Preparation and evaluation of Baicalin-loaded cationic solid lipid nanoparticles conjugated with OX26 for improved delivery across the BBB

Zhidong LiuTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China, Correspondence[email protected]

Hainan ZhaoTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China, ;Dongfang College of Beijing University of Chinese Medicine, Langfang City, Hebei Province, P.R. China,

Lexin ShuTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China, ;Department of Experimental Education, Tianjin University of Traditional Chinese Medicine, Tianjin, P.R. China, and

Yanqing ZhangDepartment of Pharmaceutical Engineering, School of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin, P.R. China

ChukwunweikeIkechukwu OkekeTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China,

Li ZhangTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China,

Jiawei LiTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin, P.R. China, ;Department of Experimental Education, Tianjin University of Traditional Chinese Medicine, Tianjin, P.R. China, and

Nan LiTianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, P.R. China, ;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, 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 < 0.01), and 1.12-fold higher than that of the CSLN (p > 0.05); the C_max value of OX26-PEG-CSLN was 7.88-fold higher than that of SOL (p < 0.01) and 1.12-fold (p < 0.01) higher than that of the CSLN, respectively.

Conclusion: These results demonstrated OX26-PEG-CSLN could be a promising carrier to deliver drugs across the BBB for the treatment of brain diseases.

Keywords

Declaration of interest

The authors report no conflicts of interest in this work. This study was financial supported by the National Natural Science Foundation of China (81001645), Program for New Century Excellent Talents in University (NCET-12-1068), Tianjin Natural Science Foundation (12JCYBJC18700), the National Key Technology Research and Development Program of China (2012ZX09304007).

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Preparation and evaluation of Baicalin-loaded cationic solid lipid nanoparticles conjugated with OX26 for improved delivery across the BBB

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Preparation and evaluation of Baicalin-loaded cationic solid lipid nanoparticles conjugated with OX26 for improved delivery across the BBB

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