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Ligustrazine Phosphate Ethosomes for Treatment of Alzheimer’s Disease, In Vitro and in Animal Model Studies

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Abstract

In the present study, we have investigated transdermal administration of ligustrazine phosphate (LP), as an antioxidant, for the treatment of Alzheimer’s disease (AD). The LP transdermal ethosomal system was designed and characterized. Franz-type diffusion cells and confocal laser scanning microscopy were used for the in vitro permeation studies. Furthermore, the effect of LP transdermal ethosomal system on AD was evaluated in the scopolamine-induced amnesia rats by evaluating the behavioral performance in the Morris water maze test. The activities of the antioxidant enzymes and the levels of the lipid peroxidation product malondialdehyde (MDA) in the brain of rats were also determined. The results showed that both the penetration ability and the drug deposition in skin of the LP ethosomal system were significantly higher than the aqueous one. The LP transdermal ethosomal system could recover the activities of the antioxidant enzymes and the levels of MDA in the brain of the amnesic rats to the similar status of the normal rats, which was also indirectly reflected by the improvement in the behavioral performance. In conclusion, LP might offer a potential alternative therapeutic drug in the fight against AD, and ethosomes could be vesicles of choice for transdermal delivery of LP.

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ACKNOWLEDGMENTS

This work was supported by the National Science Fund of China (no. 30500666) and the Tsinghua—Yuyuan Medical Funds (no. 20240000529, no. 20240000548). The authors would like to thank Prof. Lei Huang (Department of Medicine, Tsinghua University, China) for providing the CLSM platform and the technical assistance.

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Authors and Affiliations

  1. School of Pharmacy, East China University of Science and Technology, Shanghai, 200237, People’s Republic of China

    Jun Shi & Guoan Luo

  2. Department of Chemistry, Tsinghua University, Beijing, 100084, People’s Republic of China

    Jun Shi, Yiming Wang & Guoan Luo

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  1. Jun Shi
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  2. Yiming Wang
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Correspondence to Guoan Luo.

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Shi, J., Wang, Y. & Luo, G. Ligustrazine Phosphate Ethosomes for Treatment of Alzheimer’s Disease, In Vitro and in Animal Model Studies. AAPS PharmSciTech 13, 485–492 (2012). https://doi.org/10.1208/s12249-012-9767-6

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  • DOI: https://doi.org/10.1208/s12249-012-9767-6

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