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Peer-reviewedCC BYNatural products and bioprospecting

A drug-drug cocrystal of breviscapine and borneol: harnessing natural product synergy for synchronized release and improved pharmacokinetics.

  • Jiao Wang1
  • Caixian Wang1
  • Yan Ma1
  • Tong Zhang1
  • Anguo Hou1
  • Wenbin Jin1
  • Yanni Ma2
  • Wenping Wang3
  1. 1Yunnan Key Laboratory of Chinese Medicine Processing, College of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, 650500, China.
  2. 2General Hospital of Ningxia Medical University, Yinchuan, 750004, China. [email protected].
  3. 3Yunnan Key Laboratory of Chinese Medicine Processing, College of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming, 650500, China. [email protected].
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Abstract

A drug-drug cocrystal strategy harnessing natural product synergy was developed to address the oral delivery barriers of breviscapine (BRE), a natural flavonoid with poor solubility and extensive first-pass metabolism. BRE was integrated with the monoterpenoid permeation enhancer borneol (BO) via solvent evaporation to form a stable supramolecular assembly. Comprehensive solid-state characterization and density functional theory calculations confirmed that the cocrystal lattice is stabilized by specific hydrogen bonding between the flavonoid and terpenoid scaffolds. The optimized BRE-BO cocrystal exhibited highly synchronized release of both natural products (R² = 0.86), in contrast to the discordant dissolution of the physical mixture, with kinetics following the Korsmeyer-Peppas model (n = 0.45) indicative of Fickian diffusion. In vivo pharmacokinetic evaluation in rats demonstrated that the synergy conferred by co-delivered BO resulted in a 1.6-fold enhancement in oral bioavailability (AUC₀₋₂₄), a prolonged Tmax (from 2.3 to 3.3 h), and an elevated Cmax (1.2 vs. 0.8 mg/L) compared to bulk BRE. These findings demonstrate that drug-drug cocrystallization can simultaneously achieve dissolution synchronization and pharmacokinetic optimization, providing a viable strategy for the formulation of poorly bioavailable natural flavonoids without the use of polymeric excipients.

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Cite

BibTeXRIS
BibTeX
@article{wang2026drugdrug,
  title = {{A drug-drug cocrystal of breviscapine and borneol: harnessing natural product synergy for synchronized release and improved pharmacokinetics.}},
  author = {Jiao Wang and Caixian Wang and Yan Ma and Tong Zhang and Anguo Hou and Wenbin Jin and Yanni Ma and Wenping Wang},
  journal = {Natural products and bioprospecting},
  year = {2026},
  month = nov,
  doi = {10.1007/s13659-026-00648-6},
  url = {https://europepmc.org/article/MED/42970205},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - A drug-drug cocrystal of breviscapine and borneol: harnessing natural product synergy for synchronized release and improved pharmacokinetics.
AU  - Jiao Wang
AU  - Caixian Wang
AU  - Yan Ma
AU  - Tong Zhang
AU  - Anguo Hou
AU  - Wenbin Jin
AU  - Yanni Ma
AU  - Wenping Wang
PY  - 2026
DA  - 2026/11/02
JO  - Natural products and bioprospecting
DO  - 10.1007/s13659-026-00648-6
UR  - https://europepmc.org/article/MED/42970205
AB  - A drug-drug cocrystal strategy harnessing natural product synergy was developed to address the oral delivery barriers of breviscapine (BRE), a natural flavonoid with poor solubility and extensive first-pass metabolism. BRE was integrated with the monoterpenoid permeation enhancer borneol (BO) via solvent evaporation to form a stable supramolecular assembly. Comprehensive solid-state characterization and density functional theory calculations confirmed that the cocrystal lattice is stabilized by specific hydrogen bonding between the flavonoid and terpenoid scaffolds. The optimized BRE-BO cocrystal exhibited highly synchronized release of both natural products (R² = 0.86), in contrast to the discordant dissolution of the physical mixture, with kinetics following the Korsmeyer-Peppas model (n = 0.45) indicative of Fickian diffusion. In vivo pharmacokinetic evaluation in rats demonstrated that the synergy conferred by co-delivered BO resulted in a 1.6-fold enhancement in oral bioavailability (AUC₀₋₂₄), a prolonged Tmax (from 2.3 to 3.3 h), and an elevated Cmax (1.2 vs. 0.8 mg/L) compared to bulk BRE. These findings demonstrate that drug-drug cocrystallization can simultaneously achieve dissolution synchronization and pharmacokinetic optimization, providing a viable strategy for the formulation of poorly bioavailable natural flavonoids without the use of polymeric excipients.
SN  - 2192-2195
SN  - 2192-2209
ER  -