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In this study, an oral drug nanocrystals self-stabilized Pickering emulsion (NSSPE), which used nanocrystals of a poorly soluble ingredient from Puerariae Radix called puerarin as solid particle stabilizers and Ligusticum chuanxiong essential oil since the main oil phase had been developed to improve the oral bioavailability of puerarin. The appearance of emulsions, size and zeta potential of droplets, and content of puerarin in emulsified layer during a storage of six months at 4, 25, and 40 °C were investigated. The centrifugation stability at 4000× g was also studied. The micro-structure of emulsion droplets was characterized by a scanning electron micrograph (SEM), confocal laser scanning microscopy (CLSM), a fluorescence microscope (FM), and differential scanning calorimetry (DSC). The in vivo oral bioavailability of puerarin NSSPE was investigated in rats. Results showed that appearances of puerarin NSSPE kept stable after centrifugation at 4000× g for 15 min or storage for six months at 4, 25, and 40 °C. SEM, CLSM, FM, and DSC showed that the puerarin NSSPE had a stable core-shell structure of emulsion droplets formed by the adsorption of puerarin nanocrystals on the surface of oil droplets of mixed oil of Ligusticum chuanxiong essential oil and Labrafil M 1944 CS (9:1, v/v). The relative bioavailability of puerarin NSSPE to puerarin coarse powder suspension, nanocrystal suspension, and surfactant emulsion were 262.43%, 155.92%, and 223.65%, respectively. All these results indicated that puerarin nanocrystals could stabilize Pickering emulsion of Ligusticum chuanxiong essential oil without any other stabilizers and Pickering emulsion could improve the oral bioavailability of puerarin, which suggests that the drug nanocrystal self-stabilized Pickering emulsion as a promising oral drug delivery system for Traditional Chinese Medicine containing poorly soluble ingredients and volatile oils.

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Now there are few good oral preparations of puerarin used in cerebrovascular diseases because of its poor oral absorption caused by the low water solubility and the poor penetration into brain. In this study, three oral formulations of puerarin, nanocrystals suspension (NCS), inclusion compounds solution (ICS) and self-microemulsifying drug delivery system (SMEDDS) were prepared with borneol as an oral brain-targeting enhancer. A rat syngeneic in vitro model of the brain-blood barrier (BBB) was established to investigate effects of borneol on the permeability of puerarin across the BBB. The pharmacokinetics of puerarin in mice after oral administration was investigated by a high performance liquid chromatography-mass spectrometry/mass spectrometry (HPLC-MS/MS) method. The in vitro BBB model study showed the permeability of puerarin was increased significantly (p < 0.05) and the value of transepithelial electrical resistance at 2 h was decreased significantly (p < 0.01) when the concentration of borneol was over 12.5 μg/mL compared with the control group. The pharmacokinetics results indicated borneol with doses of over 50 mg/kg could obviously increase both intestinal absorption and brain penetration of puerarin. With co-administration of borneol (100 mg/kg), the AUC of puerarin both in plasma (AUC) and in brain (AUC) for SMEDDS were significantly higher than those for NCS (p < 0.01) and ICS (p < 0.05). These results suggested borneol in combination with SMEDDS could improve both the oral absorption and the brain penetration of puerarin in mice, which was promising for the development of an oral formulation of puerarin used in cerebrovascular diseases.

Catalpol and puerarin are active ingredients isolated from Rehmannia glutinosa Libosch and Radix Puerariae, respectively. They are popular in research for their poly-pharmacological effects. This research focused on effect of anti-stroke by lyophilized powder of catalpol and puerarin (C-P) and potential mechanisms. At the beginning of research, C-P was identified and analyzed by HPLC. Neurological function was evaluated by Longa score, neurological complex function score and beam balance score after permanent middle cerebral artery occlusion (PMCAO) in mice. Infarct volume and water content were evaluated after treatment of C-P. Anti-oxidative stress, anti-apoptosis, angiogenesis and neurogenesis were investigated by ELISA, WB and immunohistochemical stain respectively. With treatment of C-P, neurological deficiency of PMCAO mice was ameliorated. Morphologically, infarct volume and water content in ischemic hemisphere were significantly reduced by C-P. In vivo and in vitro, oxidative stress injury was extenuated by C-P. Meanwhile, Caspase-3 was down-regulated and Bxl-2 was up-regulated by C-P in vivo. In addition, C-P enhanced angiogenesis around the infarct of cortex and neurogenesis in the Hippocampal Dentate Gyrus (DG). Hence, C-P ameliorated stroke-induced neurological deficiency through its multiple neuroprotections. What's more, this article provides us a novel formula of active ingredients for stroke.

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