrier (BBB) and increase the ability of targeting to the brain.[Methods] MSNs-COOH was prepared by the template method,OX26 and ApoE were coupled by the carbodiimide method,and the BBR was successfully encapsulated in the channel by the dipping method. A series of characterization of the carrier were carried out by transmission electron microscope (TEM),laser particle size analyzer,N2 absorption and desorption method,etc. To investigate the vitro release of BBR through dialysis bag method. Tail vein injection to determine the drug concentration in rat plasma and brain tissue,and pharmacokinetic parameters were fitted to evaluate the drug's brain targeting.[Results] The MSNs-COOH was spherical particles with ordered pores under TEM. The average particle size was (129.83±1.27) nm,and the drug loading was (10.71~20.39)%. The vitro release showed obvious slow and controlled release characteristics. Pharmacokinetic parameters showed that the AUC of OX26/ApoE co-modified BBR-loaded MSNs (BBR-MSNs-OX26/ApoE) was significantly different from the BBR solution group,and the brain targeting index was greater than one.[Conclusion] The constructed BBR brain-targeted MSNs can improve the shortcomings of poor oral absorption of drugs,and achieve brain-targeted therapy of drugs with certain brain targeting. |
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