Nanocellulose hyperfine network achieves sustained release of berberine hydrochloride solubilized with β-cyclodextrin for potential anti-infection oral administration

• Published in: International journal of biological macromolecules 2020-06, Vol.153, p.633-640
• Main Authors: Xiao, Lin, Poudel, Abishek Jung, Huang, Lixia, Wang, Yang, Abdalla, Ahmed M.E., Yang, Guang
• Format: Article
• Language: English
• Subjects: Administration, Oral; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacokinetics; Antibacterial activity; Bacterial cellulose; Berberine - chemistry; Berberine - pharmacokinetics; Berberine hydrochloride; beta-Cyclodextrins - chemistry; Cellulose - chemistry; Delayed-Action Preparations - chemistry; Delayed-Action Preparations - pharmacokinetics; Drug release; Nanoparticles - chemistry; β-Cyclodextrin
• ISSN: 0141-8130; 1879-0003
• DOI: 10.1016/j.ijbiomac.2020.03.030

Berberine hydrochloride (BBH) has been used to treat diarrhea and other gastrointestinal diseases, however its therapeutic efficacy is compromised because of poor aqueous solubility and dissolution. In this work, BBH was solubilized with β-cyclodextrin (β-CD) in aqueous solution through formation of the BBH/β-CD inclusion complex (IC), which was confirmed by the combination of different techniques including FT-IR, XRD, DSC, 1H NMR and 1H NOESY. The aqueous solubility of BBH at 25 °C was increased by ca. 102% in the presence of 16 mM β-CD. BBH/β-CD IC-loaded bacterial cellulose (BC) hydrogels (denoted as BC/IC) were prepared by physical absorption method, resulting in higher drug loading capacity (DLC) than BC/BBH hydrogels. In vitro drug release showed that sustained drug release was achieved at different pH conditions simulating the gastrointestinal fluids by BC/IC hydrogels due to the hyperfine network of BC matrix. Furthermore, in vitro anti-bacterial test demonstrated the BC/IC hydrogels induced effective bacterial inhibition. Together with the good biocompatibility and edibility of the BC matrix, these BC/IC hydrogels appear to be promising candidates of oral administration medicine against gastrointestinal infections. •The solubilization effect of β-CD on BBH was evaluated by phase solubility.•β-CD/BBH IC was loaded into BC matrix to form BC/IC hydrogels.•Release rate of β-CD/BBH IC from BC matrix depends on pH conditions.•BC/IC hydrogels exhibited higher antimicrobial activity than BC/BBH.