Preparation and evaluation of Baicalin-loaded cationic solid lipid nanoparticles conjugated with OX26 for improved delivery across the BBB |
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| Authors: | Zhidong Liu Hainan Zhao Lexin Shu Yanqing Zhang ChukwunweikeIkechukwu Okeke Li Zhang |
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| Affiliation: | 1. Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China,;2. Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China,;3. Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China,;4. Dongfang College of Beijing University of Chinese Medicine, Langfang City, Hebei Province, P.R. China,;5. Department of Experimental Education, Tianjin University of Traditional Chinese Medicine, Tianjin, P.R. China, and;6. Department of Pharmaceutical Engineering, School of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin, P.R. China |
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| Abstract: | Purpose: A novel brain targeting drug delivery system based on OX26 antibody conjugation on PEGylated cationic solid lipid nanoparticles (OX26-PEG-CSLN) was prepared.Methods: The Baicalin-loaded PEGylated cationic solid lipid nanoparticles modified by OX26 antibody (OX26-PEG-CSLN) were prepared by emulsion evaporation–solidification at low temperature method. The immune-gold labeled OX26-PEG-CSLN was visualized by transmission electron microscopy. The mean diameter and zeta potential of OX26-PEG-CSLN, PEG-CSLN and CSLN were determined using a Zetasizer. The entrapment efficiency of OX26-PEG-CSLN, PEG-CSLN and CSLN was determined by ultrafiltration centrifugation method. And the solid-state characterization of OX26-PEG-CSLN and CSLN were analyzed by X-ray. Pharmacokinetics studies were conducted by in vivo microdialysis in rat cerebrospinal fluid.Results: The results showed that the OX26-PEG-CSLN, PEG-CSLN and CSLN had average diameters of 47.68?±?1.65, 27.20?±?1.70 and 33.89?±?5.74?nm, Zeta potentials of ?0.533?±?0.115?mV, 11.200?±?0.500?mV and 11.080?±?1.170?mV and entrapment efficiencies of 83.03?±?0.01%, 92.90?±?3.50% and 97.83?±?0.19%, respectively. In the pharmacokinetics studies, the AUC value of OX26-PEG-CSLN was11.08-fold higher than that of the Baicalin solution (SOL) (p?p?>?0.05); the Cmax value of OX26-PEG-CSLN was 7.88-fold higher than that of SOL (p?p?Conclusion: These results demonstrated OX26-PEG-CSLN could be a promising carrier to deliver drugs across the BBB for the treatment of brain diseases. |
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| Keywords: | Baicalin BBB brain target drug delivery cationic solid lipid nanoparticles OX26 |
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