Development of a Water-Soluble Nanomicellar Formulation Loaded with Trans-Resveratrol Using Polyethylene Glycol Monostearate for the Treatment of Intracerebral Hemorrhage

利用聚乙二醇单硬脂酸酯开发载有反式白藜芦醇的水溶性纳米胶束制剂,用于治疗脑出血

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作者:Kengo Banshoya, Aoi Machida, Saki Kawamura, Tetsuhiro Yamada, Riko Okada, Yui Kawamoto, Hikaru Kimura, Sachi Shibata, Yuhzo Hieda, Yoshiharu Kaneo, Tetsuro Tanaka, Masatoshi Ohnishi

Conclusions

The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment.

Methods

These formulations (stPEG/Res) were developed using five types of stPEG containing 10, 25, 40, 55 and 140 PEG repeat units. The formulations were characterized for Res content, water solubility, particle size, zeta potential, precipitation, biodistribution, and efficacy against neuronal and motor dysfunction in intracerebral hemorrhage (ICH).

Results

Intravenous administration of stPEG40/Res, which demonstrated particle size, water solubility, and biodistribution properties suitable for intravenous administration, suppressed neurological and motor dysfunction following in a collagenase-induced ICH mouse model. These effects were inhibited by zinc protoporphyrin-9, an inhibitor of the antioxidant enzyme heme oxygenase-1, suggesting that Res contributes to antioxidant enzyme expression and anti-inflammatory activity. Conclusions: The stPEG/Res micellar formulation developed in this study may offer a promising therapeutic approach for ICH treatment.

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