Preparation of bilobalide nanoemulsions and its neural-repairs effect on aluminum trichloride-induced Alzheimer’s disease mice

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Alzheimer’s disease (AD) is still one of the main causes of death in the elderly, bringing huge health problems to society. Bilobalide (BB) has a good neural-repairs effect on AD, but its poor permeability greatly limits its clinical application. Nanoemulsions (NEs) can enhance lymphatic absorption and avoid hepatic first-pass effect, thus effectively improving drug permeability, enhancing oral drug absorption and bioavailability. Our study first optimized the preparation of BB-NEs through single-factor screening and response surface methodology (RSM). Then, the appearance was observed by visual inspection, the category was identified by sudan III solution and ethylene blue solution, the particle size and potential were measured by particle size analyzer, and the morphology was observed by an electron microscope, and the encapsulation efficiency (EE) and drug loading (DL) were determined by high-performance liquid chromatography (HPLC). Then, the release mechanism of BB-NEs was explored through in vitro release kinetics model. Finally, the neural-repairs effect of BB-NEs was studied using AD mice model. After oral administration of BB-NEs in mice, compared with BB, BB-NEs showed good neural-repairs effect of improved spatial memory ability, alleviated neuronal damage, and enhanced antioxidant activity in AD mice. In conclusion, nanoemulsion is an effective method to enhance the oral absorption and therapeutic effect of BB and other BSC III drugs. This not only opens up avenues for the clinical application of BB, but also provides reference for the development of new formulations of low-permeability drugs and the expansion of their clinical application scope.