紫草素脂质体的制备及其体内外评价

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Preparation shikonin-liposomes and its in vivo-in vitro evaluation anti-aging

ZHAI Ying， YU Jiangnan， XU Ximing（ 212O13，China）

[Abstract]Objective： To prepare shikonin liposomes （SHK-L） and preliminarily evaluate their antiaging effects.Methods： The SHK-L prescription was optimized through single factor experiments to investigate its in vitro release and oral bioavailability in rats.The in vivo safety was evaluated through zebrafish toxicity experiments， and the anti-aging effect was examined by staining the β -galactosidase in aging zebrafish. Results： The optimal prescription was SHK 6mg ，lecithin 70mg ，cholesterol 10mg ， vitamin E polyethylene glycol succinate （TPGS） 30mg ，and sodium dodecyl sulphate （SDS） 1.5mg ， with a particle size （ 206.96±0.75 ）nm，polydispersity coefficient （ 0.186±0.030） ，encapsulation rate （96.88±2.19）% and drug loading was （5.36±0.01）% . SHK-L improved the drug release rate compared to SHK.According to in vivo pharmacokinetic data， SHK-L had a relative bioavailability （204号 413.37% SHK. At 96 hours post-administration， LC50 shikonin and SHK-L in zebrafish were （ 0.112±0.007 ） μg/mL and （ 0.141±0.012 ） μg/mL ，respectively. Conclusion：SHK-L can enhance the solubility and oral bioavailability insoluble drugs，as well as their anti-aging effect and safety.

[Key words] shikonin； liposomes ； in vitro release; oral bioavailability；anti-aging； safety

衰老是指机体生理功能（如血压调节、呼吸、视力等）随时间逐渐退化，并最终导致死亡的自然过程[1-2]。（剩余5203字）