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The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics
Yu, Qiuxia1; Li, Minhua2; Chen, Hanbin3,7; Xu, Lieqiang2; Cheng, Juanjuan2; Lin, Guoshu2; Liu, Yuhong2; Su, Ziren2; Yang, Xiaobo4,5,6; Li, Yucui2; Chen, Jiannan2; Xie, Jianhui4,5,6
2022-12-31
Source PublicationDrug Delivery
ISSN1071-7544
Volume29Issue:1Pages:856-870
Abstract

Berberine (BBR) has extremely low concentration and high tissue distribution. However, current pharmacokinetic studies predominantly focus on its concentration in plasma, which could hardly make a comprehensive understanding of its pharmacokinetic process. This study made a pioneering endeavor to explore the erythrocyte-hemoglobin (Hb) self-assembly system of BBR by exploring the interaction of BBR with erythrocyte and the combination of BBR with Hb. Results showed that BBR had a low bioavailability (C = 2.833 μg/mL via intravenous administration of 2.5 mg/kg BBR and C = 0.260 μg/mL via oral administration of 400 mg/kg BBR). Besides, BBR achieved higher concentrations in erythrocytes than plasma, and the erythrocytes count and Hb content were significantly decreased after intravenous administration. Hemolysis rate indicated the BBR-erythrocyte system (with 2% erythrocytes) was relatively stable without hemolysis at the concentration of 1.00 mg/mL. And the maximum percentage of drug loading was 100% when the BBR-erythrocyte concentration was 0.185 μg/mL. Furthermore, incubation of BBR and erythrocytes resulted in internalization of the erythrocyte membrane and the formation of intracellular vacuoles. The thermodynamic parameters indicated that the binding process of bovine hemoglobin (BHB) and BBR was spontaneous. UV-vis absorption spectra, synchronous fluorescence, circular dichroism and Raman spectra collectively indicated that BBR showed strong binding affinity toward BHB and affected the molecular environment of residues like tryptophan and tyrosine in BHB, resulting in the conformational changes of its secondary and tertiary structure. Molecular docking indicated BBR interacted with Arg-141 residue of BHB via hydrogen bond with the bond length of 2.55 Å. The ΔG value of the BHB-BBR system was −31.79 kJ/mol. Molecular dynamics simulation indicated the root mean square derivation of BBR-BHB was <0.025 nm, suggestive of stable conformation. Cumulatively, there was an erythrocyte-Hb self-assembled drug delivery system after oral or intravenous administration of BBR, which conceivably gained novel insight into the discrepancy between the extremely low plasma concentration and relatively high tissue concentration of BBR.

KeywordBerberine Erythrocyte Hemoglobin Pharmacokinetics Self-assembly System
DOI10.1080/10717544.2022.2036870
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000768221700001
Scopus ID2-s2.0-85126389105
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Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorLi, Yucui; Chen, Jiannan; Xie, Jianhui
Affiliation1.The Second Clinical College of Guangzhou, University of Chinese Medicine, Guangzhou, China
2.School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, China
3.The First Affiliated Hospital of Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, China
4.The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, China
5.State Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou, China
6.Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome, Guangzhou, China
7.State Key Laboratory of Quality Research in Chinese Medicine and Institute of Chinese Medical Sciences, University of Macau, Macao
Recommended Citation
GB/T 7714
Yu, Qiuxia,Li, Minhua,Chen, Hanbin,et al. The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics[J]. Drug Delivery,2022,29(1):856-870.
APA Yu, Qiuxia,Li, Minhua,Chen, Hanbin,Xu, Lieqiang,Cheng, Juanjuan,Lin, Guoshu,Liu, Yuhong,Su, Ziren,Yang, Xiaobo,Li, Yucui,Chen, Jiannan,&Xie, Jianhui.(2022).The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics.Drug Delivery,29(1),856-870.
MLA Yu, Qiuxia,et al."The discovery of berberine erythrocyte-hemoglobin self-assembly delivery system: a neglected carrier underlying its pharmacokinetics".Drug Delivery 29.1(2022):856-870.
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