Abstract
The main components of Caesalpinia sappan L. (CS) are brazilin and brazilein, which show high potential in pharmacologic applications. However, these have been drastically limited by the poor water solubility and stability. The present study investigates the formation of inclusion complexes F1, F2, and F3 between CS and β-cyclodextrin (βCD), hydroxypropyl-β-cyclodextrin (HPβCD), and methyl-β-cyclodextrin (MβCD), respectively. These complexes were characterized by Fourier transform infrared spectroscopy (FT-IR). The results showed that the highest encapsulation efficiency and loading capacity of CS extract were 44.24% and 9.67%, respectively. The solubility and stability of CS extract were significantly increased through complexation in phase solubility and stability studies. The complexes F1–F3 showed mainly significant antibacterial activities on gram-positive bacteria pathogens causing mastitis. Moreover, the expression levels of COX-2 and iNOS were significantly decreased in LPS-induced inflammatory cells at concentrations of 50 and 100 µg/mL. In addition, treatment of complex F3 (CS/MβCD) in bovine endothelial cells remarkably increased the chemokine gene expression of CXCL3 and CXCL8, which were responsible for immune cell recruitment (9.92 to 11.17 and 8.23 to 9.51–fold relative to that of the LPS-treated group, respectively). This study provides a complete characterization of inclusion complexes between CS extract and βCD, HPβCD, and MβCD for the first time, highlighting the impact of complex formation on the pharmacologic activities of bovine mastitis.
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Acknowledgements
We sincerely thank the Department of Pharmaceutical Science, Faculty of Pharmacy, Chiang Mai University, Thailand, for supporting analytical instruments and support of the work in this manuscript. We also thank Asst. Prof. Dr. Thararat Chitov, Department of Biology Faculty of Science, Chiang Mai University, for the heartwood materials of C. sappan.
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This work was supported by the National Research Council of Thailand (NRCT) 2019.
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Conceptualization and funding acquisition: RK, WC; method, design experiments, and investigation: WC, PS, KT, HP, AP; writing—original draft writing: PS, WC, HP, AP; writing—review and editing: RK; supervision and analysis of data: RK, SP, WS, SO. All authors have approved the final version of the manuscript.
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Chaisri, W., Suebsakwong, P., Pandith, H. et al. Effects of Encapsulation of Caesalpinia sappan L. with Cyclodextrins for Bovine Mastitis. AAPS PharmSciTech 24, 230 (2023). https://doi.org/10.1208/s12249-023-02687-5
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DOI: https://doi.org/10.1208/s12249-023-02687-5